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1.
J Appl Oral Sci ; 28: e20190025, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-31778442

RESUMO

INTRODUCTION: Periodontal therapy usually requires local anesthesia. If effective, a non-invasive, liposomal anesthetic gel could increase the levels of acceptance of patients in relation to periodontal therapy. OBJECTIVE: This study investigated the efficacy of liposomal anesthetic gel for pain control during periodontal therapy. METHODOLOGY: Forty volunteers with moderate to severe chronic periodontitis were recruited, of which at least three sextants required periodontal therapy. At least one of the selected teeth had one site with a probing depth of ≥4 mm. The volunteers received the following three gels: a placebo, lidocaine/prilocaine (Oraqix®), or a liposomal lidocaine/prilocaine, which were applied to different sextants. Pain frequency was registered during treatment and the volunteers received a digital counter to register any painful or uncomfortable experiences. At the end of each session, the volunteers indicated their pain intensity using rating scales (NRS-101 and VRS-4). The volunteers had their hemodynamic parameters measured by a non-invasive digital monitor. RESULTS: Pain frequency/intensity did not show statistical difference between intervention groups. The tested gels did not interfere with the hemodynamic indices. Dental anxiety, suppuration and probing depth could influence pain during periodontal therapy. CONCLUSION: Our results suggest limited indications for the use of non-invasive anesthesia when used for scaling and root planing. Intra-pocket anesthetic gel could be a good option for anxious patients, or those who have a fear of needles.


Assuntos
Anestesia Dentária/métodos , Anestésicos Locais/administração & dosagem , Raspagem Dentária/efeitos adversos , Géis/administração & dosagem , Dor/prevenção & controle , Aplainamento Radicular/efeitos adversos , Adulto , Idoso , Periodontite Crônica/complicações , Periodontite Crônica/terapia , Método Duplo-Cego , Feminino , Humanos , Lidocaína/administração & dosagem , Combinação Lidocaína e Prilocaína , Masculino , Pessoa de Meia-Idade , Medição da Dor/métodos , Bolsa Periodontal , Placebos , Prilocaína/administração & dosagem , Adulto Jovem
2.
Angiol Sosud Khir ; 25(4): 102-107, 2019.
Artigo em Russo | MEDLINE | ID: mdl-31855206

RESUMO

AIM: The purpose of the study was to assess efficacy and safety of heparin sodium gel 1000 IU/g and Detragel® in decreasing the incidence and treatment of the most common local adverse reactions in patients after endured sclerotherapy of reticular veins and telangiectasias. PATIENTS AND METHODS: Our open prospective observational study included a total of sixty 18-to-35-year-old female patients who after undergoing standardized sclerotherapy of reticular veins and telangiectasias on symmetrical portions of lower limbs were given a tube of heparin sodium gel 1000 IU/g or Detragel® to be applied onto the skin of one (left) lower limb in the projection of the sclerotherapy-exposed vessels 2-3 times daily for 10 days followed by putting on a compression class 2 (RAL standard) stocking. The women were allowed to use only the paired stocking on the contralateral extremity. Efficacy and safety of heparin sodium gel 1000 IU/g and Detragel® were evaluated based on the incidence of typical adverse reactions (ecchymoses, phlebitides, hyperpigmentation and neovasculogenesis), as well as on the patient's subjective perceptions. RESULTS: The use of heparin sodium gel 1000 IU/g and Detragel® in addition to compression after sclerotherapy of reticular veins and telangiectasias significantly and comparably decreased the incidence and accelerated the resolution of ecchymoses and phlebitides associated with phlebosclerosing treatment. The Detragel® group patients were found to develop hyperpigmentation or neovasculogenesis significantly less often as compared with the heparin sodium gel 1000 IU/g group women. What is more, using Detragel® was not accompanied by hyperkeratosis, pruritus or formation of a sticky film, the events, however, observed while applying heparin sodium gel 1000 IU/g. CONCLUSION: The use of Detragel® or heparin sodium gel 1000 IU/g for 10 days additionally to compression significantly decreased the incidence of typical undesirable reactions associated with sclerotherapy of reticular veins and telangiectasias. The Detragel® group women turned out to have lower incidence of hyperpigmentation and neovasculogenesis. Besides, Detragel® demonstrated better organoleptic properties.


Assuntos
Anticoagulantes/administração & dosagem , Heparina/administração & dosagem , Soluções Esclerosantes/efeitos adversos , Escleroterapia/efeitos adversos , Telangiectasia/terapia , Varizes/terapia , Administração Tópica , Feminino , Géis/administração & dosagem , Humanos , Hiperpigmentação/etiologia , Hiperpigmentação/prevenção & controle , Incidência , Neovascularização Patológica/etiologia , Neovascularização Patológica/prevenção & controle , Estudos Prospectivos , Meias de Compressão
3.
Medicine (Baltimore) ; 98(46): e17928, 2019 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-31725645

RESUMO

BACKGROUND: Research focusing on the efficacy of autologous platelet-rich gel (APRG) and continuous vacuum sealing drainage (CVSD) for diabetic foot ulcer (DFU) is increasing. Despite increasing knowledge on this theme, its results remain inconsistent. Thus, we will provide insight into the efficacy of APRG and CVSD for patients with DFU. METHODS: We will search electronic databases of MEDILINE, EMBASE, Cochrane Library, CINAHL, AMED, Chinese Biomedical Literature Database, and China National Knowledge Infrastructure from inception to October 1, 2019. No language limitation is utilized to these databases. Two authors will independently perform study selection, data extraction, and risk of bias assessment. Disagreements between 2 authors will be solved through discussion with a third author. RESULTS: The efficacy and safety of APRG and CVSD for patients with DFU will be assessed by the time to complete healing, proportion of ulcers healed within trial period, change of size of ulcer, health-related quality of life, patient length of hospital stay, and adverse events. CONCLUSION: The results of this study will provide helpful evidence of APRG and CVSD for patients with DFU. SYSTEMATIC REVIEW REGISTRATION: PROSPERO CRD42019153289.


Assuntos
Pé Diabético/terapia , Géis/uso terapêutico , Tratamento de Ferimentos com Pressão Negativa/métodos , Plasma Rico em Plaquetas , China , Drenagem , Géis/administração & dosagem , Géis/efeitos adversos , Humanos , Tempo de Internação , Qualidade de Vida , Ensaios Clínicos Controlados Aleatórios como Assunto , Projetos de Pesquisa , Cicatrização
4.
Drug Deliv ; 26(1): 1104-1114, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31735104

RESUMO

Nanoemulgels are composed of O/W nanoemulsion and hydrogels and are considered as ideal carriers for the transdermal drug delivery because these have high affinity to load hydrophobic drugs. The stable formulation of eprinomectin (EPR) is very challenging because of it is high hydrophobic nature. In this work, we have prepared EPR loaded nanoemulgel for the treatment of endo- and ectoparasites. The surface morphology of optimized formulations was characterized by scanning electron microscopy. Additionally, skin permeability and irritation tests were conducted for in vitro safety and in vivo skin retention and pearmeation test of EPR nanoemulgel were conducted for efficacy study. Obtained results indicated that the optimized formulation had good shear-thinning behavior, bioadhesiveness properties, and are nanosized droplets with porous internal structure, which are required for topical application. Furthermore, this formulation has showed good skin permeability in comparison to suspension and has no skin irritating property. Overall, the obtained results proved that nanoemulgel is a promising carrier for transdermal drug delivery and EPR nanoemulgel is a promising formulation for the treatment of endo- and ectoparasites.


Assuntos
Emulsões/química , Géis/química , Ivermectina/análogos & derivados , Pele/metabolismo , Administração Cutânea , Animais , Portadores de Fármacos/química , Sistemas de Liberação de Medicamentos/métodos , Emulsões/administração & dosagem , Géis/administração & dosagem , Ivermectina/administração & dosagem , Ivermectina/química , Masculino , Camundongos , Camundongos Endogâmicos ICR , Nanopartículas/química , Permeabilidade , Ratos , Ratos Sprague-Dawley , Absorção Cutânea
5.
Drug Deliv ; 26(1): 952-964, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31544551

RESUMO

The objective of this work was to investigate phytantriol-based liquid crystal (LC) gels including cubic (Q2) and hexagonal (H2) phase for ocular delivery of pilocarpine nitrate (PN) to treat glaucoma. The gels were produced by a vortex method and confirmed by crossed polarized light microscopy, small-angle X-ray scattering, and rheological measurements. Moreover, the release behaviors and permeation results of PN from the gels were estimated using in vitro studies. Finally, the anti-glaucoma effect of LC gels was evaluated by in vivo animal experiments. The inner structure of the gels was Pn3m-type Q2 and H2 phase, and both of them showed pseudoplastic fluid properties based on characterization techniques. In vitro release profiles suggested that PN could be sustainably released from LC gels within 48 h. Compared with eye drops, Q2 and H2 gel produces a 5.25-fold and 6.23-fold increase in the Papp value (p < .05), respectively, leading to a significant enhancement of corneal penetration. Furthermore, a good biocompatibility and longer residence time on precorneal for LC gels confirmed by in vivo animal experiment. Pharmacokinetic studies showed that LC gels could maintain PN concentration in aqueous humor for at least 12 h after administration and remarkably improve the bioavailability of drug. Additionally, in vivo pharmacodynamics studies indicated that LC gels had a more significant intraocular pressure-lowering and miotic effect compared to eye drops. These research findings hinted that LC gels would be a promising pharmaceutical strategy for ocular application to enhance the efficacy of anti-glaucoma.


Assuntos
Córnea/efeitos dos fármacos , Géis/administração & dosagem , Géis/química , Glaucoma/tratamento farmacológico , Cristais Líquidos/química , Pilocarpina/administração & dosagem , Pilocarpina/química , Administração Oftálmica , Animais , Humor Aquoso/efeitos dos fármacos , Disponibilidade Biológica , Sistemas de Liberação de Medicamentos/métodos , Pressão Intraocular/efeitos dos fármacos , Masculino , Nanopartículas/química , Soluções Oftálmicas/administração & dosagem , Soluções Oftálmicas/química , Tamanho da Partícula , Permeabilidade/efeitos dos fármacos , Coelhos
6.
Int J Nanomedicine ; 14: 5555-5567, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31413562

RESUMO

Background: Vinpocetine (VPN) is a synthetic derivative of the Vinca minor alkaloids. The drug is characterized by a short half-life, limited water solubility and high hepatic first-pass effect. The objective was to develop different lipid-based nanocarriers (NCs) loaded into a thermosensitive in situ gelling (ISG) system to improve VPN bioavailability and brain targeting via intranasal (IN) delivery. Methods:  Different lipid-based NCs were developed and characterized for vesicle size, zeta potential, VPN entrapment efficiency (EE) and morphological characterization using transmission electron microscope (TEM). The prepared NCs were loaded into ISG formulations and characterized for their mucoadhesive properties. Ex-vivo permeation and histological study of the nasal mucosa were conducted. Pharmacokinetic and brain tissue distribution were investigated and compared to a marketed VPN product following administration of a single dose to rats. Results: VPN-D-α-Tocopherol polyethylene glycol 1000 succinate (TPGS) micelles nano-formulation showed the smallest particle size, highest EE among the studied NCs. TEM images revealed an almost spherical shape for all the prepared NCs. Among the NCs studied, VPN-loaded TPGS micelles demonstrated the highest percent cumulative VPN ex vivo permeation. All the prepared ISG formulations revealed the presence of mucoadhesive properties and showed no signs of inflammation or necrosis upon histological examination. Rats administered IN VPN-loaded TPGS-micelles ISG showed superior VPN concentration in the brain tissue and significant high relative bioavailability when compared to that received raw VPN-loaded ISG and marketed drug oral tablets. VPN-D-α-Tocopherol polyethylene glycol 1000 succinate (TPGS) micelles nano-formulation showed the smallest particle size, highest EE among the studied NCs. TEM images revealed an almost spherical shape for all the prepared NCs. Among the NCs studied, VPN-loaded TPGS micelles demonstrated the highest percent cumulative VPN ex vivo permeation. All the prepared ISG formulations revealed the presence of mucoadhesive properties and showed no signs of inflammation or necrosis upon histological examination. Rats administered IN VPN-loaded TPGS-micelles ISG showed superior VPN concentration in the brain tissue and significant high relative bioavailability when compared to that received raw VPN-loaded ISG and marketed drug oral tablets. Conclusion: VPN-loaded TPGS-micelles ISG formulation is a successful brain drug delivery system with enhanced bioavailability for drugs with poor bioavailability and those that are frequently administered.


Assuntos
Géis/administração & dosagem , Micelas , Temperatura Ambiente , Alcaloides de Vinca/administração & dosagem , Vitamina E/química , Administração Intranasal , Animais , Disponibilidade Biológica , Encéfalo/metabolismo , Bovinos , Portadores de Fármacos/química , Sistemas de Liberação de Medicamentos/métodos , Lipídeos/química , Masculino , Nanopartículas/química , Nanopartículas/ultraestrutura , Tamanho da Partícula , Ratos Sprague-Dawley , Solubilidade , Distribuição Tecidual , Alcaloides de Vinca/sangue , Alcaloides de Vinca/farmacocinética
8.
J Clin Ultrasound ; 47(9): 540-545, 2019 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-31206707

RESUMO

OBJECTIVES: Evaluate the time taken to visualize the internal jugular vein and carotid arteries, and subjective image quality assessed on a 0-100 visual analogic scale, on an ultrasound model using either traditional ultrasound gel or normal saline. METHODS: Twenty-two anesthesiology residents and twenty anesthesiology faculty were blinded and randomized into four separate groups using gel and saline as a conduction medium, in different sequences. RESULTS: Subjective image quality was 12.2 ± 4.2 better with gel than with saline (P < 0.01). Image acquisition time did not differ significantly between the two mediums. There was no significant difference in subjective image quality or time to image acquisition between faculty and residents. CONCLUSIONS: Internal jugular vein and carotid artery identification time using ultrasonography were similar between gel and saline as conduction mediums. The difference in subjective image quality did not appear clinically relevant. Better image quality resulted in less time taken to identify the structures, as expected. We conclude that saline may be an effective alternative medium to gel for vessel imaging and access guidance. Further study in a clinical setting is warranted.


Assuntos
Artérias Carótidas/diagnóstico por imagem , Géis/administração & dosagem , Veias Jugulares/diagnóstico por imagem , Solução Salina/administração & dosagem , Ultrassonografia/métodos , Feminino , Humanos , Masculino , Reprodutibilidade dos Testes , Fatores de Tempo
9.
J Orthop Surg Res ; 14(1): 166, 2019 May 30.
Artigo em Inglês | MEDLINE | ID: mdl-31146763

RESUMO

BACKGROUND: Bone fractures are one of the most common injuries in the USA. Fiberglass tape is a commonly used casting material, and many medical professionals apply adjuvants including liquid hand soap, foam sanitizers, and ultrasound gel in the hopes of improving outcomes relating to ease of molding and eventual strength, lamination, and smoothness of cast material. However, the efficacy of these agents to improve fiberglass cast mechanics has not been scientifically evaluated. The purpose of this study was to assess the mechanical effects of commonly used adjuvants on fiberglass cast materials. METHODS: Studies compared regularly shaped samples of water-activated, untreated fiberglass tape (Ossur Techform Premium) to water-activated fiberglass tape treated with one of three commonly used adjuvants (liquid soap, foam hand sanitizer, or ultrasound gel) during lamination. Material stiffness, yield stress, and ultimate load were measured by 3-point bending. RESULTS: These studies demonstrated that that liquid soap and ultrasound gel did not affect fiberglass tape mechanical properties, but alcohol-based foam sanitizer significantly reduced stiffness (- 32.8%), yield stress (- 33.6%), and ultimate load (- 31.0%) of the cast material as compared to the control group. Regression slopes were not significantly different between groups, suggesting that no adjuvants improved material curing time. CONCLUSIONS: These data suggest that the application of adjuvants is not beneficial and potentially harmful to fiberglass cast behavior. Despite the widespread practice of adjuvant application by medical professionals during casting, results from the current study suggest that use of these agents for structural enhancement of fiberglass casts is not beneficial and should largely be discouraged.


Assuntos
Moldes Cirúrgicos , Géis/administração & dosagem , Vidro , Higienizadores de Mão/administração & dosagem , Teste de Materiais/métodos , Sabões/administração & dosagem , Moldes Cirúrgicos/normas , Fraturas Ósseas/terapia , Vidro/normas , Humanos
10.
Acta Cir Bras ; 34(5): e201900504, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31166460

RESUMO

PURPOSE: To establish a new rat model, the pathogenesis of which is closer to the clinical occurrence of chronic obstructive jaundice with liver fibrosis. METHODS: 90 SD rats were randomly divided into 3 groups. Group A common bile duct ligation, group B common bile duct injection compont and group C injection saline. The serum of three groups was extracted, and the liver function was detected by ELISA. HE staining, Masson staining and immunohistochemistry were used to detect liver pathology. RESULTS: Group B showed a fluctuant development of jaundice, obstructive degree reached a peak at 2 weeks, and decreased from 3 weeks. HA, LA and PCIII were significantly higher than control group. 3 weeks after surgery, liver tissue fibrosis occurred in group B, and a wide range of fiber spacing was formed at 5 weeks. Immunohistochemistry showed that hepatic stellate cells were more active than the control group. CONCLUSION: Intra-biliary injection of Compont gel is different from the classic obstructive jaundice animal model caused by classic bile duct ligation, which can provide an ideal rat model of chronic obstructive jaundice with liver fibrosis.


Assuntos
Ductos Biliares/efeitos dos fármacos , Modelos Animais de Doenças , Géis/administração & dosagem , Icterícia Obstrutiva/induzido quimicamente , Cirrose Hepática/induzido quimicamente , Fosfatase Alcalina/sangue , Animais , Aspartato Aminotransferases/sangue , Compostos Azo , Ductos Biliares/patologia , Bilirrubina/análise , Ensaio de Imunoadsorção Enzimática , Amarelo de Eosina-(YS) , Feminino , Imuno-Histoquímica , Injeções , Icterícia Obstrutiva/patologia , Cirrose Hepática/patologia , Verde de Metila , Distribuição Aleatória , Ratos Sprague-Dawley , Valores de Referência , Reprodutibilidade dos Testes , Albumina Sérica/análise , Fatores de Tempo , gama-Glutamiltransferase/sangue
11.
AAPS PharmSciTech ; 20(6): 240, 2019 Jun 27.
Artigo em Inglês | MEDLINE | ID: mdl-31250221

RESUMO

Sunscreens are widely prescribed and used to prevent skin cancer; however, they have been reported to contain various chemicals which mimic hormones and disrupt hormonal functioning in humans. The aim of this study was to develop topical nanogel for skin cancer prevention using an antioxidant compound quercetin (Qu) and inorganic titanium dioxide (TiO2). Two formulations of Qu nanocrystals were optimized with low and high concentration of drug using the Box-Behnken design with the quadratic response surface model and further homogenized with TiO2. Qu nanocrystal (0.08% and 0.12%) formulations showed a particle size of 249.65 ± 2.84 nm and 352.48 ± 3.56 nm with zeta potential of - 14.7 ± 0.41 mV and - 19.6 ± 0.37 mV and drug content of 89.27 ± 1.39% and 90.38 ± 1.81% respectively. Scanning electron microscopy (SEM) images showed rod-shaped nanocrystals with a particle size below 400 nm. Qu (0.08%), Qu (0.12%), Qu (0.12%) + TiO2 (5%), and Qu (0.12%) + TiO2 (15%) nanogels showed over 70% drug release with significantly (p < 0.001) enhanced skin deposition of Qu as compare with Qu suspension within 24 h. The average numbers of tumor, tumor volume, and percentage of animals with tumors at onset in the Qu (0.12%) + TiO2 (15%) nanogel-pretreated group was found to be significantly (p < 0.05) less as compared with the UV only exposed group. Further, Qu (0.12%) + TiO2 (15%) nanogel significantly (p < 0.001) downregulated COX-2, EP3, EP4, PCNA, and cyclin D1 expressions in contrast to Qu and TiO2 only pretreated groups. Therefore, novel combination of Qu (0.12%) + TiO2 (15%) with enhanced skin deposition can be used as a chemopreventive strategy in UVB-induced skin photocarcinogenesis.


Assuntos
Quimioprevenção/métodos , Géis/administração & dosagem , Nanoestruturas/administração & dosagem , Neoplasias Induzidas por Radiação/prevenção & controle , Quercetina/farmacologia , Neoplasias Cutâneas/prevenção & controle , Pele/efeitos dos fármacos , Protetores Solares/farmacologia , Titânio/farmacologia , Raios Ultravioleta , Administração Tópica , Animais , Combinação de Medicamentos , Liberação Controlada de Fármacos , Humanos , Tamanho da Partícula , Polietilenoglicóis/química , Quercetina/administração & dosagem , Quercetina/química , Pele/metabolismo , Protetores Solares/administração & dosagem , Titânio/administração & dosagem
12.
Eur J Pharm Sci ; 136: 104956, 2019 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-31202895

RESUMO

The objective of present study was to develop hydrogel based nanoemulsion (NE) drug delivery system for transdermal delivery and evaluate its potential in in vivo anti-osteoporotic activity. NE was prepared using aqueous phase titration method and characterized for droplet size, zeta potential and morphology. It was then formulated into hydrogel based NE gel using carbopol 940 as gelling agent. NE gel was evaluated for pH, viscosity, in vitro/ex vivo permeation studies and in vivo anti-osteoporotic activity. The results indicated formation of spherical, nano sized globules of NE ranging from 11.17 ±â€¯0.24 to 128.8 ±â€¯0.16 nm with polydispersity of <0.5. In vitro and ex vivo permeation studies showed significantly higher permeation of NE as well as NE gel in comparison to fluvastatin solution indicating that NE gel can effectively penetrate through skin layers. In vivo anti-osteoporotic results demonstrated formation of new bone in trabecular region of osteoporotic rat femurs through micro-CT scanning radiographs. Biomechanical strength testing demonstrated greater load bearing capacity of rat femurs in the treated animals in comparison with the osteoporotic group. Thus, developed NE gel formulation of fluvastatin demonstrated greater potential for transdermal delivery and in the treatment of osteoporosis.


Assuntos
Emulsões/administração & dosagem , Fluvastatina/administração & dosagem , Géis/administração & dosagem , Osteoporose/tratamento farmacológico , Resinas Acrílicas/química , Administração Cutânea , Animais , Portadores de Fármacos/química , Sistemas de Liberação de Medicamentos/métodos , Emulsões/química , Fluvastatina/química , Géis/química , Nanopartículas/administração & dosagem , Nanopartículas/química , Nanotecnologia/métodos , Tamanho da Partícula , Ratos , Pele/metabolismo , Absorção Cutânea/efeitos dos fármacos , Viscosidade/efeitos dos fármacos
13.
Colloids Surf B Biointerfaces ; 181: 623-631, 2019 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-31202972

RESUMO

There is a growing clinical demand for topical itraconazole (ITC) delivery systems because of the expanding potential of the drug for topical fungal and non-fungal applications. Lipid-based nanocarriers offer great promise in this respect. In the present study, a new topical ITC gel based on lipid nanocapsules (LNC) was developed. ITC-LNC were compared to ITC-loaded nanostructured lipid carriers (ITC-NLC) with more established benefits as topical vectors. Both nanocarriers showed high entrapment efficiency (EE > 98%). Compared to ITC-NLC, the ITC-LNC showed a significantly smaller particle size (∼50 vs 155 nm), narrower size distribution (0.09 vs 0.38), faster initial release rate under sink conditions and greater in vitro antifungal activity against Candida albicans (C. albicans) (inhibition zone 29.4 vs 26.4 mm). ITC-LNC and ITC-NLC-based gels significantly enhanced the dermal retention of ITC in excised human skin relative to a conventional ITC gel. Histopathological assessment of a 14-day treatment of induced cutaneous candidiasis in a rat model indicated efficacy of the gel preparations. Fungal elements developed in the superficial epidermal skin layer were cleared by the end of treatment. Equally important, no histopathological changes in the epidermal and dermal layers of rat skin were observed. Findings of this study verified efficacy of topical ITC in the treatment of superficial fungal infections as well as effectiveness of LNC as biomimetic nanocarrier for dermal drug delivery. Combining ITC and LNC would present a bioactive nanocarrier system with good potentials for fungal infections and other skin applications.


Assuntos
Antifúngicos/farmacologia , Candidíase/tratamento farmacológico , Itraconazol/farmacologia , Lipídeos/farmacologia , Pele/efeitos dos fármacos , Administração Cutânea , Adulto , Animais , Antifúngicos/administração & dosagem , Sistemas de Liberação de Medicamentos , Liberação Controlada de Fármacos , Géis/administração & dosagem , Géis/farmacologia , Humanos , Itraconazol/administração & dosagem , Lipídeos/administração & dosagem , Masculino , Pessoa de Meia-Idade , Nanocápsulas/administração & dosagem , Nanocápsulas/química , Tamanho da Partícula , Ratos , Ratos Wistar , Pele/metabolismo , Absorção Cutânea/efeitos dos fármacos , Propriedades de Superfície
14.
Ars pharm ; 60(2): 101-108, abr.-jun. 2019. graf, tab, ilus
Artigo em Inglês | IBECS | ID: ibc-186013

RESUMO

Purpose: The purpose of this study was to develop and evaluate nanoemulsion-based gel (nanogel) for transdermal delivery of ketoprofen. Among the various excipients tested, oleic acid, tween 80 and ethanol were selected as oil, surfactant, and co-surfactant respectively. Methods: The nanoemulsions region was identified by constructing pseudo-ternary phase diagrams using aqueous phase titration. The prepared nanoemulsion was subjected to different thermodynamic stability study and the nanoemulsion that passed thermodynamic stability tests were evaluated for viscosity, refractive index, droplet size, transmission electron microscopy, and ex-vivo permeation study using human cadaver skin. Results: On the basis of evaluation C1 formulation, which consists of 3.09 % wt/wt of the oil phase, 60.54 % wt/wt of Smix and 36.36 % wt/wt of distilled water were selected as an optimized formulation and were converted to nanogel using chitosan as a gelling agent. Nanogel was evaluated for ex-vivo and in vivo study. The nanogel showed a significant increase in the anti-inflammatory activity as compared to conventional gel. Conclusion: In conclusion, nanogel could be a promising system to improve transdermal delivery of the ketoprofen


Objetivo: El objetivo de este estudio fue desarrollar y evaluar un gel a base de nanoemulsión (nanogel) para el suministro transdérmico de ketoprofeno. Entre los diversos excipientes probados, se seleccionaron el ácido oleico, la mezcla de 80 y el etanol como aceite, surfactante y co-surfactante. Métodos: La región de las nanoemulsiones se identificó mediante la construcción de diagramas de fase pseudoternarios utilizando la titulación de la fase acuosa. La nanoemulsión preparada se sometió a di¬ferentes estudios de estabilidad termodinámica y la nanoemulsión que pasó las pruebas de estabilidad termodinámica se evaluó para determinar la viscosidad, el índice de refracción, el tamaño de las gotitas, la microscopía electrónica de transmisión y el estudio de permeación ex-vivo utilizando piel de cadáver humano. Resultados: Sobre la base de la evaluación, la formulación de C1, que consiste en 3.09% peso / peso de la fase oleosa, 60.54% peso / peso de Smix y 36.36% peso / peso de agua destilada se seleccionaron como una formulación optimizada y se convirtieron a nanogel utilizando quitosano como Un agente gelificante. Nanogel se evaluó para estudio ex-vivo e in vivo. El nanogel mostró un aumento significativo en la actividad antiinflamatoria en comparación con el gel convencional. Conclusión: En conclusión, el nanogel podría ser un sistema prometedor para mejorar la administración transdérmica del ketoprofeno


Assuntos
Humanos , Cetoprofeno/administração & dosagem , Cetoprofeno/química , Dor/tratamento farmacológico , Géis/administração & dosagem , Géis/química , Emulsões/administração & dosagem , Emulsões/química , Administração Cutânea , Viscosidade , Cadáver , Solubilidade
15.
J Assist Reprod Genet ; 36(7): 1481-1487, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-31104292

RESUMO

PURPOSE: To compare outcomes between daily intramuscular progesterone (IMP) and daily vaginal progesterone (VP) gel plus weekly intramuscular hydroxyprogesterone caproate (IMHPC) for luteal phase support (LPS) in single, autologous euploid frozen-thawed blastocyst transfers (FBTs) following artificial endometrial preparation (EP). METHODS: The retrospective cohort study included 767 single, autologous FBTs from 731 patients between January 2015 and March 2018. LPS was performed either with IMP (100 mg/day) or with VP gel (90 mg, twice daily) plus IMHPC (250 mg/week). Oral estrogen was prescribed in combination of both regimes. Oral estrogen was discontinued following the visualization of fetal cardiac activity on ultrasound and progesterone at 10 weeks of gestation. The primary outcome was live birth rate. The secondary outcomes included implantation, clinical pregnancy, and multiple pregnancy rates. RESULTS: Patient characteristics did not differ in LPS regimes. Of 767 FBTs, 608 had IMP (100 mg/day) for LPS and 159 had VP gel (90 mg, twice daily) plus IMHPC (250 mg/week) for LPS. The live birth rate was 51.8% and 50.3%, respectively (p = 0.737, OR 0.94, 95%CI 0.66-1.33). The implantation rate was 62.7% and 64.2%, respectively (p = 0.730, OR 1.06, 95%CI 0.74-1.53). The clinical pregnancy rates were also similar in both groups (59.5% vs. 61.6%, respectively, p = 0.631, OR 1.09, 95%CI 0.76-1.56). CONCLUSIONS: We did not observe significant differences in the rates of live birth, implantation, and clinical pregnancy between daily IMP and daily VP gel plus weekly IMHPC for LPS in single, autologous euploid FBTs after artificial EP.


Assuntos
Fertilização In Vitro , Infertilidade/tratamento farmacológico , Progesterona/administração & dosagem , Transferência de Embrião Único , Administração Intravaginal , Adulto , Blastocisto/efeitos dos fármacos , Criopreservação , Implantação do Embrião/efeitos dos fármacos , Feminino , Géis/administração & dosagem , Humanos , Infertilidade/patologia , Injeções Intramusculares , Fase Luteal/efeitos dos fármacos , Fase Luteal/genética , Gravidez , Taxa de Gravidez , Progesterona/análogos & derivados
16.
J Pharm Pharmacol ; 71(8): 1209-1221, 2019 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-31124593

RESUMO

OBJECTIVES: The aim of the current study was to minimize ocular irritation and prolong the pharmacological action of vancomycin via formulation into nanosized spherical niosomes loaded into pH-sensitive in-situ forming gel. METHODS: Stability and rheological behaviour of the various gelling systems were evaluated. The ability of the selected system to eradicate methicillin-resistant Staphylococcus aureus (MRSA) infections was examined in vitro and in vivo. Draize technique was also used to assess ocular irritation in rabbits. KEY FINDINGS: Nanosized spherical niosomes loaded with vancomycin at high entrapment efficiency were prepared and integrated into polymeric solution that forms gel in situ upon instillation into the eye, to allow for a further increase in the ocular residence time. In MRSA-infected rabbits, there were 180- and 2.5-fold increases in the antibacterial efficacy after treatment with the vancomycin niosomal gels in comparison with the untreated animals and the animals treated with the vancomycin free drug solution, respectively. CONCLUSIONS: The developed formulations demonstrated promising in-vivo biocompatibility and antibacterial efficacy, signifying their potential application as ophthalmic preparation to overcome ocular infections induced by resistant bacterial strains while minimizing drug irritation and improving patient compliance.


Assuntos
Infecções Oculares/tratamento farmacológico , Géis/administração & dosagem , Géis/química , Lipossomos/química , Vancomicina/administração & dosagem , Vancomicina/química , Animais , Antibacterianos/administração & dosagem , Antibacterianos/química , Portadores de Fármacos/química , Composição de Medicamentos/métodos , Sistemas de Liberação de Medicamentos/métodos , Olho/microbiologia , Infecções Oculares/microbiologia , Feminino , Concentração de Íons de Hidrogênio , Staphylococcus aureus Resistente à Meticilina/efeitos dos fármacos , Tamanho da Partícula , Coelhos , Infecções Estafilocócicas/tratamento farmacológico , Infecções Estafilocócicas/microbiologia
17.
Int J Radiat Oncol Biol Phys ; 104(5): 1141-1152, 2019 08 01.
Artigo em Inglês | MEDLINE | ID: mdl-31063799

RESUMO

PURPOSE: Despite the development of high-precision radiation therapy, ionizing radiation inevitably damages healthy tissues. Radiodermatitis and radioinduced oral mucositis are frequent and significant side effects among patients with breast and head and neck cancer, respectively. These radiation-related injuries negatively affect patient quality of life and can lead to unplanned therapeutic breaks and compromise treatment outcomes. Currently, no preventive or mitigating agent has emerged to address these issues. Although amifostine, a well-known free radical scavenger, has proven efficacy against specific radio- and chemo-induced toxicities, severe adverse side effects (reversible hypotension, nausea, emesis, etc) combined with logistical hurdles are associated with its recommended intravenous route of administration, limiting its use. METHODS AND MATERIALS: We developed a thermogel containing the active thiol metabolite of amifostine (CPh-1014) that polymerizes at body temperature and serves as a matrix for topical application onto the skin or mucosa. RESULTS: Applied before irradiation, CPh-1014 greatly reduced the severity of oral mucositis and dermatitis induced by either a single dose or fractionated irradiation regimens in in vivo mouse models. The cytoprotective effect of CPh-1014 was confirmed by the decrease in DNA double-strand breaks in the irradiated epithelium. Noticeably, CPh-1014 did not affect radiation therapy efficacy against tumors grafted at submucosal and subcutaneous sites. In contrast to the intravenous administration of amifostine, CPh-1014 oral application did not induce hypotension in dogs. CONCLUSIONS: CPh-1014 confers radioprotective effects in healthy tissues with reduced systemic side effects without compromising radiation therapy efficacy. We propose CPh-1014 as an easy-to-implement therapeutic approach to alleviate radiation therapy toxicity in patients with breast and head and neck cancer.


Assuntos
Amifostina/administração & dosagem , Géis/administração & dosagem , Lesões Experimentais por Radiação/prevenção & controle , Protetores contra Radiação/administração & dosagem , Radiodermatite/prevenção & controle , Estomatite/prevenção & controle , Amifostina/efeitos adversos , Animais , Pressão Sanguínea/efeitos dos fármacos , Neoplasias da Mama/radioterapia , Dano ao DNA , Modelos Animais de Doenças , Cães , Portadores de Fármacos , Feminino , Neoplasias de Cabeça e Pescoço/radioterapia , Hipotensão Ortostática/induzido quimicamente , Camundongos , Camundongos Endogâmicos C57BL , Lesões Experimentais por Radiação/tratamento farmacológico , Protetores contra Radiação/efeitos adversos , Radiodermatite/tratamento farmacológico , Distribuição Aleatória , Neoplasias Cutâneas/radioterapia , Estomatite/tratamento farmacológico , Estomatite/etiologia
18.
Nutrients ; 11(4)2019 Apr 25.
Artigo em Inglês | MEDLINE | ID: mdl-31027246

RESUMO

We aimed to explore the effects of caffeinated gel ingestion on neuromuscular performance in resistance-trained men. The participants (n = 17; mean ± standard deviation (SD): age 23 ± 2 years, height 183 ± 5 cm, body mass 83 ± 11 kg) completed two testing conditions that involved ingesting a caffeinated gel (300 mg of caffeine) or placebo. The testing outcomes included: (1) vertical jump height in the squat jump (SJ) and countermovement jump (CMJ); (2) knee extension and flexion peak torque and average power at angular velocities of 60°·s-1 and 180°·s-1; (3) barbell velocity in the bench press with loads corresponding to 50%, 75%, and 90% of one-repetition maximum (1RM); and (4) peak power output in a test on a rowing ergometer. Compared to the placebo, caffeine improved: (1) SJ (p = 0.039; Cohen's d effect size (d) = 0.18; +2.9%) and CMJ height (p = 0.011; d = 0.18; +3.3%); (2) peak torque and average power in the knee extensors at both angular velocities (d ranged from 0.21 to 0.37; percent change from +3.5% to +6.9%), peak torque (p = 0.034; d = 0.24; +4.6%), and average power (p = 0.015; d = 0.32; +6.7%) at 60°·s-1 in the knee flexors; (3) barbell velocity at 50% 1RM (p = 0.021; d = 0.33; +3.5%), 75% 1RM (p < 0.001; d = 0.42; +5.4%), and 90% 1RM (p < 0.001; d = 0.59, +12.0%). We conclude that the ingestion of caffeinated gels may acutely improve vertical jump performance, strength, and power in resistance-trained men.


Assuntos
Desempenho Atlético , Cafeína/farmacologia , Géis/administração & dosagem , Força Muscular/efeitos dos fármacos , Músculo Esquelético/efeitos dos fármacos , Adulto , Cafeína/administração & dosagem , Estudos Cross-Over , Método Duplo-Cego , Humanos , Masculino , Adulto Jovem
19.
J Cancer Res Ther ; 15(2): 415-419, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-30964120

RESUMO

Background: Natural orifice transluminal endoscopic surgery (NOTES) is a minimal invasive treatment. However, tissue dissection under endoscopy is still challenging due to the flexibility of endoscopy body and there is still no effective method for establishing a tunnel towards the targeted area. We previously showed that a new kind of thermogel could be submucosallly injected and served as a cushion for endoscopic dissection. Thus, in this study we investigated the feasibility and safety of tunnel creation using poly (lactic acid-co-glycolic acid)-poly (ethylene glycol)-poly (lactic acid-co-glycolic acid) (PLGA-PEG-PLGA) thermogel for NOTES in a porcine model. Methods: We prepared an injectable thermogel composed of PLGA-PEG-PLGA triblock copolymers which exhibited a low-viscous sol at room temperature and spontaneously transformed into a no-flowing gel at body temperature. This thermogel was used in NOTES in pigs. The success rate and adverse events were observed. Results: The PLGA-PEG-PLGA thermogels were successfully injected to the targeted areas under the guide of endoscopic ultrasonography and the tunnels were created by sucking the gel during NOTES as the endoscopy went forwards in all the three animals. The necropsy of the pigs showed no evidence of iatrogenic injury. No serious bleeding and perforation was observed. The results demonstrated that thermogel injection and tunnel creation by suction during NOTES were feasible, which simplified the procedure of tissue dissection and developed a new method of identifying the targeted area for surgical interventions without causing severe tissue damage. Conclusion: The application of thermogel for tunnel creation in NOTES could optimize current procedures and may have a promising prospect in clinical application.


Assuntos
Modelos Animais de Doenças , Géis , Cirurgia Endoscópica por Orifício Natural , Neoplasias/cirurgia , Polietilenoglicóis , Poliglactina 910 , Animais , Géis/administração & dosagem , Masculino , Cirurgia Endoscópica por Orifício Natural/efeitos adversos , Cirurgia Endoscópica por Orifício Natural/métodos , Neoplasias/diagnóstico , Polietilenoglicóis/química , Poliglactina 910/química , Cirurgia Assistida por Computador , Suínos , Resultado do Tratamento , Ultrassonografia
20.
Carbohydr Polym ; 214: 131-141, 2019 Jun 15.
Artigo em Inglês | MEDLINE | ID: mdl-30925981

RESUMO

Progress at elimination of malaria is limited by the challenges of reaching large rural population and ensuring patient adherence to adequate pharmacologic treatment. In the present study, a novel material (octadecylamine modified chondroitin sulfate) was synthesized, to fabricate a long acting release meshy gel system as an efficient weapon for protracted warfare to malaria. Ivermectin loaded meshy gels (IVM-MG) composed of different amount of phospholipids, triglyceride and modified chondroitin sulfate were formulated. They were in aqueous state with low viscosity before injection, but rapidly turned into gel state with significantly increased viscosity upon exposure to an aqueous environment after injection. In vitro study proved a sustained released effect in different releasing media. In vivo study showed no irritation at injection site and slowly drug release over a 30-day release period in rat model. Among the three IVM-MG formulations, IVM-MG-3 with the highest amount of octadecylamine modified chondroitin sulfate presented the highest viscosity increase after solution-gel transition, the least initial burst release, and the longest sustained release effect over 30 days in rat model. Furthermore, by using mathematical models, IVM-MG system could boost the efficacy of mass drug administration toward malaria elimination goals. Meshy gel systems for long-acting drug delivery have the potential to revolutionize treatment options for malaria and other diseases of which treatment adherence is essential for their efficacy.


Assuntos
Aminas/química , Antimaláricos/farmacocinética , Sulfatos de Condroitina/química , Portadores de Fármacos/química , Géis/química , Ivermectina/farmacocinética , Aminas/administração & dosagem , Aminas/síntese química , Animais , Antimaláricos/administração & dosagem , Sulfatos de Condroitina/administração & dosagem , Sulfatos de Condroitina/síntese química , Culicidae/efeitos dos fármacos , Preparações de Ação Retardada/administração & dosagem , Preparações de Ação Retardada/síntese química , Preparações de Ação Retardada/química , Portadores de Fármacos/administração & dosagem , Portadores de Fármacos/síntese química , Liberação Controlada de Fármacos , Etanol/efeitos adversos , Etanol/química , Géis/administração & dosagem , Géis/síntese química , Injeções , Inseticidas/administração & dosagem , Inseticidas/farmacocinética , Ivermectina/administração & dosagem , Masculino , Camundongos , Modelos Teóricos , Ratos Wistar , Pele/patologia , Substâncias Viscoelásticas/administração & dosagem , Substâncias Viscoelásticas/síntese química , Substâncias Viscoelásticas/química , Viscosidade
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