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1.
AAPS PharmSciTech ; 20(7): 297, 2019 Aug 23.
Artigo em Inglês | MEDLINE | ID: mdl-31444661

RESUMO

Miconazole nitrate (MZ) is a BCS class II antifungal poorly water-soluble drug with limited dissolution properties and gastrointestinal side effects. Self-nanoemulsifying delivery system-based gel of MZ can improve both solubility and oral mucosal absorption with enhanced antifungal activity. The study aims to formulate MZ self-nanoemulsion (MZ-NE) and combine it within hyaluronic acid-based gel. MZ solubility in various oils, surfactants, and cosurfactant used in NE formulations were evaluated. Mixture design was implemented to optimize the levels of NE components as a formulation variable to study their effects on the mean globule size and antifungal inhibition zones. Further, the optimized MZ-NE was loaded into a hyaluronic acid gel base. Rheological behavior of the prepared gel was assessed. Ex vivo permeability of optimized formulation across buccal mucous of sheep and inhibition against Candida albicans were examined. Mixture design was used to optimize the composition of MZ-NE formulation as 22, 67, and 10% for clove oil, Labrasol, and propylene glycol, respectively. The optimized formulation indicated globule size of 113 nm with 29 mm inhibition zone. Pseudoplastic flow with thixotropic behavior was observed, which is desirable for oral gels. The optimized formulation exhibited higher ex vivo skin permeability and enhanced antifungal activity by 1.85 and 2.179, respectively, compared to MZ-SNEDDS, and by 1.52 and 1.72 folds, respectively, compared to marketed gel. Optimized MZ-NE hyaluronic acid-based oral gel demonstrated better antifungal activity, indicating its potential in oral thrush pharmacotherapy.


Assuntos
Antifúngicos/administração & dosagem , Candidíase Bucal/tratamento farmacológico , Química Farmacêutica/métodos , Ácido Hialurônico/administração & dosagem , Miconazol/administração & dosagem , Nanocápsulas/administração & dosagem , Administração Oral , Animais , Antifúngicos/síntese química , Antifúngicos/farmacocinética , Candidíase Bucal/metabolismo , Sistemas de Liberação de Medicamentos/métodos , Avaliação Pré-Clínica de Medicamentos/métodos , Emulsões/administração & dosagem , Emulsões/síntese química , Emulsões/farmacocinética , Ácido Hialurônico/síntese química , Ácido Hialurônico/farmacocinética , Hidrogéis/administração & dosagem , Hidrogéis/síntese química , Hidrogéis/farmacocinética , Miconazol/síntese química , Miconazol/farmacocinética , Nanocápsulas/química , Ovinos
2.
J Taibah Univ Med Sci ; 19(2): 403-421, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38405382

RESUMO

The graphene family of nanomaterials acquired significant attention in the field of dentistry due to a range of interesting properties. Graphene oxide (GO) and reduced graphene oxide (rGO) are the major graphene derivatives that are widely used in dental applications. These derivatives exhibit excellent mechanical properties, superior biocompatibility, good antibacterial properties, extreme chemical stability, and favorable tribological characteristics, thus representing highly materials for dentistry. The amphiphilic nature of GO allows covalent and noncovalent modifications that are favorable for biomedical applications. Graphene can influence the differentiation of dental pulp stem cells (DPSCs) and enhance the properties of other biomaterials. Here, we review the dental applications of GO or rGO with regards to antimicrobial activity, therapeutic drug delivery, restorative dentistry, implants, pulp regeneration, bone regeneration, periodontal tissue regeneration, biosensors, and tooth whitening.

3.
Int J Biol Macromol ; 259(Pt 2): 129190, 2024 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-38185304

RESUMO

Urease is one of the most significant enzymes in the industry. The objective of this research was to isolate and partially purify urease from Vicia sativa seeds with urease characterization. With a 6.4 % yield, the purification fold was 9.0. By using chromatography, it was determined that the isolated urease had a molecular weight of 55 kDa. The maximum urease activity was found following a 60-s incubation period at 40 °C and pH 8. The activity of urease was significantly boosted by a mean of calcium, barium, DL-dithiothreitol, Na2EDTA, and citrate (16.9, 26.6, 18.6, 13.6, and 31 %), respectively. But nickel and mercury caused inhibitory effects and completely inhibited urease activity, indicating the presence of a thiol (-SH) group in the enzyme active site. The Arrhenius plot was used to analyze the thermodynamic constants of activation, Ea, ΔH*, ΔG*, and ΔS*. The results showed that the values were 30 kJ/mol, 93.14 kJ/mol, 107.17 kJ/mol/K, and -40.80 J/mol/K, respectively. The significance of urease extraction from various sources may contribute to our understanding of the metabolism of urea in plants. The current report has novelty as it explained for the first time the kinetics and thermodynamics of hydrolysis of urea and inactivation of urease from V. sativa seeds.


Assuntos
Urease , Vicia sativa , Urease/metabolismo , Vicia sativa/metabolismo , Termodinâmica , Sementes/metabolismo , Ureia/metabolismo , Cinética , Concentração de Íons de Hidrogênio
4.
Drug Deliv ; 30(1): 2184311, 2023 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-36846914

RESUMO

Numerous problems affect oral health, and intensive research is focused on essential oil-based nanoemulsions that might treat prevent or these problems. Nanoemulsions are delivery systems that enhance the distribution and solubility of lipid medications to targeted locations. Turmeric (Tur)- and curry leaf oil (CrO)-based nanoemulsions (CrO-Tur-self-nanoemulsifying drug delivery systems [SNEDDS]) were developed with the goal of improving oral health and preventing or treating gingivitis. They could be valuable because of their antibacterial and anti-inflammatory capabilities. CrO-Tur-SNEDDS formulations were produced using the response surface Box-Behnken design with different concentrations of CrO (120, 180, and 250 mg), Tur (20, 35, and 50 mg), and Smix 2:1 (400, 500, and 600 mg). The optimized formulation had a bacterial growth inhibition zone of up to 20 mm, droplet size of less than 140 nm, drug-loading efficiency of 93%, and IL-6 serum levels of between 950 ± 10 and 3000 ± 25 U/ml. The optimal formulation, which contained 240 mg of CrO, 42.5 mg of Tur, and 600 mg of Smix 2:1, was created using the acceptable design. Additionally, the best CrO-Tur-SNEDDS formulation was incorporated into a hyaluronic acid gel, and thereafter it had improved ex-vivo transbuccal permeability, sustained in-vitro release of Tur, and large bacterial growth suppression zones. The optimal formulation loaded into an emulgel had lower levels of IL-6 in the serum than the other formulations evaluated in rats. Therefore, this investigation showed that a CrO-Tur-SNEDDS could provide strong protection against gingivitis caused by microbial infections.


Assuntos
Ácido Hialurônico , Nanopartículas , Animais , Ratos , Administração Oral , Curcuma , Sistemas de Liberação de Medicamentos , Emulsões , Interleucina-6 , Tamanho da Partícula , Folhas de Planta , Projetos de Pesquisa , Solubilidade , Gengivite
5.
Metabolites ; 14(1)2023 Dec 30.
Artigo em Inglês | MEDLINE | ID: mdl-38248830

RESUMO

The main purpose of this work is to investigate the phytochemical composition of Marrubium alysson L. non-polar fraction. GC/MS analysis was used to evaluate the plant extract's saponifiable and unsaponifiable matter. Although M. alysson L. lipoidal matter saponification produced 30.3% of fatty acid methyl esters and 69.7% of unsaponifiable matter. Phytol was the most dominant substance in the unsaponifiable materials. Notably, marrubiin which is one of the most prominent metabolites of Marrubium alysson L. was not detected through our adopted GC/MS technique. Thus, further characterization was proceeded through simple and rapid HPTLC analysis which successfully managed to identify marrubiin. Based on the regression equation, the concentration of marrubiin in M. alysson L. extract was 14.09 mg/g of dry extract. Concerning acetylcholinesterase inhibitory activity, both the crude M. alysson L. total methanolic extract and the non-polar fraction displayed reasonable inhibitory activity against acetylcholinesterase (AChE), whereas the pure compound marrubiin was considered to be the most effective and potent AChE inhibitor, with an IC50 value of 52.66 (µM). According to the molecular docking studies, potential sites of interaction between the pure chemical marrubiin and AChE were examined. The results show that Tyr124 on AChE residue was critical to the activity of the aforementioned drug. Based on the depicted marrubin AChE inhibition activity and reported safety profile, this chemical metabolite is considered as a promising lead compound for further pre-clinical investigation as well as drug development and optimization.

6.
Drug Deliv ; 30(1): 2173337, 2023 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-36708105

RESUMO

The use of essential oil-based nanoemulsions (NEs) has been the subject of extensive research on a variety of conditions affecting the oral cavity. NEs are delivery methods that improve the solubility and distribution of lipid medicines to the intended areas. Because of their antibacterial and antifungal properties, itraconazole and thyme oil-based self-nanoemulsifying drug delivery systems (ItZ-ThO-SNEDDS) were created to protect oral health against oral microorganisms. The ItZ-ThO-SNEDDS were created utilizing an extreme verices mixture design, and varying concentrations of ThO (10% and 25%), labrasol (40% and 70%), and transcutol (20% and 40%) were used. The ItZ-ThO-SNEDDS had droplet sizes of less than 250 nm, a drug-loading efficiency of up to 64%, and a fungal growth inhibition zone of up to 20 mm. The accepted design was used to obtain the ideal formulation, which contained ThO in the amount of 0.18 g/ml, labrasol 0.62 g/ml, and transcutol 0.2 g/ml. The best ItZ-ThO-SNEDDS formulation was incorporated into a honey-based gel, which demonstrated improved release of ItZ in vitro and improved transbuccal permeation ex vivo. In addition, when compared with various formulations tested in rats, the optimized loaded emulgel decreased the ulcer index. This study therefore demonstrated that the ItZ-ThO-SNEDDS could offer an effective defense against oral diseases caused by microbial infections.


Assuntos
Candidíase Bucal , Mel , Nanopartículas , Ratos , Animais , Itraconazol/farmacologia , Tensoativos , Emulsões , Sistemas de Liberação de Medicamentos/métodos , Solubilidade , Administração Oral , Tamanho da Partícula
7.
J Clin Med ; 11(15)2022 Jul 30.
Artigo em Inglês | MEDLINE | ID: mdl-35956079

RESUMO

BACKGROUND: COVID-19, caused by SARS-CoV-2, has impacted the world in an unprecedented way since December 2019. SARS-CoV-2 was found in the saliva of patients, and entry points for the virus may have been through the numerous angiotensin-converting enzyme 2 receptors in the oral cavity. Oral manifestations of COVID-19 could contribute to the burden of oral disease. OBJECTIVE: To determine the prevalence of oral manifestations of COVID-19 in patients and their association with disease severity. METHODS: Interviews were conducted with adult participants diagnosed with COVID-19 between October 2021 and March 2022 to document their demographic and health status data, symptoms, and the presence of oral manifestations of COVID-19. Chi-square and the Fisher's exact test were used to compare data on the presence or absence of oral manifestations of COVID-19. RESULTS: Of 195 participants interviewed, 33% were 18 to 24 years old, 33% were 25 to 34 years old, and 75% were female. A total of 57 (29%) had oral manifestations; the most common were taste disorders (60%), xerostomia (42%), and oral ulcers (11%). There was no relationship between the severity of COVID-19 and the presence of the oral manifestations. CONCLUSION: Oral manifestations of COVID-19 were common among female patients and linked to certain general COVID-19 symptoms regarding frequency and extent.

8.
Am J Case Rep ; 23: e936585, 2022 Aug 16.
Artigo em Inglês | MEDLINE | ID: mdl-35972908

RESUMO

BACKGROUND Multiple myeloma is a hematological malignancy characterized by monoclonal plasma cell proliferation. Jaw lesions are found in nearly 35% of patients with symptomatic myeloma, and lesions occur in the mandible more often than in the maxilla. However, maxillary or mandibular lesions are rarely found as a primary manifestation of the disease. This report describes a case of a 65-year-old Palestinian woman with lytic lesions in the maxilla due to undiagnosed multiple myeloma identified incidentally on cone beam computed tomography (CBCT). CASE REPORT A 65-year-old Palestinian woman presented to the Oral Maxillofacial Surgery Clinic with an expansion of the maxilla which was initially thought of as an infection. CBCT imaging revealed diffuse osteolytic lesions involving multiple osseous structures. The patient was biopsied. Histopathological examination was suspicious for plasmacytic neoplasm. She was directly referred to the Hematology Department for further laboratory tests. These included complete blood count, liver function test, bone profile, protein electrophoresis, flow cytometry, and bone marrow biopsy, which were performed to confirm the diagnosis of multiple myeloma. The patient was treated with chemotherapy including zoledronic acid, dexamethasone, bortezomib, and cyclophosphamide. She went into remission for a year but unfortunately died 2 years later. CONCLUSIONS Primary myeloma of the maxilla is a rare presentation. The present report illustrates the role of CBCT imaging supported by a multidisciplinary approach to the diagnosis and management of myeloma. Consequently, it is recommended that dental practitioners be aware of radiographic features and possible oral manifestations to avoid any delay in medical intervention.


Assuntos
Mieloma Múltiplo , Idoso , Tomografia Computadorizada de Feixe Cônico , Odontólogos , Feminino , Humanos , Maxila/diagnóstico por imagem , Maxila/patologia , Mieloma Múltiplo/diagnóstico por imagem , Mieloma Múltiplo/patologia , Papel Profissional
9.
Artigo em Inglês | MEDLINE | ID: mdl-35162473

RESUMO

(1) Background: COVID-19 has had psychological impacts, particularly anxiety, depression, anger, and suicidal ideation, on the world's populace, including young persons who were prone to mental health disorders even before the pandemic. We described the psychological impacts of COVID-19 among emerging adults aged 18-30 years in Saudi Arabia. (2) Methods: A cross-sectional survey was done among a randomly sampled population in Saudi Arabia between July 2020 and May 2021 using the DSM-5 Self-rated Level 1 Cross-Cutting Symptom Measure and Ask Suicide Questionnaire. Logistic regression was used to assess participant characteristics associated with reporting symptoms of mental disorders under each of the 13 domains that would warrant further investigation. (3) Results: Approximately, 91% of participants experienced different mental health symptoms; these participants are more likely to be young, female students, those who had a history of being diagnosed with a mental disorder, and those diagnosed or treated for COVID-19. (4) Conclusion: This study strongly showed an increased prevalence of mental health symptoms among young persons during the COVID-19 pandemic. Addressing the mental health burden among young persons in time using simple, self-administered screening tools linked to interventions will prevent dire consequences in the future.


Assuntos
COVID-19 , Pandemias , Adolescente , Adulto , Ansiedade , Estudos Transversais , Depressão/epidemiologia , Feminino , Humanos , SARS-CoV-2 , Adulto Jovem
10.
Gels ; 8(6)2022 Jun 16.
Artigo em Inglês | MEDLINE | ID: mdl-35735729

RESUMO

Drug administration to the wound site is a potential method for wound healing. The drug retention duration should be extended, and drug permeability through the buccal mucosal layer should be regulated. Oral wounds can be caused by inflammation, ulcers, trauma, or pathological lesions; if these wounds are not treated properly, they can lead to pain, infection, and subsequent undesirable scarring. This study aimed to develop Kolliphor-407 P-based gel containing neomycin sulfate (NES) loaded in solid lipid nanoparticles (SLNs) and enhance the antimicrobial activity. By considering lipid concentrations and achieving the lowest particle size (Y1) and maximum entrapment (EE-Y2) effectiveness, the formulation of NES-SLN was optimized using the Box-Behnken design. For the selected responses, 17 runs were formulated (as anticipated by the Design-Expert software) and evaluated accordingly. The optimized formulation could achieve a particle size of 196.25 and EE of 89.27% and was further utilized to prepare the gel formulation. The NES-SLN-G formula was discovered to have a smooth, homogeneous structure and good mechanical and rheological properties. After 24 h of treatment, NES-SLN-G showed a regulated in vitro drug release pattern, excellent ex vivo permeability, and increased in vitro antibacterial activity. These findings indicate the potential application of NES-SLN-loaded gels as a promising formulation for buccal mucosal wound healing.

11.
Gels ; 8(2)2022 Feb 09.
Artigo em Inglês | MEDLINE | ID: mdl-35200484

RESUMO

The goal of the current study is to develop a chitosan alginate nanoparticle system encapsulating the model drug, simvastatin (SIM-CA-NP) using a novel polyelectrolytic complexation method. The formulation was optimized using the central composite design by considering the concentrations of chitosan and alginate at five different levels (coded as +1.414, +1, 0, -1, and -1.414) in achieving minimum particle size (PS-Y1) and maximum entrapment efficiency (EE-Y2). A total of 13 runs were formulated (as projected by the Design-Expert software) and evaluated accordingly for the selected responses. On basis of the desirability approach (D = 0.880), a formulation containing 0.258 g of chitosan and 0.353 g of alginate could fulfill the prerequisites of optimum formulation in achieving 142.56 nm of PS and 75.18% EE. Optimized formulation (O-SIM-CAN) was further evaluated for PS and EE to compare with the theoretical results, and relative error was found to be within the acceptable limits, thus confirming the accuracy of the selected design. SIM release from O-SIM-CAN was retarded significantly even beyond 96 h, due to the encapsulation in chitosan alginate carriers. The cell viability study and Caspase-3 enzyme assay showed a notable difference in contrast to that of plain SIM and control group. All these stated results confirm that the alginate-chitosan nanoparticulate system enhanced the anti-proliferative activity of SIM.

12.
Drug Deliv ; 29(1): 254-262, 2022 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-35014929

RESUMO

Candida albicans is the fungus responsible for oral candidiasis, a prevalent disease. The development of antifungal-based delivery systems has always been a major challenge for researchers. This study was designed to develop a nanostructured lipid carrier (NLC) of sesame oil (SO) loaded with miconazole (MZ) that could overcome the solubility problems of MZ and enhance its antifungal activity against oral candidiasis. In the formulation of this study, SO was used as a component of a liquid lipid that showed an improved antifungal effect of MZ. An optimized MZ-loaded NLC of SO (MZ-SO NLC) was used, based on a central composite design-based experimental design; the particle size, dissolution efficiency, and inhibition zone against oral candidiasis were chosen as dependent variables. A software analysis provided an optimized MZ-SO NLC with a particle size of 92 nm, dissolution efficiency of 88%, and inhibition zone of 29 mm. Concurrently, the ex vivo permeation rate of the sheep buccal mucosa was shown to be significantly (p < .05) higher for MZ-SO NLC (1472 µg/cm2) as compared with a marketed MZ formulation (1215 µg/cm2) and an aqueous MZ suspension (470 µg/cm2). Additionally, an in vivo efficacy study in terms of the ulcer index against C. albicans found a superior result for the optimized MZ-SO NLC (0.5 ± 0.50) in a treated group of animals. Hence, it can be concluded that MZ, through an optimized NLC of SO, can treat candidiasis effectively by inhibiting the growth of C. albicans.


Assuntos
Antifúngicos/farmacologia , Candida albicans/efeitos dos fármacos , Candidíase Bucal/tratamento farmacológico , Miconazol/farmacologia , Sistemas de Liberação de Fármacos por Nanopartículas/química , Óleo de Gergelim/química , Animais , Antifúngicos/administração & dosagem , Antifúngicos/farmacocinética , Química Farmacêutica , Portadores de Fármacos/química , Liberação Controlada de Fármacos , Lipídeos/química , Masculino , Miconazol/administração & dosagem , Miconazol/farmacocinética , Mucosa Bucal , Tamanho da Partícula , Distribuição Aleatória , Ratos , Ovinos , Solubilidade , Propriedades de Superfície
13.
Polymers (Basel) ; 13(14)2021 Jul 14.
Artigo em Inglês | MEDLINE | ID: mdl-34301073

RESUMO

Maintaining oral health helps to prevent periodontal inflammation and pain, which can progress into more detrimental issues if left untreated. Meloxicam (MX) is a commonly used analgesic for periodontal pain, but it can have adverse gastrointestinal effects and poor solubility. Therefore, this study aimed to enhance the solubility of MX by developing a self-nanoemulsifying drug delivery system (SNEDDS). Considering the anti-ulcer activity of peppermint oil (PO), it was added in a mixture with medium-chain triglyceride (MCT) to the MX-loaded SNEDDS formulation (MX-PO-SNEDDS). After optimization, MX-PO-SNEDDS exhibited a PO:MCT ratio of 1.78:1, surfactant mixture HLB value of 14, and MX:oil mix ratio of 1:15, a particle size of 47 ± 3 nm, stability index of 85 ± 4%, ex vivo Jss of 4 ± 0.6 µg/cm2min, and ulcer index of 1 ± 0.25 %. Then, orally flash disintegrating lyophilized composites (MX-SNELCs) were prepared using the optimized MX-PO-SNEDDs. Results reveal that MX-SNELCs had a wetting time of 4 ± 1 s and disintegration time of 3 ± 1 s with a high in vitro MX release of 91% by the end of 60 min. The results of pharmacokinetic studies in human volunteers further demonstrated that, compared to a marketed MX tablets, MX-SNELCs provided a higher Cmax, Tmax, and AUC and a relatively greater bioavailability of 152.97 %. The successfully developed MX-SNELCs were found to be a better alternative than the conventional tablet dosage form, thus indicating their potential for further development in a clinically acceptable strategy for managing periodontal pain.

14.
Polymers (Basel) ; 13(24)2021 Dec 12.
Artigo em Inglês | MEDLINE | ID: mdl-34960901

RESUMO

Epalrestat (EPL) is an aldose reductase inhibitor with poor aqueous solubility that affects its therapeutic efficacy. The research study was designed to prepare epalrestat-cyclodextrins (EPL-CDs) inclusion complexes to enhance the aqueous solubility by using beta-cyclodextrin (ß-CD) and sulfobutyl ether7 ß-CD (SBE7 ß-CD). Furthermore, polymeric nanoparticles (PNPs) of EPL-CDs were developed using chitosan (CS) and sodium tripolyphosphate (sTPP). The EPL-CDs complexed formulations were then loaded into chitosan nanoparticles (CS NPs) and further characterized for different physico-chemical properties, thermal stability, drug-excipient compatibility and acute oral toxicity studies. In-silico molecular docking of cross-linker with SBE7 ß-CD was also carried out to determine the binding site of the CDs with the cross-linker. The sizes of the prepared NPs were laid in the range of 241.5-348.4 nm, with polydispersity index (PDI) ranging from 0.302-0.578. The surface morphology of the NPs was found to be non-porous, smooth, and spherical. The cumulative percentage of drug release from EPL-CDs loaded CS NPs was found to be higher (75-88%) than that of the pure drug (25%). Acute oral toxicity on animal models showed a biochemical, histological profile with no harmful impact at the cellular level. It is concluded that epalrestat-cyclodextrin chitosan nanoparticles (EPL-CDs-CS NPs) with improved solubility are safe for oral administration since no toxicity was reported on vital organs in rabbits.

15.
Biomater Sci ; 9(9): 3244-3283, 2021 May 04.
Artigo em Inglês | MEDLINE | ID: mdl-33949464

RESUMO

Dental treatment is provided for a wide variety of oral health problems like dental caries, periodontal diseases, periapical infections, replacement of missing teeth and orthodontic problems. Various biomaterials, like composite resins, amalgam, glass ionomer cement, acrylic resins, metal alloys, impression materials, bone grafts, membranes, local anaesthetics, etc., are used for dental applications. The physical and chemical characteristics of these materials influence the outcome of dental treatment. It also impacts on the biological, allergic and toxic potential of biomaterials. With innovations in science and their positive results, there is also a need for awareness about the biological risks of these biomaterials. The aim of dental treatment is to have effective, yet safe, and long-lasting results for the benefit of patients. For this, it is important to have a thorough understanding of biomaterials and their effects on local and systemic health. Materials used in dentistry undergo a series of analyses before their oral applications. To the best of our knowledge, this is the first and original review that discusses the reasons for and studies on the toxicity of commonly used biomaterials for applications in dentistry. It will help clinicians to formulate a methodical approach for the selection of dental biomaterials, thus providing an awareness for forecasting their risk of toxic reactions.


Assuntos
Materiais Biocompatíveis , Cárie Dentária , Materiais Biocompatíveis/toxicidade , Resinas Compostas , Odontologia , Cimentos de Ionômeros de Vidro , Humanos
16.
Polymers (Basel) ; 14(1)2021 Dec 27.
Artigo em Inglês | MEDLINE | ID: mdl-35012115

RESUMO

Natural polymers are revolutionizing current pharmaceutical dosage forms design as excipient and gained huge importance because of significant influence in formulation development and drug delivery. Oral health refers to the health of the teeth, gums, and the entire oral-facial system that allows us to smile, speak, and chew. Since years, biopolymers stand out due to their biocompatibility, biodegradability, low toxicity, and stability. Polysaccharides such as cellulose and their derivatives possess properties like novel mechanical robustness and hydrophilicity that can be easily fabricated into controlled-release dosage forms. Cellulose attracts the dosage design attention because of constant drug release rate from the precursor nanoparticles. This review discusses the origin, extraction, preparation of cellulose derivatives and their use in formulation development of nanoparticles having multidisciplinary applications as pharmaceutical excipient and in drug delivery, as bacterial and plant cellulose have great potential for application in the biomedical area, including dentistry, protein and peptide delivery, colorectal cancer treatment, and in 3D printable dosage forms.

17.
Drug Deliv ; 28(1): 741-751, 2021 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-33840320

RESUMO

The majority of newly developed drugs need to be incorporated with delivery systems to maximize their effect and minimize side effects. Nanoemulsions (NEs) are one type of delivery system that helps to improve the solubility and dissolution of drugs, attempting to enhance their bioavailability and onset of action. The objective of this investigation was to develop an omega-3 oil-based NE loaded with loxoprofen (LXP) to enhance its dissolution, in vitro release, and mucosal penetration and decrease its mucosal ulcerative effects when applied in an oral treatment. LXP-loaded NEs were formulated with varying levels of omega-3 oil (10-30%), surfactant polyoxyethylene-C21-ethers (laureth-21) (40-60%), and co-surfactant polyethylene glycol-40 hydrogenated castor oil (HCO-40) (30-50%) using an extreme vertices mixture design. The developed NEs were characterized for globule size and drug loading capacity. The optimal formulation was tested for in vitro drug release, ex vivo permeation, and ulcer index value. The developed NE acquired a globule size ranging 71-195 nm and drug loading capacity of 43-87%. Considering the results of the in vitro release study, the optimized NE formulation achieved 2.45-fold and 2-fold increases in drug permeation across tested mucosa compared to a marketed tablet and drug aqueous dispersion, respectively. Moreover, the optimum NE exhibited the best ulcer index in comparison to drug aqueous suspension and different formulations when tested in rats. Overall, this research highlights the capacity of NEs to deliver LXP with enhanced solubility, drug release, and permeation while effectively protecting the application site from side effects of the model drug.


Assuntos
Anti-Inflamatórios não Esteroides/farmacologia , Ácidos Graxos Ômega-3/química , Nanopartículas/química , Fenilpropionatos/farmacologia , Odontalgia/tratamento farmacológico , Administração Tópica , Animais , Anti-Inflamatórios não Esteroides/administração & dosagem , Anti-Inflamatórios não Esteroides/efeitos adversos , Anti-Inflamatórios não Esteroides/farmacocinética , Química Farmacêutica , Sistemas de Liberação de Medicamentos , Liberação Controlada de Fármacos , Emulsões/química , Masculino , Fenilpropionatos/administração & dosagem , Fenilpropionatos/efeitos adversos , Fenilpropionatos/farmacocinética , Ratos , Ovinos , Absorção Cutânea/fisiologia , Solubilidade , Tensoativos
18.
Pharmaceutics ; 13(7)2021 Jul 02.
Artigo em Inglês | MEDLINE | ID: mdl-34371700

RESUMO

Oral health is a key contributor to a person's overall health and well-being. Oral microbiota can pose a serious threat to oral health. Thus, the present study aimed to develop a cinnamon oil (CO)-loaded nanoemulsion gel (NEG1) to enhance the solubilization of oil within the oral cavity, which will enhance its antibacterial, antifungal, and analgesic actions against oral microbiota. For this purpose, the CO-loaded nanoemulsion (CO-NE) was optimized using I-optimal response surface design. A mixture of Pluracare L44 and PlurolOleique CC 497 was used as the surfactant and Capryol was used as the co-surfactant. The optimized CO-NE had a globule size of 92 ± 3 nm, stability index of 95% ± 2%, and a zone of inhibition of 23 ± 1.5 mm. This optimized CO-NE formulation was converted into NEG1 using 2.5% hydroxypropyl cellulose as the gelling agent. The rheological characterizations revealed that the NEG1 formulation exhibited pseudoplastic behavior. The in vitro release of eugenol (the marker molecule for CO) from NEG1 showed an enhanced release compared with that of pure CO. The ex vivo mucosal permeation was found to be highest for NEG1 compared to the aqueous dispersion of CO-NE and pure cinnamon oil. The latency reaction time during the hot-plate test in rats was highest (45 min) for the NEG1 sample at all-time points compared with those of the other tested formulations. The results showed that the CO-NEG formulation could be beneficial in enhancing the actions of CO against oral microbiota, as well as relieving pain and improving overall oral health.

19.
Drug Deliv ; 28(1): 1043-1054, 2021 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-34060397

RESUMO

Herpes labialis, caused by herpes simplex virus type 1, is usually characterized by painful skin or mucosal lesions. Penciclovir (PV) tablets are found to be effective against herpes labialis but suffer from poor oral bioavailability. This study aimed to combine the benefits of PV and lavender oil (LO), which exhibits anesthetic activity, in the form of a self-nanoemulsifying drug delivery system (SNEDDS) for the treatment of herpes labialis. Toward this purpose, LO (oil), Labrasol:Labrafil M1944 CS in the ratio of 6:4 (surfactant mixture), and Lauroglycol-FCC (co-surfactant, selected based on the solubility of PV) were evaluated as the independent factors using a distance quadratic mixture design. The formulation was optimized for the minimum globule size and maximum stability index and was determined to contain 14% LO, 40.5% Labrasol:Labrafil 1944 (6:4), and 45.5% Lauroglycol-FCC. The optimized PV-LO-SNEDDS was embedded in chitosan hydrogel and the resulting formulations coded by (O3) were prepared and evaluated. The rheological studies demonstrated a combined pseudoplastic and thixotropic behavior with the highest flux of PV permeation across sheep buccal mucosa. Compared to a marketed 1% PV cream, the O3 formulation exhibited a significantly higher and sustained PV release, nearly twice the PV permeability, and a relative bioavailability of 180%. Overall, results confirm that the O3 formulation can provide an efficient delivery system for PV to reach oral mucosa and subsequent prolonged PV release. Thus, the PV-LO-SNEDDS embedded oral gel is promising and can be further evaluated in clinical settings to establish its therapeutic use in herpes labialis.


Assuntos
Guanina/farmacologia , Herpes Labial/tratamento farmacológico , Nanopartículas/química , Óleos Voláteis/farmacologia , Óleos de Plantas/farmacologia , Administração Tópica , Animais , Química Farmacêutica , Quitosana/química , Preparações de Ação Retardada , Sistemas de Liberação de Medicamentos , Liberação Controlada de Fármacos , Estabilidade de Medicamentos , Emulsões/química , Glicerídeos/química , Guanina/administração & dosagem , Guanina/farmacocinética , Hidrogéis/química , Lavandula , Masculino , Óleos Voláteis/administração & dosagem , Óleos Voláteis/efeitos adversos , Tamanho da Partícula , Óleos de Plantas/administração & dosagem , Óleos de Plantas/efeitos adversos , Ratos , Ratos Wistar , Reologia , Ovinos
20.
Pharmaceutics ; 12(11)2020 Nov 07.
Artigo em Inglês | MEDLINE | ID: mdl-33171816

RESUMO

Burn wound healing is a complex process that involves the repair of injured tissues and the control of infection to diminish the scar formation, pain, and discomfort associated with such injuries. The aim of this research was to formulate and optimize a self-nanoemulsion drug delivery system based on the use of coconut oil and loaded with simvastatin. Coconut oil possesses antiinflammatory and antibacterial activity, and simvastatin has interesting properties for promoting the wound-healing process because it increases the production of the vascular endothelial growth factor at the site of injury. The Box-Behnken design was employed for the optimization of the coconut oil-simvastatin self-nanoemulsion drug delivery system. The prepared formulations were characterized according to globular size and their activity in the healing of burn wounds by assessing the mean wound diameter and level of interlukin-6 in experimental animals. Additionally, the antimicrobial activity of the prepared formulations was assessed. The nanoemulsion was considered adequately formed when it had droplets of between 65 and 195 nm. The statistical design proved the important synergistic effect of coconut oil and simvastatin for burn wound management in their synergistic potentiation of wound closure and their anti-inflammatory and antimicrobial effects. The optimum formulation achieved up to a 5.3-fold decrease in the mean burn wound diameter, a 4.25-fold decrease in interleukin-6 levels, and a 6-fold increase in the inhibition zone against Staphylococcus aureus when compared with different control formulations. Therefore, the designed nanoemulsions containing a combination of coconut oil and simvastatin could be considered promising platforms for the treatment of chronic and burn wounds.

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