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1.
Int J Clin Pharmacol Ther ; 62(6): 259-266, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38529928

RESUMO

BACKGROUND: Vancomycin is being used for the treatment of a variety of infections caused by methicillin resistant Staphylococcus aureus and methicillin susceptible Staphylococcus aureus. Therapeutic drug monitoring (TDM) is highly recommended for ensuring the safe and effective therapy with vancomycin. A reliable and cost-effective bioanalytical method is required for TDM as well as pharmacokinetic studies of vancomycin. MATERIALS AND METHODS: A selective, sensitive, and cost effective HPLC method was developed and validated for quantification of vancomycin concentrations in human plasma. The mobile phase was a mixture of buffer (50 mM ammonium dihydrogen phosphate, pH 2.4) and acetonitrile 88 : 12 v/v. The separation was carried on C18 column (125 × 4.6 mm, particle size 5 µm) with isocratic flow rate of 0.370 mL/min at room temperature with UV detection at 215 nm. The method was validated for sensitivity, accuracy, and precision as well as stability of vancomycin in human plasma by following European Medicine Agency (EMA) guideline. Therapeutic drug monitoring of vancomycin was performed by quantifying the trough concentrations of vancomycin in 65 human plasma samples after administration of therapeutically relevant dose. RESULTS: The developed method was sensitive enough to quantify vancomycin concentrations as low as 0.25 mg/L in human plasma. Moreover, the method was proved accurate and precise in terms of quantifying the unknown concentration of vancomycin. The evaluation of short-term, long-term, and freeze-thaw stability proved the stability of vancomycin in human plasma. The TDM of vancomycin by using this method showed that 39 (60%) samples were within the target trough concentration range (TTCR), i.e. 10 - 20 mg/L, while 23 samples (35.4%) were below the TTCR, and 3 samples (4.6%) were above this range. CONCLUSION: The developed method is sensitive and cost effective for quantification of vancomycin in human plasma. The results of sample analysis shows that the developed method can be used reliably for TDM of vancomycin.


Assuntos
Antibacterianos , Monitoramento de Medicamentos , Vancomicina , Vancomicina/farmacocinética , Vancomicina/sangue , Humanos , Monitoramento de Medicamentos/métodos , Cromatografia Líquida de Alta Pressão/métodos , Antibacterianos/farmacocinética , Antibacterianos/sangue , Reprodutibilidade dos Testes
2.
ACS Omega ; 9(6): 7003-7011, 2024 Feb 13.
Artigo em Inglês | MEDLINE | ID: mdl-38371835

RESUMO

This study aims to assess the anti-inflammatory potential of stearic acid nanoparticles of quercetin in an arthritic rat model. This article describes the fabrication of solid lipid nanoparticles (SLNs) using the hot melt encapsulation method, followed by the anti-inflammatory study of SLNs and other characterizations such as FTIR, XRD, and SEM. Thirty male healthy albino rats were taken and treated with FCA to induce rheumatoid arthritis. Quercetin loading of quercetin to stearic acid was confirmed by FTIR. The efficacy of quercetin-loaded SLNs to reduce inflammation was evaluated with the help of inflammatory biomarker levels. Quercetin-loaded stearic acid nanoparticles were successfully prepared by using a hot melt encapsulation method. Their average size and zeta potential were 100 nm and -25 mV, respectively. Rheumatoid arthritis was significantly (p < 0.001) reduced in the quercetin-loaded SLN group, as indicated by finding out the reduced levels of inflammatory mediators such as tumor necrosis factor (TNF-α) and rheumatoid factor. Quercetin-loaded stearic acid nanoparticles were found to be potentially effective in treating RA.

3.
Pharmaceutics ; 15(12)2023 Dec 01.
Artigo em Inglês | MEDLINE | ID: mdl-38140057

RESUMO

PURPOSE: The aim of this research was to prepare adhesive nanoparticles for the topical application of Minoxidil (MXD). METHODS: Thiolated ß-CDs were prepared via conjugation of cysteamine with oxidized CDs. MXD was encapsulated within thiolated and unmodified ß-CDs. Ionic gelation method was used to prepare nanoparticles (Thio-NP and blank NP) of CDs with chitosan. Nanoparticles were analyzed for size and zetapotential. Inclusion complexes were characterized via FTIR. Drug dissolution studies were carried out. An in vitro adhesion study over human hair was performed. An in vivo skin irritation study was performed. Ex vivo drug uptake was evaluated by using a Franz diffusion cell. RESULTS: Thiolated ß-CDs presented 1804.68 ± 25 µmol/g thiol groups and 902.34 ± 25 µmol/g disulfide bonds. Nanoparticles displayed particle sizes within a range of 231 ± 07 nm to 354 ± 13 nm. The zeta potential was in the range of -8.1 ± 02 mV, +16.0 ± 05 mV. FTIR analyses confirmed no interaction between the excipients and drug. Delayed drug release was observed from Thio-NP. Thio-NP retained over hair surfaces for a significantly longer time. Similarly, drug retention was significantly improved. Thio-NP displayed no irritation over rabbit skin. CONCLUSION: Owing to the above results, nanoparticles developed with MXD-loaded thiolated ß-CDs might be a potential drug delivery system for topical scalp diseases.

4.
AAPS PharmSciTech ; 24(7): 194, 2023 Sep 26.
Artigo em Inglês | MEDLINE | ID: mdl-37752361

RESUMO

The objective of this study was to generate fluconazole-loaded mucoadhesive nanogels to address the problem of hydrophobicity of fluconazole (FL). An inclusion complex was formulated with sulfhydryl-ß-CD (SH-ß-CD) followed by nanogels formation by a Schiff base reaction of carbopol 940 (CA-940) and gelatin (GE). For characterization, PXRD, FT-IR analysis, drug content, and phase solubility studies were performed. Similarly, nanogels were assessed for particle size, zeta potential, organoleptic, and spreadability studies. Moreover, drug contents, rheological, in vitro drug permeation, release kinetics, toxicity, and stability studies of nanogels were performed. Furthermore, mucoadhesive characteristics over the buccal mucosal membrane of the goat were evaluated. The nanogels formulated with a higher amount of CA-940 and subsequently loaded with the inclusion complexes of FL showed promising results. PXRD and FT-IR analysis confirmed the physical complexes by displaying a reduction in the intensity of peaks of FL. The average particle size of nanogels was in the range of 257 to 361 nm. The highest drug content of 88% was encapsulated within the FL-SH-ß-CD complex. All formulations at 0.5-1% concentration displayed no toxicity to the Caco-2 cell lines. Nanogels loaded with FL-SH-ß-CD complexes showed 18-fold improved mucoadhesion on the buccal mucous membrane of the goat when compared to simple nanogels. The in vitro permeation study exhibited significantly enhanced permeation and first-order concentration-dependent drug release was observed. On the bases of these findings, we can conclude that a mucoadhesive nanogel-based drug delivery system can be an ideal therapy for candidiasis.

5.
Des Monomers Polym ; 25(1): 165-174, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35711622

RESUMO

Niosomes are multilamellar vesicles that efficiently deliver active substance into skin systemic circulation or skin layers. They are used in topical drug delivery system to enhance the skin permeation of active substance. So, the prime objective of this study was to develop a niosomal gel of fusidic acid to increase its skin permeation. Different formulations of niosomes of fusidic acid were designed by varying the cholesterol to surfactant ratio. Formulations containing fusidic acid, cholesterol, dihexadecyl pyridinium chloride, Span 60, or Tween 60 were prepared by thin film hydration method in rotary evaporator. The thin film formed in rotary flask was hydrated by phosphate buffer saline of pH 7.2. The niosomes formed were characterized through entrapment efficiency, size, polydispersity index (PDI), and zeta potential. The S3 formulation containing span 60 showed the highest entrapment efficiency (EE) of niosomes, so it was incorporated into Carbopol gel. Determination of pH, spreadability, rheological, and ex vivo permeation studies was conducted of niosomal gel. The results of ex vivo permeation studies showed high permeation of fusidic acid when gel was applied to an albino rat skin. According to the results and previous studies of niosomes, it can be concluded that niosomes enhanced the permeation of fusidic acid through the skin.

6.
J Microencapsul ; 39(1): 37-48, 2022 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-34919007

RESUMO

AIM: This work aims to formulate topical hybrid gel containing chitosan-coated moxifloxacin (MXF) HCl nanoparticles (NPs) with enhanced antibacterial and healing activity. METHODS: MXF HCl NPs prepared by the ionic gelation method were loaded onto a hybrid chitosan carbomer gel. Size analysis of the prepared NPs was performed using SEM and Zeta-sizer. Further characterisation was done using Fourier transforms infra-red spectroscopy (FTIR), X-ray diffraction (XRD), and Thermogravimetric analysis (TGA). Prepared gel was evaluated for its in vitro drug release, biocompatibility, antibacterial activity, and stability studies under storage conditions. In-vivo wound healing was measured by observing percentage reduction in wound. RESULTS: NPs have 359 ± 79 nm mean particle size, 31.01 mV zeta potential with 0.008 polydispersity index (PD1), 63.5% drug entrapment and 83 ± 3.5% drug release at pH 5.5. Hybrid chitosan carbomer gel showed good biocompatibility, antibacterial, in-vivo wound healing properties and stable properties. CONCLUSIONS: NP-loaded hybrid gel can be an effective treatment for acute and challenged topical wounds.


Assuntos
Quitosana , Nanopartículas , Antibacterianos/farmacologia , Portadores de Fármacos , Liberação Controlada de Fármacos , Moxifloxacina , Tamanho da Partícula , Cicatrização
7.
Molecules ; 26(9)2021 Apr 24.
Artigo em Inglês | MEDLINE | ID: mdl-33923335

RESUMO

Wound-healing is complicated process that is affected by many factors, especially bacterial infiltration at the site and not only the need for the regeneration of damaged tissues but also the requirement for antibacterial, anti-inflammatory, and analgesic activity at the injured site. The objective of the present study was to develop and evaluate the natural essential oil-containing nanofiber (NF) mat with enhanced antibacterial activity, regenerative, non-cytotoxic, and wound-healing potential. Clove essential oil (CEO) encapsulated in chitosan and poly-ethylene oxide (PEO) polymers to form NFs and their morphology was analyzed using scanning electron microscopy (SEM) that confirmed the finest NFs prepared with a diameter of 154 ± 35 nm. The successful incorporation of CEO was characterized by Fourier transform infra-red spectroscopy (FTIR) and X-ray diffractometry (XRD). The 87.6 ± 13.1% encapsulation efficiency and 8.9 ± 0.98% loading of CEO was observed. A total of 79% release of CEO was observed in acidic pH 5.5 with 117% high degree of swelling. The prepared NF mat showed good antibacterial activity against Staphylococcus aureus and Escherichia coli and non-cytotoxic behavior against human fibroblast cell lines and showed good wound-healing potential.


Assuntos
Quitosana/farmacologia , Óleo de Cravo/farmacologia , Syzygium/química , Cicatrização/efeitos dos fármacos , Antibacterianos/química , Antibacterianos/farmacologia , Infecções Bacterianas/tratamento farmacológico , Infecções Bacterianas/microbiologia , Linhagem Celular , Quitosana/química , Óleo de Cravo/química , Escherichia coli/efeitos dos fármacos , Escherichia coli/patogenicidade , Fibroblastos/efeitos dos fármacos , Humanos , Nanofibras/química , Staphylococcus aureus/efeitos dos fármacos , Staphylococcus aureus/patogenicidade
8.
Int J Nanomedicine ; 16: 1313-1330, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33628022

RESUMO

Nanotechnology has been actively integrated as drug carriers over the last few years to treat various cancers. The main hurdle in the clinical management of cancer is the development of multidrug resistance against chemotherapeutic agents. To overcome the limitations of chemotherapy, the researchers have been developing technological advances for significant progress in the oncotherapy by enabling the delivery of chemotherapeutic agents at increased drug content levels to the targeted spots. Several nano-drug delivery systems designed for tumor-targeting are evaluated in preclinical and clinical trials and showed promising outcomes in cancerous tumors' clinical management. This review describes nanocarrier's importance in managing different types of cancers and emphasizing nanocarriers for drug delivery and cancer nanotherapeutics. It also highlights the recent advances in nanocarriers-based delivery systems, including polymeric nanocarriers, micelles, nanotubes, dendrimers, magnetic nanoparticles, solid lipid nanoparticles, and quantum dots (QDs). The nanocarrier-based composites are discussed in terms of their structure, characteristics, and therapeutic applications in oncology. To conclude, the challenges and future exploration opportunities of nanocarriers in chemotherapeutics are also presented.


Assuntos
Antineoplásicos/administração & dosagem , Antineoplásicos/farmacologia , Portadores de Fármacos/química , Sistemas de Liberação de Medicamentos , Nanopartículas/química , Animais , Antineoplásicos/química , Humanos , Lipídeos/química , Neoplasias/tratamento farmacológico , Pontos Quânticos/química
9.
Int J Nanomedicine ; 16: 8353-8373, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-35002232

RESUMO

BACKGROUND: Epalrestat (EPL) is a carboxylic acid derivative with poor aqueous solubility and its pharmacokinetic features are not fully defined. PURPOSE: Current research aimed to fabricate inclusion complexation of EPL with SBE7 ß-CD (IC) and EPL/SBE7 ß-CD CS NPs (NP). METHODS: EPL was complexed with SBE7 ß-CD using the co-precipitation method, and the prepared complex was fabricated into nanoparticles using the ionic gelation method. The prepared formulations were characterized for particle size analysis, surface morphology, and in vitro dissolution study. The % inhibition of EPL against α-glucosidase enzyme was also conducted to check the drug's antidiabetic activity. Finally, an in vivo pharmacokinetic investigation was carried out to determine the concentration of EPL in rabbit plasma of the prepared formulation. In vivo pharmacokinetic studies were conducted by giving a single dose of pure EPL, IC, and NP. RESULTS: The size of NP was found to be 241.5 nm with PDI 0.363 and zeta potential of +31.8 mV. The surface of the prepared NP was non-porous, smooth and spherical when compared with pure EPL, SBE7 ß-CD and IC. The cumulative drug release (%) from IC and NP was 73% and 88%, respectively, as compared to pure drug (25%). The % inhibition results for in vitro α-glucosidase was reported to be 74.1% and the predicted binding energy for in silico molecular docking was calculated to be -6.6 kcal/mol. The calculated Cmax values for EPL, IC and NP were 4.75±3.64, 66.91±7.58 and 84.27±6.91 µg/mL, respectively. The elimination half-life of EPL was 4 h and reduced to 2 h for IC and NP. The AUC0-α for EPL, IC and NP were 191.5±164.63, 1054.23±161.77 and 1072.5±159.54 µg/mL*h, respectively. CONCLUSION: Taking these parameters into consideration it can be concluded that IC and NP have prospective applications for greatly improved delivery and regulatedt release of poorly water soluble drugs, potentially leading to increase therapeutic efficacy and fewer side effects.


Assuntos
Quitosana , Nanopartículas , Animais , Disponibilidade Biológica , Portadores de Fármacos , Simulação de Acoplamento Molecular , Tamanho da Partícula , Coelhos , Rodanina/análogos & derivados , Tiazolidinas
10.
Pak J Pharm Sci ; 32(4(Supplementary)): 1873-1877, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-31680086

RESUMO

Zingeber officinale (ginger) has been used for a long time in conventional medicine for the management of many diseases most important of which is inflammatory diseases. The aim of this study was formulation of topical microemulsion system to enhance the solubility, stability and release profile of ginger extract, as it is unstable in the presence of light, air, heat and long term storage. The solubility of ginger extract in different oils, surfactants, and cosurfactants was determined in order to find the optimal components for microemulsion. Isopropyl myristate (IPM) was selected as oil phase, tween 80 and PEG 400 were selected as surfactant and co-surfactant respectively based on highest solubility values. Pseudo-ternary phase diagram was constructed in order to find out the microemulsion region. The prepared microemulsions were evaluated for pH, viscosity, conductivity, refractive index, globular size, zeta potential, polydispersity index, ginger extract content, in-vitro and ex-vivo release profiles. The formulation GE1 showed best physicochemical properties with smallest globular size (19.75nm), highest release rate and flux value. It also showed significant (p<0.05) anti-inflammatory effect as compared to reference piroxicam drug solution. It is concluded that ginger extract can be used to develop stable microemulsion system with better skin permeation and promising antiinflammatory activity.


Assuntos
Emulsões/farmacologia , Extratos Vegetais/farmacologia , Zingiber officinale/química , Administração Cutânea , Animais , Sistemas de Liberação de Medicamentos/métodos , Camundongos , Miristatos/química , Polietilenoglicóis/química , Polissorbatos/química , Pele/metabolismo , Absorção Cutânea/efeitos dos fármacos , Solubilidade/efeitos dos fármacos , Tensoativos/química , Viscosidade/efeitos dos fármacos
11.
Pak J Pharm Sci ; 32(3 Special): 1327-1332, 2019 May.
Artigo em Inglês | MEDLINE | ID: mdl-31551211

RESUMO

Zingeber officinale is a commonly used plant which has been shown to possess anti-inflammatory activity. The active compounds present in ginger are gingerols, shagaols and paradol. The aim of this study was formulation of topical microemulsion system to enhance the solubility and stability of ginger extract, as it is unstable in the presence of light, air, heat and long term storage, and to evaluate its anti-inflammatory activity. The solubility of ginger extract in different oils, surfactants, and co-surfactants was determined in order to find the optimal components for microemulsion. IPM was selected as oil phase, tween 80 and PEG 400 were selected as surfactant and co-surfactant respectively based on highest solubility values. Pseudo-ternary phase diagram was constructed in order to find out the microemulsion region. The prepared microemulsions were evaluated for pH, viscosity, conductivity, refractive index, globular size, zeta potential, polydispersity index, ginger extract content. The formulation F1 showed best physicochemical properties with smallest globular size. It also showed significant (p<0.05) anti-inflammatory effect as compared to reference piroxicam drug solution. Based on the results, it is concluded that ginger extract can be used to develop stable microemulsion system and promising anti-inflammatory activity.


Assuntos
Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/farmacologia , Emulsões/farmacologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Zingiber officinale/química , Sistemas de Liberação de Medicamentos , Estabilidade de Medicamentos , Emulsões/administração & dosagem , Concentração de Íons de Hidrogênio , Polietilenoglicóis/química , Polissorbatos/química , Desnaturação Proteica/efeitos dos fármacos , Refratometria , Solubilidade , Tensoativos/química , Viscosidade
12.
Front Pharmacol ; 10: 317, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31068804

RESUMO

Introduction: Athletes train physically to reach beyond their potential maximum aerobic threshold. Whey protein supplements (WPS) are often used in conjunction with physiotherapy and psychotherapy to regain better vital sign and physical performances. This review aimed to explore the clinical evidence on the efficacy and safety of WPS in sports performance and recovery among athletes. Methodology: A comprehensive literature search was performed to identify relevant randomized control trials (RCTs) that investigated the efficacy and safety of WPS on the vital sign and physical performance among athletes. The Cochrane Risk of Bias (ROB) Assessment tools were used to assess the quality of the studies. Meta-analysis was conducted using the frequentist model with STATA version 14.2®. Results: A total of 333,257 research articles were identified out of which 20 RCTs were included for qualitative synthesis and network meta-analysis with 351 participants. Among the studies, 7 had low ROB and 3 RCTs had high ROB. Of these 20 trials, 16 trials were randomized clinical trials which compared whey protein supplements (WPS) with various comparators i.e., L-alanine, bovine colostrum, carbohydrate, casein, leucine, maltodextrin, rice, protein + caffeine were compared with placebo. Analysis from the pairwise meta-analysis revealed that for respiratory exchange ratio (RER) WPS was found to be significantly improving compared to maltodextrin (WMD = 0.012; 95%CI = 0.001, 0.023). Similarity to RPE (Rate Perceived Exertion), slight difference between WPS and the comparators, however, when the estimation was favorable to the comparators, there was moderate-high heterogeneity. For VO 2max, high heterogeneity appeared when WPS compared to maltodextrin with the I 2 = 97.8% (WMD = 4.064; 95% CI = -4.230, 12.359), meanwhile bovine colostrum (WMD = -2.658; 95%CI = -6.180, 0.865) only comparator that was better than WPS. According to the estimated effect of the supplements on physical performance outcome results, maximum power (8 studies, 185 athletes), highest ranked was bovine colostrum (SUCRA = 70.7%) and the lowest ranked was placebo (SUCRA = 17.9%), yet all insignificant. Then again, on average power (nine studies, 187 athletes), WPS was the highest ranked (SUCRA = 75.4 %) about -112.00 watt (-187.91, -36.08) and most of the estimations were significant. Body mass was reported in 10 studies (171 athletes), carbohydrate may be at the highest ranked (SUCRA = 66.9%) but it is insignificant. Thought the second highest ranked was WPS (SUCRA = 64.7%) and it is significant (WMD = -6.89 kg; CI = -8.24, -5.54). Conclusion: The findings of this review support the efficacy and safety of WPS as an ergogenic aid on athletes' sports performance and recovery. The overall quality of clinical evidence was found to be valid and reliable from the comprehensive search strategy and ROB assessment.

13.
Pak J Pharm Sci ; 31(6 (Supplementary): 2623-2628, 2018 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-30587470

RESUMO

Among immunosuppressive agents cyclosporine A is drug of unique importance. This drug has a low therapeutic index, and it has many toxic effects. After oral administration its absolute bioavailability is variable due to poor absorption. Niosomes are new and versatile carriers to deliver drug. The bioavailability of immunosuppressant drug cyclosporine A can be increased by niosomal drug delivery system. So our basic theme was to prepare niosomes of immunosuppressant drug using cholesterol, span 60 and tween 60 etc. Niosomes were characterized for zeta potential, size, poly dispersivity index(PDI), entrapment efficiency and In vitrorelease profiles. Six niosomal formulations (F1-F6) were successfully developed using thin film hydration technique. Among various formulations F2 showed the highest entrapment efficiency 77.29 %. The DSC thermograms of physical mixtures and niosomal formulations indicated the presence of drug in crystalline form. In vitro drug release study demonstrated higher drug release values as compared to drug aqueous dispersion. Niosomal formulations were capable of releasing drug in sustained manner. The overall results demonstrated that developed niosomal carriers are competitive candidates for improving dissolution profile of cyclosporine A leading to increased bioavailability at the site of action.


Assuntos
Ciclosporina/farmacocinética , Portadores de Fármacos/farmacocinética , Composição de Medicamentos/métodos , Desenvolvimento de Medicamentos/métodos , Imunossupressores/farmacocinética , Ciclosporina/química , Portadores de Fármacos/química , Imunossupressores/química , Lipossomos
14.
Drug Dev Ind Pharm ; 44(12): 2061-2070, 2018 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-30081679

RESUMO

OBJECTIVE: This study was designed to optimize and develop matrix type transdermal drug delivery system (TDDS) containing tizanidine hydrochloride (TZH) using different polymers by solvent evaporation method. SIGNIFICANCE: A strong need exists for the development of transdermal patch having improved bioavailability at the site of action with fewer side effects at off-target organs. METHODS: The patches were physically characterized by texture analysis (color, flexibility, smoothness, transparency, and homogeneity), in vitro dissolution test and FTIR analysis. Furthermore, functional properties essential for TDDS, in vitro percentage of moisture content, percentage of water uptake, in vitro permeation by following different kinetic models, in vivo drug content estimation and skin irritation were determined using rabbit skin. RESULTS: The optimized patches were soft, of uniform texture and thickness as well as pliable in nature. Novel transdermal patch showed ideal characteristics in terms of moisture content and water uptake. FTIR analysis confirmed no interaction between TZH and cellulose acetate phthalate (CAP). The patch showed sustained release of the drug which increased the availability of short acting TZH at the site of action. The patch also showed its biocompatibility to the in vivo model of rabbit skin. CONCLUSIONS: The results demonstrated that topically applied transdermal patch will be a potential medicated sustain release patch for muscle pain which will improve patient compliance.


Assuntos
Clonidina/análogos & derivados , Sistemas de Liberação de Medicamentos/métodos , Relaxantes Musculares Centrais/administração & dosagem , Adesivo Transdérmico , Administração Cutânea , Animais , Disponibilidade Biológica , Clonidina/administração & dosagem , Clonidina/farmacocinética , Preparações de Ação Retardada/administração & dosagem , Preparações de Ação Retardada/farmacocinética , Liberação Controlada de Fármacos , Excipientes/química , Teste de Materiais , Relaxantes Musculares Centrais/farmacocinética , Mialgia/tratamento farmacológico , Polímeros/química , Coelhos , Pele/efeitos dos fármacos , Pele/metabolismo , Absorção Cutânea/efeitos dos fármacos
15.
J Food Drug Anal ; 26(2): 887-902, 2018 04.
Artigo em Inglês | MEDLINE | ID: mdl-29567261

RESUMO

The purpose of this study was to fabricate a triple-component nanocomposite system consisting of chitosan, polyethylene glycol (PEG), and drug for assessing the application of chitosan-PEG nanocomposites in drug delivery and also to assess the effect of different molecular weights of PEG on nanocomposite characteristics. The casting/solvent evaporation method was used to prepare chitosan-PEG nanocomposite films incorporating piroxicam-ß-cyclodextrin. In order to characterize the morphology and structure of nanocomposites, X-ray diffraction technique, scanning electron microscopy, thermogravimetric analysis, and Fourier transmission infrared spectroscopy were used. Drug content uniformity test, swelling studies, water content, erosion studies, dissolution studies, and anti-inflammatory activity were also performed. The permeation studies across rat skin were also performed on nanocomposite films using Franz diffusion cell. The release behavior of films was found to be sensitive to pH and ionic strength of release medium. The maximum swelling ratio and water content was found in HCl buffer pH 1.2 as compared to acetate buffer of pH 4.5 and phosphate buffer pH 7.4. The release rate constants obtained from kinetic modeling and flux values of ex vivo permeation studies showed that release of piroxicam-ß-cyclodextrin increased with an increase in concentration of PEG. The formulation F10 containing 75% concentration of PEG showed the highest swelling ratio (3.42±0.02) in HCl buffer pH 1.2, water content (47.89±1.53%) in HCl buffer pH 1.2, maximum cumulative drug permeation through rat skin (2405.15±10.97 µg/cm2) in phosphate buffer pH 7.4, and in vitro drug release (35.51±0.26%) in sequential pH change mediums, and showed a significantly (p<0.0001) higher anti-inflammatory effect (0.4 cm). It can be concluded from the results that film composition had a particular impact on drug release properties. The different molecular weights of PEG have a strong influence on swelling, drug release, and permeation rate. The developed films can act as successful drug delivery approach for localized drug delivery through the skin.


Assuntos
Sistemas de Liberação de Medicamentos/instrumentação , Nanocompostos/química , Administração Cutânea , Animais , Anti-Inflamatórios não Esteroides/administração & dosagem , Anti-Inflamatórios não Esteroides/química , Portadores de Fármacos/química , Sistemas de Liberação de Medicamentos/métodos , Masculino , Microscopia Eletrônica de Varredura , Piroxicam/administração & dosagem , Piroxicam/química , Polietilenoglicóis/química , Ratos , Ratos Sprague-Dawley , Difração de Raios X , beta-Ciclodextrinas/administração & dosagem , beta-Ciclodextrinas/química
16.
Postepy Dermatol Alergol ; 34(4): 339-345, 2017 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-28951709

RESUMO

INTRODUCTION: Intracellular and extracellular oxidative stress triggered by free radicals promotes skin aging, which is designated by atypical pigmentation and wrinkles. The consumption of antioxidants is an efficacious measure to avert symptoms involved in skin aging. AIM: The current research was commenced to explore the anti-aging potential of antioxidants present in Tamarindus indica seeds extract. MATERIAL AND METHODS: Tamarindus indica seeds extract was obtained by concentrating the ethanolic extract of seeds. The antioxidant activities of the extract were measured by nitric oxide radical scavenging assay, 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay, hydroxyl radical scavenging assay and superoxide radical scavenging assay. Formulation comprising 4% of the concentrated extract of seeds was formulated by loading it in the internal aqueous phase of water-in-oil (W/O) cosmetic emulsion. The base, used as control, consisted of the same emulsion but without loading Tamarindus indica seeds extract. The cosmetic emulsions were applied to the cheeks of 11 healthy male volunteers for duration of 12 weeks. Both base and formulation were assessed for their antioxidant effects on different skin parameters i.e. skin moisture contents, elasticity and surface evaluation of living skin (SELS). RESULTS: The formulation showed statistically significant (p ≤ 0.05) and the base showed insignificant (p > 0.05) effects on skin elasticity and skin moisture contents. There is a significant decline in SELS, skin scaliness (SEsc), skin wrinkles (SEw), skin smoothness (SEsm), and skin roughness (SEr) parameters after application of the formulation. CONCLUSIONS: Topical application of the cosmetic emulsion entrapped with Tamarindus indica seeds extract containing various antioxidants exerts potential skin antiaging effects.

17.
Pak J Pharm Sci ; 29(1): 173-8, 2016 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-26826810

RESUMO

The aim of current research was to develop a water-in-oil emulsion containing grape seed extract for application in cosmeceuticals. Finally grinded dried grape seeds powder was extracted with hydro alcoholic mixture. Emulsions consisting of different concentrations of cetyl dimethicone (Abile EM90), the nonionic emulsifier, liquid paraffin as oily phase and water as aqueous phase were developed. Color, odor, pH, viscosity, liquefaction, phase separation, centrifugation and thermal stability of the formulated emulsions were observed at various storage temperatures i.e. 8±0.5°C, 25±0.5°C, 40±0.5°C and 40°C±0.5°C with 70% RH. The stable formulation consist of 16% mineral oil, 4% of ABIL EM 90(®), 4% grape seeds extract, 1% rose oil and 75% distilled water. All the results derived from this study showed good stability over the three months study period which indicates w/o emulsion can be used as carrier of 4% grape seeds extract to enhance desired effects when applied topically.


Assuntos
Extrato de Sementes de Uva/química , Compostos de Trimetilsilil/química , Estabilidade de Medicamentos , Emulsões , Concentração de Íons de Hidrogênio , Viscosidade
18.
Acta Pol Pharm ; 72(1): 3-11, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-25850195

RESUMO

Glycine max, known as the soybean or soya bean, is a species of legume native to East Asia. Soya beans contain many functional components including phenolic acids, flavonoids, isoflavonoids (quercetin, genistein, and daidzein), small proteins (Bowman-Birk inhibitor, soybean trypsin inhibitor) tannins, and proanthocyanidins. Soybean seeds extract and fresh soymilk fractions have been reported to possess the cosmeceutical and dermatological benefits such as anti-inflammatory, collagen stimulating effect, potent anti-oxidant scavenging peroxyl radicals, skin lightening effect and protection against UV radiation. Thus, present review attempts to give a short overview on dermatological and cosmeceutical studies of soybean and its bioactive compounds.


Assuntos
Cosméticos/farmacologia , Glycine max/metabolismo , Extratos Vegetais/farmacologia , Pele/efeitos dos fármacos , Animais , Humanos
19.
Artigo em Inglês | MEDLINE | ID: mdl-24311867

RESUMO

Aiming at the exploration of herbal use by society, crude extracts of the seeds of some commonly used medicinal plants (Vitis vinifera, Tamarindus indica and Glycin max) were screened for their free radical scavenging properties using ascorbic acid as standard antioxidant. Free radical scavenging activity was evaluated using 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical. The overall antioxidant activity of grape seeds (Vitis vinifera) was the strongest, followed in descending order by soybean (Glycin max) and tamarind (Tamarindus indica). The seeds extract of Vitis vinifera, Glycin max and Tamarindus indica showed 85.61%, 83.45% and 79.26%, DPPH scavenging activity respectively.


Assuntos
Sequestradores de Radicais Livres/análise , Glycine max/química , Extratos Vegetais/análise , Sementes , Tamarindus/química , Vitis/química , Antioxidantes/análise , Antioxidantes/química , Compostos de Bifenilo , Sequestradores de Radicais Livres/química , Radicais Livres , Indicadores e Reagentes , Picratos , Extratos Vegetais/química
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