Formulation and Evaluation Thermoreversible Gel of Antifungal Agent for Treatment of Vaginal Infection

Aims:TheaimthisresearchworkistoformulateandevaluatethermoreversiblegelofantifungalagentClotrimazolefortreatmentofvaginalinfection.PlaceandDurationofStudy:DepartmentofBiopharmaceutics,GovernmentCollegeofPharmacy,Karad,Maharashtra,India,betweenJune2009andJuly2010.Methodology:DifferentFormulationsofthermoreversiblegelofantifungalagentClotrimazolewerepreparedbyusingvariousconcentrationsofethanol,PEG400,sodiumdodecylsulphate,polycarbophilandpluronicF127andpluronicF68.Thegelformulationsweresubjectedforevaluationonthebasisofrheologicalbehaviour,mucoadhesivebehaviour,in-vitroperformance.Results:TheresultsindicatethatPolymerssuchaspolycarbophil,PEG-400invariousconcentrationstoprepareformulationswerefoundtoreleasedrugforperiodover12hrs.Withoutgettingdislodged.Theformulationshavesatisfactoryrheologicalbehaviorandtheirdiffusionprofileiscomparabletothemarketedgelformulation.Significantdifferencewasobservedintherheologicalbehaviorofformulations.Gelstrength,spreadability,mucoadhesivestrengthofformulationBandCweredesirable.DrugdiffusionofformulationBandCwere95.2%releaseafte 11hrs98.5%releaseafter11hrs,respectivelywhichwasgoodascomparedtomarketedformulationshowingdrugdiffusionof102.2%after10hrs.Conclusion:OnbasisoftheresultsweconcludedthatdevelopedthermoreversiblegelofClotrimazolewillbebetteralternativetoconventionaldosageformClotrimazole&willimprovepatientcompliance

Optimization of Formulation of Fufang Huangqi Cream by D-optimal Mixture Design Based on AHP-CRITIC Analysis / 中国实验方剂学杂志

Objective::To optimize the matrix prescription of Fufang Huangqi cream and evaluate its rheological properties. Method::With appearance, spreadability and stability as evaluation indexes, the weighting coefficient of each evaluation index was determined by analytic hierarchy process (AHP), criteria importance through intercriteria correlation method (CRITIC) and AHP-CRITIC mixed weighting method. The formulation of Fufang Huangqi cream was optimized by D-optimal mixture design and its rheological properties were evaluated. Result::The weight coefficients of appearance, spreadability and stability according to AHP-CRITIC mixed weighting method were 0.185, 0.282 and 0.532, respectively. According to D-optimal mixture design based on AHP-CRITIC analysis, the optimized formulation of Fufang Huangqi cream was liquid paraffin of 3.70 g, vaseline of 2.00 g, stearic acid of 2.00 g, sodium dodecyl sulfate of 5.90 g, glycerin of 6.00 g and extract of 20.40 g. The rheological parameters of Fufang Huangqi cream was non-newtonian index<1, storage modulus>loss modulus. Conclusion::The preferred matrix formulation is stable and feasible. Fufang Huangqi cream has good appearance and is a shear thinning non-newtonian fluid. Its viscosity and ductility meet the needs of industrial production and clinical application.

Screening of mucoadhesive vaginal gel formulations

Rational design of vaginal drug delivery formulations requires special attention to vehicle properties that optimize vaginal coating and retention. The aim of the present work was to perform a screening of mucoadhesive vaginal gels formulated with carbomer or carrageenan in binary combination with a second polymer (carbomer, guar or xanthan gum). The gels were characterised using in vitro adhesion, spreadability and leakage potential studies, as well as rheological measurements (stress and frequency sweep tests) and the effect of dilution with simulated vaginal fluid (SVF) on spreadability. Results were analysed using analysis of variance and multiple factor analysis. The combination of polymers enhanced adhesion of both primary gelling agents, carbomer and carrageenan. From the rheological point of view all formulations presented a similar behaviour, prevalently elastic and characterised by loss tangent values well below 1. No correlation between rheological and adhesion behaviour was found. Carbomer and carrageenan gels containing the highest percentage of xanthan gum displayed good in vitro mucoadhesion and spreadability, minimal leakage potential and high resistance to dilution. The positive results obtained with carrageenan-xanthan gum-based gels can encourage the use of natural biocompatible adjuvants in the composition of vaginal products, a formulation field that is currently under the synthetic domain.

O planejamento racional de formulações para a liberação vaginal de fármacos requer atenção especial às propriedades do veículo, que otimizem o revestimento e a retenção vaginal. O objetivo do presente trabalho foi realizar uma triagem de géis vaginais mucoadesivos formulados com carbomero ou carragenina em combinação binária com um segundo polímero (carbomero, goma guár ou xantana). Os géis foram caracterizados usando estudos in vitro de aderência, espalhabilidade e potencial de vazamento, bem como medições reológicas (testes de varredura de tensão e frequência) e o efeito de diluição com fluido vaginal simulado (SVF) na espalhabilidade. Os resultados foram analisados utilizando a análise de variância e de fator múltiplo. A combinação de polímeros reforçou a adesão de ambos os agentes gelificantes primários, carbomero e carragenina. Do ponto de vista reológico todas as formulações apresentaram comportamento semelhante, predominantemente elástico e caracterizado por valores de tangente de perda bem abaixo de 1. Não se encontrou correlação entre as medições reológicas e o comportamento de adesão. Os géis de carbomero e carragenina contendo o maior porcentual de goma xantana apresentaram melhor mucoadesão e espalhabilidade, menor potencial de vazamento e maior resistência à diluição in vitro. Os resultados positivos obtidos com géis de carragenina-goma xantana podem incentivar o uso de adjuvantes biocompatíveis naturais na composição dos produtos vaginais, um campo de formulação atualmente sob o domínio de produtos sintéticos.

Characterization and stability studies of emulsion systems containing pumice

Emulsions are the most common form of skin care products. However, these systems may exhibit some instability. Therefore, when developing emulsions for topical application it is interesting to verify whether they have suitable physical and mechanical characteristics and further assess their stability. The aim of this work was to study the stability of emulsion systems, which varied in the proportion of the emulsifying agent cetearyl alcohol (and) sodium lauryl sulfate (and) sodium cetearyl sulfate (LSX), the nature of the oily phase (decyl oleate, cyclomethicone or dimethicone) and the presence or absence of pumice (5% w/w). While maintaining the samples at room temperature, rheology studies, texture analysis and microscopic observation of formulations with and without pumice were performed. Samples were also submitted to an accelerated stability study by centrifugation and to a thermal stress test. Through the testing, it was found that the amount of emulsifying agent affects the consistency and textural properties such as firmness and adhesiveness. So, formulations containing LSX (5% w/w) and decyl oleate or dimethicone as oily phase had a better consistency and remained stable with time, so exhibited the best features to be used for skin care products.

Emulsões são a forma de apresentação mais comum dos produtos para aplicação na pele. No entanto estes sistemas podem exibir alguma instabilidade. Por esta razão, quando do desenvolvimento de emulsões para aplicação tópica é importante verificar se estas apresentam propriedades físicas ou mecânicas adequadas e avaliar a sua estabilidade. O objetivo deste trabalho consistiu no estudo da estabilidade de emulsões, cujas variações entre elas foi a proporção de agente emulsificante álcool estearílico (mais) laurilsulfato de sódio (mais) estearilsulfato de sódio (LSX), a natureza da fase oleosa (decil oleato, ciclometicona ou dimeticona) e a presença ou ausência de pedra-pomes (5% m/m). Mantendo as amostras à mesma temperatura, realizaram-se o estudo da reologia, a análise de textura e observação microscópica das formulações com e sem pedra-pomes. Amostras foram, também, submetidas a estudo de estabilidade acelerada por centrifugação e a ensaio de estresse térmico. Através dos testes realizados, constatou-se que a quantidade de agente emulsificante influencia a consistência e as propriedades de textura, como a firmeza e a adesividade. As formulações contendo LSX (5% m/m) e decil oleato ou dimeticona como fase oleosa exibiram melhores caraterísticas como produtos para aplicação na pele, uma vez que estas formulações apresentaram menor firmeza e consistência e permaneceram estáveis com o tempo.