Formulation development and optimization of transungual drug delivery system of terbinafine hydrochloride for the treatment of onychomycosis
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- 作者：Mayur M. Patel ; Zeal M. Vora
- 刊名：Drug Delivery and Translational Research
- 出版年：2016
- 出版时间：June 2016
- 年：2016
- 卷：6
- 期：3
- 页码：263-275
- 全文大小：3,971 KB
- 刊物主题：Pharmaceutical Sciences/Technology;
- 出版者：Springer US
- ISSN：2190-3948
- 卷排序：6
文摘
The aim of present investigation was to develop transungual drug delivery system (nail lacquer) of terbinafine hydrochloride for treatment of onychomycosis. Different types of penetration enhancers, viz. 2-mercaptoethanol, n-acetyl-l-cysteine and thioglycolic acid, were evaluated to determine their effect on drug permeation. Various types of polymers, both hydrophobic (Eudragit® RL 100 and Eudragit® RS 100) and hydrophilic polymers (hydroxypropyl methyl cellulose (HPMC) E15), were evaluated for their film-forming and drug permeation characteristics. The nail lacquer was optimised statistically by applying 32 full factorial design. Polymer ratio (Eudragit® RL 100/HPMC E15; X1) and solvent ratio (ethanol/water; X2) were selected as independent variable, and viscosity (cPs), nail plate hydration (%) and in vitro drug permeated at the end of 24 h (μg/cm2) were selected as dependent variable. The optimised batch comprises of polymer ratio (70:30) and solvent ratio (75:25). Ex vivo drug permeation study was performed using human cadaver toe nail plate. The results revealed that the amount of drug permeated at the end of 24 h was 61.55 ± 3.2 μg/cm2, which was found to be higher than the minimum inhibitory concentration of drug. This study confirms that the developed drug-loaded nail lacquer could be used as a promising tool for the effective treatment of onychomycosis.KeywordsNail lacquerBovine hoof membranesDrug permeationEx vivo antifungal activityOnychomycosis