Effect of Borneol to Enhance Topical Drug Penetration for Lipophilic Drug
Pharmaceutical Science-Pharmaceutics
DOI:
https://doi.org/10.22376/ijlpr.2023.13.SP1.P46-P54Keywords:
Micro-Emulation, Gel formulation, Borneol, Penetration Enhancer, Transdermal Drug Delivery SystemAbstract
Abstract: Progesterone is a C21-steroid hormone, lipophilic, having log P of 3.56 and therefore, poor permeation of active moiety in the skin is a major challenge of transdermal delivery. There are many strategies to overcome the permeation of drugs through the skin, such as using nanocarriers, applying physical and chemical permeation enhancers and others. Penetration enhancers act by modifying the hydration properties of stratum corneum and altering the structure of lipids and proteins in the intercellular channels carrier mechanism. The present work estimates the in-vitro permeation of progesterone from microemulsionbased transdermal formulations containing Borneol as penetration enhancers. Progesterone was taken as a model drug. The microemulsion was formulated by a simple stirring method, followed by adding Myritol as oil, Tween 80 as a surfactant, and + PEG 400 as a co-surfactant. The globule size of the final microemulsion formulation was found to be in the range of 200- 394 nm with PDI 0.123, and Zeta potential study indicated -23.1 mV showing good stability. TEM images showed that the F14 batch is spherical, and its size was identical to that obtained from laser diffraction. For ease of application, microemulsion was converted to gel using Carbopol 980. Borneol with a concentration of 4% showed a drug release of 83% after 9hrs. The formulation's viscosity, pH and texture profile was found to be optimum. The final formulation follows Korsmeyer-Peppas release kinetics. A stability study of microemulsion gel was performed for 180 days at refrigerated temperature and room temperature. The formulation showed better storage via stability study with good spreadability. Thus, developed Borneol containing microemulsion-based transdermal formulation can be a promising alternative to deliver progesterone for hormone replacement therapy in any indication such as breast tenderness, infertility, lumpy (fibrocystic) breasts, low blood sugar, increased blood clotting etc.
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Copyright (c) 2022 Anupama Diwan, Shekhar Sharma, Rani Mansuri, Rupali Sharma
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