Development of the Forskolin Microemulsion Formula and its Irritation Test on Rabbits.

Abstract

This study aimed to develop a microemulsion formula that can increase the solubility and stability of forskolin and its safety for topical use. The materials used for the development of the microemulsion formula were triglyceride oil, non-ionic surfactants, and polyethylene glycol (PEG) for cosurfactants, which were selected on the basis of the results of the forskolin solubility test using high performance liquid chromatography (HPLC). The microemulsion was formulated by the phase titration method. Formula stability was determined by storage for 90 days in a refrigerator at room temperature, and an accelerated stability test was performed by determining globule size, forskolin concentration, and pH. The safety of using microemulsions was determined by skin irritation tests on albino rabbits. The optimum microemulsion formula consisted of Maisine® CC, polyoxyethylene sorbitan 20 (POE 20), and PEG 400 with a ratio of 4:25:5 w/v, which increased the solubility of forskolin the most, namely 2.19 mg mL-1. Based on globule size (<50 nm), forskolin concentration (2 mg.mL-1), and pH (6.0-6.35), the formula was stable in refrigerator storage and room temperature but unstable in the accelerated stability test (40 °C) starting on day 21. This optimum formula exhibits a primary irritation index (PII) of 0.11, which is categorized as feeble irritation and can be ignored. The microemulsion prepared by the phase titration method containing Maisine® CC, POE 20, and PEG 400 (4:25:5, w/v) as a base and 0.2% forskolin was stable in refrigerator storage and at room temperature. This microemulsion is mild or negligible irritant with a PII: 0.11.