Factorial Design for the Optimization of Clindamycin HCl-Loaded Ethosome with various concentrations of Phospholipon 90g and Ethanol

Abstract

Clindamycin HCl is a drug for the treatment of acne. Clindamycin can act as an anti-acne by interfering with bacterial protein synthesis. The concentration of clindamycin used in the treatment of acne is 1%. Still, the bioavailability of the drug in the serum only reaches 0.7 – 12.4% of the total active substance in the preparation, so it is necessary to develop preparations that can increase the bioavailability of the drug Clindamycin HCl, one of which is in the form of ethosomes. This study aimed to optimize the clindamycin HCl loaded ethosomes formula with variations in the concentration of Phospholipon 90G and ethanol using the 22 factorial design method to obtain four formulas. The concentrations of phospholipon 90G used were 2% and 4%, while ethanol was 20% and 40%, respectively. Ethosomes were prepared using the thin layer hydration method and characterized by percent entrapment efficiency (%EE), particle size, and polydispersity index to determine the optimum formula. Based on the factorial design analysis results, the concentration of Phosholipon 90G, ethanol, and their two interactions significantly affected the value of entrapment efficiency, particle size, and polydispersity index with p<0.05. The optimum formula was obtained using 2% phospolipon 90G and 40% ethanol with an entrapment efficiency of 98.31±0.06, a particle size of 179.6±8.6nm, and a polydispersity index of 0.361±0.015. The optimum formula also showed good solubility in distilled water and acid solvents and good physical stability.