Posaconazole Loaded Quatsomes For Topical Delivery : Development And Optimization By 32 Factorial Design

Abstract

Objective: The self-assembling quatsomes, as a new-generation nanovesicle, provide a great advantage over older lipid-based carriers such as liposomes and niosomes, as quatsomes resolve many of the limitations associated, such as chemical instability and encapsulation inefficiency. These nanostructures are created from a single-chain cationic surfactant and cholesterol. The study aimed to formulate posaconazole-loaded quatsomes while determining the impact of cetylpyridinium chloride (CPC) and cholesterol on the selected responses like particle size, entrapment efficiency, and in vitro drug release.

Method:Posconazole is BCS-II drug with the criteria low solubility and high permeability, this limitation of poorly soluble nature of the drug can enhanced by loading in proper carrier-based system like quatsomes. Posconazole loaded quatsomes was prepared by thin film hydration method and a total of nine formulations were prepared by selecting a 32 factorial design using design expert software version 13.0, which were then analyzed using response surface methodology (RSM).

Results: Statistical analysis like ANOVA was used to determine the significance of the models; p <0.05 was considered as significant. All three responses were found statistically significant with R² being greater than 0.97. Cholesterol was found to be a highly significant factor for particle size; as increase in concentration of lipid resulted in increased particle size. For entrapment efficiency, the significant factors like CPC and cholesterol, increase in cholesterol level was found to decrease efficiency. Through the obtained results it was concluded that selected factors shows a major impact on responses.

Conclusion: Out of all nine formulations, F3 for which a desirability function was maximized contained 100mg of cationic surfactant CPC and 150 mg of cholesterol. These particles in optimized formulation found to be with a size of 133.7nm, 93.68% entrapment efficiency, and 92.5% invitro drug release.