Optimization of Lipid-Based Ketoconazole Nanoformulations Through Stirring Techniques and Ingredient Quantity Adjustments

Abstract

The Biopharmaceutical Classification System (BCS) classifies drugs on the basis of solubility and permeability. Ketoconazole belongs to class II drugs of the Biopharmaceutical Classification System (BCS) which are characterized by high permeability but low solubility issues. The current research work aimed to formulate optimized nano-formulation for ketoconazole by altering stirring time, speed, and ingredient ratios. In this study, a stirring speed minimum of 600 rpm and a maximum of 1200 rpm was used. The minimum stirring time of 7 minutes and a maximum of 30 minutes was noted. Olive oil was used as a lipid, Tween 80 was incorporated as a surfactant, and polyethylene glycol (PEG 6000) was used as a co-surfactant. Different ratios of Surfactants and Co-surfactants were used. Formulations with different particle sizes and polydispersity index were obtained. The quantity of surfactant (tween 80) used was 1.5g, the Co-surfactant (polyethylene glycol) was 0.4g, the lipid used was 1g, and drug quantity was 0.12g in the optimized formulation (KZME 1). The stirring time applied for optimized ketoconazole nano-formulation was 15 minutes and a stirring speed of 800 rpm was applied while keeping the drug quantity at 120 mg. The optimized ketoconazole nano-formulation obtained has a particle size of 50.29nm and a Polydispersity index of 0. 377. It was observed that optimized and stable ketoconazole nano-formulation can be achieved with the help of proper stirring speed and time which can improve the solubility of ketoconazole drug, and can lead to an increase in the bioavailability and therapeutic efficacy of ketoconazole.