Ketoconazole Loaded Proliposomes Lab Report

Preparation of ketoconazole loaded Proliposomes

Ketoconazole (KTZ) loaded proliposomal gel formulations were formulated by method reported by Perret et al. 1991 with slight modification. Constant amount of drug was added to varying ratios of phophatidylcholine and cholesterol which constitute lipid component of 1mmol quantity. This lipid mixture was prepared in clean and dry, wide mouthed glass vials to which 400µL of absolute alcohol was added and after confirming the formation of homogenous dispersion, the glass vials were heated thermostatically on a water bath at 60-70oC with intermittent shaking. Add 160µL of double distilled water maintained at the same temperature to the transparent solutions formed, these upon cooling change to yellow translucent liquid/gel or white creamy proliposomal gel. Proliposomal gel formulations with positive and negative charge were prepared in above mentioned manner by adding 10 mol% of total lipid of stearylamine

In the donor compartment, proliposomal formulation and control (drug suspended in sodium CMC) equivalent to 10mg of KTZ were placed separately. 30% v/v acetonitrile containing phosphate buffer saline (pH 7.4) was taken as receptor medium and kept under constant stirring upto 24 h. In order to avoid evaporation of the contents, donor compartment and sampling port are covered with aluminium foil. 500 µL of aliquots are drawn at predetermined time intervals and equal volumes have been replaced so as to maintain receptor phase volume. All the samples withdrawn were estimated for drug content using HPLC and the data was fitted into mathematical equations (zero order, first order and Higuchi models) (Szuts et al., 2010) to derive the kinetics and mechanism of drug release from proliposomal gel