DESIGN, FABRICATION AND EVALUATION OF ROSUVASTATIN PHARMACOSOME - A NOVEL SUSTAINED RELEASE DRUG DELIVERY SYSTEM

Pal Tapas Kumar*, Jayita Mishra and Abhishekh Podder

ABSTRACT

Pharmacosomes are amphiphilic lipid vesicular systems containing phospholipid complexes with characteristic potential to improve solubility, absorptivity and bioavailability of both poorly water soluble as well as poorly lipophilic drugs. With an objective to improve the aqueous solubility and subsequent bioavailability of a model BCS class III drug, Rosuvastatin Calcium, its Pharmacosomes were developed and subjected to evaluation of physicochemical characteristics. The cumulative release profile and permeation studies had been also done by in-vitro dissolution test, in-vitro diffusion study by modified Franz diffusion cell using egg membrane and in-vivo study for antihyperlipidemic effect by Tritron induced hyperlipidemia animal model. Solubility of prepared Pharmacosomes was found to be higher than pure Rosuvastatin Calcium. Drug content was found to be in the range of 90.4±0.52% to 94.4±0.61% in all the batches of Pharmacosomes. FTIR data also demonstrated superimposed curves to confirm the stability of Pharmacosome complex after 2 months stability study at 40 deg C temp and 75% RH. After 24 hours, maximum drug released from formulation F1 was found as 66.93% in the dissolution study and maximum drug permeated by diffusion through egg membrane from formulation F1 was 49.50% in the diffusion study. In-vitro and in-vivo experiments justify and confirm Rosuvastatin Pharmacosomes formulations as significantly better than Rosuvastatin Calcium as a unique sustained release delivery system with simultaneous reduction of Dosage and improved bioavailability.

Keywords: Pharmacosome, Hand shaking method, Hyperlipidemic, Statins, Log P value, Vesicular systems.