Probilosomes: A Novel Bile Salt Containing Nanocarrier for Enhancing Oral Bioavailability

Abstract

Objective: Probilosomes vesicular drug delivery system was developed to prevent acid degradation of the drug and to improve its oral bioavailability by resisting the drug release in acidic pH of the stomach. Method: Thin-film hydration technique was adopted to prepare probilosomes using soybean phosphatidylcholine (lipoid S100) bile salt (Sodium Deoxycholate) and mannitol as a carrier. The formulations were optimized using (32) general full factorial design. Results: The prepared probilosomal formulations were evaluated for entrapment efficiency, drug content and in vitro dissolution studies. Based on the entrapment efficiency values and sustained drug release (PB9) formulation is optimized and further evaluated for surface morphology (SEM), particle size, polydispersity index, zeta potential and ex vivo studies. The optimized formulation (PB 9) showed particle size, polydispersity index (PDI) of 76.4 nm, 0.45 and zeta potential of -9.17 mV respectively. In vitro dissolution studies showed less than 20% of drug release at pH 1.2 and sustained release in pH 6.8 phosphate buffer up to 8 hr. The ex vivo studies indicated a 2 fold increase in the oral bioavailability of the probilosomal formulation compared to pure drug. Conclusion: Rosuvastatin calcium probilosomes were successfully prepared to resist the drug release in stomach pH and prevent the acid degradation of the drug. Ex vivo studies showed increased oral bioavailability of the probilosomal formulations compared to pure drug. Hence, these formulations can be used as an alternative to conventional enteric dosage forms.