동결건조법을 이용한 proliposomes의 제조 및 평가

Abstract

Purpose. proliposomes are novel vesicular drug carrier system having several advantages over conventional liposomes. However, conventional methods of preparing proliposomes have limitation in terms of low drug content. Because the drug content of the proliposomes is proportional to the content of lipid, the aim of this study was to find a new method to increase the lipid content, resulting in increase in drug content. Simvastatin(SV) was selected as a model drug to increase bioavailability by improving its solubility and dissolution. Methods. SV-proliposomes were prepared by freeze-drying technique using different contents ratio of lipid and SV for optimizing the formulation. The formulations were characterized for surface morphology, size, zeta potential and encapsulation efficiency. In vitro dissolution study of SV-proliposomes formulations was carried out comparing with SV powder and commercial SV tablet. Results. The particle size of reconstituted liposomes was decreased with increasing the lipid /drug ratio. The particle size and zeta potential of reconstituted particles were in the range of 525~1090 nm and –48.8~46.7mV, respectively. The percentage encapsulation of drug was increased with increasing the lipid/drug ratio, in the range of 50.8~78.6%. Moreover, SV release from the formulation was higher than commercial tablet and SV powder. Conclusion. Drug loading of proliposomes can be enhanced by using freeze- drying method. Improvement in dissolution of SV from proliposomess formulations suggests the potential of proliposomes as a suitable carrier for improving oral delivery of SV.