Drug-in-cyclodextrin-in-liposomes: A novel drug delivery system for flurbiprofen

作者：Zhang, Lina; Zhang, Qi; Wang, Xin; Zhang, Wenji; Lin, Congcong; Chen, Fen; Yang, Xinggang; Pan, Weisan^*

来源：International Journal of Pharmaceutics, 2015, 492(1-2): 40-45.

DOI：10.1016/j.ijpharm.2015.07.011

• Flurbiprofen
• Cyclodextrins
• Liposomes
• In vitro
• In vivo
• Bioavailability

A novel delivery system based on drug-cyclodextrin (CD) complexation and liposomes has been developed to improve therapeutic effect. Three different means, i.e., co-evaporation (COE), co-ground (GR) and co-lyophilization (COL) and three different CDs (beta-CD, HP-beta-CD and SBE-beta-CD) were contrasted to investigate the characteristics of the end products. FP/FP-CD loaded liposomes were obtained by thin layer evaporation technique. Size, zeta potential and encapsulation efficiency were investigated by light scattering analysis and minicolumn centrifugation. Differential scanning calorimetry (DSC) and transmission electron microscopy (TEM) showed the amorphous form of complexes and spherical morphology of FP-HP-beta-CD COE loaded liposomes. The pH 7.4 phosphate buffer solution (PBS) was selected as the medium for the in vitro release. Wistar rats were put into use to study the pharmacokinetic behavior in vivo. FP-HP-beta-CD COE loaded liposomes showed the better physicochemical characters that followed the average particle size, polydispersity index, zeta potential and mean encapsulation efficiency 158 +/- 10 nm, 0.19 +/- 0.1, -12.4 +/- 0.1 mW and 56.1 +/- 0.5%, separately. The relative bioavailability of FP-HP-beta-CD COE loaded liposomes was 420%, 201% and 402% compared with FP solution, FP-HP-beta-CD and FP-liposomes, respectively. In conclusion, the novel delivery system improved the relative bioavailability of FP significantly and provided a perspective way for delivery of insoluble drugs.

• 出版日期2015-8-15
• 单位沈阳药科大学