Key Laboratory of Drug Targeting and Drug Delivery Systems, Ministry of Education, West China School of Pharmacy, Sichuan University, Sichuan, PR China.
Drug Dev Ind Pharm. 2010 Jul;36(7):823-31. doi: 10.3109/03639040903520975.
In order to prolong the duration of drug in the circulation, multivesicular liposome (MVL, namely DepoFoam) was utilized as a sustained-release delivery system for hydroxycamptothecin (HCPT).
HCPT is insoluble in both water and physiological acceptable organic solvents; therefore, HCPT-phospholipid complex (HCPT-PCC) was prepared by solvent evaporation method to improve its liposolubility. In this study, preparation, characterization, in vitro release, and in vivo pharmacokinetics of HCPT-phospholipid complex-loaded MVLs (HCPT-MVLs) were investigated.
The results showed that the average particle size of HCPT-MVL was 9 mum and the encapsulation efficiency was 90%. In addition, HCPT-MVLs could improve both in vitro release and in vivo pharmacokinetic behaviors of the original drug, with a sustained release of drugs over 5-6 days.
These data suggested that by combined use of DepoFoam and phospholipid complex formation technique HCPT could be successfully entrapped into the MVLs, which might provide a paradigm for sustained release of insoluble drugs.
为了延长药物在循环中的持续时间，多泡脂质体（即 DepoFoam）被用作羟基喜树碱（HCPT）的缓释递送系统。
HCPT 在水和生理可接受的有机溶剂中均不溶；因此，通过溶剂蒸发法制备 HCPT-磷脂复合物（HCPT-PCC）以提高其脂溶性。本研究考察了载有 HCPT-磷脂复合物的多泡脂质体（HCPT-MVLs）的制备、表征、体外释放和体内药代动力学。
结果表明，HCPT-MVL 的平均粒径为 9 微米，包封率为 90%。此外，HCPT-MVLs 可以改善原药的体外释放和体内药代动力学行为，使药物能够持续释放 5-6 天。
这些数据表明，通过联合使用 DepoFoam 和磷脂复合物形成技术，HCPT 可以成功地包封到 MVLs 中，这可能为难溶性药物的缓释提供一种范例。
