Preparation of Hydroxycampothecinum Microspheres and Its Distribution in Mice
- VernacularTitle:羟基喜树碱微球的制备及其小鼠体内分布研究
- Author:
Xiaolong KONG
- Publication Type:Journal Article
- Keywords:
Hydroxycampothecinum;
Polylactic acid;
Microspheres;
Mice;
Lung targeting;
Sustained-release
- From:
China Pharmacy
2005;0(22):-
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVE:To prepare lung-targeting hydroxycampothecinum(HCPT) microspheres and evaluate its in vitro release characteristics and its lung-targeting property in mice.METHODS:The microspheres was prepared by solvent volatilization with polylactic acid as chief excipient.The particle size,entrapment efficiency(EE) and drug loading(DL) of the microspheres were studied and the in vitro release rate was compared with that of the crude drug.12 mice enrolled were injected via vena caudalis with HCPT micropheres or HCPT crude drug,at 30 min,the drug level in plasma and tissues were determined and the relative distribution rates(RDR) were computed.RESULTS:81.6% of the microspheres ranged from 7～ 30 ?m in particle size,the mean diameter was (14.2?3.1) ?m,the EE was 72.36%,the DL was (40.6?3.6)%,and the in vitro drug release parameter T50 was 85 min for microspheres vs.18 min for crude drug.The drug level of the microspheres in lung was the highest at (32.2?2.48) ?g?mL-1 with a RDR of 58.1%;The drug level of the crude drug group in plasma was the highest at (13.52?2.58) ?g?mL-1 with a RDR of 25.24%.CONCLUSION:The prepared HCPT microspheres had the distinctive characteristics of sustained-release and lung targeting.
