Preparation and in vitro and in vivo evaluations of 10-hydroxycamptothecin liposomes modified with stearyl glycyrrhetinate

Drug Delivery

Jianfang Feng¹  Wei Zhang²  Wei Wu²  Ting Zhou²  Xin Tang³ 

[1] School of Pharmacy, Guangxi University of Chinese Medicine, Nanning, P.R. Chin;School of Pharmacy, Guilin Medical University, Guilin, P.R. China;School of Public Health, Guilin Medical University, Guilin, P.R. China;

关键词: 10-hydroxycamptothecin;    stearyl glycyrrhetinate;    liposomes;    pharmacokinetics;    biodistribution;   

DOI  :  10.1080/10717544.2019.1636422

来源: publisher

【 摘 要 】

10-Hydroxycamptothecin (HCPT) liposomes surface modified with stearyl glycyrrhetinate (SG) were prepared by the film dispersion method. Characterization of the liposomes, including drug release in vitro, pharmacokinetics and tissue distribution, was done. HCPT in plasma and tissues was determined by high-performance liquid chromatography (HPLC). Compared with the conventional HCPT-liposomes and commercially available hydroxycamptothecin injection (HCPT Inject), pharmacokinetic parameters indicated that SG-HCPT-liposomes had better bioavailability. Regarding tissue distribution, the concentration of HCPT loaded by SG modified liposomes in the liver was higher than other tissues and the risk to the kidney was lower than HCPT-liposomes and HCPT Inject. These results support the hypothesis that the HCPT-liposomes modified with SG show enhanced liver-targeting through the glycyrrhetinic acid (GA) receptor to be an efficient drug carrier, which may help to improve therapeutic methods for hepatic diseases in the future.

【 授权许可】

CC BY