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

Ting Zhou; Xin Tang; Wei Zhang; Jianfang Feng; Wei Wu

doi:10.1080/10717544.2019.1636422

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

Drug Deliv. 2019 Dec;26(1):673-679. doi: 10.1080/10717544.2019.1636422.

Authors

Ting Zhou¹, Xin Tang², Wei Zhang¹, Jianfang Feng³, Wei Wu¹

Affiliations

¹ a School of Pharmacy , Guilin Medical University , Guilin , P.R. China.
² b School of Public Health , Guilin Medical University , Guilin , P.R. China.
³ c School of Pharmacy , Guangxi University of Chinese Medicine , Nanning , P.R. China.

Abstract

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.

Keywords: 10-hydroxycamptothecin; biodistribution; liposomes; pharmacokinetics; stearyl glycyrrhetinate.

MeSH terms

Animals
Antineoplastic Agents, Phytogenic / administration & dosage*
Antineoplastic Agents, Phytogenic / pharmacokinetics
Biological Availability
Camptothecin / administration & dosage
Camptothecin / analogs & derivatives*
Camptothecin / pharmacokinetics
Drug Carriers / chemistry*
Drug Carriers / pharmacokinetics
Female
Glycyrrhetinic Acid / analogs & derivatives*
Liposomes / chemistry*
Liposomes / pharmacokinetics
Liposomes / ultrastructure
Mice
Particle Size
Rats
Tissue Distribution

Substances

Antineoplastic Agents, Phytogenic
Drug Carriers
Liposomes
stearyl glycyrrhetinate
10-hydroxycamptothecin
Glycyrrhetinic Acid
Camptothecin

Grants and funding

This work was supported by the National Natural Science Foundation of China (No. 81560653, 81760704) and Natural Science Foundation of Guangxi (No. 2016GXNSFAA380081, 2018GXNSFAA281332).