Novel liposomal drug delivery system actively targeting Cryptococcus neoformans and elimination of infection
10.16438/j.0513-4870.2016-0239
- VernacularTitle:主动靶向新生隐球菌的脂质体递药系统及其抗隐球菌肺脑合并感染的初步研究
- Author:
Shuang WU
1
;
Zhuo-xuan LI
1
;
Guo-jian LIAO
1
;
Zhang-bao CHEN
1
;
Chong LI
1
Author Information
1. College of Pharmaceutical Sciences, Southwest University, Chongqing 400716, China
- Publication Type:ORIGINAL ARTICLES
- Keywords:
phage display;
cryptococcosis;
liposome;
itraconazole;
targeting drug delivery system
- From:
Acta Pharmaceutica Sinica
2016;51(7):1150-
- CountryChina
- Language:Chinese
-
Abstract:
The purpose of this study is to develop a liposomal drug delivery system actively targeting Cryptococcus neoformans and explore its feasibility in therapy of cryptococcal infection. The specific fungibinding peptide was screened from 12-mer random phage display library, and linked to PEG-DSPE as the functional material of liposomes. The targeting capability of peptide-modified liposomes were investigated by fungi binding assay in vitro and fluorescence imaging in vivo. Itraconazole as a model drug were then encapsulated in the liposomes and were evaluated in pharmacodynamic test in vitro and for therapeutic effects against cryptococcal meningitis complicated with pulmonary cryptococcosis in vivo. The results showed that the peptide (sequence:NNHREPPDHRTS) could selectively recognize Cryptococcus and effectively mediate the corresponding liposomal formulation to accumulate in the infection site in vivo. This peptide-modified liposome has a small particle size (mean diameter of 88.25±2.43 nm) with a homogeneous distribution and high encapsulation efficiency (88.05±0.25%) of itraconazole. After intravenous administration, the pathogens were obviously eliminated in lung and brain, and the life-span of model mice were significantly prolonged, suggesting a promising potential of this cryptococcosis targeting strategy.
