Stability and pharmacokinetics of hyaluronic acid-modified asparaginase self-assembled biomimetic nanocapsules
10.11665/j.issn.1000-5048.20200411
- VernacularTitle:透明质酸修饰天冬酰胺酶自组装仿生纳米囊的稳定性及其体内药代动力学
- Author:
Yuying LIU
1
;
Yao LI
;
Qiang YANG
;
Ran CHEN
;
Kailing LI
;
Jingqing ZHANG
Author Information
1. 重庆医科大学重庆药物高校工程研究中心
- Publication Type:Journal Article
- Keywords:
asparaginase;
hyaluronic acid;
nanocapsules;
pharmacokinetics;
self-assembly;
drug delivery
- From:
Journal of China Pharmaceutical University
2020;51(4):462-466
- CountryChina
- Language:Chinese
-
Abstract:
The stability and pharmacokinetic properties of hyaluronic acid-modified asparaginase (Asp) self-assembled bionic nanocapsules (ASNCs) were preliminarily investigated. ASNCs were prepared by molecular self-assembly method to investigate their morphology, particle size, zeta potential and antitrypsin stability. After intravenous injection of free Asp and ASNCs, rat plasma samples at different times were taken to determine Asp activity. Pharmacokinetic parameters were calculated by DAS pharmacokinetic software. The particle size of ASNCs was (99.17 ± 0.21) nm and the potential was -(13.13 ± 0.60) mV. In trypsin solution, ASNCs showed more excellent stability. The area under the activity-time curve (AUC0-48 h) of ASNCs was about 2 times higher than that of Asp; the mean residence time (MRT0-48 h) was about 1.7 times higher than that of Asp, and the bioavailability was 195% of Asp. The results showed that ASNCs could improve the stability and bioavailability of Asp against trypsin and prolong the circulation time of Asp in vivo.
