Preparation and characterization of PEGylated long-circulating liposomes encapsulating costunolide and dehydrocostus lactone
10.7501/j.issn.0253-2670.2019.17.010
- Author:
Wen-Jun WANG
1
Author Information
1. Key Laboratory of Standardization of Chinese Herbal Medicine, Ministry of Education, State Key Laboratory Breeding Base of Characteristic Chinese Medicine Resources in Southwest China, School of Pharmacy, Chengdu University of Traditional Chinese Medicine
- Publication Type:Journal Article
- Keywords:
Box-Behnken response surface method;
Costunolide;
Dehydrocostus lactone;
Encapsulation efficiency;
In vitro release;
Long-circulating liposomes;
PEG;
Single-factor experiment;
Stability;
Thin film hydration method
- From:
Chinese Traditional and Herbal Drugs
2019;50(17):4068-4075
- CountryChina
- Language:Chinese
-
Abstract:
Objective: To prepare pegylated long-circulating liposomes co-encapsulated by costunolide (Cos) and dehydrocostus lactone (DL), optimize the formulation and process, and evaluate the quality. Methods: The pegylated long-circulating liposomes co-encapsulated by Cos and DL were prepared by film hydration method. Single factor test and Box-Behnken response surface methodology were used to optimize the preparation process with encapsulation efficiency of Cos and DL as the index. The particle size, surface potential, encapsulation efficiency and in vitro release of the liposomes were evaluated. Results: The optimal preparation conditions were as follows: drug-to-lipid ratio was 0.14, ratio of cholesterol to phospholipid was 0.05, mPEG-2000-DSPE addition amount was 6%, hydration time was 30 min, and probe ultrasonic time was 4 min. The obtained liposome was round and uniform in distribution, with an average particle size of (104.8 ± 2.48) nm, a polydispersity index (PDI) of (0.245 ± 0.031), and a Zeta potential of (-9.7 ± 0.23) mV, the encapsulation efficiency of Cos and DL were (91.9 ± 2.6)% and (94.41 ± 1.23)%, respectively. Conclusion: The PEGylated long-circulating liposome prepared by the process and prescription optimization has good appearance and high encapsulation efficiency, which can meet the application requirements.
