Preparation,Characterization,and Anti-Ulcerative Colitis Efficacy of Cockroach Extract Liposomes
10.14148/j.issn.1672-0482.2023.1211
- VernacularTitle:蜚蠊提取物脂质体的制备、表征及其抗溃疡性结肠炎的疗效
- Author:
Ting-Mei LYU
1
;
Heng LIU
;
Xi-Tong WANG
;
Yu-Tong WANG
;
Zhi-Peng CHEN
Author Information
1. 南京中医药大学江苏省中药炮制重点实验室,江苏 南京 210023;大理大学云南省昆虫生物医药研发重点实验室/云南省药用昆虫资源开发与综合利用工程研究中心,云南 大理 671000
- Keywords:
cockroach extract;
liposomes;
orthogonal experiment;
ulcerative colitis
- From:
Journal of Nanjing University of Traditional Chinese Medicine
2023;39(12):1211-1223
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVE This study aimed to explore the optimal process for preparing long-acting liposomes loaded with cock-roach extract(CE-Lip)and to evaluate their therapeutic efficacy against ulcerative colitis(UC).METHODS The CE-Lip was pre-pared using a thin film dispersion method.Orthogonal experiments were conducted to optimize the formulation and freeze-drying process of CE-Lip.Morphological characterization and in vitro release rate assessment were performed.The therapeutic efficacy of CE-Lip was evaluated using a mouse model of UC.RESULTS The optimal preparation process involved a cholesterol-phospholipid mass ratio of 1∶5,an extract-phospholipid mass ratio of 1∶4,hydration time of 0.75 h,hydration volume of 3 mL,and hydration temperature of 30℃.The optimal freeze-drying process utilized a mixture of 5%mannitol and 10%trehalose as protective agents.The resulting CE-Lip exhibited an average particle size of(276.7±5.6)nm,with a vesicular structure.The stability of CE-Lip after freeze-drying was excellent,and its in vitro release rate was significantly lower than that of the raw material.Pharmacological results demonstrated that CE-Lip significantly reduced DAI scores,colon length,CMDI scores,TNF-α expression,and HS scores in UC mice,while increasing EGF expression and mucin expression in goblet cells.CONCLUSION A simple,stable,and reproducible process for preparing CE-Lip is established.The resulting CE-Lip exhibits uniform size distribution,good stability,and sustained release effects.Compared to conventional formulations,CE-Lip significantly enhanced the therapeutic effect of CE against UC in mice.This study provides a foun-dation for further development and research of CE-Lip.