Preparation and in Vitro Evaluation of Matrine Lipid-based Cubic Liquid Crystalline Nanoparticle Gels
10.13422/j.cnki.syfjx.20220646
- VernacularTitle:苦参碱脂质立方液晶纳米粒凝胶的制备及体外评价
- Author:
Qin SI
1
;
Huimin GAO
1
;
Chun LI
1
;
Zhimin WANG
1
;
Shuo SHEN
1
;
Lihua YAN
1
;
Fengqian GUO
1
;
Dinghua XIANG
1
;
Ping WANG
1
;
Dejing FU
1
;
Xiaoqian LIU
1
;
Hong YI
1
Author Information
1. National Engineering Laboratory for Quality Control Technology of Chinese Materia Medica， Institute of Chinese Materia Medica，China Academy of Chinese Medical Sciences，Beijing 100700，China
- Publication Type:Journal Article
- Keywords:
matrine;
cubic liquid crystalline nanoparticles;
gels;
extreme vertex mixture design;
in vitro release;
in vitro transdermal;
retention
- From:
Chinese Journal of Experimental Traditional Medical Formulae
2023;29(2):27-36
- CountryChina
- Language:Chinese
-
Abstract:
ObjectiveTo prepare matrine lipid-based cubic liquid crystalline nanoparticle （MAT-LLCN） gels and investigate its in vitro release and transdermal absorption behavior. MethodTaking entrapment efficiency as the index， the optimal formulation of MAT-LLCN was screened by extreme vertex mixture method based on the optimal ratio of glycerol monooleate （GMO） to poloxamer 407 （P407）， and its drug loading was investigated. MAT-LLCN gels was prepared by mixing MAT-LLCN with pre-swelled carbomer 940 as the gel matrix. The structure of MAT-lipid-based cubic liquid crystalline （LLC） was characterized by polarized light microscopy （PLM） and small angle X-ray scattering （SAXS）. The in vitro release and transdermal absorption properties of MAT-LLCN gels and MAT ordinary gels were compared by modified Franz diffusion cell method， skin structure changes caused by them were observed by hematoxylin-eosin （HE） staining. ResultThe optimal formulation of MAT-LLCN gels was 5.5% of GMO-P407 （9∶1）， 1%-6% of MAT， 0.6% of carbomer 940， adding water to sufficient amount. The prepared MAT-LLC was confirmed as body-centered （Im3m） LLC. The in vitro release behavior of MAT-LLCN gels was in accordance with the Weibull equation （R2=0.954 0）， and the release mechanism was the Fick diffusion. In vitro transdermal test showed that all the parameters of MAT-LLCN gels were higher than those of MAT ordinary gels （P<0.05）， including cumulative release rate， steady-state release rate and the amount of drug retention in skin. HE staining results showed that MAT-LLCN gels could loose the cellular arrangement of skin stratum corneum， and maintain the stability of the cell structure of the dermis. ConclusionThe prepared MAT-LLCN gels can accelerate the transdermal drug transport and form drug storage in the dermis by rapidly opening the skin stratum corneum barrier， suggesting that LLC has good application prospects in the field of transdermal drug delivery.
