Preparation and in Vitro Release of Glycyrrhetinic Acid-tanshinone IIA-salvianolic acid B Compound Liposomes with Glycyrrhetinic Acid Derivative as Targeting Molecule
10.11842/wst.2014.10.024
- VernacularTitle:甘草次酸衍生物受体靶向复方脂质体的制备及其体外释放研究
- Author:
Huida GUAN
;
Xiuli WANG
;
Jiahao LIN
;
Xin XU
;
Fuhao CHU
;
Yurong WANG
- Publication Type:Journal Article
- Keywords:
Glycyrrhetinic acid derivative;
glycyrrhetinic acid;
tanshinone IIA;
salvianolic acid B;
compound li-posomes;
preparation optimization;
in vitro release
- From:
World Science and Technology-Modernization of Traditional Chinese Medicine
2014;(10):2190-2196
- CountryChina
- Language:Chinese
-
Abstract:
This article was aimed to study the preparation process of glycyrrhetinic acid (GA)-tanshinone IIA (TSN)-salvianolic acid B (SalB) compound liposomes with 3-succinic-30-stearyl glycyrrhetinic acid (18-GA-Suc) which is one of amphiphilicglycyrrhetinic acid derivatives as targeting molecule. The structure of the targeting molecule was validated by 1H-NMR and 13C-NMR methods. The feed ratio of 18-GA-Suc was optimized through single factor test and the incorporation ratio of 18-GA-Suc was determined by low-speed centrifugation. Meanwhile, physicochemi-cal properties between Suc-GTS-Lip and GTS-Lip were compared. In vitro release studies of three components in Suc-GTS-Lip were conducted by equilibrium dialysis method. The results showed that the optimum conditions were when the feed ratio of 18-GA-Suc was 10%lipid liposomal membrane (mol·mol-1). It revealed that the incorpora-tion ratio of 18-GA-Suc was 96.58%, and the encapsulation efficiencies of GA, TSN, and SalB were about 86.15%, 81.70%, and 91.05%, respectively. In addition, the Suc-GTS-Lip was spherical and uniformly dispersed with parti-cle size of 128.7 nm and zeta potential of-15.5 mV. The release model of GA and TSN was fitted well with Higuchi equation, while SalB was fitted well with Hixon-crowell equation. It was concluded that Glycyrrhetinic acid deriva-tives (18-GA-Suc) can be successfully expressed in the liposome membrane, and the optimal preparation method of Suc-GTS-Lip was stable. All three components encapsulated into liposomes had sustained-release effects, which laid a good foundation for its further study about liver-targeting.
