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Open AccessArticle

Glycyrrhetinic Acid Liposomes Containing Mannose-Diester Lauric Diacid-Cholesterol Conjugate Synthesized by Lipase-Catalytic Acylation for Liver-Specific Delivery

by Jing Chen 1,†, Yuchao Chen 2,3,4,†, Yi Cheng 1,* and Youheng Gao 1,*
1
Shool of Chinese Materia Medica, Guangzhou University of Chinese Medicine, Guangzhou 510006, China
2
The Second Affiliated Hospital of Guangzhou University of Chinese Medicine, Guangzhou 510115, China
3
Section of Immunology, Guangdong Provincial Academy of Chinese Medical Sciences, Guangzhou 510006, China
4
Postdoctoral Programme, Guangzhou University of Chinese Medicine, Guangzhou 510006, China
*
Authors to whom correspondence should be addressed.
These authors contributed equally to this work.
Molecules 2017, 22(10), 1598; https://doi.org/10.3390/molecules22101598
Received: 12 August 2017 / Revised: 7 September 2017 / Accepted: 17 September 2017 / Published: 24 September 2017
(This article belongs to the Special Issue Lipases and Lipases Modification)
Mannose-diester lauric diacid-cholesterol (Man-DLD-Chol), as a liposomal target ligand, was synthesized by lipase catalyzed in a non-aqueous medium. Its chemical structure was confirmed by mass spectrometry (MS) and nuclear magnetic resonance (NMR) spectroscopy. Glycyrrhetinic acid (GA) liposomes containing Man-DLD-Chol (Man-DLD-Chol-GA-Lp) were prepared by the film-dispersion method. We evaluated the characterizations of liposomes, drug-release in vitro, the hemolytic test, cellular uptake, pharmacokinetics, and the tissue distributions. The cellular uptake in vitro suggested that the uptake of Man-DLD-Chol-modified liposomes was significantly higher than that of unmodified liposomes in HepG2 cells. Pharmacokinetic parameters indicated that Man-DLD-Chol-GA-Lp was eliminated more rapidly than GA-Lp. In tissue distributions, the targeting efficiency (Te) of Man-DLD-Chol-GA-Lp on liver was 54.67%, relative targeting efficiency (RTe) was 3.39, relative uptake rate (Re) was 4.78, and peak concentration ratio (Ce) was 3.46. All these results supported the hypothesis that Man-DLD-Chol would be an efficient liposomal carrier, and demonstrated that Man-DLD-Chol-GA-Lp has potential as a drug delivery for liver-targeting therapy. View Full-Text
Keywords: lipase-catalytic acylation; mannose-diester lauric diacid-cholesterol; glycyrrhetinic acid liposomes; mannose receptor; liver-targeting lipase-catalytic acylation; mannose-diester lauric diacid-cholesterol; glycyrrhetinic acid liposomes; mannose receptor; liver-targeting
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Chen, J.; Chen, Y.; Cheng, Y.; Gao, Y. Glycyrrhetinic Acid Liposomes Containing Mannose-Diester Lauric Diacid-Cholesterol Conjugate Synthesized by Lipase-Catalytic Acylation for Liver-Specific Delivery. Molecules 2017, 22, 1598.

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