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已发表论文
一种新型的抗水解亲脂性叶酸衍生可稳定靶向脂质体的体内传递
Authors Huang Y, Yang T, Zhang W, Lu Y, Ye P, Yang G, Li B, Qi S, Liu Y, He X, Lee RJ, Xu C, Xiang G
Published Date September 2014 Volume 2014:9(1) Pages 4581—4595
DOI http://dx.doi.org/10.2147/IJN.S69115
Received 10 June 2014, Accepted 10 July 2014, Published 29 September 2014
Abstract: Instability of targeting ligand is a roadblock towards successful development of folate targeted liposomes. Folate ligands have been linked to polyethylene glycol (PEG) and cholesterol by an amide bond to form folate-CONH-PEG-CONH-Cholesterol (F-CONH-PEG-CONH-Chol), which is subject to hydrolysis. To increase the stability of folate ligands and promote the long circulation and targeting effects, we synthesized a chemically stable lipophilic folate derivative, folate-CONH-PEG-NH-Cholesterol (F-CONH-PEG-NH-Chol), where the amide bond was replaced by a C-N bond, to deliver liposomal doxorubicin (Dox). Its physical stability, cellular uptake, cellular toxicity, pharmacokinetics, distribution, anti-tumor efficacy, and cardiac toxicity were investigated. Our results indicate that F-CONH-PEG-NH-Chol conjugated liposomes are taken up selectively by folate receptor-positive HeLa and KB cells. Compared with F-CONH-PEG-CONH-Chol with two carbonate linkages, F-CONH-PEG-NH-Chol better retained its drug entrapment efficiency and folate receptor-targeting activity during prolonged circulation. F-CONH-PEG-NH-Chol thus represents a physically stable and effective ligand for delivering folate receptor-targeted liposomes, with prolonged circulation time and efficient tissue distribution, as well as higher efficacy and less cardiac toxicity. Collectively, these results suggest that this novel conjugate can serve as a promising derivative for the delivery of anti-tumor therapeutic agents.
Keywords: liposome, doxorubicin, folate ligand, FR-targeting, stability
Keywords: liposome, doxorubicin, folate ligand, FR-targeting, stability
