已发表论文
本文章已被撤回:对含有马钱子碱 (Brucine) 的新型 NGR 修饰的脂质体的体外和体内评价
***本文章已被撤回***
Abstract: In this study, a novel NGR
(Asn-Gly-Arg) peptide-modified liposomal brucine was prepared by using
spray-drying method. The surface morphology of the liposomes, encapsulation
efficiency and particle size were investigated. The data showed that the
addition of NGR did not produce any significant influence on brucine liposomes
in terms of particle size or zeta potential. In addition, after 3 months of
storage, no dramatic change such as visible aggregation, drug content changes
or precipitation in the appearance of NGR-brucine liposomes occurred. The in
vitro release results indicated that the release of brucine from NGR liposomes
was similar to that of liposomes, demonstrating that the NGR modification did
not affect brucine release. The in vitro drug-release kinetic model of
NGR-brucine liposomes fitted well with the Weibull’s equation. In vivo,
NGR-brucine liposomes could significantly extend the bioavailability of
brucine; however, there was no significant difference observed in the
pharmacokinetic parameters between liposomes and NGR liposomes after
intravenous administration. Antitumor activity results showed that NGR-modified
liposomes exhibited less toxicity and much higher efficacy in HepG2-bearing
mice compared with non-modified liposomes. The enhanced antitumor activity
might have occurred because brucine was specifically recognized by NGR receptor
on the surface of tumor cells, which enhanced the intracellular uptake of
drugs.
Keywords: brucine,
liposome, NGR, HepG2, in vivo, in vitro