本文選題：去唾液酸糖蛋白受體　切入點(diǎn)：N-乙酰半乳糖胺　出處：《中國(guó)新藥雜志》2017年16期

【摘要】：目的:本研究采用酶促法構(gòu)建N-乙酰半乳糖胺(N-acetylgalactosamine,Gal NAc)修飾的脂質(zhì)體作為熒光標(biāo)記物-香豆素-6的載體,對(duì)其修飾的脂質(zhì)體理化性質(zhì)進(jìn)行評(píng)價(jià)。方法:采用酶催化法偶聯(lián)合成Gal NAc-C8-Chol,利用MS,NMR對(duì)其結(jié)構(gòu)進(jìn)行表征,并以此作為導(dǎo)向性材料,采用薄膜分散-擠出法制備載香豆素-6的Gal NAc修飾肝靶向脂質(zhì)體(NGAL-LP),并對(duì)脂質(zhì)體的包封率、粒徑、Zeta電位、體外釋放度及RCA120體外結(jié)合效率等性質(zhì)進(jìn)行了考察。結(jié)果:合成的Gal NAc-C8-Chol經(jīng)MS,NMR鑒定為目標(biāo)產(chǎn)物。與普通香豆素-6脂質(zhì)體(LP)相比,本研究所制備的主動(dòng)肝靶向脂質(zhì)體(NGAL-LP)的粒徑、Zeta電位、包封率、體外釋放等理化性質(zhì)無(wú)顯著差異,包封率≥98%,平均粒徑為(86.74±1.7)nm,平均Zeta電位為(-51.47±0.9)m V。體外釋放結(jié)果表明,36 h內(nèi)香豆素-6脂質(zhì)體在PBS和血漿中的累積釋放率8%。RCA120凝集實(shí)驗(yàn)表明,只有Gal NAc-C8-Chol修飾的脂質(zhì)體可經(jīng)RCA120誘導(dǎo)產(chǎn)生凝集效應(yīng)。結(jié)論:采用酶促法成功構(gòu)建了Gal NAc修飾的香豆素-6肝靶向脂質(zhì)體,以期望顯著提高體內(nèi)肝腫瘤的靶向治療效果。
[Abstract]:Aim: to construct N-acetylgalactosamine- Gal NAc-modified liposome by enzymatic method as the carrier of coumarin -6 as a fluorescent marker. Methods: Gal NAc-C8-Cholwas synthesized by enzymatic coupling method, and its structure was characterized by MS NMR. Gal NAc loaded coumarin -6 was prepared by thin-film dispersion-extrusion method to modify liposome NGAL-LPN. The encapsulation efficiency and particle size of liposome were determined. The in vitro release and in vitro binding efficiency of RCA120 were investigated. Results: the synthesized Gal NAc-C8-Chol was identified as the target product by MS NMR. Compared with the conventional coumarin -6 liposome, the active liposome (NGAL-LPN) prepared in this study was characterized by its particle size and Zeta potential. There was no significant difference in entrapment efficiency and in vitro release. The entrapment efficiency was 鈮，

本文編號(hào)：1666760