Vesicle size and stability of biomimetic liposomes from 3'-sulfo-Lewis a (SuLea) containing glycolipids.
Vesicle size and stability of biomimetic liposomes from 3'-sulfo-Lewis a (SuLea) containing glycolipids.
复制标题
含有糖脂的 3-磺基-Lewis a (SuLea) 仿生脂质体的囊泡大小和稳定性。
DOI：
10.1016/j.colsurfb.2007.03.016
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发表时间：
2007
期刊：
影响因子：
--
通讯作者：
Marchant,RogerE
中科院分区：
文献类型：
--
作者：
Zhu,Junmin;Xue,Jie;Guo,Zhongwu;Marchant,RogerE
我们报道了一种天然的刘易斯型糖配体3′-磺基-刘易斯a（SuLea）对脂质体进行糖萼模拟物表面修饰。合成了两种含SuLea的糖脂：单价SuLea-脂质和三价SuLea（TSuLea）-脂质，并将其与1，2-二硬脂酰-sn-甘油-3-磷酸胆碱（DSPC）和胆固醇通过冻融和挤出法制备单层囊泡（ULV）。利用光子相关光谱（PCS）研究了糖脂浓度和挤出膜孔径对囊泡大小和稳定性的影响。通过50 nm挤出获得的具有5%SuLea-或TSuLea-脂质的糖脂体与100 nm挤出相比具有25-30%的直径小于100 nm的囊泡。TSuLea-脂质体总是产生比SuLea-脂质体更大的囊泡尺寸，我们将其归因于更大的TSuLeaheadgroup。SuLea-和TSuLea-脂质体都随着糖脂浓度从5%增加到15%而增加其囊泡尺寸，并且在室温下超过1个月表现出良好的稳定性。进一步将糖脂浓度增加至20%导致TSuLea-脂质体在5天后出现大的囊泡聚集，而SuLea-脂质体保持稳定10天。具有15%糖脂的SuLea-和TSuLea-脂质体由于带负电荷的SuLea和TSuLea头部基团的静电效应而表现出更好的稳定性。结果表明，具有5 - 15%掺入的SuLea-和TSuLea-脂质的仿生脂质体具有足够的稳定性，可用于靶向药物递送的潜在应用。
We report on the use of a natural Lewis type saccharide ligand, 3′-sulfo-Lewis a (SuLea) for glycocalyx-mimetic surface modification of liposomes. Two SuLea-containing glycolipids, monovalent SuLea-lipid and trivalent SuLea(TSuLea)-lipid, were synthesized, and used with 1,2-distearoyl-sn-glycero-3-phosphocholine (DSPC) and cholesterol to prepare unilaminar vesicles (ULVs) by a freeze–thaw and extrusion method. The effects of the glycolipid concentrations and the pore sizes of extrusion membranes on vesicle size and stability were investigated by photon correlation spectroscopy (PCS). Glycoliposomes, with 5% SuLea- or TSuLea-lipids obtained by 50nm extrusion, had 25–30% more vesicles less than 100nm in diameter compared with the 100nm extrusion. TSuLea-liposomes always produced larger vesicle size than SuLea-liposomes, which we attribute to the larger TSuLeaheadgroup. Both SuLea- and TSuLea-liposomes increased their vesicle size with increasing glycolipid concentration from 5% to 15%, and demonstrated good stability at room temperature for over 1 month. Further increasing the glycolipid concentration to 20% resulted in large vesicle aggregation after 5 days for TSuLea-liposomes, while the SuLea-liposomes remained stable for 10 days. SuLea- and TSuLea-liposomes with 15% glycolipids demonstrated better stability due to the electrostatic effect from the negatively charged SuLeaand TSuLeaheadgroups. The results indicate that the biomimetic liposomes with SuLea- and TSuLea-lipids with 5 to 15% incorporation are sufficiently stable for the potential applications in targeted drug delivery.