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Production of PEG-coated liposomes using a continuous supercritical assisted process
The Journal of Supercritical Fluids ( IF 3.9 ) Pub Date : 2020-09-21 , DOI: 10.1016/j.supflu.2020.105048
Paolo Trucillo , Ernesto Reverchon

Liposomes are spherical vesicles, characterized by spontaneous aggregation tendency. To overcome this problem, in this work, liposomes coating was attempted, using polyethylene glycol (PEG), at different polymer to lipid ratios (1, 5, 10 % w/w) and proposing two experimental protocols, based on a supercritical assisted process.

Only one protocol was successful; in that case, size and SEM analysis confirmed that vesicles did not aggregate thanks to the repulsion created by PEG surface, as confirmed by zeta potential measurements (about -25 mV). Liposomes with mean size ranging between 134 ± 30 and 166 ± 45 nm, stable for at least 70 day, were produced. The efficiency of SuperLip to produce PEG-coated liposomes was also tested, entrapping artesunate, obtaining encapsulation efficiencies up to 92 %. Drug release tests for standard and PEG-coated liposomes were compared: PEGylated vesicles produced a controlled release at least three times longer, without a significant initial burst release.



中文翻译:

使用连续超临界辅助过程生产PEG包被的脂质体

脂质体是球形囊泡,其特征是自发聚集趋势。为了克服这个问题,在这项工作中,尝试使用聚乙二醇(PEG)以不同的聚合物与脂质比率(1、5、10%w / w)涂覆脂质体,并基于超临界辅助方法提出了两个实验方案。

只有一个协议成功。在这种情况下,大小和SEM分析证实,由于zeta电势测量(约-25 mV)证实,由于PEG表面产生的排斥作用,囊泡没有聚集。产生的脂质体的平均大小在134±30至166±45 nm之间,至少可稳定70天。还测试了SuperLip产生PEG包衣脂质体的效率,截留青蒿琥酯,获得高达92%的包封效率。比较了标准脂质体和PEG包衣脂质体的药物释放测试:PEG化囊泡产生的控释时间至少长了三倍,而没有明显的初始突释。

更新日期:2020-09-29
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