Cholesteryl to improve the cellular uptake of polymersomes within HeLa cells

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• 作者：Chloe Martin ; Nino Marino ; Ciara Curran ; Anthony P. McHale ; John F. Callan ; Bridgeen Callan ; ^{b.callan@ulster.ac.uk" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Drug delivery system (DDS) ; Amphiphilic polymer ; Polymersome ; Cholesteryl ; Poly(ethylene) glycol
• 刊名：International Journal of Pharmaceutics
• 出版年：2016
• 出版时间：10 September 2016
• 年：2016
• 卷：511
• 期：1
• 页码：570-578
• 全文大小：1482 K

文摘

The need to develop a greater understanding of drug delivery systems has arisen through the development of alternative biological based therapeutics. Drug delivery systems need to adapt and respond to this increasing demand for cellular transportation of highly charged species. Polymersomal drug delivery systems have displayed great potential and versatility for such a task. In this manuscript we present the synthesis, characterisation and biological evaluation of six amphiphilic random co polymers with varying amounts of cholesteryl (0⿿39%wt) before the subsequent formation into polymersomes. The polymersomes were then analysed for size, zeta potential, encapsulation efficiency, release kinetics and cellular uptake. Results confirmed that the polymersome containing 12%wt cholesteryl polymer displayed a ten-fold increase in cellular uptake of Fitc-CM-dextran when compared to un-encapsulated drug, crossing the cellular membrane via endocytosis. The size of these vehicles ranged between 100 and 500 nm, zeta potential was shown to be neutral at ⿿0.82 mV ±0.2 with encapsulation efficiencies in the region of 60%. The ease of adaptability and preparation of such systems renders them a viable alternative to liposomal drug delivery systems.