title: Cholesteryl to improve the cellular uptake of polymersomes within HeLa cells.
abstract: 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 500nm, zeta potential was shown to be neutral at -0.82mV ±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.
authors.affiliation: School of Pharmacy and Pharmaceutical Sciences, University of Ulster, Coleraine, Northern Ireland, BT52 1SA, United Kingdom.
authors.forename: Chloe
authors.initials: C
authors.lastname: Martin
authors.affiliation: School of Pharmacy and Pharmaceutical Sciences, University of Ulster, Coleraine, Northern Ireland, BT52 1SA, United Kingdom.
authors.forename: Nino
authors.initials: N
authors.lastname: Marino
authors.affiliation: School of Pharmacy and Pharmaceutical Sciences, University of Ulster, Coleraine, Northern Ireland, BT52 1SA, United Kingdom.
authors.forename: Ciara
authors.initials: C
authors.lastname: Curran
authors.affiliation: School of Pharmacy and Pharmaceutical Sciences, University of Ulster, Coleraine, Northern Ireland, BT52 1SA, United Kingdom.
authors.forename: Anthony P
authors.initials: AP
authors.lastname: McHale
authors.affiliation: School of Pharmacy and Pharmaceutical Sciences, University of Ulster, Coleraine, Northern Ireland, BT52 1SA, United Kingdom.
authors.forename: John F
authors.initials: JF
authors.lastname: Callan
authors.affiliation: School of Pharmacy and Pharmaceutical Sciences, University of Ulster, Coleraine, Northern Ireland, BT52 1SA, United Kingdom. Electronic address: b.callan@ulster.ac.uk.
authors.forename: Bridgeen
authors.initials: B
authors.lastname: Callan
mesh_terms: D002784:Cholesterol / Q000737:chemistry* / Q000378:metabolism* / Q000494:pharmacology; D016503:Drug Delivery Systems / Q000379:methods*; D004705:Endocytosis / Q000187:drug effects / Q000502:physiology*; D006367:HeLa Cells; D006801:Humans; D011108:Polymers / Q000737:chemistry* / Q000378:metabolism* / Q000494:pharmacology
chemical_list: D011108:Polymers; D002784:Cholesterol
keywords: Amphiphilic polymer; Cholesteryl; Drug delivery system (DDS); Poly(ethylene) glycol; Polymersome