PLGA公司
鼻腔给药
洛哌丁胺
药理学
Zeta电位
化学
乙醇酸
精氨酸
体外
生物物理学
乳酸
纳米颗粒
生物化学
医学
纳米技术
细菌
材料科学
内科学
生物
腹泻
氨基酸
遗传学
作者
Aisling T. O’Donnell,Azeema Moollan,Samantha Baneham,Melike Özgül,Ritesh M. Pabari,Dermot Cox,Brian P. Kirby,Zebunnissa Ramtoola
摘要
Abstract Objectives The potential of poly(lactic-co-glycolic acid) (PLGA) nanoparticles (NPs) surface modified with octa-arginine (R8) for central nervous system (CNS) delivery was investigated. Methods PLGA NPs containing coumarin-6 or loperamide were surface modified using R8 and characterised for size, zeta potential, drug loading and release. We examined the cellular uptake of NPs in Madin-Darby Canine Kidney (MDCK) cells and CNS delivery of loperamide in a mouse model following intranasal (i.n.) and intravenous (i.v.) administration. Key findings NPs were 300–350 nm in diameter and of negative zeta potential which neutralised on R8 conjugation. Cellular uptake of R8-PLGA NPs was rapid compared with PLGA NPs and correlated with a high antinociceptive effect in mice by both the i.n. and i.v. routes. Little antinociceptive effect for PLGA NPs was observed reflecting their slow uptake in the in-vitro cell model. Conclusion This study demonstrates the potential of R8-PLGA NPs as carriers of therapeutic agents to the CNS.
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