School of Food and Biological Engineering, National "111" Center for Cellular Regulation and Molecular Pharmaceutics, Key Laboratory of Fermentation Engineering (Ministry of Education), Hubei University of Technology, Wuhan, People's Republic of China.
Division of Pharmacoengineering and Molecular Pharmaceutics and Center for Nanotechnology in Drug Delivery, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.
Int J Nanomedicine. 2019 May 8;14:3361-3373. doi: 10.2147/IJN.S202063. eCollection 2019.
To fabricate multifunctional nanocapsule via Pickering emulsion route to facilitate tumor-targeted delivery. Poly(N-isopropylacrylamide-co-acrylic acid) nanoparticles (PNA) stabilized nanocapsules were fabricated by Pickering emulsion (PE) technology. For controllable drug-release and enhancing targeted antitumor effects, the nanocapsules were crosslinked with cystamine and coupled on cell-surface molecule markers (cRGDfK) to achieve on-demand drug release and targeted delivery. The fabricated PE and nanocapsules with average particle sizes (250 and 150 nm) were obtained. Encapsulation efficiency of hydrophobic anticancer drug (DOX) was determined as >90%. Release kinetic profiles for encapsulated nanocapsules displayed circulation stability and redox-sensitive releasing behavior with the supposed increase bioavailability. Both cytotoxicity assay, cellular uptake analysis and anticancer efficacy in B16F10 murine model demonstrated these redox-responsive drug-release and active targeted delivery. The results clearly demonstrated nanocapsule via PE route as promising candidate to provide an effective platform for incorporating hydrophobic drug for targeted cancer chemotherapy.
通过 Pickering 乳液途径制造多功能纳米胶囊，以促进肿瘤靶向递药。通过 Pickering 乳液（PE）技术制备了聚（N-异丙基丙烯酰胺-co-丙烯酸）纳米粒子（PNA）稳定的纳米胶囊。为了实现可控药物释放和增强靶向抗肿瘤效果，将纳米胶囊用胱胺交联并与细胞表面分子标记物（cRGDfK）偶联，以实现按需药物释放和靶向递送。获得了平均粒径为（250 和 150nm）的制备的 PE 和纳米胶囊。疏水性抗癌药物（DOX）的包封效率被确定为>90％。封装纳米胶囊的释放动力学曲线显示出循环稳定性和氧化还原敏感的释放行为，假设生物利用度增加。B16F10 鼠模型中的细胞毒性测定、细胞摄取分析和抗癌功效均表明了这些氧化还原响应性药物释放和主动靶向递送。结果清楚地表明，通过 PE 途径制造的纳米胶囊是一种很有前途的候选物，可以为靶向癌症化疗提供一种有效的平台来结合疏水性药物。
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