Naidu Priya S R, Norret Marck, Dunlop Sarah A, Fitzgerald Melinda, Clemons Tristan D, Iyer K Swaminathan
School of Molecular Sciences and School of Biological Sciences, The University of Western Australia, 35 Stirling Highway, Crawley, WA 6009, Australia.
Curtin Health Innovation Research Institute, Curtin University and the Perron Institute for Neurological and Translational Science, Ralph and Patricia Sarich Neuroscience Research Institute Building, QEII Medical Centre, Nedlands, WA 6009, Australia.
ACS Omega. 2019 Oct 11;4(17):17083-17089. doi: 10.1021/acsomega.8b02894. eCollection 2019 Oct 22.
Nanoparticle drug delivery applications have predominantly focused on the entrapment and delivery of hydrophobic molecules with poor water solubility. However, benefits can also be obtained from nanoparticle-based delivery of hydrophilic therapeutics. This study reports on the development of a p(HEMA--GMA)-based nanoparticle synthesized via a spontaneous water-in-oil inverse nanoemulsion to deliver doxorubicin, a water-soluble chemotherapeutic. High drug loading efficiency and sustained release of doxorubicin from Cy5-functionalized p(HEMA--GMA) nanoparticles enabled effective inhibition of the MCF-7 human breast cancer derived cell line. Direct comparative analyses with a hydrophobic PGMA nanoparticle demonstrated enhanced capabilities of the p(HEMA--GMA)-based nanoparticle in vitro. The results suggest that p(HEMA--GMA)-based nanoparticles, which are better suited for hydrophilic drug loading and delivery, may have the potential for the improved therapeutic effect in vivo by enhanced permeation and retention of the nanoparticles by avoidance of off-site side effects of the chemotherapeutic.
纳米颗粒药物递送应用主要集中于包裹和递送水溶性差的疏水分子。然而,基于纳米颗粒递送亲水性治疗药物也能带来益处。本研究报道了一种通过自发的油包水反相纳米乳液合成的基于聚(甲基丙烯酸羟乙酯-甲基丙烯酸缩水甘油酯)[p(HEMA-GMA)]的纳米颗粒,用于递送水溶性化疗药物阿霉素。阿霉素在Cy5功能化的p(HEMA-GMA)纳米颗粒中的高载药效率和持续释放能够有效抑制MCF-7人乳腺癌衍生细胞系。与疏水性聚甲基丙烯酸缩水甘油酯(PGMA)纳米颗粒的直接对比分析表明,基于p(HEMA-GMA)的纳米颗粒在体外具有更强的能力。结果表明,更适合亲水性药物装载和递送的基于p(HEMA-GMA)的纳米颗粒,可能通过避免化疗药物的非靶向副作用增强纳米颗粒的渗透和滞留,从而在体内具有提高治疗效果的潜力。