Maney Vareessh, Singh Moganavelli
Nano-Gene and Drug Delivery Group, Discipline of Biochemistry, University of KwaZulu-Natal, Private Bag X54001, Durban, South Africa.
Pharmaceutics. 2019 Sep 1;11(9):439. doi: 10.3390/pharmaceutics11090439.
Nanoparticle application has significantly impacted the field of medicine. The need to develop novel drugs with higher therapeutic potential has stimulated the development of innovative delivery strategies to mitigate the potent side effects associated with known chemotherapeutic drugs. This paper describes the synthesis of platinum-gold bimetallic nanoparticles (PtAuBNps), their functionalisation with chitosan, and entrapment of the anticancer drug 5-fluorouracil (5-FU). All PtAuBNps and their drug nanocomposites were physico-chemically characterised, displaying desirable properties with regards to shape, size (<120 nm) and colloidal stability. 5-FU binding and loading capacities in PtAuBNps were found to be 90.17% and 22.56%, respectively. In vitro cytotoxicity profiles determined using the MTT and SRB assays reflected up to 65% cell death in the MCF-7, HepG2 and Caco-2 cell lines. These nanocomposites exhibited excellent physiochemical attributes, high specificity towards cancer cells, with a pH-sensitive drug release in a simulated acidic tumour microenvironment through zero-order release kinetics. In addition, they possessed the potential to traverse the mucosal lining facilitating oral drug administration. Overall, 5-FU encapsulation improved the bioavailability of the drug in cancer cells, with the promise of enhancing its therapeutic effect, biocompatibility and safety. These positive results highlight PtAuBNps as promising in vitro delivery systems and merits future in vivo research.
纳米颗粒的应用对医学领域产生了重大影响。开发具有更高治疗潜力的新型药物的需求刺激了创新给药策略的发展，以减轻与已知化疗药物相关的强效副作用。本文描述了铂-金双金属纳米颗粒（PtAuBNps）的合成、壳聚糖对其的功能化修饰以及抗癌药物5-氟尿嘧啶（5-FU）的包封。对所有PtAuBNps及其药物纳米复合材料进行了物理化学表征，在形状、尺寸（<120 nm）和胶体稳定性方面表现出理想的性质。发现PtAuBNps中5-FU的结合和负载能力分别为90.17%和22.56%。使用MTT和SRB测定法确定的体外细胞毒性谱显示，MCF-7、HepG2和Caco-2细胞系中细胞死亡高达65%。这些纳米复合材料表现出优异的物理化学特性，对癌细胞具有高特异性，在模拟酸性肿瘤微环境中通过零级释放动力学实现pH敏感的药物释放。此外，它们具有穿越粘膜层以促进口服给药的潜力。总体而言，5-FU包封提高了该药物在癌细胞中的生物利用度，有望增强其治疗效果、生物相容性和安全性。这些积极结果突出了PtAuBNps作为有前景的体外给药系统的潜力，值得未来进行体内研究。
