Institute of Chemistry and Materials, 17 Hoang Sam, Cau Giay, Hanoi 100000, Vietnam.
NTT Hi-Tech Institute, Nguyen Tat Thanh University, Ho Chi Minh City 700000, Vietnam.
Int J Mol Sci. 2019 Apr 24;20(8):2016. doi: 10.3390/ijms20082016.
Polyamidoamine (PAMAM) dendrimers are extensively researched as potential drug delivery system thanks to their desirable features such as controlled and stable structures, and ease of functionalization onto their surface active groups. However, there have been concerns about the toxicity of full generation dendrimers and risks of premature clearance from circulation, along with other physical drawbacks presented in previous formulations, including large particle sizes and low drug loading efficiency. In our study, carboxyl-terminated PAMAM dendrimer G3.5 was grafted with poly (ethylene glycol) methyl ether (mPEG) to be employed as a nano-based drug delivery system with great cytocompatibility for the delivery of carboplatin (CPT), a widely prescribed anticancer drug with strong side effects so that the drug will be effectively entrapped and not exhibit uncontrolled outflow from the open structure of unmodified PAMAM G3.5. The particles formed were spherical in shape and had the optimal size range (around 36 nm) that accommodates high drug entrapment efficiency. Surface charge was also determined to be almost neutral and the system was cytocompatible. In vitro release patterns over 24 h showed a prolonged CPT release compared to free drug, which correlated to the cytotoxicity assay on malignant cell lines showing the lack of anticancer effect of CPT/mPEG-G3.5 compared with CPT.
聚酰胺-胺（PAMAM）树枝状聚合物因其结构可控、稳定以及易于在其表面活性基团上进行功能化等优点，被广泛研究作为潜在的药物传递系统。然而，全代树枝状聚合物的毒性以及过早从循环中清除的风险，以及以前制剂中存在的其他物理缺陷，包括较大的颗粒尺寸和较低的药物载药效率，引起了人们的关注。在我们的研究中，羧基封端的 PAMAM 树枝状聚合物 G3.5 接枝了聚乙二醇甲醚（mPEG），用作具有良好细胞相容性的纳米药物传递系统，用于输送卡铂（CPT），CPT 是一种广泛应用于临床的具有强烈副作用的抗癌药物，以防止药物从未经修饰的 PAMAM G3.5 的开放结构中不受控制地流出并被有效包封。形成的颗粒呈球形，具有最佳的尺寸范围（约 36nm），可实现高药物包封效率。表面电荷也几乎呈中性，该系统具有细胞相容性。在 24 小时的体外释放模式中，与游离药物相比，CPT 的释放时间延长，这与对恶性细胞系的细胞毒性测定结果相关，表明 CPT/mPEG-G3.5 与 CPT 相比缺乏抗癌作用。
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