Zhang Guangyan, Jiang Xulin
Hubei Provincial Key Laboratory of Green Materials for Light Industry, Hubei University of Technology, Wuhan 430068, China.
Key Laboratory of Biomedical Polymers of Ministry of Education & Department of Chemistry, Wuhan University, Wuhan 430072, China.
Polymers (Basel). 2019 Feb 13;11(2):316. doi: 10.3390/polym11020316.
The temperature responsive PEGylated polyaspartamide derivative, denoted as mPEG-PAAHP, was synthesized by the click reaction. FTIR and ¹H NMR were adopted to characterize and confirm the chemical structures of the obtained mPEG-PAAHPs. The temperature responsive behavior investigated by transmittance and dynamic light scattering showed that some of the obtained mPEG-PAAHPs exhibited obvious temperature responsiveness and could be used to prepare nanoparticles by quickly heating. Drug paclitaxel can be encapsulated into mPEG-PAAHP based nanoparticles with a high encapsulation efficiency up to 99% (corresponding to a drug loading content of around 9.9%). Dynamic light scattering results showed that the PTX-loaded nanoparticles had a mean size around 80 nm (PDI<0.2) and good stability in PBS with 150 mM ionic strength. In vitro cytotoxicity results showed that mPEG-PAAHP did not show any toxicity to HeLa cells, but the PTX-loaded nanoparticles based on mPEG-PAAHP exhibited obvious anti-cancer activity. Thus, the temperature responsive PEGylated polyaspartamide derivative mPEG-PAAHP may be a promising drug delivery system.
通过点击反应合成了温度响应性聚乙二醇化聚天冬酰胺衍生物，记为mPEG - PAAHP。采用傅里叶变换红外光谱（FTIR）和核磁共振氢谱（¹H NMR）对所得mPEG - PAAHP的化学结构进行表征和确认。通过透射率和动态光散射研究温度响应行为表明，部分所得mPEG - PAAHP表现出明显的温度响应性，可用于通过快速加热制备纳米颗粒。药物紫杉醇可被高效包封到基于mPEG - PAAHP的纳米颗粒中，包封率高达99%（对应药物负载量约为9.9%）。动态光散射结果表明，负载紫杉醇的纳米颗粒平均粒径约为80 nm（多分散指数<0.2），在离子强度为150 mM的磷酸盐缓冲盐溶液（PBS）中具有良好的稳定性。体外细胞毒性结果表明，mPEG - PAAHP对宫颈癌HeLa细胞未表现出任何毒性，但基于mPEG - PAAHP的负载紫杉醇纳米颗粒表现出明显的抗癌活性。因此，温度响应性聚乙二醇化聚天冬酰胺衍生物mPEG - PAAHP可能是一种有前景的药物递送系统。
