a Biomedical Engineering, Faculty of Engineering , University of Manitoba , Winnipeg , Canada.
b Laboratory for Drug Delivery and Biomaterials, Faculty of Health Sciences, College of Pharmacy , University of Manitoba , Winnipeg , Canada.
J Biomater Sci Polym Ed. 2017 Dec;28(17):2082-2099. doi: 10.1080/09205063.2017.1374032. Epub 2017 Sep 12.
New amphiphilic PEGylated poly(aspartic acid) graft copolymer (PASP-PEG-Ph) was synthesized as a nanocarrier for intravaginal drug delivery of poorly water-soluble drugs. PASP-PEG-Ph self-assembled into negatively charged spherically shaped nanoparticles in the presence of pH 4.5 and pH 7.0 vaginal fluid simulants with a diameter of approximately 200 nm as evidenced by Zeta-potentiometer, scanning electron microscope (SEM), dynamic light scattering (DLS) analysis. A significant number of stable NPs could be maintained at pH 4.5, 37 °C for 13 days. The PASP-PEG-Ph NP showed no significant cytotoxicity toward the T-cell line SupT1 and human vaginal epithelial cell line Vk2/E6E7 up to 1 mg/mL. The highest encapsulation efficiency of the model drug coumarin 6 (C6) by PASP-PEG-Ph was 92.0 ± 5.7%. The sustained release profile of the encapsulated C6 was demonstrated by an in vitro release study. An in vitro cellular uptake study revealed strong cellular uptake of the C6 loaded NP by SupT1 cells within 2 h.
新的两亲性聚乙二醇化聚（天冬氨酸）接枝共聚物（PASP-PEG-Ph）被合成作为一种纳米载体，用于阴道内递送给水溶解度差的药物。在 pH 4.5 和 pH 7.0 的阴道液模拟物存在下，PASP-PEG-Ph 自组装成带负电荷的球形纳米颗粒，直径约为 200nm，这一点通过 Zeta 电位计、扫描电子显微镜（SEM）和动态光散射（DLS）分析得到证实。在 pH 4.5、37°C 下，相当数量的稳定 NPs 可以维持 13 天。PASP-PEG-Ph NP 对 T 细胞系 SupT1 和人阴道上皮细胞系 Vk2/E6E7 的细胞毒性在 1mg/mL 以下没有显著影响。PASP-PEG-Ph 对模型药物香豆素 6（C6）的最高包封效率为 92.0±5.7%。体外释放研究表明，包封的 C6 呈现出持续释放的特征。体外细胞摄取研究表明，在 2 小时内，C6 负载的 NP 被 SupT1 细胞强烈摄取。
