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J Biomater Sci Polym Ed. 2017 Dec;28(17):2082-2099. doi: 10.1080/09205063.2017.1374032. Epub 2017 Sep 12.

Self-assembled nanoparticles made from a new PEGylated poly(aspartic acid) graft copolymer for intravaginal delivery of poorly water-soluble drugs.

Author information

1
a Biomedical Engineering, Faculty of Engineering , University of Manitoba , Winnipeg , Canada.
2
b Laboratory for Drug Delivery and Biomaterials, Faculty of Health Sciences, College of Pharmacy , University of Manitoba , Winnipeg , Canada.
3
c School of Chemical Engineering , Sungkyunkwan University , Suwon , South Korea.
4
d Faculty of Agricultural and Food Sciences, Department of Biosystems Engineering , University of Manitoba , Winnipeg , Canada.
5
e Faculty of Science, Department of Chemistry , University of Manitoba , Winnipeg , Canada.

Abstract

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.

KEYWORDS:

Intravaginal nanocarrier; anti-HIV drug delivery; poly(aspartic acid)

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