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Updated: May 9, 2025

Preparation and Characterization of Lipophilic Doxorubicin Pro-drug Micelles
Published on: August 2, 2016
A doxorubicin-loaded polymeric nanocarrier with 2,2'-binaphthyl-1,1'-diol-based backbone and tannic acid coating for
Xiaoxia Guo1, Chaofan Wang2, Lihong Fan3
1Hubei University of Technology, School of Life and Health Sciences, Hubei University of Technology, No. 28, Nanli Road, Wuhan 430068, China, Wuhan, Hubei, 430068, CHINA.
Abstract:
This study presents PBVT, a polyurethane-based nano-drug delivery system incorporating BINOL (2,2'-binaphthyl-1,1'-diol), tannic acid (TA), and phenylboronic acid (PBA), to overcome critical challenges in cancer therapy such as low drug-loading capacity, nanoparticle instability, and systemic toxicity. Polyurethane was chosen as the base material due to its exceptional versatility, offering tunable mechanical properties, biocompatibility, and chemical stability, making it ideal for constructing robust nanocarriers for drug delivery. BINOL is incorporated for the first time into a nano polyurethane framework, featuring dual naphthalene rings that enable strong π-π stacking interactions with doxorubicin (DOX), achieving a high drug-loading capacity (48.6%) and encapsulation efficiency (89.8%). TA enhances system stability and biocompatibility through hydrogen bonding, while its phenolic hydroxyl groups provide antioxidant and antibacterial properties, reducing infection risks during chemotherapy. PBA is integrated into the polyurethane backbone adding pH-responsive drug release capabilities, allowing selective and controlled release of DOX in acidic tumor microenvironments. In vitro, cellular experiments confirmed the low cytotoxicity of PBVT against normal cells and the potent anticancer activity of PBVT-DOX in tumor cells in a dose-dependent manner. The system demonstrated sustained drug release and stability for over two weeks under physiological conditions. PBVT-DOX represents a novel, efficient platform for targeted cancer therapy and the development of advanced polyurethane-based nanomaterials for biomedical applications.
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