期刊
CARBOHYDRATE POLYMERS
卷 181, 期 -, 页码 150-158出版社
ELSEVIER SCI LTD
DOI: 10.1016/j.carbpol.2017.09.017
关键词
Hyaluronic acid; Paclitaxel; Conjugate; Targeted drug delivery; Antitumor efficacy
资金
- National Natural Science Foundation of China [81473216]
- Fundamental Research Funds for the Central Universities [2015XPT02]
- Innovative Scientific Research Team Fund of Jiangsu Province
- Traditional Chinese Medicine Scientific Research Fund Project of Zhejiang Province [2015ZB106]
- Natural Science Foundation of Ningbo [2016A610236]
- Priority Academic Program Development of Jiangsu Higher Education Institutions
Polymer-based paclitaxel (PTX) conjugates have demonstrated application potentials to improve the water solubility and enhance the efficiency of drug delivery. In this study, a novel HA-based drug conjugate, HA-6-PTX, was designed and successfully synthesized by chemically grafting PTX to the C-6 position of N-acetyl-D-glucosamine (GlcNAc) of hyaluronic acid (HA) using hexanediamine as the linker. Leaving the carboxylate of HA chain unaffected, the conjugate with drug loading as high as 21.8% showed an excellent water solubility of 168 mg/mL and exhibited increased drug release in the presence of hyaluronidase. Compared to free PTX, HA-6-PTX demonstrated increased cytotoxicity and enhanced apoptosis-inducing effect against HepG2 and A549 cells due to the increased cellular uptake of drug via HA-receptor mediated endocytosis. It was concluded that the HA6-PTX conjugate could be potentially utilized for further exploration as targeted drug delivery to enhance antitumor efficacy.
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