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Mol Pharm. 2018 Dec 3;15(12):5534-5545. doi: 10.1021/acs.molpharmaceut.8b00687. Epub 2018 Nov 13.

Redox- and pH-Sensitive Glycan (Polysialic Acid) Derivatives and F127 Mixed Micelles for Tumor-Targeted Drug Delivery.

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1
College of Pharmacy , Shenyang Pharmaceutical University , 103 Wenhua Road , Shenyang , Liaoning 110016 , China.

Abstract

With increasing application of PEGylated products, drawbacks are beginning to emerge such as the "PEG dilemma". Other promising materials may need to be found in the current situation. Endogenous polysialic acid (PSA), which is highly expressed on mammalian, bacterial, and malignant surface, may be a promising material in oncology. In this study, a dual-responsive amphiphilic PSA cholesterol derivative (PSA-CS-CH) was synthesized to explore the opportunity of PSA in targeted drug delivery systems. PSA-CS-CH, F127 mixed micelles (PF-M), and pure F127 micelles (F-M) were prepared for comparative antitumor experiments. The in vitro experiments showed that modification of PSA-CS-CH significantly increased cytotoxicity and cellular uptake. PF-M had excellent tumor microenvironment response release behavior on acidic media with high GSH levels. The in vivo fluorescence imaging and antitumor experiments showed that PF-M had excellent tumor targeting ability and great tumor suppression ability. In summary, biodegradable PSA may contribute to cancer therapy.

KEYWORDS:

drug delivery system; dual-responsive; pH-sensitive; polysialic acid; tumor-targeted

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