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Mater Sci Eng C Mater Biol Appl. 2017 Feb 1;71:1231-1240. doi: 10.1016/j.msec.2016.11.014. Epub 2016 Nov 8.

Ursolic acid liposomes with chitosan modification: Promising antitumor drug delivery and efficacy.

Author information

1
Applying Chemistry Key Lab of Hebei Province, Yanshan University, No.438 Hebei Street, Qinhuangdao 066004, China.
2
The First Hospital of Qinhuangdao, No. 258 Cultural Road, Qinhuangdao 066000, China.
3
Applying Chemistry Key Lab of Hebei Province, Yanshan University, No.438 Hebei Street, Qinhuangdao 066004, China. Electronic address: dwgao@ysu.edu.cn.

Abstract

There are tremendous challenges on antitumor and its therapeutic drugs, and preparation of highly efficient nano-vehicles represents one of the novel topics in antitumor pharmaceutical field. Herein, the novel chitosan-coated ursolic acid (UA) liposome (CS-UA-L) was efficiently prepared with highly tumor targeting, drug controlled release and low side-effect. The CS-UA-L was uniformly spherical particles with diameter of ~130nm, and the size was more easily trapped into the tumor tissues. Chitosan modification can make liposomes carrying positive charges, which were inclined to combine with the negative charges on the surface of tumor cells, and then the CS-UA-L could release UA rapidly at pH5.0 comparing with pH7.4. Meanwhile, the CS-UA-L exhibited obvious anti-proliferative effect (76.46%) on HeLa cells and significantly antitumor activity (61.26%) in mice bearing U14 cervical cancer. The tumor tissues of CS-UA-L treated mice had enhanced cell apoptosis, extensive necrosis and low cell proliferation activity. These results demonstrated that the multifunctional CS-UA-L allowed a precision treatment for localized tumor, and reducing the total drug dose and side-effect, which hold a great promise in new safe and effective tumor therapy.

KEYWORDS:

Antitumor; Chitosan; Liposomes; Ursolic acid; pH-responsive release

PMID:
27987679
DOI:
10.1016/j.msec.2016.11.014
[Indexed for MEDLINE]

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