Effect of a Drug Delivery System Made of Quercetin Formulated into PEGylation Liposomes on Cervical Carcinoma In Vitro and In Vivo

Author:

Li Jian123ORCID,Li Zhen12ORCID,Gao Yanting12ORCID,Liu Shihe12ORCID,Li Kun123ORCID,Wang Shuai4ORCID,Gao Liming5ORCID,Shi Ming1236ORCID,Liu Zhiwei1236ORCID,Han Zengsheng123ORCID,Qiu Yan7ORCID

Affiliation:

1. College of Environmental & Chemical Engineering, Yanshan University, Qinhuangdao, Hebei Province 066004, China

2. Applied Chemistry Key Laboratory of Hebei Province, Yanshan University, Qinhuangdao, Hebei Province 066004, China

3. Engineering Research Center of Functional Nucleic Acids in Qinhuangdao, Qinhuangdao, Hebei Province 066004, China

4. The Harbour Hospital of Qinhuangdao City, Qinhuangdao, Hebei Province 066000, China

5. The First Hospital of Qinhuangdao City, Qinhuangdao, Hebei Province 066000, China

6. Qinhuangdao Biopha Biotechnology Co., Ltd, Qinhuangdao, Hebei Province 066000, China

7. Department of Life Science, School of Biological Science and Engineering, Hebei University of Science & Technology, Shijiazhuang, Hebei Province 050018, China

Abstract

Quercetin is a well-known flavonoid for its potent antitumor and antiproliferative effects on a wide range of human cancer cell lines. However, the delivery of quercetin is challenging due to its extreme insolubility in water. The intention of this study was to evaluate the antitumor effect of quercetin-loaded PEGylated liposomes (PEG-Que-NLs) in vitro and in vivo. We first prepared PEG-Que-NLs by method of thin film hydration; further determined, the optimum ratios of quercetin to Soybean phosphatidylcholine (SPC), to cholesterol (CHL), and to PEG-4000 were 1 : 8, 1 : 2, and 1 : 2 ( w / w ), respectively, and the optimal hydration temperature was 55°C when the mean vesicle diameter and apparent Zeta potential of PEG-Que-NLs were found to be 171.3 ± 10.4  nm and 13.1 ± 2.1  mV, respectively; the encapsulation efficiency and the drug loading of PEG-Que-NLs were 81.25 ± 3.12 % and 8.5 ± 0.77 % , respectively. Drug release study in vitro showed that PEG-Que-NLs exhibited a slow-release effect without significant burst effect. Furthermore, the inhibition effect of PEG-Que-NLs on HeLa cells was considerably higher than free quercetin (free-Que) and quercetin liposomes (Que-NLs). Intravenous injection of PEG-Que-NLs into U14 bearing mouse models inhibited the cervical carcinoma growth significantly, and the tumor inhibition rate was much higher than free-Que and Que-NLs. These results of this study indicated that PEG-Que-NLs exhibited potential application prospects in the treatment of malignant tumors because of its tumor targeting, slow-release properties, and the solubility improvement of quercetin.

Funder

Science and Technology Research Projects of Colleges and Universities in Hebei Province, China

Publisher

Hindawi Limited

Subject

General Materials Science

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