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叶酸修饰的脂质载体共递送顺铂和紫杉醇用于治疗头颈癌。

Cisplatin and paclitaxel co-delivered by folate-decorated lipid carriers for the treatment of head and neck cancer.

作者信息

Yang Jiying, Ju Zengjuan, Dong Shufang

机构信息

a Department of Pharmacy , Linyi People's Hospital , Linyi , Shandong Province , PR China.

出版信息

Drug Deliv. 2016 Nov;24(1):792-799. doi: 10.1080/10717544.2016.1236849.

Abstract

CONTEXT

For head and neck cancer therapy, co-delivery of two drugs, cisplatin (DDP) plus paclitaxel (PTX), are more effective than single drug therapy. Lipid carriers are promising drug carriers for anti-cancer delivery.

OBJECTIVE

The aim of this study is to construct a folate (FA) decorated nanostructured lipid carriers (NLCs) as nanocarriers for DDP and PTX delivery.

MATERIALS AND METHODS

In this study, DDP and PTX were incorporated into NLCs. Folate-PEG-DSPE (FA-PEG-DSPE) was synthesized and decorated the drugs-loaded NLCs (FA-DDP/PTX NLCs). Their average size, zeta potential, drug encapsulation efficiency, drug loading capacity, and in vitro drug release were evaluated. Head and neck cancer cells (FaDu cells) were used for the testing of in vitro cytotoxicity, and in vivo transfection efficiency of NLC was evaluated on mice bearing FaDu cells model.

RESULTS

The size of FA-DDP/PTX NLCs was around 127 nm, with a positive zeta potential of 26.7 mV. FA-DDP/PTX NLCs showed the highest cytotoxicity and synergistic effect of two drugs in head and neck cancer cells (FaDu cells) in vitro. The in vivo study revealed the greatest anti-tumor activity than all the other formulations in murine-bearing head and neck cancer model.

DISCUSSION AND CONCLUSION

FA-DDP/PTX NLCs effectively improves anticancer efficiency for head and neck cancer in vitro and in vivo. The constructed NLCs could be used as a novel carrier to co-delivery DDP and PTX for head and neck cancer therapy.

摘要

背景

对于头颈癌治疗,顺铂(DDP)加紫杉醇(PTX)两种药物联合递送比单一药物治疗更有效。脂质载体是用于抗癌递送的有前景的药物载体。

目的

本研究的目的是构建一种叶酸(FA)修饰的纳米结构脂质载体(NLCs)作为DDP和PTX递送的纳米载体。

材料与方法

在本研究中,将DDP和PTX载入NLCs。合成叶酸-聚乙二醇-二硬脂酰磷脂酰乙醇胺(FA-PEG-DSPE)并修饰载药NLCs(FA-DDP/PTX NLCs)。评估它们的平均粒径、zeta电位、药物包封率、载药量和体外药物释放。使用头颈癌细胞(FaDu细胞)测试体外细胞毒性,并在携带FaDu细胞模型的小鼠上评估NLC的体内转染效率。

结果

FA-DDP/PTX NLCs的粒径约为127nm,zeta电位为正26.7mV。FA-DDP/PTX NLCs在体外对头颈癌细胞(FaDu细胞)显示出最高的细胞毒性和两种药物的协同作用。体内研究表明,在携带头颈癌的小鼠模型中,其抗肿瘤活性比所有其他制剂都高。

讨论与结论

FA-DDP/PTX NLCs在体外和体内均有效提高了对头颈癌的抗癌效率。构建的NLCs可作为一种新型载体,用于联合递送DDP和PTX以治疗头颈癌。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4aed/8241145/97c9469da1bc/IDRD_A_1236849_F0001_C.jpg

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