The Preparation of Cationic Folic Acid and Its Application in Drug Delivery System

Citation: Yang Hu, Lu Gan, Qian-xuan Li, Hong Tao, Lin Ye, Ai-ying Zhang, Zeng-guo Feng. The Preparation of Cationic Folic Acid and Its Application in Drug Delivery System[J]. Chinese Journal of Polymer Science, 2014, 32(12): 1714-1723. doi: 10.1007/s10118-014-1542-6 shu

The Preparation of Cationic Folic Acid and Its Application in Drug Delivery System

1.
1. School of Materials Science and Engineering, Beijing Institute of Technology, Beijing 100081, China
2.
2. Information Center, China Food and Drug Administration, Beijing 100053, China
3.
4.
School of Materials Science and Engineering, Beijing Institute of Technology, Beijing 100081, China
5.
2. Graduate School of Frontier Science, University of Tokyo, Chiba 277-8561, Japan

通讯作者: Lin Ye,

基金项目:
This work is financially supported by National Undergraduate Training Programs for Innovation and Entrepreneurship (201310007048), the Basic Research Foundation of Beijing Institute of Technology (No. 20120942005), and the National Natural Science Foundation of China (No. 21104005).

摘要: The cationic folic acid (CFA) was prepared by introducing triethylenetetramine into folic acid with EDCI/NHS and characterized by IR, NMR and mass spectra. It was found that approximately one of two carboxyls in the folic acid molecule was substituted to form CFA. The conversion of -carboxyl is found to be 59% higher than 30% of -carboxyl. The CFA and doxorubicin hydrochloride can be loaded on the ionic shell of PTX-encapsulated micelle to form CFA loaded binary drug carrier via static interaction in aqueous solutions. The successful loading was demonstrated by zeta potential measurement and the drug load amount (DLA) of CFA was measured by HPLC. In vitro cytotoxicity results revealed the CFA drug carrier showed higher cytotoxicity to cancer cell MDA-MB-321 than the binary drug carrier without CFA and the positive control, while it showed lower cytotoxicity to normal cell HUVEC than the positive control, and similar cytotoxicity with the binary drug carrier without CFA. These results as well as confocal laser scanning microscopy observation indicate the synthesized CFA drug carrier possesses active tumor-targeting property.

关键词:

English

The Preparation of Cationic Folic Acid and Its Application in Drug Delivery System

1.
1. School of Materials Science and Engineering, Beijing Institute of Technology, Beijing 100081, China
2.
2. Information Center, China Food and Drug Administration, Beijing 100053, China
3.
4.
School of Materials Science and Engineering, Beijing Institute of Technology, Beijing 100081, China
5.
2. Graduate School of Frontier Science, University of Tokyo, Chiba 277-8561, Japan

Corresponding author: Lin Ye,

Received Date: 08 April 2014
Revised Date: 11 June 2014
Available Online: 05 December 2014
Fund Project:
This work is financially supported by National Undergraduate Training Programs for Innovation and Entrepreneurship (201310007048), the Basic Research Foundation of Beijing Institute of Technology (No. 20120942005), and the National Natural Science Foundation of China (No. 21104005).

Abstract: The cationic folic acid (CFA) was prepared by introducing triethylenetetramine into folic acid with EDCI/NHS and characterized by IR, NMR and mass spectra. It was found that approximately one of two carboxyls in the folic acid molecule was substituted to form CFA. The conversion of -carboxyl is found to be 59% higher than 30% of -carboxyl. The CFA and doxorubicin hydrochloride can be loaded on the ionic shell of PTX-encapsulated micelle to form CFA loaded binary drug carrier via static interaction in aqueous solutions. The successful loading was demonstrated by zeta potential measurement and the drug load amount (DLA) of CFA was measured by HPLC. In vitro cytotoxicity results revealed the CFA drug carrier showed higher cytotoxicity to cancer cell MDA-MB-321 than the binary drug carrier without CFA and the positive control, while it showed lower cytotoxicity to normal cell HUVEC than the positive control, and similar cytotoxicity with the binary drug carrier without CFA. These results as well as confocal laser scanning microscopy observation indicate the synthesized CFA drug carrier possesses active tumor-targeting property.

Key words:

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沈阳化工大学材料科学与工程学院沈阳 110142

The Preparation of Cationic Folic Acid and Its Application in Drug Delivery System

通讯作者: Lin Ye,

English

The Preparation of Cationic Folic Acid and Its Application in Drug Delivery System

Corresponding author: Lin Ye,

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通讯作者: 陈斌, bchen63@163.com

中国化学会秘书处

The Preparation of Cationic Folic Acid and Its Application in Drug Delivery System

通讯作者: Lin Ye,

English

The Preparation of Cationic Folic Acid and Its Application in Drug Delivery System

Corresponding author: Lin Ye,

CCS Chemistry：嵌段共聚物自组装成 “三明治”二维有机材料，实现纳米级压力传感功能

CCS Chemistry：颜徐州、鲍哲南： 你的皮肤可能是一片SPMs

CCS Chemistry：工作高效不疲劳，只须让催化剂动起来

CCS Chemistry：静电组装导向聚合- 聚电解质纳米凝胶量化制备新策略

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