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

Yang Hu; Lu Gan; Qian-xuan Li; Hong Tao; Lin Ye; Ai-ying Zhang; Zeng-guo Feng

doi:10.1007/s10118-014-1542-6

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

Updated：2021-06-21

- The Preparation of Cationic Folic Acid and Its Application in Drug Delivery System
- Chinese Journal of Polymer Science Vol. 32, Issue 12, Pages: 1714-1723(2014)
- Affiliations：
  
  a.School of Materials Science and Engineering, Beijing Institute of Technology, Beijing 100081, China
  b.Information Center, China Food and Drug Administration, Beijing 100053, China
  c.Graduate School of Frontier Science, University of Tokyo, Chiba 277-8561, Japan
- Author bio：
  
  **Lin Ye (叶霖), E-mail: yelin@bit.edu.cn
- Funds：
- DOI：10.1007/s10118-014-1542-6
  CLC：
- Received：08 April 2014，
  
  Revised：2014-05-23，
  
  Accepted：11 June 2014，
  
  Published：2014-12
- Accepted：
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Yang Hu, Lu Gan, Qian-xuan Li, et al. 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：

Yang Hu, Lu Gan, Qian-xuan Li, et al. 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.

摘要

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.

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