2-Deoxyglucose-Modified Folate Derivative: Self-Assembling Nanoparticle Able to Load Cisplatin.

Shaoming Jin,Zhongyao Du,Pengjie Wang,Xingen Lei,Fazheng Ren,Hao Zhang,Huiyuan Guo

doi:10.3390/molecules24061084

Shaoming Jin, Zhongyao Du + Show 5 more

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https://doi.org/10.3390/molecules24061084

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Abstract

Folic acid has been widely introduced into nano-drug delivery systems to give nanoparticle-targeted characteristics. However, the poor water solubility of folic acid may hinder the exploitation of its ability to load antineoplastic drugs. In the present study, we designed a new folate derivative (FA-2-DG) synthesized from folic acid and 2-Deoxyglucose (2-DG). The aim of this study was to evaluate the self-assembly characteristics of FA-2-DG, and its ability of loading cisplatin. The critical micelle concentration was 7.94 × 10−6 mol L−1. Fourier transform infrared spectroscopy indicated that hydrogen bonding interaction is a main driving force for the self–assembly of FA-2-DG. The particle was stable in pure water or 0.5% bovine serum albumin dispersions. By forming a coordination bond, the particles assembled from FA-2-DG can load cisplatin. The loading efficiency was maximal when the molar ratio of FA-2-DG to cisplatin was 2:1.

Highlights

The targeting of active substances to the tumor region is an effective chemotherapy therapeutic protocol for cancer
Known as a water-soluble vitamin, the water solubility of folic acid is poor and greatly affected by the pH value of the surrounding chemical environment, which may hinder the development of its loading ability for antineoplastic drugs
The results shown in Figure absorption at a wavelength of nm of solution is close to that of solution

Summary

Introduction

The targeting of active substances to the tumor region is an effective chemotherapy therapeutic protocol for cancer. Known as a water-soluble vitamin, the water solubility of folic acid is poor and greatly affected by the pH value of the surrounding chemical environment, which may hinder the development of its loading ability for antineoplastic drugs. To overcome this problem, many forms of folic-acid-based nanoparticles have been developed [9,10,11,12,13,14,15,16,17,18,19]. One of the most effective ways to improve the water solubility of folic-acid-based nanoparticles is glycosylation modification [20,21,22,23]

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