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Int. J. Mol. Sci. 2015, 16(4), 7195-7209; doi:10.3390/ijms16047195

In Vitro Investigation of Self-Assembled Nanoparticles Based on Hyaluronic Acid-Deoxycholic Acid Conjugates for Controlled Release Doxorubicin: Effect of Degree of Substitution of Deoxycholic Acid

College of Marine Life Science, Ocean University of China, Yusan Road No. 5, Qingdao 266003, China
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Author to whom correspondence should be addressed.
Academic Editor: Bing Yan
Received: 22 September 2014 / Revised: 6 January 2015 / Accepted: 22 January 2015 / Published: 31 March 2015
(This article belongs to the Special Issue Bioactive Nanoparticles 2014)
View Full-Text   |   Download PDF [795 KB, uploaded 31 March 2015]   |  

Abstract

Self-assembled nanoparticles based on a hyaluronic acid-deoxycholic acid (HD) chemical conjugate with different degree of substitution (DS) of deoxycholic acid (DOCA) were prepared. The degree of substitution (DS) was determined by titration method. The nanoparticles were loaded with doxorubicin (DOX) as the model drug. The human cervical cancer (HeLa) cell line was utilized for in vitro studies and cell cytotoxicity of DOX incorporated in the HD nanoparticles was accessed by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. In addition, cellular uptake of fluorescently labeled nanoparticles was also investigated. An increase in the degree of deoxycholic acid substitution reduced the size of the nanoparticles and also enhanced their drug encapsulation efficiency (EE), which increased with the increase of DS. A higher degree of deoxycholic acid substitution also lead to a lower release rate and an initial burst release of doxorubicin from the nanoparticles. In summary, the degree of substitution allows the modulation of the particle size, drug encapsulation efficiency, drug release rate, and cell uptake efficiency of the nanoparticles. The herein developed hyaluronic acid-deoxycholic acid conjugates are a good candidate for drug delivery and could potentiate therapeutic formulations for doxorubicin–mediated cancer therapy. View Full-Text
Keywords: hyaluronic acid; deoxycholicacid; nanoparticles; doxorubicin hyaluronic acid; deoxycholicacid; nanoparticles; doxorubicin
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Wei, W.-H.; Dong, X.-M.; Liu, C.-G. In Vitro Investigation of Self-Assembled Nanoparticles Based on Hyaluronic Acid-Deoxycholic Acid Conjugates for Controlled Release Doxorubicin: Effect of Degree of Substitution of Deoxycholic Acid. Int. J. Mol. Sci. 2015, 16, 7195-7209.

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