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Nanomaterials 2016, 6(9), 165; doi:10.3390/nano6090165

Cholesterol-Modified Amino-Pullulan Nanoparticles as a Drug Carrier: Comparative Study of Cholesterol-Modified Carboxyethyl Pullulan and Pullulan Nanoparticles

1
Department of Pharmacy, School of Medicine, Hunan Normal University, Changsha 410013, China
2
Department of Pharmacology, Hubei University of Medicine, Shiyan 442000, China
*
Author to whom correspondence should be addressed.
Academic Editors: Alina Maria Holban and Alexandru Mihai Grumezescu
Received: 1 July 2016 / Revised: 14 August 2016 / Accepted: 30 August 2016 / Published: 8 September 2016
(This article belongs to the Special Issue Nanoarchitectonics: A Novel Approach for Drug Delivery and Targeting)
View Full-Text   |   Download PDF [4117 KB, uploaded 8 September 2016]   |  

Abstract

To search for nano-drug preparations with high efficiency in tumor treatment, we evaluated the drug-loading capacity and cell-uptake toxicity of three kinds of nanoparticles (NPs). Pullulan was grafted with ethylenediamine and hydrophobic groups to form hydrophobic cholesterol-modified amino-pullulan (CHAP) conjugates. Fourier transform infrared spectroscopy and nuclear magnetic resonance were used to identify the CHAP structure and calculate the degree of substitution of the cholesterol group. We compared three types of NPs with close cholesterol hydrophobic properties: CHAP, cholesterol-modified pullulan (CHP), and cholesterol-modified carboxylethylpullulan (CHCP), with the degree of substitution of cholesterol of 2.92%, 3.11%, and 3.46%, respectively. As compared with the two other NPs, CHAP NPs were larger, 263.9 nm, and had a positive surface charge of 7.22 mV by dynamic light-scattering measurement. CHAP NPs showed low drug-loading capacity, 12.3%, and encapsulation efficiency of 70.8%, which depended on NP hydrophobicity and was affected by surface charge. The drug release amounts of all NPs increased in the acid media, with CHAP NPs showing drug-release sensitivity with acid change. Cytotoxicity of HeLa cells was highest with mitoxantrone-loaded CHAP NPs on MTT assay. CHAP NPs may have potential as a high-efficiency drug carrier for tumor treatment. View Full-Text
Keywords: amino pullulan; degree of substitution; surface charge; drug release; cytotoxicity amino pullulan; degree of substitution; surface charge; drug release; cytotoxicity
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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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Tao, X.; Xie, Y.; Zhang, Q.; Qiu, X.; Yuan, L.; Wen, Y.; Li, M.; Yang, X.; Tao, T.; Xie, M.; Lv, Y.; Wang, Q.; Feng, X. Cholesterol-Modified Amino-Pullulan Nanoparticles as a Drug Carrier: Comparative Study of Cholesterol-Modified Carboxyethyl Pullulan and Pullulan Nanoparticles. Nanomaterials 2016, 6, 165.

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