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

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-pullula...

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Main Authors: Xiaojun Tao, Yongchao Xie, Qiufang Zhang, Ximin Qiu, Liming Yuan, Yi Wen, Min Li, Xiaoping Yang, Ting Tao, Minghui Xie, Yanwei Lv, Qinyi Wang, Xing Feng
Format: Article
Language:English
Published: MDPI AG 2016-09-01
Series:Nanomaterials
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Online Access:http://www.mdpi.com/2079-4991/6/9/165
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author Xiaojun Tao
Yongchao Xie
Qiufang Zhang
Ximin Qiu
Liming Yuan
Yi Wen
Min Li
Xiaoping Yang
Ting Tao
Minghui Xie
Yanwei Lv
Qinyi Wang
Xing Feng
author_facet Xiaojun Tao
Yongchao Xie
Qiufang Zhang
Ximin Qiu
Liming Yuan
Yi Wen
Min Li
Xiaoping Yang
Ting Tao
Minghui Xie
Yanwei Lv
Qinyi Wang
Xing Feng
author_sort Xiaojun Tao
collection DOAJ
description 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.
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spelling doaj.art-157f282d7fb048f8b391e2681d69e8992022-12-21T23:15:17ZengMDPI AGNanomaterials2079-49912016-09-016916510.3390/nano6090165nano6090165Cholesterol-Modified Amino-Pullulan Nanoparticles as a Drug Carrier: Comparative Study of Cholesterol-Modified Carboxyethyl Pullulan and Pullulan NanoparticlesXiaojun Tao0Yongchao Xie1Qiufang Zhang2Ximin Qiu3Liming Yuan4Yi Wen5Min Li6Xiaoping Yang7Ting Tao8Minghui Xie9Yanwei Lv10Qinyi Wang11Xing Feng12Department of Pharmacy, School of Medicine, Hunan Normal University, Changsha 410013, ChinaDepartment of Pharmacy, School of Medicine, Hunan Normal University, Changsha 410013, ChinaDepartment of Pharmacology, Hubei University of Medicine, Shiyan 442000, ChinaDepartment of Pharmacy, School of Medicine, Hunan Normal University, Changsha 410013, ChinaDepartment of Pharmacy, School of Medicine, Hunan Normal University, Changsha 410013, ChinaDepartment of Pharmacy, School of Medicine, Hunan Normal University, Changsha 410013, ChinaDepartment of Pharmacy, School of Medicine, Hunan Normal University, Changsha 410013, ChinaDepartment of Pharmacy, School of Medicine, Hunan Normal University, Changsha 410013, ChinaDepartment of Pharmacy, School of Medicine, Hunan Normal University, Changsha 410013, ChinaDepartment of Pharmacy, School of Medicine, Hunan Normal University, Changsha 410013, ChinaDepartment of Pharmacy, School of Medicine, Hunan Normal University, Changsha 410013, ChinaDepartment of Pharmacy, School of Medicine, Hunan Normal University, Changsha 410013, ChinaDepartment of Pharmacy, School of Medicine, Hunan Normal University, Changsha 410013, ChinaTo 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.http://www.mdpi.com/2079-4991/6/9/165amino pullulandegree of substitutionsurface chargedrug releasecytotoxicity
spellingShingle Xiaojun Tao
Yongchao Xie
Qiufang Zhang
Ximin Qiu
Liming Yuan
Yi Wen
Min Li
Xiaoping Yang
Ting Tao
Minghui Xie
Yanwei Lv
Qinyi Wang
Xing Feng
Cholesterol-Modified Amino-Pullulan Nanoparticles as a Drug Carrier: Comparative Study of Cholesterol-Modified Carboxyethyl Pullulan and Pullulan Nanoparticles
Nanomaterials
amino pullulan
degree of substitution
surface charge
drug release
cytotoxicity
title Cholesterol-Modified Amino-Pullulan Nanoparticles as a Drug Carrier: Comparative Study of Cholesterol-Modified Carboxyethyl Pullulan and Pullulan Nanoparticles
title_full Cholesterol-Modified Amino-Pullulan Nanoparticles as a Drug Carrier: Comparative Study of Cholesterol-Modified Carboxyethyl Pullulan and Pullulan Nanoparticles
title_fullStr Cholesterol-Modified Amino-Pullulan Nanoparticles as a Drug Carrier: Comparative Study of Cholesterol-Modified Carboxyethyl Pullulan and Pullulan Nanoparticles
title_full_unstemmed Cholesterol-Modified Amino-Pullulan Nanoparticles as a Drug Carrier: Comparative Study of Cholesterol-Modified Carboxyethyl Pullulan and Pullulan Nanoparticles
title_short Cholesterol-Modified Amino-Pullulan Nanoparticles as a Drug Carrier: Comparative Study of Cholesterol-Modified Carboxyethyl Pullulan and Pullulan Nanoparticles
title_sort cholesterol modified amino pullulan nanoparticles as a drug carrier comparative study of cholesterol modified carboxyethyl pullulan and pullulan nanoparticles
topic amino pullulan
degree of substitution
surface charge
drug release
cytotoxicity
url http://www.mdpi.com/2079-4991/6/9/165
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