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. 2016 Sep 8;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

Xiaojun Tao  1 , Yongchao Xie  2 , Qiufang Zhang  3 , Ximin Qiu  4 , Liming Yuan  5 , Yi Wen  6 , Min Li  7 , Xiaoping Yang  8 , Ting Tao  9 , Minghui Xie  10 , Yanwei Lv  11 , Qinyi Wang  12 , Xing Feng  13
Affiliations

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

Xiaojun Tao et al. Nanomaterials (Basel). .

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.

Keywords: amino pullulan; cytotoxicity; degree of substitution; drug release; surface charge.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
The synthesis route of the cholesterol-modified amino-pullulan (CHAP) conjugate.
Figure 2
Figure 2
Infrared spectra of pullulan (a); amino-pullulan (b); and CHAP(c).
Figure 3
Figure 3
1H-NMR spectra for pullulan (a); amino-pullulan (b); and CHAP (c).
Figure 4
Figure 4
Zeta potential (a); size distribution (b); and transmission electron microscopy (c) of CHAP NPs.
Figure 5
Figure 5
The mitoxantrone (MTO) release of nanoparticles in phosphate buffered saline (PBS) at 37 °C in vitro (▼ free mitoxantrone, ■ CHP, ● CHCP, ▲ CHAP).
Figure 6
Figure 6
MTO release from NPs in phosphate buffered saline buffer (pH 6.8) at 37 °C in vitro and acetate buffer (pH 4.0) (pH 6.8: ■ CHP, ● CHCP, ▲ CHAP; pH 4.0: ◄ CHCP, ▼ CHP, ► CHAP).
Figure 7
Figure 7
In vitro viability of HeLa cells with NPs at 12 and 24 h. Data are mean ± SD (n = 3).
Figure 8
Figure 8
In vitro viability of HeLa cells with MTO alone and MTO-loaded NPs at 24 h. Data are mean ± SD (n = 3).
Figure 9
Figure 9
The cell uptake illustration of nanoparticles with surface positive charge.
Figure 10
Figure 10
Illustration of movement of NPs from blood to targeted tissue.
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