A pH-Sensitive Polymeric Micellar System Based on Chitosan Derivative for Efficient Delivery of Paclitaxel

Han, Yang; Pan, Jieyi; Liang, Na; Gong, Xianfeng; Sun, Shaoping

doi:10.3390/ijms22136659

Open AccessArticle

A pH-Sensitive Polymeric Micellar System Based on Chitosan Derivative for Efficient Delivery of Paclitaxel

by

Yang Han

^1,2,†,

Jieyi Pan

^1,†,

Na Liang

^1,*,

Xianfeng Gong

² and

Shaoping Sun

^2,*

¹

Department of Pharmaceutical Engineering, College of Chemistry and Chemical Engineering, Harbin Normal University, Harbin 150025, China

²

Department of Pharmaceutical Engineering, School of Chemistry and Material Science, Heilongjiang University, Harbin 150080, China

^*

Authors to whom correspondence should be addressed.

^†

The authors contributed equally to this paper.

Int. J. Mol. Sci. 2021, 22(13), 6659; https://doi.org/10.3390/ijms22136659

Submission received: 6 May 2021 / Revised: 13 June 2021 / Accepted: 15 June 2021 / Published: 22 June 2021

(This article belongs to the Special Issue Chitosan Functionalizations, Formulations and Composites 2.0)

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Abstract

In this study, an amphiphilic conjugate based on mPEG and cholesterol-modified chitosan with hydrazone bonds in the molecules (mPEG-CS-Hz-CH) was successfully synthesized. Using the polymer as the carrier, the paclitaxel (PTX)-loaded mPEG-CS-Hz-CH micelles were prepared by an ultrasonic probe method. The mean particle size and zeta potential of the optimized PTX-loaded micelles were 146 ± 4 nm and +21.7 ± 0.7 mV, respectively. An in vitro drug release study indicated that the PTX-loaded mPEG-CS-Hz-CH micelles were stable under normal physiological conditions (pH 7.4), whereas rapid drug release was observed in the simulated tumor intracellular microenvironment (pH 5.0). An in vitro cytotoxicity study demonstrated the non-toxicity of the polymer itself, and the PTX-loaded micelles exhibited superior cytotoxicity and significant selectivity on tumor cells. An in vivo antitumor efficacy study further confirmed that the PTX-loaded micelles could improve the therapeutic efficacy of PTX and reduce the side effects. All these results suggested that the mPEG-CS-Hz-CH micelles might be promising pH-sensitive nanocarriers for PTX delivery.

Keywords: chitosan; drug delivery; paclitaxel; pH-sensitive; polymeric micelles

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MDPI and ACS Style

Han, Y.; Pan, J.; Liang, N.; Gong, X.; Sun, S. A pH-Sensitive Polymeric Micellar System Based on Chitosan Derivative for Efficient Delivery of Paclitaxel. Int. J. Mol. Sci. 2021, 22, 6659. https://doi.org/10.3390/ijms22136659

AMA Style

Han Y, Pan J, Liang N, Gong X, Sun S. A pH-Sensitive Polymeric Micellar System Based on Chitosan Derivative for Efficient Delivery of Paclitaxel. International Journal of Molecular Sciences. 2021; 22(13):6659. https://doi.org/10.3390/ijms22136659

Chicago/Turabian Style

Han, Yang, Jieyi Pan, Na Liang, Xianfeng Gong, and Shaoping Sun. 2021. "A pH-Sensitive Polymeric Micellar System Based on Chitosan Derivative for Efficient Delivery of Paclitaxel" International Journal of Molecular Sciences 22, no. 13: 6659. https://doi.org/10.3390/ijms22136659

APA Style

Han, Y., Pan, J., Liang, N., Gong, X., & Sun, S. (2021). A pH-Sensitive Polymeric Micellar System Based on Chitosan Derivative for Efficient Delivery of Paclitaxel. International Journal of Molecular Sciences, 22(13), 6659. https://doi.org/10.3390/ijms22136659

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A pH-Sensitive Polymeric Micellar System Based on Chitosan Derivative for Efficient Delivery of Paclitaxel

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