β-Cyclodextrin-based inclusion complexation bridged biodegradable self-assembly macromolecular micelle for the delivery of paclitaxel

Yanzuo Chen, Yukun Huang, Dongdong Qin, Wenchao Liu, Chao Song, Kaiyan Lou, Wei Wang, Feng Gao

Research output: Contribution to journalArticlepeer-review

27 Scopus citations

Abstract

In this study, a novel adamantanamine-paclitaxel (AD-PTX) incorporated oligochitosancarboxymethyl-β-cyclodextrin (CSO-g-CM-β-CD) self-assembly macromolecular (CSO-g-CM-β-CD@AD-PTX) micelle was successfully prepared in water through sonication. The formed molecules were characterized by Fourier transform infrared spectroscopy, proton nuclear magnetic resonance (NMR) spectroscopy, two-dimensional NMR, elemental analysis, and liquid chromatography-mass spectrometry, while the correspondent micelles were characterized by dynamic light scattering and transmission electron microscopy. We showed that the macromolecular micelle contained a spherical core-shell structure with a diameter of 197.1 ± 3.3 nm and zeta potential of -19.1 ± 4.3 mV. The CSO-g-CM-β-CD@AD-PTX micelle exhibited a high drug-loading efficacy up to 31.3%, as well as a critical micelle concentration of 3.4 × 10-7 M, which indicated good stability. Additionally, the in vitro release profile of the CSO-g-CM-β-CD@AD-PTX micelle demonstrated a long-term release pattern, 63.1% of AD-PTX was released from the micelle during a 30-day period. Moreover, the CSO-g-CM-β-CD@AD-PTX micelle displayed cytotoxicity at a sub-μM scale similar to PTX in U87 MG cells, and CSO-g-CM-β-CD exhibited a good safety profile by not manifesting significant toxicity at concentrations up to 100 μM. These results indicated that β-CD-based inclusion complexation resulting in biodegradable self-assembled macromolecular micelles can be utilized as nanocarrier, and may provide a promising platform for drug delivery in the future medical applications.

Original languageEnglish (US)
Article numbere0150877
JournalPloS one
Volume11
Issue number3
DOIs
StatePublished - Mar 2016
Externally publishedYes

ASJC Scopus subject areas

  • General

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