Synthesis, structural andin vitrostudies of well-dispersed monomethoxy-poly(ethylene glycol)–honokiol conjugate micelles

Qiu, N., Cai, L.-l., Xie, D., Wang, G., Wu, W., Zhang, Y., Song, H., Yin, H. and Chen, L. (2010) Synthesis, structural andin vitrostudies of well-dispersed monomethoxy-poly(ethylene glycol)–honokiol conjugate micelles. Biomedical Materials, 5(6), 065006. (doi:10.1088/1748-6041/5/6/065006) (PMID:20966535)

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Abstract

Honokiol, an active principle extracted from Magnolia officinalis, has great potential as a cancer treatment. However, its poor water solubility greatly hampers its delivery to the tumor sites at an effective concentration. In this study, an amphiphilic polymer–drug conjugate was successfully prepared by condensation of low molecular weight monomethoxy-poly(ethylene glycol) (MPEG)-2000 with honokiol (HK) through an ester linkage to increase the hydrophilicity of honokiol. The MPEG–honokiol (MPEG–HK) conjugate prepared formed nano-sized micelles, with a mean particle size of less than 20 nm (MPEG–HK, 360 µg ml−1) in water, which could be well dispersed in water. The nanoparticles obtained were characterized by particle size distribution, morphology and zeta potential. The stability and hydrolysis profile of the polymeric pro-drug in phosphate-buffered saline (PBS) and plasma were also studied and the results showed that only 20% of the conjugated honokiol was released in 2.0 h in beagle dog plasma, while in PBS the time required to reach 20% of honokiol release was >200 h. Meanwhile, the inhibitory activity of the honokiol conjugate was found to be retained in vitro against LL/2 cell lines with an IC50 value of 10.7 µg ml−1. These results suggest that the polymer–drug conjugate provides a potential new approach to hydrophobic drugs, such as honokiol, in formulation design.

Item Type:Articles
Status:Published
Refereed:Yes
Glasgow Author(s) Enlighten ID:Yin, Professor Huabing
Authors: Qiu, N., Cai, L.-l., Xie, D., Wang, G., Wu, W., Zhang, Y., Song, H., Yin, H., and Chen, L.
College/School:College of Science and Engineering > School of Engineering > Biomedical Engineering
Journal Name:Biomedical Materials
Publisher:IOP Publishing
ISSN:1748-6041
ISSN (Online):1748-605X

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