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Folate-modified Annonaceous acetogenins nanosuspensions and their improved antitumor efficacy

Authors Hong JY, Sun ZH, Li YJ, Guo YF, Liao YH, Liu MF, Wang XT

Received 17 February 2017

Accepted for publication 14 June 2017

Published 14 July 2017 Volume 2017:12 Pages 5053—5067

DOI https://doi.org/10.2147/IJN.S134284

Checked for plagiarism Yes

Review by Single anonymous peer review

Peer reviewer comments 5

Editor who approved publication: Dr Lei Yang


Jingyi Hong,1 Zhonghao Sun,1 Yijing Li,1 Yifei Guo,1 Yonghong Liao,1 Meifeng Liu,2 Xiangtao Wang1

1Key Laboratory of Bioactive Substances and Resources Utilization of Chinese Herbal Medicine, Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing, 2Key Laboratory of Functional Molecular Engineering of Guangdong Province, School of Chemistry and Chemical Engineering, South China University of Technology, Guangzhou, China

Abstract:
Annonaceous acetogenins (ACGs) are a large family of fatty acid derived natural products that are exclusively isolated from the Annonaceae species. Many members of this diverse family have a broad spectrum of biological activities, the most impressive of which is anticancer activity. However, their poor solubility and severe toxicity restrict their clinical application, and their complicated composition hinders their formulation and drug delivery. In this study, β-cyclodextrin was modified with folic acid (FA) and then combined with soybean lecithin to prepare FA-modified ACGs nanosuspensions (FA-ACGs-NSps). The obtained FA-ACGs-NSps had a high drug payload of 57.59% and average particle size of 199.5 nm, and they exhibited sustained drug release within 142 hours. In comparison with ACGs-NSps, FA-ACGs-NSps showed significantly enhanced cytotoxicity and higher cell uptake toward folate receptor-positive 4T1 cell lines. An in vivo study demonstrated that FA-ACGs-NSps more effectively accumulated in tumors and enhanced the antitumor therapeutic efficacy with less toxicity in 4T1 tumor bearing mice. Therefore, FA-ACGs-NSps may be a promising drug delivery system for ACGs to improve their therapeutic window and may be suitable for clinical application to treat folate-positive tumors.

Keywords: Annonaceous acetogenins, nanosuspensions, folate, targeted drug delivery, antitumor activity

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