A Novel Folic Acid Receptor-Targeted Drug Delivery System Based on Curcumin-Loaded β-Cyclodextrin Nanoparticles for Cancer Treatment

Overview

Journal Drug Des Devel Ther

Specialty Pharmacology

Date 2021 Jul 8

PMID 34234415

Citations 18

Authors

Weiyong Hong

Fangyuan Guo

Nan Yu

Sanjun Ying

Bang Lou

Jiangqing Wu

Ying Gao

Xugang Ji

Haiying Wang

Aiqin Li

Guoping Wang

Gensheng Yang

Affiliations

Soon will be listed here.

Abstract

Purpose: A novel folate receptor-targeted β-cyclodextrin (β-CD) drug delivery vehicle was constructed to improve the bioavailability, biosafety, and drug loading capacity of curcumin. Controlled release and targeted delivery was achieved by modifying the nanoparticles with folic acid (FA).

Methods: Folate-conjugated β-CD-polycaprolactone block copolymers were synthesized and characterized. Curcumin-loaded nanoparticles (FA-Cur-NPs) were structured by self-assembly. The physicochemical properties, stability, release behavior and tumor-targeting ability of the fabricated nanoparticles were studied.

Results: The average particle size and drug loading of FA-Cur-NPs was 151.8 nm and 20.27%, respectively. Moreover, the FA-Cur-NPs exhibited good stability in vitro for 72 h. The drug release profiles showed that curcumin from FA-Cur-NPs was released significantly faster in a pH 6.4 phosphate buffered solution (PBS) than in pH 7.4, indicating that curcumin can be enriched around the tumor site compared with normal cells. Additionally, the internalization of FA-Cur-NPs was aided by FA receptor-mediated endocytosis, and its cytotoxicity was proportional to the cellular uptake efficiency. Furthermore, in vivo studies confirmed that FA-Cur-NPs exhibited marked accumulation in the tumor site and excellent antitumor activity.

Conclusion: These findings suggest that FA-Cur-NPs are a promising approach for improving cancer therapy through active targeting and controllable release.

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