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Int J Pharm. 2014 May 15;466(1-2):314-20. doi: 10.1016/j.ijpharm.2014.03.030. Epub 2014 Mar 20.

Preparation of novel curcumin-loaded multifunctional nanodroplets for combining ultrasonic development and targeted chemotherapy.

Author information

1
Department of Pharmaceutical Science, Nanfang Hospital, Southern Medical University, No. 1838 Guangzhou Ave., Guangzhou, 510515, PR China.
2
Department of Pharmaceutics, School of Pharmacy, Ningxia Medical University, No. 1160 Shengli South Street, Yinchuan, 750004, PR China.
3
Department of Pharmaceutical Science, Nanfang Hospital, Southern Medical University, No. 1838 Guangzhou Ave., Guangzhou, 510515, PR China. Electronic address: jhchen06@126.com.

Abstract

Recently, a new class of multifunctional nanodroplets that combine the properties of polymeric drug carriers, ultrasound imaging contrast agents, and enhancers of ultrasound-mediated drug delivery has been developed. We studied the formation mechanism of nanodroplets of a drug and its application in chemotherapy. Curcumin was loaded in polymeric micelles as a anti-cancer drug using polyethylene glycol block-poly(caprolactone) with encapsulation efficiency of 95.60%. At room temperature, the developed systems comprised perfluorocarbon nanodroplets stabilized by walls comprising biodegradable block copolymers. Upon heating to 37°C, the nanodroplets were converted to nano/microbubbles. Under ultrasound, nanobubbles cavitated and collapsed, resulting in release of the encapsulated drug. The percentage release of curcumin-loaded nanodroplets by insonation was 90.95%, showing enhancement compared with the non-ultrasound group. Nanodroplets strongly retained the loaded drugs in vivo yet, under ultrasound-mediated vaporization, they released the drugs, thereby implementing effective targeting into the tumor. The tumor inhibition of the group in which curcumin-loaded nanodroplets were combined with ultrasound was 71.30%, more than that of the group of curcumin-loaded nanodroplets (53.00%). Nanodroplets showed high enhancement of anti-cancer effects under ultrasound. Upon intravenous injection, a long-lasting, strong and selective ultrasound contrast was observed, suggesting their coalescence into larger, highly echogenic microbubbles. These multifunctional nanodroplets, which manifest excellent therapeutic and ultrasound properties, could be promising anti-cancer drug delivery systems.

KEYWORDS:

Curcumin; Drug delivery; Nanodroplets; PEG-PCL; Ultrasound

PMID:
24657138
DOI:
10.1016/j.ijpharm.2014.03.030
[Indexed for MEDLINE]

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