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Direct chemical grafted curcumin on halloysite nanotubes as dual-responsive prodrug for pharmacological applications.

作者信息

Massaro M, Amorati R, Cavallaro G, Guernelli S, Lazzara G, Milioto S, Noto R, Poma P, Riela S

机构信息

Dipartimento STEBICEF, Sez. Chimica, Università degli Studi di Palermo, Viale delle Scienze, Parco d'Orleans II, Ed. 17, 90128 Palermo, Italy.

Dipartimento di Chimica "Giacomo Ciamician", Via S.Giacomo 11, Bologna, Italy.

出版信息

Colloids Surf B Biointerfaces. 2016 Apr 1;140:505-513. doi: 10.1016/j.colsurfb.2016.01.025. Epub 2016 Jan 18.


DOI:10.1016/j.colsurfb.2016.01.025
PMID:26812638
Abstract

Covalently functionalized halloysite nanotubes (HNTs) were successfully employed as dual-responsive nanocarriers for curcumin (Cur). Particularly, we synthesized HNT-Cur prodrug with a controlled curcumin release on dependence of both intracellular glutathione (GSH) and pH conditions. In order to obtain HNT-Cur produgs, halloysite was firstly functionalized with cysteamine through disulphide linkage. Afterwards, curcumin molecules were chemically conjugated to the amino end groups of halloysite via Schiff's base formation. The successful functionalization of halloysite was proved by thermogravimetric analysis, FT-IR spectroscopy, dynamic light scattering and scanning electron microscopy. Experimental data confirmed the presence of curcumin on HNT external surface. Moreover, we investigated the kinetics of curcumin release by UV-vis spectroscopy, which highlighted that HNT-Cur prodrug possesses dual stimuli-responsive ability upon exposure to GSH-rich or acidic environment. In vitro antiproliferative and antioxidant properties of HNT-Cur prodrug were studied with the aim to explore their potential applications in pharmaceutics. This work puts forward an efficient strategy to prepare halloysite based nanocarriers with controlled drug delivery capacity through direct chemical grafting with stimuli-responsive linkage.

摘要

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