Dual drug-loaded halloysite hybrid-based glycocluster for sustained release of hydrophobic molecules

M. Massaro; S. Riela; C. Baiamonte; J. L. J. Blanco; C. Giordano; P. Lo Meo; S. Milioto; R. Noto; F. Parisi; G. Pizzolanti; G. Lazzara

doi:10.1039/C6RA14657K

Dual drug-loaded halloysite hybrid-based glycocluster for sustained release of hydrophobic molecules†

M. Massaro,^a S. Riela,*^a C. Baiamonte,^b J. L. J. Blanco,^c C. Giordano,^b P. Lo Meo,

^a S. Milioto,^d R. Noto,^a F. Parisi,^d G. Pizzolanti^b and G. Lazzara*^d

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* Corresponding authors

^a Dipartimento STEBICEF, Sez. Chimica, Università degli Studi di Palermo, Viale delle Scienze, Parco d'Orleans II, Ed. 17, 90128 Palermo, Italy
E-mail: serena.riela@unipa.it
Tel: +39-09123897546

^b Dipartimento Biomedico di Medicina Interna e Specialistica, Sez. Endocrinologia, Diabetologia, Metabolismo, Università degli Studi di Palermo, 90127 Palermo, Italy

^c Department of Organic Chemistry, Faculty of Chemistry, University of Sevilla, E-41012 Sevilla, Spain

^d Dipartimento di Fisica e Chimica, Università degli Studi di Palermo, Viale delle Scienze, Parco d'Orleans II, Ed. 17, 90128 Palermo, Italy
E-mail: giuseppe.lazzara@unipa.it

Abstract

A dual drug-loaded HNT–CD glycocluster delivery system based on halloysite nanotubes and carbohydrate functionalized cyclodextrin was developed by a green protocol using solvent-free microwave irradiation. The nanohybrid was employed for concurrent load and release of silibinin and curcumin. The new delivery system was characterized by means of TGA, FT-IR spectroscopy, SEM and DLS. These techniques confirm the successful loading of the two drugs in the system. SEM and DLS measurements highlighted that the nanomaterial preserves a tubular structure with an average hydrodynamic radius of ca. 200 nm. The release of the drugs from the HNT glycocluster was investigated by means of UV-vis spectroscopy at two different pH values simulanting the typical physiological conditions of either gastric or intestinal fluids. Enzyme-linked lectin assays (ELLA) demonstrated that highly mannoside–cyclodextrins HNT entities display high affinity towards mannose selective ConA lectin. Biological assays showed that the new drug delivery system exhibits anti-proliferative activity against the investigated cell lines. Fluorescence microscopy confirmed ELLA results and it showed a high propensity of this drug delivery system to cross cell membranes and to penetrate into the cell nucleus. The results revealed that the synthesized multicavity system is a material of suitable size and nanoarchitecture to transport drugs into living cells.

This article is part of the themed collection: Drug delivery

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Dual drug-loaded halloysite hybrid-based glycocluster for sustained release of hydrophobic molecules†

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Dual drug-loaded halloysite hybrid-based glycocluster for sustained release of hydrophobic molecules

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