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Journal of Nanomaterials
Volume 2015, Article ID 701979, 12 pages
http://dx.doi.org/10.1155/2015/701979
Research Article

Development of Polymeric Nanoparticles of Garcinia mangostana Xanthones in Eudragit RL100/RS100 for Anti-Colon Cancer Drug Delivery

1Department of Pharmacology, School of Pharmaceutical Sciences, Universiti Sains Malaysia, 11800 Minden Barracks, Pulau Pinang, Malaysia
2Department of Pharmaceutical Chemistry, School of Pharmaceutical Sciences, Universiti Sains Malaysia, 11800 Minden Barracks, Pulau Pinang, Malaysia
3Chair of “Medical Applications of Nanomaterials”, King Abdullah Institute for Nanotechnology, King Saud University, Riyadh 11451, Saudi Arabia
4Nanomedicine Section, King Abdullah International Medical Research Center, King Abdulaziz Medical City, Riyadh 11426, Saudi Arabia

Received 25 May 2015; Revised 12 September 2015; Accepted 5 October 2015

Academic Editor: Ilaria Armentano

Copyright © 2015 Abdalrahim F. A. Aisha et al. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

Abstract

Xanthones are a group of oxygenated heterocyclic compounds with anticancer properties, but poor aqueous solubility and low oral bioavailability hinder their therapeutic application. This study sought to prepare a xanthones extract (81%  α-mangostin and 16%  γ-mangostin) in polymeric nanoparticles and to investigate its intracellular delivery and cytotoxicity toward colon cancer cells. The nanoparticles were prepared in Eudragit RL100 and Eudragit RS100 by the nanoprecipitation method at drug loading and entrapment efficiency of 20% and >95%, respectively. Freeze-drying of bulk nanoparticle solutions, using glucose or sucrose as cryoprotectants, allowed the collection of nanoparticles at >95% yield. Solubility of the xanthones extract was improved from 0.1 µg/mL to 1250 µg/mL. Transmission electron microscopy (TEM) and dynamic light scattering (DLS) of the freeze-dried final formulation showed the presence of cationic round nanoparticles, with particle size in the range of 32–130 nm. Scanning electron microscopy (SEM) showed the presence of nanospheres, and Fourier transform infrared (FTIR) spectroscopy indicated intermolecular interaction of xanthones with Eudragit polymers. Cellular uptake of nanoparticles was mediated via endocytosis and indicated intracellular delivery of xanthones associated with potent cytotoxicity (median inhibitory concentration µg/mL). Presented results suggest that cationic nanoparticles of xanthones may provide a novel oral drug delivery system for chemoprevention or treatment of intestinal and colon tumors.