Sustained release of an antitumoral drug from alginate‐chitosan hydrogel beads and its potential use as colonic drug delivery

Abstract

Few researches are directed at drug delivery systems for b-lapachone (b-lap), a powerful anticancer agent but with limited pharmaceutical use. To overcome its limitations, we investigated controlled delivery systems of b-lap in simulated gastric fluids in vitro from chitosan (CS) and alginate (AL) hydrogel beads with purpose for oral administration. The AL-CS hydrogel beads were formed by coacervation and were characterized by morphology, swelling ratio, and their physicochemical properties. The hydrogel beads, with sizes of roughly 1 mm, presented good stability, and low porosity. The in vitro drug release profile was in good agreement with kinetics profiles and the Fickian model indicating diffusion as the release mechanism, with low burst effect, especially in an acid medium and allowing a prolonged release of $ 72 h (pH 1.2; k 2 ¼ 0.19 6 0.04) and (pH 7.4; k 2 ¼ 0.20 6 0.01). The beads were resistant to the acid medium and may be an alternative for b-lap therapy of colorectal cancer. V C 2012Wiley Periodicals, Inc. J Appl Polym Sci 126: E408-E417, 2012

Design of chitospheres loaded with pristine polymer particles for extended drug delivery via polyelectrolyte complexation and particulate leaching

“…Yang et al (2011) investigated the mechanical properties of STPP/ genipin co-crosslinked chitosan beads whereas Harris et al (2010) employed a series of chitosan hydrochloride genipin crosslinking reactions for the controlled release of drugs and proteins. Another widespread method employed for enhancing the drug delivery properties of chitosan beads involve the polyelectrolyte complexation of chitosan with anionic polymers either via blending of polymers prior to bead formation or coating of the beads employing a series of layering techniques using mainly alginates (Wang et al, 2010;Gong et al, 2011;Zhang et al, 2011;Torelli-Souza et al, 2012;Zhou et al, 2013) and pectins (Maestrelli et al, 2012;Ribeiro et al, 2014).…”

Local Delivery of Cannabinoid-Loaded Microparticles Inhibits Tumor Growth in a Murine Xenograft Model of Glioblastoma Multiforme

“…Cannabinoids have been shown to produce a potent anticancer action in different types of tumour xenografts including some of the ones that exhibit a higher resistance to standard chemotherapies such as gliomas [8]–[10], pancreatic adenocarcinomas [31] and hepatocellular carcinomas [32], three tumour types that are susceptible of being treated with drug-loaded MPs [33]–[41]. This anticancer action of cannabinois is based on the ability of these compounds to enhance apoptosis, inhibit proliferation of cancer cells and inhibit tumour angiogenesis.…”

Biodegradable Polysaccharides for Controlled Drug Delivery

“…Alginate and chitosan were crosslinked by coacervation to provide a controlled β‐lapachone delivery system. The resulting crosslinked beads were resistant to the acidic medium and might be an alternative for the β‐lapachone therapy of colorectal cancer …”