Journal
PHARMACEUTICAL RESEARCH
Volume 30, Issue 12, Pages 3214-3224Publisher
SPRINGER/PLENUM PUBLISHERS
DOI: 10.1007/s11095-013-1230-1
Keywords
local drug delivery; monoolein; monostearin; oleic acid-modified iron oxide nanoparticles; thermo-responsive monoglycerides
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To develop a novel monoglycerides-based thermal-sensitive drug delivery system, specifically for local intracavitary chemotherapy. Lipid matrices containing mixtures of glyceryl monooleate (GMO) and glyceryl monostearate (GMS) were evaluated for their potential application as magnetically induced thermo-responsive local drug delivery systems using a poorly water-soluble model drug, nifedipine (NF). Oleic acid-modified iron oxide (OA-Fe3O4) nanoparticles were embedded into the GMO-GMS matrix for remote activation of the drug release using an alternating magnetic field (AMF). The crystallization behavior of binary blends of GMO and GMS as characterized by DSC did show temperature dependent phase transition. GMO-GMS (75:25 wt%) blend showed a melting (T (m) ) and crystallization (T (c) ) points at 42A degrees C and 37A degrees C, respectively indicating the potential of the matrix to act as an 'on-demand' drug release. The matrix released only 35% of the loaded drug slowly in 10 days at 37A degrees C whereas 96% release was obtained at 42A degrees C. A concentration of 0.5% OA-Fe3O4 heated the matrix to 42.3 and 45.5A degrees C within 5 min and 10 min of AMF exposure, respectively. The in vitro NF release profiles form the monoglycerides matrix containing 0.5% OA-Fe3O4 nanoparticles after AMF activation confirmed the thermo-responsive nature of the matrix that could provide pulsatile drug release 'on-demand'.
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