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Please use this identifier to cite or link to this item: http://repository.li.mahidol.ac.th/dspace/handle/123456789/34906
Title: Development and characterization of lyophilized diazepam-loaded polymeric micelles
Authors: Jiraphong Suksiriworapong
Tanaporn Rungvimolsin
Atitaya A-Gomol
Varaporn Buraphacheep Junyaprasert
Doungdaw Chantasart
Mahidol University
Keywords: Pharmacology, Toxicology and Pharmaceutics
Issue Date: 1-Feb-2014
Citation: AAPS PharmSciTech. Vol.15, No.1 (2014), 52-64
Abstract: Polymeric micelles were studied as delivery carriers of diazepam, a practically insoluble drug in water, for rectal administration. The diazepam-loaded polymeric micelles were developed by using poloxamer 407 (P407), poloxamer 188, and d-α-tocopheryl poly(ethylene glycol) 1000 succinate (TPGS). Among the used polymers, TPGS resulted in polymeric micelles with good characteristics for encapsulation of diazepam which had the small particle size of 8-12 nm and narrow size distribution (PI 0.053-0.275). Additionally, 7.5% w/v of TPGS could entirely entrap the desired concentration of diazepam (5 mg/mL). To improve the physical stability upon lyophilization, an addition of P407 of 1% w/v prevented aggregation, increased physical stability, and maintained chemical stability of the lyophilized powders of diazepam-loaded polymeric micelles for 3 months storage at 4 C. The rate and amount of diazepam release from TPGS polymeric micelles mainly depended on the concentration of TPGS. The release data were fitted to Higuchi's model suggesting that the drug release mechanism was controlled by Fickian diffusion. In conclusion, 10% w/v TPGS and 1% w/v P407 were the optimum formulation of lyophilized diazepam-loaded polymeric micelles. © 2013 American Association of Pharmaceutical Scientists.
URI: https://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=84893704496&origin=inward
http://repository.li.mahidol.ac.th/dspace/handle/123456789/34906
ISSN: 15309932
Appears in Collections:Scopus 2011-2015

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