Physicochemical characterization of drug-loaded rigid and elastic vesicles

International Journal of Pharmaceutics
Tomonobu UchinoJoke A Bouwstra

Abstract

Ketorolac loaded rigid and elastic vesicles were prepared by sonication and the physicochemical properties of the drug loaded-vesicle formulations were examined. Rigid and elastic vesicles were prepared from the double chain surfactant sucrose-ester laurate (L-595) and the single chain surfactant octaoxyethylene-laurate ester (PEG-8-L). Sulfosuccinate (TR-70) was used as a negative charge inducer. Evaluation of the prepared vesicle was performed by dynamic light scattering, extrusion and by (1)H NMR (T(2) relaxation studies). The vesicles mean size varied between 90 and 150 nm. The elasticity of the vesicles was enhanced with increasing PEG-8-L/L-595 ratio, while an increase in loading of ketorolac resulted in a reduction in vesicle elasticity. (1)H NMR measurements showed that the molecular mobility of ketorolac was restricted, which indicates that ketorolac molecules were entrapped within the vesicle bilayers. The T(2) values of the aromatic protons of ketorolac increased gradually at higher PEG-8-L levels, indicating that ketorolac mobility increased in the vesicle bilayer. The chemical stability of ketorolac was dramatically improved in the vesicle formulation compared to a buffer solution. The strong interactions of ketoro...Continue Reading

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Citations

Oct 17, 2013·Journal of Controlled Release : Official Journal of the Controlled Release Society·Ming ChenSamir Mitragotri
Mar 19, 2013·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Tomonobu UchinoJoke Bouwstra
Aug 5, 2017·Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan·Tomonobu UchinoYoshiyuki Kagawa
Jun 4, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Angela AbruzzoTeresa Cerchiara

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