Improved solubilization of Celecoxib in U-type nonionic microemulsions and their structural transitions with progressive aqueous dilution

Journal of Colloid and Interface Science
Nissim GartiAbraham Aserin

Abstract

Celecoxib (clxb) is an important drug for treatment of rheumatoid arthritis and osteoarthritis by specifically inhibiting the enzyme cyclooxygenase-2 (COX-2). Clxb is a type 2 drug characterized by low water solubility (<5 mug/ml) and fast transmembrane transport. The present formulations require high dosage since the transmembrane transport fluctuates and is very difficult to control. Dissolving the drug within an oil phase was not practical since its dissolution was very small and its dispersion in water was impossible. In our recent studies, we learned to construct U-type phase diagrams and to formulate reverse microemulsions (oil-based concentrates) that are progressively and fully dilutable with aqueous phase. In the present study, we solubilized clxb in nanostructures of reverse micelles of U-type nonionic microemulsions that consisted of R(+)-limonene, alcohol, propylene glycol (PG), and hydrophilic surfactant (Tween 60). The solubilization capacity of the drug in these systems is many times higher than in either the oil or the aqueous phase. The clxb solubilized microemulsions are fully diluted with aqueous phase without phase separation. The solubilization capacity decreases as the water content increases. Electrical c...Continue Reading

References

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Citations

Mar 5, 2014·Pharmaceutics·Luciana B Lopes
Sep 1, 2007·Journal of Microencapsulation·Miha HomarPhilippe Maincent
Aug 22, 2009·Journal of Microencapsulation·Miha HomarMirjana Gasperlin
Sep 3, 2013·Drug Development and Industrial Pharmacy·Natascia MenniniPaola Mura
Jan 24, 2012·Journal of Controlled Release : Official Journal of the Controlled Release Society·Michal BacharDganit Danino
Aug 17, 2010·Colloids and Surfaces. B, Biointerfaces·Orit AmsalemNissim Garti
Sep 8, 2009·The Journal of Nutritional Biochemistry·Michelle A Micallef, Manohar L Garg
May 12, 2009·International Journal of Pharmaceutics·Andrej DolencOdon Planinsek
May 29, 2009·Colloids and Surfaces. B, Biointerfaces·Orit AmsalemNissim Garti
Jul 5, 2008·Colloids and Surfaces. B, Biointerfaces·Anna KoganNissim Garti
May 17, 2008·Nuclear Medicine and Biology·Erik F J de VriesHans C Klein
May 14, 2008·Journal of Controlled Release : Official Journal of the Controlled Release Society·Mao-Bo ChengQiang Zhang
Dec 20, 2007·Advanced Drug Delivery Reviews·Sagar S Rane, Bradley D Anderson
Nov 17, 2007·Journal of Colloid and Interface Science·Aviram SpernathNissim Garti
Aug 4, 2007·Journal of Colloid and Interface Science·Shoshana RoznerNissim Garti
May 4, 2007·Journal of Controlled Release : Official Journal of the Controlled Release Society·Aviram SpernathNissim Garti
Jan 19, 2007·Advances in Colloid and Interface Science·Aviram Spernath, Abraham Aserin
Nov 2, 2015·Journal of Colloid and Interface Science·Nina LidichNissim Garti
Nov 29, 2015·Journal of Colloid and Interface Science·Nina LidichNissim Garti
Jun 21, 2015·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Shruti V Patel, Sarsvatkumar Patel
May 2, 2018·Current Cancer Drug Targets·Oliesia Gonzalez Quiñones, Maria Bernadete Riemma Pierre
Nov 29, 2020·Colloids and Surfaces. B, Biointerfaces·Eva Abramov, Nissim Garti
Jan 1, 2008·Langmuir : the ACS Journal of Surfaces and Colloids·Anna KoganNissim Garti
Jan 1, 2009·The Journal of Physical Chemistry. B·Anna KoganMaria Francesca Ottaviani

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