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Title: Developing Transdermal Applications of Ketorolac Tromethamine Entrapped in Stimuli Sensitive Block Copolymer Hydrogels
Author: Mallandrich Miret, Mireia
Fernández Campos, Francisco
Clares Naveros, Beatriz
Halbaut, Lyda
Alonso, C.
Coderch, L.
Garduño Ramírez, M. L.
Andrade Carrera, Berenice
Pozo Carrascosa, Alfonso del
Lane, ME
Calpena Campmany, Ana Cristina
Keywords: Farmacologia
Tecnologia farmacèutica
Administració de medicaments
Agents antiinflamatoris
Fórmules magistrals
Medicació transdèrmica
Pharmaceutical technology
Administration of drugs
Antiinflammatory agents
Medical formularies
Transdermal medication
Issue Date: 24-May-2017
Publisher: Springer Science + Business Media
Abstract: Purpose: In order to obtain dermal vehicles of ketorolac tromethamine (KT) for the local treatment of inflammation and restrict undesirable side effects of systemic levels hydrogels (HGs) of poloxamer and carbomer were developed. Methods: KT poloxamer based HG (KT-P407-HG) and KT carbomer based HG (KT-C940-HG) were elaborated and characterized in terms of swelling, degradation, porosity, rheology, stability, in vitro release, ex vivo permeation and distribution skin layers. Finally, in vivo anti-inflammatory efficacy and skin tolerance were also assessed. Results: HGs were transparent and kept stable after 3 months exhibiting biocompatible near neutral pH values. Rheological patterns fitted to Herschel-Bulkley for KT-C940-HG and Newton for KT-P407-HG due to its low viscosity at 25°C. Rapid release profiles were observed through first order kinetics. Following the surface the highest concentration of KT from C940-HG was found in the epidermis and the stratum corneum for P407-HG. Relevant anti-inflammatory efficacy of KT-P407-HG revealed enough ability to provide sufficient bioavailability KT to reach easily the site of action. The application of developed formulations in volunteers did not induce any visual skin irritation. Conclusions: KT-P407-HG was proposed as suitable formulation for anti-inflammatory local treatment without theoretical systemic side effect.
Note: Versió postprint del document publicat a:
It is part of: Pharmaceutical Research, 2017, vol. 34, num. 8, p. 1728-1740
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ISSN: 0724-8741
Appears in Collections:Articles publicats en revistes (Farmàcia, Tecnologia Farmacèutica i Fisicoquímica)

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