Developing Transdermal Applications of Ketorolac Tromethamine Entrapped in Stimuli Sensitive Block Copolymer Hydrogels

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 (...

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Detalles Bibliográficos
Autores: Mallandrich Miret, Mireia, Fernández Campos, Francisco, Clares Naveros, Beatriz, Halbaut, Lyda, Alonso, Cristina, Coderch Negra, Ma. Luisa, Garduño Ramírez, María Luisa del Carmen, Andrade Carrera, Berenice, Pozo Carrascosa, Alfonso del, Lane, ME, Calpena Campmany, Ana Cristina
Tipo de recurso: artículo
Estado:Versión aceptada para publicación
Fecha de publicación:2017
País:España
Institución:Universidad de Barcelona
Repositorio:Dipòsit Digital de la UB
OAI Identifier:oai:diposit.ub.edu:2445/128389
Acceso en línea:https://hdl.handle.net/2445/128389
Access Level:acceso abierto
Palabra clave:Farmacologia
Tecnologia farmacèutica
Administració de medicaments
Agents antiinflamatoris
Reologia
Fórmules magistrals
Medicació transdèrmica
Pharmacology
Pharmaceutical technology
Administration of drugs
Antiinflammatory agents
Rheology
Medical formularies
Transdermal medication
Descripción
Sumario: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.

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