Mireia Mallandrich1,2, Francisco Fernández-Campos1, Beatriz Clares3,4, Lyda Halbaut1,2, Cristina Alonso5, Luisa Coderch5, Maria L Garduño-Ramírez6, Berenice Andrade6, Alfonso Del Pozo1, Majella E Lane7, Ana C Calpena1,2. 1. Department of Pharmacy, Pharmaceutical Technology and Physical Chemistry, School of Pharmacy and Food Sciences, University of Barcelona, 27-31 Joan XXIII Av,, 08028, Barcelona,, Spain. 2. Nanoscience and Nanotechnology Institute (IN2UB), University of Barcelona, 27-31 Joan XXIII Av, 08028, Barcelona, Spain. 3. Nanoscience and Nanotechnology Institute (IN2UB), University of Barcelona, 27-31 Joan XXIII Av, 08028, Barcelona, Spain. beatrizclares@ugr.es. 4. Department of Pharmacy and Pharmaceutical Technology, School of Pharmacy, University of Granada, Campus of Cartuja s/n,, 18071, Granada,, Spain. beatrizclares@ugr.es. 5. Institute of Advanced Chemistry of Catalonia, 18-26 Jordi Girona St, 08034, Barcelona, Spain. 6. Centro de Investigaciones Químicas, Universidad Autónoma del Estado de Morelos, Avenida Universidad 1001,, 62209, Cuernavaca, Morelos, Mexico. 7. Department of Pharmaceutics, UCL School of Pharmacy, 29-39 Brunswick Square,, London,, WC1N 1AX, UK.
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.
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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