Cyclodextrin/Adamantane-Grafted Polyethylene Glycol–Based Self-assembling Constructs for Topical Delivery of Ketorolac Tromethamine: Formulation, Characterization, and In Vivo Studies

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R.S.R. Murthy

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2021 ◽  
Vol 13 (11) ◽  
pp. 1784
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Salima El Moussaoui ◽  
Ismael Abo-Horan ◽  
Lyda Halbaut ◽  
Cristina Alonso ◽  
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...  

This study describes the preparation and evaluation of two formulations, a hydrogel and a nanostructured system, containing ketorolac tromethamine as an anti-inflammatory agent for the local therapy against the inflammatory process derived from the surgical excision of Condyloma acuminata. Both formulations were physicochemically characterized.In vitrorelease profiles show that the nanoparticles release 92%±2.3 of the total ketorolac tromethamine encapsulated, while the chitosan gel releases 18.6%±0.2. Theex vivo permeation and distribution through human skin were also assayed and was observed how the main amount of ketorolac tromethamine is retained in the epidermis. In vivo studies were accomplished to evaluate the anti-inflammatory efficacy in mice which also involved the histological analysis to confirm thein vivoresults. The nanoparticles present a significantly higher anti-inflammatory efficacy than chitosan gel. The tolerability of developedformulations was assessed by monitoring the biomechanical properties of the skin before and after application of both formulations. No statistical differences in trans-epidermal water loss and skin hydration with respect to the basal values were observed and the formulations exhibited higher anti-inflammatory activity compared to a reference ketotorlac tromethamine solution. Therefore, it can be concluded that both formulations can be proposed as outstanding candidates for offering a local anti-inflammatory therapeutical toolwith potential clinical application.


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