Preparation and In Vivo Evaluation of Rosmarinic Acid-Loaded Transethosomes After Percutaneous Application on a Psoriasis Animal Model
| Autor: | M.L. González-Rodríguez, Azahara Rodríguez-Luna, Antonio M. Rabasco, Virginia Motilva, Javier Ávila-Román, Elena Talero, Ana María Fernández Romero |
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| Rok vydání: | 2021 |
| Předmět: |
Antioxidant
Drug Compounding medicine.medical_treatment Pharmaceutical Science Aquatic Science Pharmacology Administration Cutaneous Depsides Dexamethasone Mice chemistry.chemical_compound Drug Delivery Systems In vivo Edema Drug Discovery medicine Caffeic acid Animals Psoriasis Ecology Evolution Behavior and Systematics Drug Carriers Mice Inbred BALB C Ecology Viscosity Chemistry Rosmarinic acid General Medicine In vitro Drug Liberation Cinnamates Female medicine.symptom Nanocarriers Gels Agronomy and Crop Science medicine.drug |
| Zdroj: | AAPS PharmSciTech. 22 |
| ISSN: | 1530-9932 |
| DOI: | 10.1208/s12249-021-01966-3 |
| Popis: | The topical use of rosmarinic acid (RA) in skin inflammatory pathologies is restricted due to its poor water solubility, poor permeability, and chemical instability. In this study, RA-loaded transethosomes-in-Carbopol® formulations have been developed to evaluate its anti-inflammatory activity on imiquimod-induced psoriasis-like skin inflammation in mice. In vitro release profiles demonstrated sustained behavior due to the retentive action of gel and the entrapment of RA into the vesicles. However, the low viscosity of the combined formulation increased the drug release rate. Animal evaluation of anti-inflammatory activity demonstrated that transethosomes-in-gel containing dexamethasone (Dex-TE-Gel), as positive control, showed effect in all the pro-inflammatory parameters evaluated, evidencing that these drug-loaded nanocarriers have been effectively reached the site of action. In addition, transethosomes-in-gel containing RA (RA-TE-Gel) formulations produced a great reduction in the punch edema (P < 0.001) and in TNF-α and IL-6 (P < 0.05). However, non-significant differences were obtained for IL-1β, IL17, and MPO. Despite the protecting effect of Carbopol® and transethosomes on oxidation index and antioxidant activity of RA over the 7 days of treatment, however, a degradation process of this antioxidant to caffeic acid may be the cause of these in vivo results. We have also checked that the pH existing into the intercellular space of damaged cells (pH 6.8) may be affecting. Therefore, our results suggest that RA-TE-Gel could act as an effective RA formulation for skin delivery; further studies will help to understand the loss of activity at the cellular level. |
| Databáze: | OpenAIRE |
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