Design and Characterization of Lipid-Surfactant-Based Systems for Enhancing Topical Anti-Inflammatory Activity of Ursolic Acid

Author(s)

Fonseca-Santos, Bruno ; Araujo, Giovanna Angeli ; Ferreira, Paula Scanavez ; Victorelli, Francesca Damiani ; Pironi, Andressa Maria ; Araujo, Victor Hugo Sousa ; Carvalho, Suzana Goncalves ; Chorilli, Marlus

• Document type: Journal article
• Source: PHARMACEUTICS; v. 15, n. 2, p. 14-pg., 2023-02-01.

Abstract

Skin inflammation is a symptom of many skin diseases, such as eczema, psoriasis, and dermatitis, which cause rashes, redness, heat, or blistering. The use of natural products with anti-inflammatory properties has gained importance in treating these symptoms. Ursolic acid (UA), a promising natural compound that is used to treat skin diseases, exhibits low aqueous solubility, resulting in poor absorption and low bioavailability. Designing topical formulations focuses on providing adequate delivery via application to the skin surface. The aim of this study was to formulate and characterize lipid-surfactant-based systems for the delivery of UA. Microemulsions and liquid crystalline systems (LCs) were characterized by polarized light microscopy (PLM), rheology techniques, and textural and bioadhesive assays. PLM supported the self-assembly of these systems and elucidated their formation. Rheologic examination revealed pseudoplastic and thixotropic behavior appropriate, and assays confirmed the ability of these formulations to adhere to the skin. In vivo studies were performed, and inflammation induced by croton oil was assessed for response to microemulsions and LCs. UA anti-inflammatory activities of similar to 60% and 50% were demonstrated by two microemulsions and 40% and 35% by two LCs, respectively. These data support the continued development of colloidal systems to deliver UA to ameliorate skin inflammation. (AU)

• FAPESP's process: 17/10016-2 - Liquid crystal precursor systems as a strategy for vaginal administration of CTT1 peptide: pharmacotechnical development and potential application for the treatment of cervical cancer
• Grantee: Marlus Chorilli
• Support Opportunities: Regular Research Grants
• FAPESP's process: 17/22928-6 - Liquid-crystalline systems as a potential strategy for vaginal administration of p-coumaric acid in the treatment of vulvovaginal candidiasis
• Grantee: Paula Scanavez Ferreira
• Support Opportunities: Scholarships in Brazil - Master
• FAPESP's process: 17/23357-2 - Potential evaluation of liquid crystal precursors systems for vaginal administration of curcumin in the cervical cancer treatment
• Grantee: Francesca Damiani Victorelli
• Support Opportunities: Scholarships in Brazil - Master
• FAPESP's process: 19/10761-5 - Multifunctional systems for the specific colonoscopy of bevacizumab for the treatment of Colorectal Cancer
• Grantee: Suzana Gonçalves Carvalho
• Support Opportunities: Scholarships in Brazil - Doctorate
• FAPESP's process: 15/05394-2 - Evaluating the potential of nanostructured surfactant-based systems to intranasal administration of trans-resveratrol in the optimization of Alzheimer's disease therapy
• Grantee: Bruno da Fonseca dos Santos
• Support Opportunities: Scholarships in Brazil - Doctorate
• FAPESP's process: 16/22544-0 - Solid dispersions of ursolic acid incorporated in hydrogels to topical administration: development, characterization and in vitro and in vivo biological evaluation
• Grantee: Andressa Maria Pironi
• Support Opportunities: Scholarships in Brazil - Master