Micropartículas poliméricas biodegradáveis contendo ácido cafeico para aplicação tópica

Author(s)

Caroline Magnani Spagnol

• Document type: Doctoral Thesis
• Press: Araraquara. 2018-09-27.
• Institution: Universidade Estadual Paulista (Unesp). Faculdade de Ciências Farmacêuticas. Araraquara
• Defense date: 2018-07-27
• Advisor: Marcos Antonio Corrêa; Herida Regina Nunes Salgado

Abstract

Phenolic compounds occur universally in the plant kingdom, with cinnamic acids being part of this group of organic compounds. Caffeic acid (CA) is one representative, with potent antioxidant action, preventing the premature aging of the skin. The classic emulsions are widely used by the consumer for the pleasant and refreshing sensory they provide, however, preparations developed in the form of dry film present themselves as a technological alternative for their ease and safety in transportation. To overcome the cutaneous barrier, micro and nanostructured systems have been developed to facilitate the delivery of substances by making them available to the tissue for an extended period of time, without causing damage or toxicity. The objective of this work was the exploratory evaluation of the antioxidant and antimicrobial activities of CA in order to use it as a multifunctional active carried in microparticles (MP) of chitosan. Thus, the chitosan microparticles containing CA were obtained by spray drying and physico-chemically characterized, and then they were incorporated into an emulsion and a cosmetic preparation on film. The antimicrobial and antioxidant activity of caffeic acid was determined and the profile of the release, permeation and in vitro retention of the microparticles of CA from the emulsion and the film were evaluated. The antioxidant activity values of CA were similar to the standards in all tests. In addition, CA showed higher antioxidant activity than ascorbic acid and trolox, and has the advantage of being more stable than ascorbic acid and extracted from natural sources when compared to trolox. The present study showed that caffeic acid has antimicrobial activity against S. aureus, S. epidermidis, E. coli, P. aeruginosa and P. acnes with concentrations varying from 375 to 1500 μg/ mL, being a promising compound for its multifunctionality. in addition to meeting the growing demand for substances that replace or reduce the concentrations of classical antimicrobials. The development of the emulsion and cosmetic preparation on film has shown that this is a crucial step in the execution of a project, since choosing the raw materials in a non-judgmental manner can compromise the entire planning of the research. Thus, it was possible to obtain formulations compatible with the microparticles under study and that had the most suitable sensorial aspect and physicochemical characteristics. The results showed that spray drying is an efficient method to obtain MP of chitosan containing CA, producing microstructures of 1 to 5 μm in diameter. The MPII originated from aqueous solution proved to be spherical and with smooth surface, suitable for controlled release, whereas those from hydroalcoholic solution (MPI) had become porous with waste material not internalized. This result was consistent with the release and permeation profile since the MPII showed slower and more controlled release and permeation than those obtained from MPI. The results were promising in relation to the development of formulations containing AC as a multifunctional active in microparticles (MP) of chitosan for facial application. (AU)

• FAPESP's process: 15/02619-3 - Biodegradable polymeric microparticles containing caffeic acid for dermal application
• Grantee: Caroline Magnani Spagnol
• Support Opportunities: Scholarships in Brazil - Doctorate