The Development and Pre-Clinical Anti-Inflammatory Efficacy of a New Transdermal Ureasil–Polyether Hybrid Matrix Loaded with Flavonoid-Rich Annona muricata Leaf Extract

Author:

Araújo Camila Beatriz Barros1,Alves Júnior José de Oliveira2ORCID,Sato Mariana Rillo1,Costa Kammila Martins Nicolau3,Lima Jéssica Roberta4,Damasceno Bolívar Ponciano Goulart de Lima12,Lima Junior Francisco José Batista de5,Andréo Bruna Galdorfini Chiari4,Santos Vanda Lucia dos12,Oshiro-Junior João Augusto12ORCID

Affiliation:

1. Pharmaceutical Sciences Postgraduate Center for Biological and Health Sciences, Paraiba State University, Av. Juvêncio Arruda, S/N, Campina Grande 58429-600, Brazil

2. Department of Pharmacy, Center for Biological and Health Sciences, Paraiba State University, Av. Juvêncio Arruda, S/N, Campina Grande 58429-500, Brazil

3. Postgraduate Program in Development and Technological Innovation in Medicines, Federal University of Paraíba, Campus I, Lot. Cidade Universitária, S/N, João Pessoa 58051-900, Brazil

4. Department of Pharmacy, University of Araraquara (UNIARA), Rua Carlos Gomes, 1338—Centro Araraquara, São Paulo 14801-340, Brazil

5. Department of Pharmacy, Unifacisa University Center, Rua Manoel Cardoso Palhano, 124-152—Itararé, Campina Grande 58408-326, Brazil

Abstract

This study aimed to develop a novel ureasil–polyether transdermal hybrid matrix (U-PEO) loaded with Annona muricata concentrated extract (AMCE), which exhibits potent anti-inflammatory activity. The extract was obtained by maceration, a method that allowed for the extraction of a high concentration of flavonoids (39.27 mg/g of extract). In vivo tests demonstrated that 10 mg/kg of AMCE inhibited inflammation for 6 h. The physicochemical characterization of U-PEO with AMCE was conducted via a thermogravimetric analysis (TGA), while its surface was recorded using atomic force microscopy (AFM). The in vitro macroscopic swelling and release tests demonstrated the hydrophilic profile of the material and the percentage of AMCE released. The TGA results demonstrated that the system exhibited physical compatibility due to the thermal stability of U-PEO. Additionally, the AFM analysis revealed a rough and porous surface, with a particular emphasis on the system with AMCE. The release resulted in the liberation of 23.72% of AMCE within 24 h. Finally, the preclinical tests demonstrated that U-PEO with AMCE was also capable of effectively inhibiting inflammation for 6 h, a duration comparable to that of a commercial formulation. The results permit the advancement of the study towards the development of a transdermal system, thereby rendering its application in clinical studies feasible.

Funder

Coordenação deAperfeiçoamento de Pessoal de Nível Superior Brazil

National Council for Scientific and Technological Development—Brazil

Paraiba State University

Publisher

MDPI AG

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