Nanoemulsion Improves the Anti-Inflammatory Effect of Intraperitoneal and Oral Administration of Carvacryl Acetate

Author:

Souza Rafael Limongi de1,Opretzka Luíza Carolina França2ORCID,Morais Mayara Castro de3ORCID,Melo Camila de Oliveira1,Oliveira Brunna Emanuelly Guedes de1,Sousa Damião Pergentino de3ORCID,Villarreal Cristiane Flora2ORCID,Oliveira Elquio Eleamen1ORCID

Affiliation:

1. Laboratory of Synthesis and Drug Delivery, State University of Paraíba, Rua Horácio Trajano, SN, João Pessoa 58071-160, PB, Brazil

2. Laboratório de Farmacologia e Terapêutica Experimental, Faculdade de Farmácia, Universidade Federal da Bahia, Rua Barão de Jeremoabo, 147, Ondina, Salvador 40170-115, BA, Brazil

3. Department of Pharmaceutical Sciences, Federal University of Paraíba, João Pessoa 58051-970, PB, Brazil

Abstract

Carvacryl acetate (CA) is a monoterpene obtained from carvacrol, which exhibits anti-inflammatory activity. However, its low solubility in aqueous media limits its application and bioavailability. Herein, we aimed to develop a carvacryl acetate nanoemulsion (CANE) and assess its anti-inflammatory potential in preclinical trials. The optimized nanoemulsion was produced by ultrasound, and stability parameters were characterized for 90 days using dynamic light scattering after hydrophilic–lipophilic balance (HLB) assessment. To evaluate anti-inflammatory activity, a complete Freund’s adjuvant-induced inflammation model was established. Paw edema was measured, and local interleukin (IL)-1β levels were quantified using ELISA. Toxicity was assessed based on behavioral changes and biochemical assays. The optimized nanoemulsion contained 3% CA, 9% surfactants (HLB 9), and 88% water and exhibited good stability over 90 days, with no signs of toxicity. The release study revealed that CANE followed zero-order kinetics. Dose–response curves for CA were generated for intraperitoneal and oral administration, demonstrating anti-inflammatory effects by both routes; however, efficacy was lower when administered orally. Furthermore, CANE showed improved anti-inflammatory activity when compared with free oil, particularly when administered orally. Moreover, daily treatment with CANE did not induce behavioral or biochemical alterations. Overall, these findings indicate that nanoemulsification can enhance the anti-inflammatory properties of CA by oral administration.

Funder

National Council for Research and Development of Brazil

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior

State University of Paraiba

Publisher

MDPI AG

Subject

Drug Discovery,Pharmaceutical Science,Molecular Medicine

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