(-)-linalool-Loaded Polymeric Nanocapsules Are a Potential Candidate to Fibromyalgia Treatment.

Abstract

Fibromyalgia (FM) is a chronic disease that has as main characteristic generalized musculoskeletal pain, which can cause physical and emotional problems to patients. However, pharmacological therapies show side effects that hamper the adhesion to treatment. Given this, (-)-linalool (LIN), a monoterpene with several therapeutic properties already reported in scientific literature as anti-depressive, antinociceptive, anti-inflammatory, and antihyperalgesic also demonstrated therapeutic potential in the treatment of FM. Nevertheless, physicochemical limitations as high volatilization and poor water-solubility make its use difficult. In this perspective, this present research had performed the incorporation of LIN into polymeric nanocapsules (LIN-NC). Size, morphology, encapsulation efficiency, cytotoxicity, and drug release were performed. The antihyperalgesic effect of LIN-NC was evaluated by a chronic non-inflammatory muscle pain model. The results demonstrated that the polymeric nanocapsules showed particle size of 199.1 ± 0.7 nm with a PDI measurement of 0.13 ± 0.01. The drug content and encapsulation efficiency were 13.78 ± 0.05 mg/mL and 80.98 ± 0.003%, respectively. The formulation did not show cytotoxicity on J774 macrophages. The oral treatment with LIN-NC and free-LIN increased the mechanical withdrawal threshold on all days of treatment in comparison with the control group. In conclusion, LIN-NC is a promising proposal in the development of phytotherapy-based nanoformulations for future clinical applications.

• Authors: Tatianny de Araujo Andrade, Paula Dos Passos Menezes, Yasmim Maria Barbosa Gomes de Carvalho, Bruno Dos Santos Lima, Eloísa Portugal Barros Silva Soares de Souza, Adriano Antunes de Souza Araujo, Marlange Almeida Oliveira Melo, Lucindo José Quintans-Júnior, Jullyana de Souza Siqueira Quintans, Sílvia Stanisçuaski Guterres, Adriana Raffin Pohlmann, Saravanan Shanmugam, Luiza Abrahão Frank, Mairim Russo Serafini
• Journal: AAPS PharmSciTech (AAPS PharmSciTech) Vol. 21 Issue 5 Pg. 184 (Jul 06 2020) ISSN: 1530-9932 [Electronic] United States
• PMID: 32632735 (Publication Type: Journal Article)

Chemical References

• Acyclic Monoterpenes
• Anti-Inflammatory Agents
• Nanocapsules
• Polymers
• linalool

Topics

• Acyclic Monoterpenes (administration & dosage, pharmacokinetics, therapeutic use)
• Animals
• Anti-Inflammatory Agents (administration & dosage, pharmacokinetics)
• Drug Liberation
• Fibromyalgia (drug therapy)
• Humans
• Nanocapsules
• Particle Size
• Polymers (administration & dosage)
• Solubility