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Development and characterization of trans-anethole-containing solid lipid microparticles: antiinflammatory and gastroprotective effects in experimental inflammation.

Edvalkia Magna Teobaldo da RochaLívia BrachtOdinei Hess GonçalvesFernanda Vitória LeimannFranciele Queiroz AmesLarissa Carla Lauer SchneiderJoão Victor DudaGabriel Fernando Esteves CardiaCarla Indianara BonettiRoberto Kenji Nakamura CumanCiomar Aparecida Bersani-Amado
Published in: Naunyn-Schmiedeberg's archives of pharmacology (2022)
The present study prepared, optimized, and characterized solid lipid microparticles that contained trans-anethole (SLMAN), evaluated their antiinflammatory activity in acute and chronic inflammation models, and investigated their effects on the gastric mucosa in arthritic rats. The microparticles were obtained by a hot homogenization process and characterized by physicochemical analyses. The acute inflammatory response was induced by an intradermal injection of 0.1 ml of carrageenan solution (200 μg) in the hind paw. The rats were treated orally with a single dose of SLMAN 1 h before induction of the inflammatory response. The chronic inflammatory response was induced by the subcutaneous application of 0.1 ml of complete Freund's adjuvant suspension (500 µg) in the hind paw. SLMAN was orally administered, starting on the day of arthritis induction, and continued for 21 days. The results showed that SLMAN was obtained with good encapsulation efficiency. Treatment with SLMAN at doses of 25 and 50 mg/kg was as effective as trans-anethole (AN) at a dose of 250 mg/kg on acute and chronic inflammatory responses. Histological analyses showed that treatment with SLMAN did not aggravate lesions in the gastric mucosa in arthritic rats. These results indicated that treatment with SLMAN at a dose that was 5-10 times lower than non-encapsulated AN exerted an inhibitory effect on acute and chronic inflammatory responses, suggesting the better bioavailability and efficacy of microencapsulated AN without aggravating lesions in the gastric mucosa in arthritic rats.
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