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Betulinic Acid Nanogels: Rheological, Microstructural Characterization and Evaluation of their Anti-inflammatory Activity

Author(s):

Dalis Sosa-Gutierrez, Jorge Toro-Vazquez, Cynthia Cano-Sarmiento, Peter Grube-Pagola, Alejandro Aparicio-Saguilan, Cristobal Torres-Palacios, Andres Acosta-Osorio and Hugo Garcia*   Pages 1 - 12 ( 12 )

Abstract:


Background: Betulinic acid (BA) is a lipophilic compound with proven beneficial results in topical inflammation. Nanogels (NG) are carriers of bioactive compounds with properties that make them good candidates to treat skin diseases.

Objective: The objective of this study was to evaluate the anti-inflammatory activity of BA carried in NG.

Methods: NG were composed of a nanoemulsion and a crosslinking agent (Carbopol 940®) applied at three concentrations (0.5, 1, and 1.5 %) and three activation times (6, 12 and 24 h). In order to select the optimal formulation, the NG were characterized mechanically and micro-structurally followed by evaluation of the BA anti-inflammatory activity in an in vivomodel of auricular edema. We determined the edema inhibition activity aspercent weight. Additionally, the anti-inflammatory activity of NG was validated through histological analysis.

Results: The formulation with the best viscoelastic properties was the one prepared with 0.5% carbopol and 6 h of activation. Microstructural examination of this formulation showed mostly spherical structures with a mean diameter of 65 nm. From the evaluation of edema and the histological analyses, we established that the NG of BA produced 52% inhibition. In contrast, a conventional gel and freeBA produced 28% and 19% inhibition, respectively.

Conclusion: The NG of BA showed to be good vehicles to treat skin inflammation.

Keywords:

Nanogel, betulinic acid, inflammation, auricular edema, skin.

Affiliation:

UNIDA, Tecnológico Nacional de México/IT de Veracruz. Miguel Ángel de Quevedo 2779. Veracruz, Ver. 91897, Universidad Autónoma de San Luis Potosí, Facultad de Ciencias Químicas-CIEP, Av. Dr. Manuel Nava 6, Zona Universitaria, San Luis Potosí, SLP 78210, CONACyT-Tecnológico Nacional de México/IT de Veracruz. Miguel Ángel de Quevedo 2779. Veracruz, Ver. 91897, México, Universidad Veracruzana, Instituto de Investigaciones Médico Biológicas, Iturbide s/n, Veracruz, Ver. 91700, Instituto de Biotecnología. Universidad del Pa-paloapan, Avenida Circuito Central # 200, Col. Parque Industrial, Tuxtepec, Oax. 68301, UNIDA, Tecnológico Nacional de México/IT de Veracruz. Miguel Ángel de Quevedo 2779. Veracruz, Ver. 91897, CONACyT-Tecnológico Nacional de México/IT de Veracruz. Miguel Ángel de Quevedo 2779. Veracruz, Ver. 91897, UNIDA, Tecnológico Nacional de México/IT de Veracruz. Miguel Ángel de Quevedo 2779. Veracruz, Ver. 91897



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