Nanoemulsions of betulinic acid stabilized with modified phosphatidylcholine increase the stability of the nanosystems and the drug's bioavailability.

Autor: Bravo-Alfaro DA; Tecnologico de Monterrey, Institute of Advanced Materials for Sustainable Manufacturing, Epigmenio González 500 Fracc., Qro., San Pablo, Querétaro 76130, Mexico., Ochoa-Rodríguez LR; Centro de Investigación y de Estudios Avanzados del Instituto Politécnico Nacional, Libramiento Norponiente 2000, Fracc. Real de Juriquilla, Santiago de Querétaro, Qro, 76230, Mexico., Prokhorov Y; Centro de Investigación y de Estudios Avanzados del Instituto Politécnico Nacional, Libramiento Norponiente 2000, Fracc. Real de Juriquilla, Santiago de Querétaro, Qro, 76230, Mexico., Pérez-Robles JF; Centro de Investigación y de Estudios Avanzados del Instituto Politécnico Nacional, Libramiento Norponiente 2000, Fracc. Real de Juriquilla, Santiago de Querétaro, Qro, 76230, Mexico., Sampieri-Moran JM; Unidad de Investigación y Desarrollo de Alimentos, Tecnológico Nacional de México/IT de Veracruz, M.A. de Quevedo 2779, col. Formando Hogar, Veracruz, Ver, 91897, Mexico., García-Casillas PE; Centro de Investigación en Química Aplicada, Enrique Reyna H. 140, San José de los Cerritos, Coahuila 25294, Mexico., Paul S; Tecnologico de Monterrey, School of Engineering and Sciences, Campus Queretaro, Av. Epigmenio Gonzalez, No. 500 Fracc., San Pablo, Querétaro CP 76130, Mexico., García HS; Unidad de Investigación y Desarrollo de Alimentos, Tecnológico Nacional de México/IT de Veracruz, M.A. de Quevedo 2779, col. Formando Hogar, Veracruz, Ver, 91897, Mexico. Electronic address: hugo.gg@veracruz.tecnm.mx., Luna-Bárcenas G; Tecnologico de Monterrey, Institute of Advanced Materials for Sustainable Manufacturing, Epigmenio González 500 Fracc., Qro., San Pablo, Querétaro 76130, Mexico. Electronic address: gabriel.luna@tec.mx.
Jazyk: angličtina
Zdroj: Colloids and surfaces. B, Biointerfaces [Colloids Surf B Biointerfaces] 2024 Oct 02; Vol. 245, pp. 114291. Date of Electronic Publication: 2024 Oct 02.
DOI: 10.1016/j.colsurfb.2024.114291
Abstrakt: Betulinic acid (BA) is a natural compound with significant potential for treating various diseases, including cancer and AIDS, and possesses additional anti-inflammatory and antibacterial properties. However, its clinical application is limited because of its low solubility in water, which impairs its distribution within the body. To overcome this challenge, nanoemulsions have been developed to improve the bioavailability of such poorly soluble drugs. This study investigated modified phosphatidylcholine (PC), where some fatty acids were replaced with conjugated linoleic acid (CLA) to stabilize BA nanoemulsions. The modified PC was used to prepare nanoemulsions with droplet sizes of up to 45 nanometers. These nanoemulsions maintained stability for 60 days at room temperature (25°C±2°C) and under refrigeration (5°C±1°C), with no signs of instability. Nanoemulsions stabilized with CLA-modified PC achieved a higher drug encapsulation rate (93.5±4.3 %) than those using natural PC (82.8±4.2 %). In an in vivo model, both nanoemulsion formulations significantly increased BA absorption, with CLA-modified PC enhancing absorption by 21.3±1.3 times and natural PC by 20±2.3 times compared to the free drug. This suggests that nanoemulsions with modified PC could improve the stability and efficacy of BA in clinical applications.
Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.
(Copyright © 2024 Elsevier B.V. All rights reserved.)
Databáze: MEDLINE
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