Self-microemulsifying system of an ethanolic extract of Heliopsis longipes root for enhanced solubility and release of affinin

AAPS Open

Research

Miriam Estévez¹  Carlos T. Quirino-Barreda²  Alejandra Rojas-Molina³  Francisco J. Luna-Vázquez³  César Ibarra-Alvarado³  Eremy Miranda Ledesma⁴  Dailenys Marrero-Morfa⁴ 

[1] Centro de Física Aplicada y Tecnología Avanzada (CFATA), Universidad Nacional Autónoma de México (UNAM), Blvd. Juriquilla 3000, 76230, Querétaro, México;División de Ciencias Biológicas y de La Salud, Departamento de Sistemas Biológicos, Unidad Xochimilco, Universidad Autónoma Metropolitana, Ciudad de México, México;Laboratorio de Investigación Química y Farmacológica de Productos Naturales, Facultad de Química, Universidad Autónoma de Querétaro, Centro Universitario, 76010, Querétaro, México;Posgrado en Ciencias Químico Biológicas, Facultad de Química, Universidad Autónoma de Querétaro, Cerro de Las Campanas S/N, 76010, Querétaro, México;

关键词: Self-microemulsifying drug delivery systems (SMEDDS);    Heliopsis longipes;    Affinin;    Spilanthol;    Herbal medicines;   

DOI  :  10.1186/s41120-023-00086-5

 received in 2023-06-20, accepted in 2023-09-22,  发布年份 2023

来源: Springer

【 摘 要 】

Self-microemulsifying or self-nanoemulsifying drug delivery systems (SMEDDS/SNEDDS) are well known to improve the dissolution and increase the oral bioavailability of hydrophobic drugs, including herbal extracts. Organic extracts of Heliopsis longipes root and affinin, its main component, induce a vasodilator effect; however, they are poorly water soluble and therefore are difficult to administer and dose by the oral route. This research aimed to develop, through pseudo-ternary phase diagrams, a self-microemulsifying system prepared from an ethanolic extract of H. longipes root (HL-SMDS). In addition, the optimized lipid-based formulation was characterized and its in vitro gastrointestinal simulated dissolution was determined. The formulation composed of Transcutol, 55% (solubilizer); Tween80/PG, 10% (surfactant/co-solvent); Labrasol, 35% (surfactant); and the herbal extract was selected as optimal and identified as a SMEDDS, since when coming into contact with water, it forms a micro-emulsion with droplet sizes less than 100 nm. The stability tests showed that HL-SMDS remained stable over time under extreme conditions. Furthermore, the amount of affinin released from HL-SMDS at pH 1 and 6.8 was higher than that of the ethanolic extract from H. longipes root. These results indicate that HL-SMDS is a novel alternative to improve the aqueous solubility and therefore the oral bioavailability of the ethanolic extract of H. longipes root.

【 授权许可】

CC BY   
© American Association of Pharmaceuticals Scientists 2023

【 图 表 】

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