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含叶提取物的磷脂复合物的开发与评价:一种啮齿动物模型中肥胖症治疗的临床前研究方法

Development and Evaluation of Phytosomes Containing Leaf Extract: A Preclinical Approach for the Treatment of Obesity in a Rodent Model.

作者信息

Ortega-Pérez Luis Gerardo, Ayala-Ruiz Luis Alberto, Magaña-Rodríguez Oliver Rafid, Piñón-Simental Jonathan Saúl, Aguilera-Méndez Asdrubal, Godínez-Hernández Daniel, Rios-Chavez Patricia

机构信息

Facultad de Biología, Universidad Michoacana de San Nicolás de Hidalgo, Morelia 58000, Michoacán, Mexico.

Instituto de Investigaciones Químico Biológicas, Universidad Michoacana de San Nicolás de Hidalgo, Morelia 58000, Michoacán, Mexico.

出版信息

Pharmaceutics. 2023 Aug 22;15(9):2178. doi: 10.3390/pharmaceutics15092178.

Abstract

has several biological effects; it is anti-inflammatory, anti-obesogenic, antioxidant, hepatoprotection, and chemoprotective. Its bioactive compounds include terpenoids, phenolic acids, and flavonoids which have low oral bioavailability and absorption. This study aimed at developing phytosomes of to improve oral bioavailability and absorption. Phytosomes were formulated with soybean phosphatidylcholine and leaf extract using the thin layer sonication method. Phytosomes were evaluated by scanning electron microscopy (SEM), entrapment efficiency, solubility, and particle size determination. Antioxidant capacity and total phenolic, flavonoid, and terpenoid contents were also measured. The in vivo anti-obesogenic activity was evaluated. Phytosomes loaded with (P ) extract had small spherical shapes. The average particle size was 129.98 ± 18.30 nm, encapsulation efficiency 80.49 ± 0.07%, and solubility 90.00%; the stability study presented no significant changes in the average particle size at 20 °C. P presented high antioxidant capacity. For the first time, ellagic acid is reported in this plant. The in vivo obesity study showed a strong anti-obesogenic activity of phytosomes with to reduce 40% body weight as well as morphometric and biochemical parameters.

摘要

具有多种生物学效应;它具有抗炎、抗肥胖、抗氧化、肝脏保护和化学保护作用。其生物活性化合物包括萜类、酚酸和黄酮类,它们的口服生物利用度和吸收率较低。本研究旨在开发[植物名称]的磷脂复合物以提高口服生物利用度和吸收率。采用薄层超声法用大豆磷脂酰胆碱和[植物名称]叶提取物制备磷脂复合物。通过扫描电子显微镜(SEM)、包封率、溶解度和粒径测定对磷脂复合物进行评估。还测定了抗氧化能力以及总酚、黄酮和萜类含量。评估了体内抗肥胖活性。负载[植物名称](P[具体编号])提取物的磷脂复合物呈小的球形。平均粒径为129.98±18.30nm,包封效率为80.49±0.07%,溶解度为90.00%;稳定性研究表明在20℃下平均粒径无显著变化。P[具体编号]具有较高的抗氧化能力。首次在该植物中报道了鞣花酸。体内肥胖研究表明,含有[植物名称]的磷脂复合物具有很强的抗肥胖活性,可使体重减轻40%以及改善形态学和生化参数。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/69b6/10535757/3497eb5316ca/pharmaceutics-15-02178-g001.jpg

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