Isolation, Purification of Phenolic Glycoside 1 from Moringa oleifera Seeds and Formulation of Its Liposome Delivery System.

IF 3.4 4区 医学 Q2 PHARMACOLOGY & PHARMACY AAPS PharmSciTech Pub Date : 2024-08-22 DOI:10.1208/s12249-024-02911-w
Feng Shi, Mingjie Gong, Michael Adu-Frimpong, Xia Jiang, Xiaowen Wang, Qinyang Hua, Tingyuan Li, Jiaying Li, Jiangnan Yu, Elmurat Toreniyazov, Xia Cao, Qilong Wang, Ximing Xu
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Abstract

In this study, N, N '-bis {4- [(α-L- rhamnosyloxy) benzyl]} thiourea (PG-1), a phenolic glycoside compound was purified from Moringa seed. The PG-1 has attracted extensive attention due to its anti-cancer, antioxidant, anti-inflammatory and hypoglycemic properties. However, some of its physicochemical properties such as oral bioavailability has not been studied. Herein, a highly purified PG-1 was extracted and incorporated in multiple layered liposomes (PG-1-L) to avoid its burst release and enhance oral bioavailability. After appropriate characterization, it was discovered that the obtained PG-1-L was stable, homogeneous and well dispersed with the average particle size being 89.26 ± 0.23 nm. Importantly, the in vitro release and in vivo oral bioavailability of PG-1-L were significantly improved compared with PG-1. In addition, MTT results showed that compared with the free PG-1, PG-1-L displayed obvious inhibitory effect on the HepG2 cells, while the inhibitory effect on healthy non-malignant 3T6 and LO-2 cells was not significant, indicating that PG-1-L had high safety. In conclusion, PG-1-L can be used as a promising delivery system and an ideal novel approach to improve the oral bioavailability and anticancer activity of PG-1.

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从油辣木籽中分离、纯化酚醛苷 1 并配制其脂质体输送系统
本研究从辣木籽中纯化出一种酚苷化合物 N, N '-bis {4- [(α-L- rhamnosyloxy) benzyl]} thiourea (PG-1)。PG-1 因其抗癌、抗氧化、抗炎和降血糖特性而受到广泛关注。然而,它的一些理化特性(如口服生物利用度)尚未得到研究。本文提取了高度纯化的 PG-1,并将其加入多层脂质体(PG-1-L)中,以避免其猝灭释放并提高口服生物利用度。经过适当的表征后发现,获得的 PG-1-L 稳定、均质、分散性好,平均粒径为 89.26 ± 0.23 nm。重要的是,与 PG-1 相比,PG-1-L 的体外释放和体内口服生物利用度都有显著提高。此外,MTT 结果表明,与游离 PG-1 相比,PG-1-L 对 HepG2 细胞有明显的抑制作用,而对健康的非恶性 3T6 和 LO-2 细胞的抑制作用不明显,表明 PG-1-L 具有较高的安全性。总之,PG-1-L 是一种很有前景的给药系统,是提高 PG-1 口服生物利用度和抗癌活性的理想新方法。
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来源期刊
AAPS PharmSciTech
AAPS PharmSciTech 医学-药学
CiteScore
6.80
自引率
3.00%
发文量
264
审稿时长
2.4 months
期刊介绍: AAPS PharmSciTech is a peer-reviewed, online-only journal committed to serving those pharmaceutical scientists and engineers interested in the research, development, and evaluation of pharmaceutical dosage forms and delivery systems, including drugs derived from biotechnology and the manufacturing science pertaining to the commercialization of such dosage forms. Because of its electronic nature, AAPS PharmSciTech aspires to utilize evolving electronic technology to enable faster and diverse mechanisms of information delivery to its readership. Submission of uninvited expert reviews and research articles are welcomed.
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