Lee You Zhuan, Seow Eng Kwong, Lim Sheau Chin, Yuen Kah Hay, Abdul Karim Khan Nurzalina
School of Pharmaceutical Sciences, Universiti Sains Malaysia, George Town 11800, Penang, Malaysia.
Pharmaceutics. 2021 Oct 25;13(11):1777. doi: 10.3390/pharmaceutics13111777.
Self-emulsifying drug delivery systems (SEDDS) can improve the oral bioavailability of poorly water-soluble drugs. Solid self-emulsifying drug delivery systems (s-SEDDS) offer several advantages including improved drug stability, ease of administration, and production. Most compounds employed in developing s-SEDDS are solid in nature, with a high amount of surfactants added. The aim of this study was to develop an s-SEDDS using a tocotrienol-rich fraction (TRF) as the model liquid active substance via a simple adsorption method. The solid formulation was developed using magnesium aluminosilicate as the carrier with 70% TRF and 30% surfactants (poloxamer and Labrasol). The formulation showed good self-emulsification efficiency with stable emulsion formed, excellent powder flowability, and small emulsion droplet size of 210-277 nm. The s-SEDDS with combined surfactants (poloxamer and Labrasol) showed a faster absorption rate compared to preparations with only a single surfactant and enhanced oral bioavailability (3.4-3.8 times higher) compared to the non-self-emulsifying oily preparation when administered at a fasted state in rats. In conclusion, an s-SEDDS containing a high amount of TRF was successfully developed. It may serve as a useful alternative to a liquid product with enhanced oral bioavailability and the added advantage of being a solid dosage form.
自乳化药物递送系统(SEDDS)可以提高难溶性药物的口服生物利用度。固体自乳化药物递送系统(s-SEDDS)具有多种优势,包括提高药物稳定性、易于给药和生产。大多数用于开发s-SEDDS的化合物本质上是固体,需要添加大量表面活性剂。本研究的目的是通过一种简单的吸附方法,以富含生育三烯酚的组分(TRF)作为模型液体活性物质来开发一种s-SEDDS。使用硅铝酸镁作为载体,70%的TRF和30%的表面活性剂(泊洛沙姆和Labrasol)来制备固体剂型。该制剂表现出良好的自乳化效率,形成的乳液稳定,具有优异的粉末流动性,乳液滴粒径小,为210 - 277 nm。与仅含有单一表面活性剂的制剂相比,含有复合表面活性剂(泊洛沙姆和Labrasol)的s-SEDDS在大鼠禁食状态下给药时,吸收速率更快,与非自乳化油性制剂相比,口服生物利用度提高(高3.4 - 3.8倍)。总之,成功开发了一种含有大量TRF的s-SEDDS。它可能是液体产品的一种有用替代物,具有提高的口服生物利用度以及作为固体剂型的额外优势。