Mohamad Nur-Vaizura
Centre for Drug and Herbal Development, Faculty of Pharmacy, Universiti Kebangsaan Malaysia, Kuala Lumpur 50300, Malaysia.
Pharmaceuticals (Basel). 2023 Oct 3;16(10):1403. doi: 10.3390/ph16101403.
Tocotrienols have higher medicinal value, with multiple sources of evidence showing their biological properties as antioxidant, anti-inflammatory, and osteoprotective compounds. However, tocotrienol bioavailability presents an ongoing challenge in its translation into viable products. This is because tocotrienol oil is known to be a poorly water-soluble compound, making it difficult to be absorbed into the body and resulting in less effectiveness. With the potential and benefits of tocotrienol, new strategies to increase the bioavailability and efficacy of poorly absorbed tocotrienol are required when administered orally. One of the proposed formulation techniques was self-emulsification, which has proven its capacity to improve oral drug delivery of poorly water-soluble drugs by advancing the solubility and bioavailability of these active compounds. This review discusses the updated evidence on the bioavailability of tocotrienols formulated with self-emulsifying drug delivery systems (SEDDSs) from in vivo and human studies. In short, SEDDSs formulation enhances the solubility and passive permeability of tocotrienol, thus improving its oral bioavailability and biological actions. This increases its medicinal and commercial value. Furthermore, the self-emulsifying formulation presents a useful dosage form that is absorbed in vivo independent of dietary fats with consistent and enhanced levels of tocotrienol isomers. Therefore, a lipid-based formulation technique can provide an additional detailed understanding of the oral bioavailability of tocotrienols.
生育三烯酚具有更高的药用价值，多项证据表明其具有抗氧化、抗炎和骨保护化合物的生物学特性。然而，生育三烯酚的生物利用度在转化为可行产品方面一直是一项挑战。这是因为已知生育三烯酚油是一种水溶性差的化合物，难以被人体吸收，导致效果较差。鉴于生育三烯酚的潜力和益处，口服给药时需要新的策略来提高难吸收的生育三烯酚的生物利用度和疗效。一种提议的制剂技术是自乳化，它已证明有能力通过提高这些活性化合物的溶解度和生物利用度来改善水溶性差的药物的口服给药。这篇综述讨论了来自体内和人体研究的关于用自乳化药物递送系统（SEDDSs）配制的生育三烯酚生物利用度的最新证据。简而言之，SEDDSs制剂提高了生育三烯酚的溶解度和被动通透性，从而改善其口服生物利用度和生物学作用。这增加了其药用和商业价值。此外，自乳化制剂呈现出一种有用的剂型，其在体内的吸收独立于膳食脂肪，且生育三烯酚异构体的水平持续且增强。因此，基于脂质的制剂技术可以提供对生育三烯酚口服生物利用度的额外详细理解。
