固体自乳化药物传递系统:用于口服传递疏水性载药的优越方式。
Solid self emulsifying drug delivery system: Superior mode for oral delivery of hydrophobic cargos.
机构信息
Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad, Telangana, India.
Department of Biological Sciences, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad, Telangana, India.
出版信息
J Control Release. 2021 Sep 10;337:646-660. doi: 10.1016/j.jconrel.2021.08.013. Epub 2021 Aug 10.
A significant proportion of recently approved drug molecules possess poor aqueous solubility which further restrains their desired bioavailability. Poor aqueous solubility of these drugs poses significant hurdles in development of novel drug delivery systems and achieving target response. Self-emulsifying drug delivery systems (SEDDS) emerged as an insightful approach for delivering highly hydrophobic entities to enhance their bioavailability. Conventional SEDDS were developed in a liquid form which owned numerous shortcomings like low stability and drug loading efficiency, fewer choices of dosage forms and irreversible precipitation of drug or excipients. To address these curbs solid-SEDDS (S-SEDDS) was introduced as an efficient strategy that combined advantages of solid dosage forms such as increased stability, portability and patient compliance along with substantial improvement in the bioavailability. S-SEDDS are isotropic mixtures of oil, surfactant, solvent and co-solvents generated by solidification of liquid or semisolid self-emulsifying ingredients onto powders. The present review highlights components of S-SEDDS, their peculiarities to be considered while designing solid dosage forms and various methods of fabrication. Lastly, key challenges faced during development, applications and future directions for the research in this area are thoroughly summarized.
相当一部分最近批准的药物分子具有较差的水溶性,这进一步限制了它们的预期生物利用度。这些药物的水溶性差给新型药物输送系统的开发和实现目标反应带来了重大障碍。自乳化药物输送系统 (SEDDS) 的出现为提高疏水性药物的生物利用度提供了一种有见地的方法。传统的 SEDDS 以液体形式开发,存在许多缺点,如低稳定性和载药效率、较少的剂型选择以及药物或赋形剂的不可逆沉淀。为了解决这些限制,固体 SEDDS(S-SEDDS)被引入作为一种有效的策略,它结合了固体剂型的优点,如增加了稳定性、便携性和患者依从性,同时大大提高了生物利用度。S-SEDDS 是油、表面活性剂、溶剂和共溶剂的各向同性混合物,通过将液体或半固体自乳化成分固化到粉末上而产生。本综述重点介绍了 S-SEDDS 的组成部分、在设计固体剂型时需要考虑的特点以及各种制造方法。最后,彻底总结了在该领域研究的开发、应用和未来方向所面临的关键挑战。