Buya Aristote B, Beloqui Ana, Memvanga Patrick B, Préat Véronique
Advanced Drug Delivery and Biomaterials, Louvain Drug Research Institute, Université Catholique de Louvain, Avenue Mounier 73, B1.73.12, 1200 Brussels, Belgium.
Pharmaceutics and Phytopharmaceutical Drug Development Research Group, Faculty of Pharmaceutical Sciences, University of Kinshasa, Kinshasa XI BP 212, Democratic Republic of the Congo.
Pharmaceutics. 2020 Dec 9;12(12):1194. doi: 10.3390/pharmaceutics12121194.
Approximately one third of newly discovered drug molecules show insufficient water solubility and therefore low oral bio-availability. Self-nano-emulsifying drug-delivery systems (SNEDDSs) are one of the emerging strategies developed to tackle the issues associated with their oral delivery. SNEDDSs are composed of an oil phase, surfactant, and cosurfactant or cosolvent. SNEDDSs characteristics, their ability to dissolve a drug, and in vivo considerations are determinant factors in the choice of SNEDDSs excipients. A SNEDDS formulation can be optimized through phase diagram approach or statistical design of experiments. The characterization of SNEDDSs includes multiple orthogonal methods required to fully control SNEDDS manufacture, stability, and biological fate. Encapsulating a drug in SNEDDSs can lead to increased solubilization, stability in the gastro-intestinal tract, and absorption, resulting in enhanced bio-availability. The transformation of liquid SNEDDSs into solid dosage forms has been shown to increase the stability and patient compliance. Supersaturated, mucus-permeating, and targeted SNEDDSs can be developed to increase efficacy and patient compliance. Self-emulsification approach has been successful in oral drug delivery. The present review gives an insight of SNEDDSs for the oral administration of both lipophilic and hydrophilic compounds from the experimental bench to marketed products.
大约三分之一新发现的药物分子表现出不足的水溶性，因此口服生物利用度较低。自纳米乳化药物递送系统（SNEDDSs）是为解决与其口服给药相关的问题而开发的新兴策略之一。SNEDDSs由油相、表面活性剂和助表面活性剂或助溶剂组成。SNEDDSs的特性、溶解药物的能力以及体内因素是选择SNEDDSs辅料的决定性因素。SNEDDS制剂可通过相图法或实验统计设计进行优化。SNEDDSs的表征包括全面控制SNEDDS制造、稳定性和生物学命运所需的多种正交方法。将药物封装在SNEDDSs中可导致溶解度增加、胃肠道稳定性提高以及吸收增加，从而提高生物利用度。已证明将液体SNEDDSs转化为固体剂型可提高稳定性和患者顺应性。可以开发过饱和、黏液渗透和靶向的SNEDDSs以提高疗效和患者顺应性。自乳化方法在口服药物递送中已取得成功。本综述深入介绍了从实验台到市售产品的用于口服亲脂性和亲水性化合物的SNEDDSs。
