Drug Delivery, Disposition and Dynamics, Monash Institute of Pharmaceutical Sciences, Monash University (Parkville Campus), Parkville, Victoria 3052, Australia.
Gattefossé SAS, 36 Chemin de Genas, 69804 Saint-Priest, France.; Lonza Pharma & Biotech, Parc d'Innovation, Rue Tobias Stimmer - BP 30442, 67412 Illkirch Graffenstaden, France.
Adv Drug Deliv Rev. 2019 Mar 1;142:16-34. doi: 10.1016/j.addr.2019.01.008. Epub 2019 Jan 21.
Self-dispersing lipid-based formulations, particularly self-microemulsifying drug delivery systems (SMEDDS) have gained an increased interest in recent times as a means to enhance the oral bioavailability of poorly water-soluble lipophilic drugs. Upon dilution, SMEDDS self-emulsify in an aqueous fluid and usually form a kinetically stable oil-in-water emulsion or in some rare cases a true thermodynamically stable microemulsion. The digestion of the formulation leads to the production of amphiphilic digestion products that interact with endogenous amphiphilic components and form self-assembled colloidal phases in the aqueous environment of the intestine. The formed colloidal phases play a pivotal role in maintaining the lipophilic drug in the solubilised state during gastrointestinal transit prior to absorption. Thus, this review describes the structural characterisation techniques employed for SMEDDS and the recent literature studies that elucidated the colloidal aspects during dispersion and digestion of SMEDDS and solid SMEDDS. Possible future studies are proposed to gain better understanding on the colloidal aspects of SMEDDS and solid SMEDDS.
自分散型脂质体制剂,特别是自微乳药物传递系统(SMEDDS),作为提高脂溶性差的亲水性药物口服生物利用度的手段,近年来受到了越来越多的关注。SMEDDS 在稀释时会在水性流体中自乳化,通常形成动力学稳定的油包水型乳剂,在某些罕见情况下形成真正的热力学稳定的微乳剂。制剂的消化会产生两亲性消化产物,这些产物与内源性两亲性成分相互作用,并在肠内的水性环境中形成自组装胶体相。形成的胶体相在胃肠道转运过程中吸收前对维持脂溶性药物的溶解状态起着关键作用。因此,本综述描述了用于 SMEDDS 的结构特征化技术,以及近期阐明了 SMEDDS 分散和消化过程中胶体方面的文献研究。提出了可能的未来研究,以更好地了解 SMEDDS 和固态 SMEDDS 的胶体方面。