Kolluru Lakshmi Prasanna, Atre Prachi, Rizvi Syed A A
Vaccine Nanotechnology Laboratory, College of Pharmacy, Mercer University, 3001 Mercer University Drive, Atlanta, GA 30341, USA.
Capstone Development Services, Rosemont, IL 60018, USA.
Pharmaceuticals (Basel). 2021 Jan 29;14(2):108. doi: 10.3390/ph14020108.
Preparing a suitable formulation for parenteral administration is already a difficult task; this, coupled with poor water-soluble new chemical entity (NCE), complicates this situation even further. There are several methodologies available to enhance water solubility, but this alone does not entail successful formulation. Making a micro/nano emulsion with a suitable surfactant not only increases the drug solubility but also the cell membrane permeability. Thus, not only biopharmaceutic classification system (BCS)-II (low solubility compounds) but also BCS-III (low permeability) and BCS-IV drugs (low solubility and low permeability) can be further exploited. Those drug candidates otherwise will not move further in NCE evaluation or clinical trials. This succinct review article delves into various aspects of biphasic micro/nano emulsion systems for parenteral drug delivery including the structure of the biphasic colloidal systems, characterization parameters, stability issues, regulatory considerations, and applications in life sciences.
制备适合肠胃外给药的制剂已然是一项艰巨的任务;再加上新化学实体(NCE)水溶性差,使得这种情况更加复杂。有几种方法可用于提高水溶性,但仅靠这一点并不意味着能成功制成制剂。用合适的表面活性剂制备微/纳米乳剂不仅能提高药物溶解度,还能提高细胞膜通透性。因此,不仅生物药剂学分类系统(BCS)中的II类药物(低溶解度化合物),而且III类药物(低通透性)和IV类药物(低溶解度和低通透性)都能得到进一步开发利用。否则,那些候选药物在新化学实体评估或临床试验中就无法取得进一步进展。这篇简洁的综述文章深入探讨了用于肠胃外给药的双相微/纳米乳剂系统的各个方面,包括双相胶体系统的结构、表征参数、稳定性问题、监管考量以及在生命科学中的应用。