Jacob Shery, Nair Anroop B, Shah Jigar
1Department of Pharmaceutical Sciences, College of Pharmacy, Gulf Medical University, Ajman, UAE.
2Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa, Saudi Arabia.
Biomater Res. 2020 Jan 15;24:3. doi: 10.1186/s40824-020-0184-8. eCollection 2020.
Rapid advancement in drug discovery process is leading to a number of potential new drug candidates having excellent drug efficacy but limited aqueous solubility. By virtue of the submicron particle size and distinct physicochemical properties, nanosuspension has the potential ability to tackle many formulation and drug delivery issues typically associated with poorly water and lipid soluble drugs. Conventional size reduction equipment such as media mill and high-pressure homogenizers and formulation approaches such as precipitation, emulsion-solvent evaporation, solvent diffusion and microemulsion techniques can be successfully implemented to prepare and scale-up nanosuspensions. Maintaining the stability in solution as well as in solid state, resuspendability without aggregation are the key factors to be considered for the successful production and scale-up of nanosuspensions. Due to the considerable enhancement of bioavailability, adaptability for surface modification and mucoadhesion for drug targeting have significantly expanded the scope of this novel formulation strategy. The application of nanosuspensions in different drug delivery systems such as oral, ocular, brain, topical, buccal, nasal and transdermal routes are currently undergoing extensive research. Oral drug delivery of nanosuspension with receptor mediated endocytosis has the promising ability to resolve most permeability limited absorption and hepatic first-pass metabolism related issues adversely affecting bioavailability. Advancement of enabling technologies such as nanosuspension can solve many formulation challenges currently faced among protein and peptide-based pharmaceuticals.
药物研发过程的快速发展使得许多潜在的新药候选物具有出色的药效，但水溶性有限。由于亚微米级的粒径和独特的物理化学性质，纳米混悬液有潜力解决许多通常与水溶解性和脂溶性差的药物相关的制剂和药物递送问题。传统的粒度减小设备如介质磨和高压均质机，以及制剂方法如沉淀法、乳液-溶剂蒸发法、溶剂扩散法和微乳技术，都可以成功用于制备和放大纳米混悬液。保持溶液状态以及固态的稳定性、无聚集的再分散性是纳米混悬液成功生产和放大需要考虑的关键因素。由于生物利用度的显著提高、表面修饰的适应性以及用于药物靶向的粘膜粘附性，这种新型制剂策略的应用范围得到了显著扩展。纳米混悬液在不同药物递送系统如口服、眼部、脑部、局部、口腔、鼻腔和透皮途径中的应用目前正在进行广泛研究。通过受体介导的内吞作用进行纳米混悬液的口服药物递送有希望解决大多数影响生物利用度的渗透性受限吸收和肝脏首过代谢相关问题。诸如纳米混悬液等使能技术的进步可以解决目前基于蛋白质和肽的药物所面临的许多制剂挑战。
