Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Galala University, Suez, Egypt.
Department of Pharmaceutics, Faculty of Pharmacy, Zagazig University, Zagazig, 44519, Egypt.
Curr Pharm Des. 2023;29(29):2297-2312. doi: 10.2174/1381612829666230911105922.
The poor water solubility of numerous novel drug candidates presents significant challenges, particularly in terms of oral administration. This limitation can result in various undesirable clinical implications, such as inter-patient variability, poor bioavailability, difficulties in achieving a safe therapeutic index, increased costs, and potential risks of toxicity or inefficacy. Biopharmaceutics Classification System (BCS) class II drugs face particular hurdles due to their limited solubility in the aqueous media of the gastrointestinal tract. In such cases, parenteral administration is often employed as an alternative strategy. To address these challenges, nanosuspension techniques offer a promising solution for enhancing drug solubility and overcoming oral delivery obstacles. This technique has the potential to bridge the gap between drug discovery and preclinical use by resolving problematic solubility. This literature review has delved into contemporary nanosuspension preparation technologies and the incorporation of stabilizing ingredients within the formulation. Furthermore, the manuscript explores nanosuspension strategies for both oral and parenteral/other delivery routes, and separate discussions have been presented to establish a suitable flow that addresses the challenges and strategies relevant to each administration method.
众多新型候选药物的水溶性差，给药物研发带来了巨大挑战，尤其是口服剂型。这种局限性可能导致各种不理想的临床后果，如个体间变异性、生物利用度差、难以达到安全治疗指数、成本增加以及毒性或无效的潜在风险。由于在胃肠道的水性介质中的溶解度有限，生物药剂学分类系统（BCS）Ⅱ类药物面临着特殊的障碍。在这种情况下，通常采用注射剂作为替代策略。为了解决这些挑战，纳米混悬技术为提高药物溶解度和克服口服给药障碍提供了一种有前途的解决方案。该技术有可能通过解决溶解度问题，在药物发现和临床前应用之间架起桥梁。本文综述了当代纳米混悬剂制备技术以及在制剂中加入稳定成分的情况。此外，本文还探讨了纳米混悬剂在口服和其他（如注射/局部）给药途径中的应用策略，并分别进行了讨论，为每种给药方法提出了合适的解决策略。
