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纳米混悬液创新:拓展药物递送技术的视野

Nanosuspension Innovations: Expanding Horizons in Drug Delivery Techniques.

作者信息

Jacob Shery, Kather Fathima Sheik, Boddu Sai H S, Attimarad Mahesh, Nair Anroop B

机构信息

Department of Pharmaceutical Sciences, College of Pharmacy, Gulf Medical University, Ajman 4184, United Arab Emirates.

Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, Ajman University, Ajman P.O. Box 346, United Arab Emirates.

出版信息

Pharmaceutics. 2025 Jan 19;17(1):136. doi: 10.3390/pharmaceutics17010136.

Abstract

Nanosuspensions (NS), with their submicron particle sizes and unique physicochemical properties, provide a versatile solution for enhancing the administration of medications that are not highly soluble in water or lipids. This review highlights recent advancements, future prospects, and challenges in NS-based drug delivery, particularly for oral, ocular, transdermal, pulmonary, and parenteral routes. The conversion of oral NS into powders, pellets, granules, tablets, and capsules, and their incorporation into film dosage forms to address stability concerns is thoroughly reviewed. This article summarizes key stabilizers, polymers, surfactants, and excipients used in NS formulations, along with ongoing clinical trials and recent patents. Furthermore, a comprehensive analysis of various methods for NS preparation is provided. This article also explores various in vitro and in vivo characterization techniques, as well as scale-down technologies and bottom-up methods for NS preparation. Selected examples of commercial NS drug products are discussed. Rapid advances in the field of NS could resolve issues related to permeability-limited absorption and hepatic first-pass metabolism, offering promise for medications based on proteins and peptides. The evolution of novel stabilizers is essential to overcome the current limitations in NS formulations, enhancing their stability, bioavailability, targeting ability, and safety profile, which ultimately accelerates their clinical application and commercialization.

摘要

纳米混悬液(NS)具有亚微米级的粒径和独特的物理化学性质,为增强水或脂质中溶解性不佳的药物的给药效果提供了一种通用解决方案。本综述重点介绍了基于NS的药物递送的最新进展、未来前景和挑战,特别是在口服、眼部、透皮、肺部和肠胃外给药途径方面。全面综述了将口服NS转化为粉末、微丸、颗粒、片剂和胶囊,以及将它们纳入薄膜剂型以解决稳定性问题的情况。本文总结了NS制剂中使用的关键稳定剂、聚合物、表面活性剂和辅料,以及正在进行的临床试验和近期专利。此外,还对NS制备的各种方法进行了全面分析。本文还探讨了各种体外和体内表征技术,以及NS制备的缩小技术和自下而上的方法。讨论了商业NS药品的选定实例。NS领域的快速发展可能解决与渗透性限制吸收和肝脏首过代谢相关的问题,为基于蛋白质和肽的药物带来希望。新型稳定剂的发展对于克服NS制剂目前的局限性至关重要,可增强其稳定性、生物利用度、靶向能力和安全性,最终加速其临床应用和商业化。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6345/11768797/69c9e9afe348/pharmaceutics-17-00136-g001.jpg

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