Discipline of Pharmaceutical Sciences, School of Health Sciences, University of KwaZulu-Natal, Durban, South Africa.
Product Development, Odin Pharmaceuticals LLC, Somerset, NJ, USA.
Expert Opin Drug Deliv. 2022 Oct;19(10):1303-1316. doi: 10.1080/17425247.2022.2110579. Epub 2022 Aug 8.
Controlled/extended-release formulations offer numerous benefits over conventional especially reduced side effects, improved therapeutic outcomes, and high patient compliance. Controlled release nanocrystal is extremely versatile technology with several advantages such as very high drug loading, ease of manufacturing, avoidance of dose dumping, reproducible drug release. Usually, nanonization of drug is performed to improve dissolution rate, intrinsic solubility, and thereby bioavailability. Most of the times, this is done for immediate release dosage forms where objective is quick onset of action. However, nanocrystals can also provide a sustained, reproducible plasma concentration profile for weeks to months based on tissue microenvironment, surface coating and administration route.
This review briefly describes the methods for producing nanocrystals, summarizes preclinical research and commercial products demonstrating tremendous potential of controlled release nanocrystals.
Lipophilic drugs are attractive candidates for the development of nanocrystal based controlled release formulations. However, constraint should be practiced while generalizing the technology for the controlled release purpose. Not all drugs fit in the requirement from the perspectives of physicochemical properties or pharmacokinetics. Additionally, technologies should be explored which can convert the nanocrystal into its final dosage form for administration yet preserves the benefits of small particle size and controlled release.
与传统制剂相比，控释/缓释制剂具有许多优势，特别是减少了副作用、改善了治疗效果和提高了患者的顺应性。控释纳米晶体是一种极具多功能性的技术，具有许多优点，如很高的载药量、易于制造、避免剂量突释、可重现的药物释放。通常，药物的纳米化是为了提高药物的溶解速率、内在溶解度，从而提高生物利用度。大多数情况下，这是为了即时释放剂型，其目的是快速起效。然而，纳米晶体也可以根据组织微环境、表面涂层和给药途径，提供长达数周至数月的持续、可重现的血浆浓度曲线。
本文简要描述了制备纳米晶体的方法，总结了临床前研究和商业产品，这些研究和产品展示了控释纳米晶体的巨大潜力。
亲脂性药物是开发基于纳米晶体的控释制剂的理想候选药物。然而，在将该技术推广用于控释目的时，应该谨慎行事。并非所有药物都符合从物理化学性质或药代动力学角度的要求。此外，还应探索一些技术，这些技术可以将纳米晶体转化为最终的给药形式，同时保留小颗粒尺寸和控释的优势。
