Tsiaxerli Anastasia, Vardaka Elisavet, Moutroupidis Christos, Taylor Kevin M G, Kachrimanis Kyriakos, Malamatari Maria
Department of Pharmaceutical Technology, Faculty of Pharmacy, Aristotle University of Thessaloniki, 54124, Thessaloniki, Greece.
Department of Pharmaceutics, UCL School of Pharmacy, 29-39 Brunswick Square, London, WC1 1AX, UK.
J Food Drug Anal. 2024 Dec 15;32(4):398-411. doi: 10.38212/2224-6614.3525.
Pharmaceutical nanosuspensions, also called nanocrystals, are heterogeneous mainly aqueous dispersions of insoluble drug particles stabilised by surfactants and/or polymers. Nanosuspensions as liquid formulations suffer from instability. Solidification of nanosuspensions to solid dosage forms is a way to combine the advantages of nanocrystals with the advantages of the solid state. In this review, advances regarding stabilisation and production of nanosuspensions are briefly covered. Updates on the methods used to convert nanosuspensions to solid oral dosage forms (e.g., powder, granules, pellets, tablets, and films) are presented in depth. From these methods, spray drying and freeze drying are widely used. Granulation and hot-melt extrusion allow straightforward downstream processing, while printing exhibits the potential for dose personalisation. Focus is given on novel formulations (e.g., nano-cocrystals, nanocrystalline solid dispersions) which could further enhance the dissolution and bioavailability of poorly soluble drugs.
药物纳米混悬液，也称为纳米晶体，是主要由表面活性剂和/或聚合物稳定的不溶性药物颗粒的非均相水分散体。作为液体制剂的纳米混悬液存在稳定性问题。将纳米混悬液固化为固体剂型是一种将纳米晶体的优点与固态优点相结合的方法。在这篇综述中，简要介绍了纳米混悬液的稳定化和生产方面的进展。深入介绍了用于将纳米混悬液转化为固体口服剂型（如粉末、颗粒、微丸、片剂和薄膜）的方法。在这些方法中，喷雾干燥和冷冻干燥应用广泛。制粒和热熔挤出便于直接进行下游加工，而打印显示出剂量个性化的潜力。重点关注新型制剂（如纳米共晶体、纳米晶固体分散体），它们可以进一步提高难溶性药物的溶出度和生物利用度。
