Nanocrystal Preparation: Low-Energy Precipitation Method Revisited

doi:10.1021/cg4000473

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	Nanocrystal Preparation: Low-Energy Precipitation Method Revisited
	Khan, Shahzeb 2; de Matas, Marcel 1; Zhang, Jiwen3 ; Anwar, Jamshed 4
刊名	CRYSTAL GROWTH & DESIGN
	2013-07
卷号	13 期号:7 页码:2766-2777
ISSN号	1528-7483
DOI	10.1021/cg4000473
文献子类	Article
英文摘要	Nanocrystals have the potential to address the challenges of delivering drugs with low aqueous solubility. In this study, the use of low energy anti-solvent precipitation for producing nanocrystals has been investigated. Stable nanocrystals with uniform particle size were prepared for the three model compounds, glyburide, ibuprofen, and artemisinin, which are all practically insoluble in water and have diverse molecular structures and crystal packings. The choice of crystal growth inhibitors/stabilizers was found to be critical and specific for each drug. The effect of the process variables, temperature, stirring rate, and the solute solution infusion rate into the antisolvent, was rationalized in terms of how these factors influence the local supersaturation attained at the earliest stages of precipitation. The dissolution of the nanocrystals in aqueous media under physiological conditions was shown in all cases to occur almost instantaneously, being markedly more rapid than that observed for micronized suspensions of the model drugs and their marketed tablet formulations. Rationalization of the choice of optimum stabilizers in terms of molecular interaction with the exposed crystal surfaces proved to be difficult. The study demonstrates that standard crystallization technology is effective in producing nanocrystals with the primary challenge being physicochemical (rather than mechanical), involving the identification of molecule specific crystal growth inhibitors and/or stabilizers.
资助项目	Pakistani Higher Education Commission (HEC) under the Faculty Development Programme[00000000] ; University of Malakand Chakdara (KPK), Pakistan under the Faculty Development Programme[00000000] ; EPSRC (Bradford-China Science Bridges)[EP/G042365/1]
WOS关键词	POORLY SOLUBLE DRUGS ; HIGH-PRESSURE HOMOGENIZATION ; PARTICLE-SIZE ; SUPERCRITICAL FLUIDS ; NANOPARTICLES ; STABILIZATION ; NANOSUSPENSIONS ; DISSOLUTION ; FORMULATION ; STABILITY
WOS研究方向	Chemistry ; Crystallography ; Materials Science
语种	英语
出版者	AMER CHEMICAL SOC
WOS记录号	WOS:000321542900011
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/277545]
专题	药物制剂研究中心中科院受体结构与功能重点实验室新药研究国家重点实验室
通讯作者	Anwar, Jamshed
作者单位	1.AstraZeneca, Formulat Sci, Macclesfield SK10 2NA, Cheshire, England; 2.Univ Bradford, Life Sci Res Inst, Computat Biophys Lab, Bradford BD7 1DP, W Yorkshire, England; 3.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Ctr Drug Delivery Syst, Shanghai 201203, Peoples R China; 4.Univ Lancaster, Dept Chem, Lancaster LA1 4YB, England
推荐引用方式 GB/T 7714	Khan, Shahzeb,de Matas, Marcel,Zhang, Jiwen,et al. Nanocrystal Preparation: Low-Energy Precipitation Method Revisited[J]. CRYSTAL GROWTH & DESIGN,2013,13(7):2766-2777.
APA	Khan, Shahzeb,de Matas, Marcel,Zhang, Jiwen,&Anwar, Jamshed.(2013).Nanocrystal Preparation: Low-Energy Precipitation Method Revisited.CRYSTAL GROWTH & DESIGN,13(7),2766-2777.
MLA	Khan, Shahzeb,et al."Nanocrystal Preparation: Low-Energy Precipitation Method Revisited".CRYSTAL GROWTH & DESIGN 13.7(2013):2766-2777.