School of Chemical and Biomedical Engineering, Nanyang Technological University, Singapore 637459.
Curr Pharm Des. 2013;19(35):6229-45. doi: 10.2174/1381612811319350002.
The conversion of drugs into drug nanoparticles (nano-drugs) represents a feasible method to enhance bioavailability of otherwise sparingly soluble-drugs. Nano-drugs enhance bioavailability through the improvement of dissolution rate and saturation solubility of drugs, by virtue of their small sizes. Nano-drugs available in the market are usually produced by top-down methods, such as wet milling and high pressure homogenization. These conventional top-down methods, however, suffer from high energy and time requirement, as well as wide and inconsistent nano-drug size distribution. Furthermore, commercially available nano-drugs are predominantly crystalline while amorphous nano-drugs are largely neglected despite their propensity to generate high saturation solubility. In this review, nonconventional methods to prepare crystalline and amorphous nano-drugs are discussed, with the bioavailability enhancing characteristics highlighted. Both top-down and bottom-up methods are covered, finally, a sustainability-based perspective comparing amorphous and crystalline nano-drugs is presented.
药物转化为药物纳米颗粒（纳米药物）代表了一种提高生物利用度的可行方法，否则溶解度低的药物的生物利用度会提高。纳米药物通过提高药物的溶解速率和饱和溶解度来提高生物利用度，这得益于它们的小尺寸。市场上的纳米药物通常是通过自上而下的方法生产的，如湿磨和高压匀浆。然而，这些传统的自上而下的方法存在能量和时间需求高、纳米药物尺寸分布宽且不一致的问题。此外，尽管无定形纳米药物具有提高饱和溶解度的倾向，但商业上可获得的纳米药物主要是结晶的，而无定形纳米药物则被忽视了。在这篇综述中，讨论了制备结晶和无定形纳米药物的非传统方法，并强调了提高生物利用度的特点。涵盖了自上而下和自下而上的方法，最后，基于可持续性的角度比较了无定形和结晶纳米药物。
