AbstractMany active ingredients of traditional Chinese medicine (TCM), exhibiting excellent pharmacological activity in early-stage development, still need to face the formulation development and application challenges due to druggability issues caused by low solubility, poor membrane permeability, and inadequate stability. Nanocrystal technology is an effective strategy that involves nano-sizing drug particles to improve the biopharmaceutics of drug molecules, which can be used to overcome these inherent limitations of TCM active ingredients. Beyond its conventional application as a standalone dosage form, this technology has recently been extended and integrated with novel delivery systems including Pickering emulsions, hydrogels, soluble microneedles, microspheres, and liposomes, demonstrating broad application prospects. This article systematically outlined the formation mechanisms and physicochemical properties of TCM active ingredient nanocrystals, and discussed their capability and constraints in enhancing druggability from four perspectives: solubility, dissolution rate, bioavailability, and stability. Furthermore, we focused on reviewing recent advances in hybrid systems combining nanocrystals with various novel drug delivery platforms, with the aim of offering insights and references to improve the druggability of TCM active ingredients and facilitate the development of efficient formulations.
| 科 Family | 属数 Number of genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) | 属 Genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) |
|---|---|---|---|---|---|---|
| 鹅膏菌科Amanitaceae | 2 | 11 | 5.26 | 鹅膏菌属 Amanita | 10 | 4.78 |
| 小菇科 Mycenaceae | 2 | 12 | 5.74 | 丝盖伞属 Inocybe | 5 | 2.39 |
| 多孔菌科 Polyporaceae | 8 | 14 | 6.70 | 蜡蘑属 Laccaria | 5 | 2.39 |
| 红菇科 Russulaceae | 3 | 23 | 11.00 | 小皮伞属 Marasmius | 6 | 2.87 |
| 小菇属 Mycena | 11 | 5.26 | ||||
| 光柄菇属 Pluteus | 5 | 2.39 | ||||
| 红菇属 Russula | 17 | 8.13 | ||||
| 栓菌属 Trametes | 5 | 2.39 |