This project belongs to the field of biopharmaceutical technology. The project targets the properties of several different types of active ingredients/constituents in traditional Chinese medicine, and based on the principles and methods of modern biopharmaceutics, has designed and constructed a variety of new nano-drug delivery systems. Research spanning over more than ten years has been conducted in three aspects: improving the oral bioavailability of poorly soluble traditional Chinese medicine components, promoting the transdermal absorption of active pharmaceutical ingredients, and achieving targeted delivery of anti-cancer components from traditional Chinese medicine. Innovative achievements have been made: (1) Developed a variety of new technologies for preparing nano-drug delivery systems for traditional Chinese medicine, including a one-step reaction method for preparing biodegradable polymer PCL-PEO-PCL triblock copolymers; developed a method for modifying lipid nanoparticles with WGA; established a new method for modifying poly(lactic acid) drug-loaded nanoparticles with RGD; A semi-flow method for determining the solubility of insoluble components in supercritical fluids and its device have been established, which has been applied to the preparation of solid dispersions of effective components from insoluble traditional Chinese medicines; a variety of lipid transdermal nanopharmaceutical delivery systems have been constructed; the combination of nano-powder technology and nano-carrier technology has been applied to mineral traditional Chinese medicine realgar and its compound Niuhuang Xingxiao Pills; the design concept of multi-component nanopharmaceutical delivery systems has been proposed for the first time. (2) A new method for evaluating traditional Chinese medicine nanopharmaceutical delivery systems has been established, and a preliminary technical system for the evaluation of traditional Chinese medicine nanopharmaceutical delivery systems has been constructed. The fingerprinting technology of traditional Chinese medicine has been applied for the first time to the evaluation of the preparation process of nanopharmaceutical delivery systems; in vitro methods for evaluating oral absorption of lipid nanoparticles have been established using dynamic lipid digestion models, etc.; an in vivo evaluation method based on microdialysis technology for transdermal drug delivery has been established. This is the first study to apply fluorescence tracing combined with Nanosight technology to the transdermal absorption process of nanocarriers. (3) Clarified the mechanisms for improving the biological effects of several active components of traditional Chinese medicine, such as oridonin, bufotalin, aconitine, volatile oils from frankincense and myrrh, realgar, etc., in more than ten different types of effective components/constituents of traditional Chinese medicine, including oral absorption, transdermal penetration, and targeted delivery by injection, and studied their mechanisms from multiple aspects such as in vivo, in vitro, cells, and whole organisms; discovered that skin activity has a significant impact on the retention of drugs in the skin. This project has been authorized with 7 national invention patents and applied for 1 international patent; a total of 56 papers have been published, including 32 SCI papers with an overall impact factor of 111.3, and the papers have been cited 311 times domestically and internationally, with 193 citations from SCI journals, and the highest single citation from SCI was 67 times. 1 paper was selected as a Key Scientific Article by the international pharmaceutical information organization Global Medical Discovery; 24 graduate students were trained; participated in 12 academic conferences, and presented at 4 international conferences; research results have been applied and achieved good effects in the research and development of innovative formulations for traditional Chinese medicine by multiple units such as Jiangsu Provincial Institute of Traditional Chinese Medicine, Anhui University of Chinese Medicine, Anhui Xingxing Pharmaceutical Development Co., Ltd., Shanghai Functional Material Chemistry Key Laboratory (East China University of Science and Technology), Hubei University of Chinese Medicine, etc.; through long-term research and accumulation, young scientific talents have been cultivated, new disciplinary growth points have been formed, stable research directions have been promoted, and the development of the discipline of TCM pharmaceutics has been facilitated.