This project belongs to the field of health and medicine (Pharmacology and Traditional Chinese Medicine). The effective parts of traditional Chinese medicine are an important component of single or compound prescriptions, occupying a significant position in clinical medication and new drug development. However, due to issues with poor absorption in clinical applications or safety concerns during injection, their therapeutic effects have not been fully realized. Nanoparticle delivery systems are currently hotspots of research both domestically and internationally, playing an important role in targeted drug delivery or enhancing oral absorption of drugs. They are mainly studied or applied in chemical drugs at present. Compared to chemical drugs, the effective parts of traditional Chinese medicine consist of multiple monomer components and have complex properties that vary greatly, severely restricting the progress of effective part nanomedicine development. This project, under the support of national projects such as the 973 Plan and four Shanghai Municipal Science and Technology Commission projects, The first method for preparing solid lipid nanoparticles of Chinese medicine active ingredients using glycerides of behenic acid as materials and the cold pressing homogenization-high pressure emulsification method was established. A characteristic method for evaluating the in vitro and in vivo behavior of Chinese medicine active ingredient nanoparticles was formed based on a multi-component content weight comprehensive evaluation method. The effectiveness of improving the oral and intravenous injection effects of Chinese medicine active ingredient nanoparticles through nanotechnology was achieved. The main scientific and technological innovation points are as follows: (1) For the first time, a method for preparing Chinese medicine active ingredient nanoparticles using glycerides of behenic acid as materials and represented by the cold pressing homogenization-high pressure emulsification method was established, forming a technical platform for the preparation of Chinese medicine active ingredient nanoparticles. Models such as silymarin, toad venom extract, hydroxycamptothecin, docetaxel, etc., were used to construct solid lipid nanoparticles of Chinese medicine active ingredients, long-circulating nanoparticles, and long-circulating liposomes. (2) Formulated an in vitro and in vivo evaluation method characterized by nano-particles of active components from traditional Chinese medicine: using a multi-component content weight comprehensive evaluation method to comprehensively evaluate the encapsulation rate, in vitro drug release, in vivo distribution, bioavailability, etc., of nano-particles of active components from traditional Chinese medicine, reflecting more objectively the characteristics of these active components. (3) Nanotechnology has significantly improved the oral bioavailability of active components from traditional Chinese medicine, promoting the application of nano-formulation of these active components. Compared with oral reference formulations, the relative bioavailability of water-soluble silybin solid lipid nanoparticles in vivo was 310% for Livailong and 459% for Yiganling, confirming that the nanoparticle drug delivery system can significantly improve the bioavailability of poorly soluble drugs when administered orally, and successfully achieved industrialization. Together with Inner Mongolia Yuanhe Pharmaceutical Co., Ltd., this formulation was applied for production approval. Became the first domestic variety to apply for a traditional Chinese medicine (TCM) nanomedicine formulation with the State Food and Drug Administration (SFDA). (4) Discussed the mechanisms by which nanomedicines enhance the oral bioavailability of active ingredients and monomers in TCMs. Conducted studies on the oral administration transport mechanisms of silymarin solid lipid nanoparticles and paclitaxel liposomal nanoparticles, exploring how particle size, P-glycoprotein efflux inhibitors, and lymphatic transport affect oral absorption mechanisms. (5) Constructed long-circulating nanoliposomes and long-circulating nanoparticles using F68 as a material modifier, enhancing the in vivo residence time and efficacy of model TCM active components and effective sites such as hydroxycamptothecin (HCPT) and bufotoxin. This was one of the earlier studies at home and abroad that applied Pluronic F68 to construct long-circulating nanoparticles. During the project research period, 14 papers were published, and 11 graduate students were trained. Among them, there are 2 doctoral students), applied for 14 patents, authorized 10 patents, and declared a new traditional Chinese medicine (TCM) certificate (received acceptance number). Two technologies have been promoted and applied in two pharmaceutical companies. This project has established the first technical platform for the preparation and evaluation of nano-particles from effective parts of TCM, enriched and developed dosage forms of TCM effective parts, improved the oral bioavailability and in vivo effects of TCM effective parts, accelerated the industrialization process of TCM effective part nano-formulations, and produced significant social benefits.