Home Latest Articles
Latest Articles
  • Chinese Traditional and Herbal Drugs. 2026, 57(10): 3886-3901.
    Objective To explore the syndrome differentiation and medication, and formulation rules of renowned traditional Chinese medicine (TCM) practitioners in treating type 2 diabetes mellitus (T2DM) using data mining technology, and validate the efficacy of the identified core formula using an animal model. Methods A total of 200 medical cases of T2DM treated by famous TCM practitioners were collected from databases such as China National Knowledge Infrastructure (CNKI), Wangfang, VIP. A database was established using the TCM Inheritance Computing Platform (V3.5). The silhouette coefficient was introduced to evaluate K-means clustering performance, and hierarchical clustering was used for cross-validation to screen for core formulas. For the experimental validation, 40 male Sprague-Dawley (SD) rats were randomly divided into four groups (n = 10 each): control, model, core formula, and metformin. Except for the control group, T2DM models with “qi-yin deficiency” syndrome were induced by a 4-week high-fat and high-sugar diet combined with daily oral administration of Qingpi Fuzi decoction (15.75 g/kg), followed by an intraperitoneal injection of streptozotocin (STZ, 30 mg/kg). After successful modeling, the core formula group received the core formula (10.5 g/kg), and the Metformin group received metformin (200 mg/kg) via gavage daily; Control and Model groups received equal volumes of saline, each group was given the drug once a day for four weeks of intervention. Body weight (BW) and fasting blood glucose (FBG) were monitored during the administration period. Serum levels of insulin (INS), glycated hemoglobin (IFCC-HbA1c), interleukin-1β (IL-1β), IL-6, superoxide dismutase (SOD), and malondialdehyde (MDA) were measured by ELISA. The proportion of insulin-positive areas was assessed via immunohistochemical staining. Oil red O staining was used to observe lipid deposition in the liver. PAS staining was used to evaluate the pathological changes of renal tissue. Protein expressions of the phosphatidylinositol-3-hydroxykinase (PI3K)/protein kinase B (Akt), nuclear factor-κB (NF-κB), nuclear factor erythroid-2-related factor 2 (Nrf2)/heme oxygenase-1 (HO-1) pathways in liver tissues were detected by Western blotting. Results Data mining revealed that qi-yin deficiency was the primary syndrome of T2DM. High-frequency herbs included Huangqi (Astragali Radix), Huanglian (Coptidis Rhizoma), and Fuling (Poria). The medicinal properties were predominantly cold, warm, and neutral, while flavors were mainly sweet, bitter, and pungent, targeting the spleen, lung, and liver meridians. These types of drugs such as tonifying deficiency, clearing heat, promoting diuresis, and activating blood circulation were most prevalent. Association rule analysis identified Astragali Radix-Gengen (Puerariae Lobatae Radix) and Astragali Radix-Coptidis Rhizoma as core herb pairs. Clustering identified a core formula consisting of Astragali Radix, Shanyao (Dioscoreae Rhizoma), Puerariae Lobatae Radix, Shanzhuyu (Corni Fructus), and Poria. In vivo experiments showed that the core formula group had significantly lower FBG, INS, and IFCC-HbA1c levels compared to the Model group (P < 0.05, 0.01, 0.001), with a gradual recovery in BW. Furthermore, IL-1β and IL-6 were significantly decreased (P < 0.01, 0.001), SOD was increased (P < 0.01), and MDA was decreased (P < 0.05). Pathologically, the core formula group showed a significantly higher ratio of insulin-positive area (P < 0.05), reduced hepatic lipid deposition (P < 0.01), and lower renal pathological injury scores (P < 0.05). Western blotting analysis indicated that core formula significantly up-regulated the expression of p-PI3K/PI3K, p-Akt/Akt, Nrf2, and HO-1 (P < 0.05, 0.01), while down-regulating p-NF-κB p65/NF-κB p65 (P < 0.05). Conclusion The core formula exhibits a definite hypoglycemic effect. Its mechanism of action is associated with activating the PI3K/Akt signaling pathway to enhance insulin sensitivity, inhibiting NF-κB-mediated pro-inflammatory responses, and up-regulating the Nrf2/HO-1 pathway to ameliorate oxidative stress. This formula effectively maintains the number and structure of pancreatic islet cells and protects liver and kidney tissues from diabetic pathological damage, providing a scientific basis for the prevention and treatment of T2DM with TCM.
  • Chinese Traditional and Herbal Drugs. 2026, 57(11): 4196-4211.
    Objective To elucidate the mechanism by which Danhong Injection (丹红注射液, DHI) ameliorates mitochondrial dynamics imbalance and inhibits NOD-like receptor family pyrin domain containing 3 (NLRP3)-mediated pyroptosis in H9c2 cells subjected to oxygen-glucose deprivation based on AMP-activated protein kinase (AMPK)/dynamin-related protein 1 (Drp1) pathway. Methods Ultra-high performance liquid chromatography-mass spectrometry (UHPLC-MS) was employed to identify the core active components of DHI. Molecular docking was performed using AutoDock Vina software to assess the affinity between DHI core components and target proteins, including AMPK, Drp1, optic atrophy 1 (OPA1) and cystein-asparate protease-1 (Caspase-1). An H9c2 cell oxygen-glucose deprivation model was established, control group, model group, DHI group, DHI + Compound C (AMPK inhibitor) group, AICAR (AMPK agonist) group, MCC950 (NLRP3 inhibitor) group and Mdivi-1 (Drp1 inhibitor) group were set up. The optimal intervention concentration of DHI was screened using CCK-8 assay. Mitochondrial membrane potential (MMP) was measured using JC-1 probe, and mitochondrial reactive oxygen species (mtROS) level was determined using MitoSOXTM. Mitochondrial ultrastructure was observed via transmission electron microscopy. Immunofluorescence was used to detect the protein expressions of p-AMPK and p-Drp1. Western blotting was performed to detect the expressions of AMPK/Drp1 pathway-related proteins, mitochondrial dynamics-related proteins [mitochondrial fission 1 protein (FIS1), mitofusin 2 (MFN2) and OPA1] and pyroptosis-related proteins [NLRP3, apoptosis-associated speck-like protein containing a CARD (ASC), Caspase-1 and N-terminal fragment of gasdermin D (GSDMD-NT)]. ELISA was used to determine the levels of interleukin-1β (IL-1β), IL-18 and adenosine triphosphate (ATP). Results UHPLC-MS identified eight active components of DHI, including salvianolic acid, lithospermic acid B, danshensu, caffeic acid, sodium danshensu, etc. The molecular docking results showed that each target and active ingredient had strong affinity. The in vitro experimental results showed that compared with model group, mitochondrial morphology in DHI group was significantly improved, with continuous outer membrane and relatively intact cristae structure, increased quantity, and matrix density restored to near normal. MMP and ATP levels were increased (P < 0.01), mtROS release was decreased (P < 0.01), p-AMPK/AMPK value was increased (P < 0.01), p-Drp1/Drp1 value was decreased (P < 0.01), MFN2 and OPA1 protein expressions were upregulated (P < 0.01), FIS1, NLRP3, ASC, Caspase-1 and GSDMD-NT protein expressions were downregulated (P < 0.01), and IL-1β and IL-18 levels were significantly decreased (P < 0.01), consistent with the effects of AICAR, MCC950 and Mdivi-1. Compound C could partially inhibit the above-mentioned effects of DHI. Conclusion DHI activates AMPK/Drp1 pathway, inhibits mitochondrial excessive division and promotes mitochondrial fusion, reduces NLRP3 inflammasome activation and pyroptosis, thereby alleviating hypoxia/hypoglycemia induced H9c2 cell damage.
  • HUANG Yanfen, SU Qian, ZOU Xianmin, SHEN Pengfei, LIAO Lianting, XIAO Linyu, YANG Shilin, YUAN Renyikun, GAO Hongwei
    Chinese Traditional and Herbal Drugs. 2026, 57(11): 4212-4223.
    Objective To investigate the therapeutic effect of pedunculoside (PE) on dextran sulfate sodium salt (DSS)-induced ulcerative colitis (UC) and elucidate its molecular mechanism through in vitro and in vivo models. Methods DSS was used to establish a mouse UC model, combined with transcriptome analysis, the effect of PE on changes in body weight, colon length, colon tissue pathology, pro-inflammatory cytokine levels in colon tissue, and expressions of tight junction proteins (Occludin, E-cadherin, Claudin-1) were evaluated. Caco-2 monolayer cell model was established, the cell permeability was detected using fluorescein isothiocyanate-glucan (FITC-glucan) to evaluate the effect of PE on intestinal mucosal barrier function. Further validation of the regulatory effect of PE on phosphatidylinositol 3-kinase (PI3K)/protein kinase B (Akt) signaling pathway, inflammatory factors, and tight junction protein expression and distribution was achieved through molecular biology experiments such as Western blotting and ELISA. Results The results of in vivo experiments showed that PE could significantly reduce the disease activity index (DAI) score of mice (P < 0.001), alleviate pathological damage to colon tissue, reduce pro-inflammatory cytokine levels (P < 0.05, 0.001), and upregulate the expressions of tight junction proteins in colon tissue (P < 0.001). Transcriptome sequencing revealed that PE had a significant inhibitory effect on the overactivated PI3K/Akt signaling pathway in colon tissue of UC mice (P < 0.001). In vitro experimental results showed that PE could significantly reduce the permeability of Caco-2 monolayer cells (P < 0.001), inhibit the phosphorylation of Akt and PI3K in DSS-induced Caco-2 cell model (P < 0.01, 0.001), reduce the levels of inflammatory factors (P < 0.01, 0.001), and upregulate the expressions of Occludin, E-cadherin and Claudin-1 (P < 0.001). Conclusion PE could downregulate inflammatory response and enhance intestinal epithelial barrier function by inhibiting PI3K/Akt signaling pathway in both in vivo and in vitro models, thereby exerting a protective effect on DSS-induced UC.
  • Chinese Traditional and Herbal Drugs. 2026, 57(11): 4339-4350.
    Objective To explore the molecular mechanisms underlying the morphological differences in fruits and seeds of Ziziphus jujuba var. spinosa from different sources and to identify key genes influencing the morphological variation in Z. jujuba var. spinosa fruits and seeds. Methods Wild and grafted Z. jujuba var. spinosa fruits and seeds were used as materials. Phenotypic differences in their appearance were analyzed using a phenotypic group approach. Transcriptome sequencing was performed using the Illumina HiSeq platform. After data quality control, assembly, and gene annotation, differentially expressed genes (DEGs) were analyzed and screened. Quantitative real-time PCR (qRT-PCR) was used to assess the expression levels of key genes in different tissues, under gibberellin (GA3) and drought stress treatments. Results The transverse and longitudinal diameters, as well as the weight of grafted Z. jujuba var. spinosa fruits, were significantly larger than those of wild Z. jujuba var. spinosa fruits. Similarly, the longitudinal diameter, thickness, and weight of grafted Z. jujuba var. spinosa seeds were significantly higher than those of wild Z. jujuba var. spinosa seeds. Transcriptome sequencing revealed that DEGs between grafted and wild Z. jujuba var. spinosa fruits and seeds were related to stress response, transcriptional regulation, plant hormone signal transduction, and phenylpropanoid biosynthesis. Through qRT-PCR, core DEGs influencing the morphological development of Z. jujuba var. spinosa fruits and seeds were identified, including WRKY53, WRKY40, TIFY9, NCED3, TSJT1, NRT3.1, BZIP9, TEN1, BXL1, and LRX4. After treatment with 150 mg/L GA3, the expression levels of WRKY53, LRX4, NRT3.1, and TIFY9 were significantly upregulated, whereas BZIP9 and NCED3 were significantly downregulated. Under PEG-6000 drought stress, the expression levels of WRKY53, WRKY40, TEN1, TSJT1, and TIFY9 were significantly upregulated, while those of BZIP9 and LRX4 were significantly down-regulated. Conclusion This study preliminarily elucidated the molecular mechanisms underlying the morphological differences between grafted and wild Z. jujuba var. spinosa fruits and seeds. It also identified key candidate genes influencing the morphological development of fruits and seeds and their expression patterns under different stress conditions. These findings provide a theoretical basis and key targets for molecular breeding, environmental adaptability studies, and resource improvement of Z. jujuba var. spinosa.
  • Chinese Traditional and Herbal Drugs. 2026, 57(10): 3861-3877.
    Objective To identify the blood-absorbed constituents of ethanol extract of Tetrastigma hemsleyanum (SYQ) and investigate its anti-breast cancer activity and underlying mechanisms. Methods Blood-absorbed components of SYQ were identified using ultra-high performance liquid chromatography-quadrupole time-of-flight tandem mass spectrometry. The effects of SYQ drug containing serum on proliferation and migration of 4T1 cells were evaluated by MTT, colony formation and wound-healing assays. A 4T1 tumor-bearing mouse model was established, control group, model group, cyclophosphamide (20 mg/kg) group, SYQ low-, medium-, and high-dose (5, 10, 20 g/kg) groups were set up. After drug intervention, ELISA was used to detect the levels of interleukin-6 (IL-6) and tumor necrosis factor-α (TNF-α) in serum. Hematoxylin-eosin (HE) staining was used to observe pathological changes in tumor tissue. Immunohistochemistry was used to detect CD68 and Ki67 expressions in tumor tissue. Western blotting was used to detect the expressions of TNF-α/protein kinase B (Akt)/signal transducer and activator of transcription 3 (STAT3) signaling axis and apoptosis related proteins in tumor tissues. Results A total of 19 blood components were identified by UHPLC-Q-TOF-MS/MS, mainly including flavonoids (rutin, tangeretin, narcissoside), phenylpropanoids, and other glycoside compounds (forsythoside E, darendoside B). The in vitro experimental results showed that SYQ drug containing serum significantly inhibited the proliferation, migration and colony formation of 4T1 cells (P < 0.01, 0.001). The in vivo experimental results showed that SYQ significantly inhibited tumor volume growth in tumor bearing mice (P < 0.001), with a tumor inhibition rate of 25.95% in high-dose group. SYQ reduced the levels of IL-6 and TNF-α in serum (P < 0.05, 0.001), induced tumor tissue necrosis and significantly reduced the expressions of CD68 and Ki67 (P < 0.001), while downregulated the expression levels of TNF-α, p-Akt/Akt, p-STAT3/STAT3 and B-cell lymphoma-2 (Bcl-2) in tumor tissue (P < 0.05, 0.01, 0.001). Conclusion SYQ could exerts anti-breast cancer effects by reducing the levels of inflammatory factors, inhibiting tumor cell proliferation and inducing tumor tissue necrosis. The mechanism may be related to the inhibition of TNF-α/Akt/STAT3 signaling axis.
  • TANG Ruying, LIU Yuling, LIN Longfei, LI Hui
    Chinese Traditional and Herbal Drugs. 2026, 57(11): 4302-4318.
    Objective To explore the research status, trends and hotspots of plant-derived exosomes (PDEs) using bibliometric visualization analysis, so as to provide a theoretical basis for their basic research and practical applications. Methods Utilizing CiteSpace, VOSviewer, and Scimago Graphica software, we conducted a comprehensive visualization analysis of Chinese and English literature on PDEs indexed in the China National Knowledge Infrastructure (CNKI) and the Web of Science Core Collection (WOSCC). The analysis encompassed publication trends, geographical distribution, institutional collaboration networks, author contributions, and keyword co-occurrence to identify research frontiers and evolving trajectories in PDEs research. Results A total of 2 815 eligible publications were included in this study, comprising 160 Chinese-language publications (5.68%) and 2 655 English-language publications (94.32%). Research activity in the PDEs field is predominantly concentrated in China and the United States, with global academic attention demonstrating a consistent annual increase. Institutional network analysis revealed distinct modular collaboration patterns, with Chinese institutions—including the Chinese Academy of Sciences, Zhejiang University, Capital Medical University, and Nanjing University of Chinese Medicine—alongside international institutions such as the University of California and the University of Illinois, occupying central positions in collaboration networks. High-frequency keyword co-occurrence analysis identified current research focal points, including PDEs derived from sources such as Jianghuang (Curcumae Longae Rhizoma), Renshen (Ginseng Radix et Rhizoma), tea, Gouqi (Lycii Fructus), and Machixian (Portulacae Herba), with investigations concentrating on molecular mechanisms underlying skin wound healing, neuroprotective effects, oncological therapy, anti-inflammatory and antioxidant activities, and blood-brain barrier modulation. Additionally, sustained research attention is directed toward applied domains including extraction and purification methodologies, establishment of quality evaluation standards, and the development of PDEs as drug delivery vehicles. Conclusion PDEs demonstrate substantial research potential in neuroprotection, oncological therapy, and wound healing applications. Future research trajectories will likely focus on optimizing extraction and purification protocols for PDEs from diverse botanical sources, developing novel formulations tailored to precision medicine requirements, and expanding their therapeutic indications. Furthermore, strengthening interdisciplinary collaboration and integrating emerging technologies will be essential for fully realizing the translational potential of PDEs.
  • Chinese Traditional and Herbal Drugs. 2026, 57(11): 4376-4387.
    Objective To evaluate the quality of Urtica laetevirens from different producing areas based on multi-index quantification, combined with chemical pattern recognition technology, weighted TOPSIS and grey relational analysis(GRA) fusion model. Methods A total of 20 batches of U. laetevirens were collected from the main producing areas. The contents of protocatechuic acid, chlorogenic acid, caffeic acid, ferulic acid, hyperoside, rutin, quercetin, apigenin, kaempferol, luteolin, daucosterol, β-sitosterol were detected by HPLC, and the extract, total ash and acid-insoluble ash were examined. Combined with chemical pattern recognition technology, the differences between U. laetevirens from different producing areas were discussed, and the main landmark components leading to the quality differences of U. laetevirens from different producing areas were screened. The weighted TOPSIS model was constructed with the VIP value of each index as the weight, and then integrated with the GRA method to rank the quality of 20 batches of U. laetevirens. Results Under the established HPLC conditions. The linear ranges of protocatechuic acid, chlorogenic acid, caffeic acid, ferulic acid, hyperoside, rutin, quercetin, apigenin, kaempferol, luteolin, daucosterol, β-sitosterol showed a good linear relationship within the range of 0.21—10.50, 1.15—57.50, 0.28—14.00, 0.46—23.00, 3.35—167.50, 4.47—223.50, 1.70—85.00, 0.14—7.00, 0.37—18.50, 0.79—39.50, 0.65—32.50, 1.31—65.50 μg/mL, respectively. The established method had good repeatability and high instrument precision. The stability of the sample solution of nettle extracted by 70% methanol ultrasonic extraction was good within 24 h. The average recovery rates of each component were 98.43%, 97.91%, 98.24%, 99.06%, 100.03%, 99.68%, 100.01%, 97.81%, 98.92%, 98.23%, 96.77% and 98.34%, respectively. The RSD was between 0.73% and 1.86%. The contents of various components were 0.66—0.129, 0.270—0.577, 0.093—0.184, 0.164—0.281, 1.440—2.465, 1.911—3.204, 0.331—1.188, 0.036—0.106, 0.078—0.209, 0.187—0.456, 0.196—0.418, 0.383—0.613 mg/g, The contents of extract, total ash and acid-insoluble ash were 14.3%—31.5%, 7.3%—16.2%, 0.5%—3.4%, respectively. It showed that the quality difference between batches was large. The 20 batches of U. laetevirens samples were divided into three groups by chemical pattern recognition technology, among them, S1—S8 from Sichuan, Gansu and Yunnan, S9-S14 from Guangxi, Guizhou and Hunan, and S15—S20 from Qinghai and Xizang were each group, showing obvious regional characteristics. The marker components that distinguish the quality differences of each sample were rutin, hyperoside, quercetin, chlorogenic acid, luteolin and β-sitosterol. The analysis results of weighted TOPSIS and GRA fusion model showed that the comprehensive relative closeness of 20 batches of samples was between 0.285 4 and 0.673 6. The comprehensive relative closeness of S15—S20 samples from Qinghai and Xizang were 0.652 2, 0.663 3, 0.628 3, 0.673 6, 0.597 0 and 0.583 7, respectively, which was higher than that of other batches, and the quality was relatively better. Conclusion The established multi-index quantitative method is stable and reliable, which can be used to perfect the quality standard of U. laetevirens. The chemical pattern recognition combined with weighted TOPSIS and GRA fusion model comprehensively and scientifically evaluated the quality of U. laetevirens from different producing areas, laying a foundation for the quality analysis and evaluation of U. laetevirens.
  • YU Zheyuan, WANG Xiaoxia, LI Xiaofang, FAN Dongqin
    Chinese Traditional and Herbal Drugs. 2026, 57(10): 3902-3911.
    Objective To improve the YOLOv8 model and provide a high-accuracy and high-efficiency automated detection solution for Chinese herbal slices in practical scenarios such as production, dispensing, and teaching. Methods Taking YOLOv8 as the baseline model, a lightweight residual depthwise-attention Bottleneck (RDA-Bottleneck) is proposed to replace the Bottleneck blocks in C2f, reduce redundant computations and enhance the expression of channel features. To strengthen the discriminative capability of the detector during multi-scale feature learning, a frequency-aware spatial attention (FASA) module is introduced to replace the Conv blocks in the Backbone and Neck of YOLOv8. To evaluate the performance of the improved model, a dedicated dataset containing 10 categories of Chinese herbal slices [e.g., Banlangen (Isatidis Radix) and Gancao (Glycyrrhizae Radix et Rhizoma)] is constructed, comprising 8 281 images. Results Compared with YOLOv8, the proposed model reduces parameters by 39.5% and floating point operations (FLOPs) by 34.1%, while improving single-threshold average accuracy mAP50 by 0.2% and multi-threshold average accuracy mAP50-95 by 0.2%. Conclusion The improved model achieves higher detection accuracy and inference efficiency for Chinese herbal slice detection under complex backgrounds and diverse appearances, providing an effective method for automatic detection of Chinese herbal slices.
  • Chinese Traditional and Herbal Drugs. 2026, 57(10): 3963-3973.
    Objective To establish a detection method that combines the appearance characteristics (color, odor, taste) and internal chemical components of Baihe (Lilii Bulbus) to conduct a comprehensive evaluation of the overall quality of lily medicinal materials. Methods Using intelligent sensory technology to detect the color, odor, and taste of 15 batches Lilii Bulbus from the perspectives of vision, smell, and taste. At the same time, HPLC fingerprint spectra and multi-index content determinations were established to compare the content differences of specific components (regaloside C, regaloside A, 2-acetate regaloside A and regaloside E) among medicinal materials from the perspective of chemical composition. Multivariate statistical analysis methods such as hierarchical cluster analysis (HCA), principal component analysis (PCA), and partial least squares discriminant analysis (PLS-DA) were used to analyze the color, odor, taste, and fingerprint spectra of Lilii Bulbus from different origins, and screen for differential components. Pearson correlation analysis was used to reveal the correlation between appearance color, odor, taste, and exclusive ingredients. Results The results of the colorimeter showed that the colors of the 15 batches of Lilii Bulbus medicinal materials were all bright white and lighter, and Zhejiang and Hunan were whiter than those of Jiangsu. The electronic nose analysis results indicated that sensors W3S, W5C, W6S, and W1S, corresponding to 15 batches of Lilii Bulbus medicinal materials contained relatively high levels of alkanes and aromatic compounds. However, Zhejiang Lilii Bulbus also exhibited elevated hydrides. Electronic tongue results revealed that all taste indicators showed obvious responses except sourness. Intelligent sensory analysis demonstrated that Lilii Bulbus from different regions exhibited significant differences in color, odor and taste. A total of 15 common peaks were identified in the fingerprint spectra. Content determination results indicated obvious quality differences among Lilii Bulbus samples from different origins. Among them, Peak 13, peak 6 (regaloside A) and peak 11 (regaloside E) were the main marker components causing compositional differences of Lilii Bulbus from different producing areas. The correlation analysis results indicated that yellow blue chromaticity(b*), total color value(E*ab), W1S, W6S, sweetness, astringency, aftertaste-A in Lilii Bulbus were correlated with regaloside C, regaloside A, 2-acetate regaloside A and regaloside E. Conclusion The method of integrating intelligent sensory technology with chemical composition research for comprehensive quality evaluation of Lilii Bulbus medicinal materials is feasible. It can be used to evaluate the comprehensive quality of Lilii Bulbus from different origins, providing reference for the quality control and application of Lilii Bulbus.
  • Chinese Traditional and Herbal Drugs. 2026, 57(10): 3778-3791.
    Objective To prepare lentinan-buddleoside self-assembled nanoparticles (Len-Bud-SANs), and evaluate investigate its physicochemical properties, oral pharmacokinetic behavior and acute toxicity. Methods Len-Bud-SANs were prepared by self-assembled method. Envelopment efficiency, drug loading and particle size were employed as indicators, single factor experiments combined with Box-Behnken design-response surface method (BBD-RSM) were used to obtainoptimal prescriptions of Len-Bud-SANs. The appearance of Len-Bud-SANs was observed by transmission electron microscope (TEM) was, crystal form of Len-Bud-SANs powder was analyzed by X-ray powder diffraction (XRPD). Molecular simulation docking and Fourier transform infrared spectroscopy (FTIR) were used to study the binding mechanism between lentinan and buddleoside. The solubility and drug release behavior of Len-Bud-SANs were determined in phosphate buffer solution (PBS) at pH 2.0 and pH 6.8. SD rats in each group were administered intragastrically with buddleoside suspension and Len-Bud-SANs powder, then buddleoside concentration in plasma was analyzed by HPLC method, and main pharmacokinetic parameters were calculated. Safety evaluation of Len-Bud-SANs powder was performed by indicators of body weight, food intake, thymus index and spleen index. Pathological conditions of the important organs were observed by hematoxylin-eosin (HE) staining. Results Optimal formulation of Len-Bud-SANs: mass fraction of lentinan was 0.39%, preparation temperature was 65.00 ℃, and preparation time was 1.50 h. Envelopment efficiency, drug loading, particle size and ζ potential were (88.57 ±0.83)%, (8.02 ±0.11)%, (57.54 ±4.90) nm and (−32.10 ±1.36) mV, respectively. Microscopic appearance of Len-Bud-SANs was spherical, and buddleoside existed as an amorphous form in Len-Bud-SANs powder. Solubility of Len-Bud-SANs in phosphate buffer solution of pH 2.0 and pH 6.8 was increased to 59.89 times and 42.95 times, and cumulative release rate were increased to 90.80% and 91.73%, respectively. Drug release behavior of Len-Bud-SANs conformed to Weibull model. Oral pharmacokinetic results showed that t1/2 of Len-Bud-SANs was increased to (4.45 ±0.80) h, Cmax and AUC0-t were increased to 3.00-fold and 5.60-fold. Compared with the blank group, there was no significant change in body weight, food intake, thymus index, spleen index and pathology of important organs in the Len-Bud-SANs group. Conclusion Len-Bud-SANs significantly promoted oral absorption of buddleoside effectively, and no obvious toxicity was observed, which laid the foundation for subsequent research and development.