1.Applications of Vaterite in Drug Loading and Controlled Release
Xiao-Hui SONG ; Ming-Yu PAN ; Jian-Feng XU ; Zheng-Yu HUANG ; Qing PAN ; Qing-Ning LI
Progress in Biochemistry and Biophysics 2025;52(1):162-181
Currently, the drug delivery system (DDS) based on nanomaterials has become a hot interdisciplinary research topic. One of the core issues is drug loading and controlled release, in which the key lever is carriers. Vaterite, as an inorganic porous nano-material, is one metastable structure of calcium carbonate, full of micro or nano porous. Recently, vaterite has attracted more and more attention, due to its significant advantages, such as rich resources, easy preparations, low cost, simple loading procedures, good biocompatibility and many other good points. Vaterite, gained from suitable preparation strategies, can not only possess the good drug carrying performance, like high loading capacity and stable loading efficiency, but also improve the drug release ability, showing the better drug delivery effects, such as targeting release, pH sensitive release, photothermal controlled release, magnetic assistant release, optothermal controlled release. At the same time, the vaterite carriers, with good safety itself, can protect proteins, enzymes, or other drugs from degradation or inactivation, help imaging or visualization with loading fluorescent drugs in vitro and in vivo, and play synergistic effects with other therapy approaches, like photodynamic therapy, sonodynamic therapy, and thermochemotherapy. Latterly, some renewed reports in drug loading and controlled release have led to their widespread applications in diverse fields, from cell level to clinical studies. This review introduces the basic characteristics of vaterite and briefly summarizes its research history, followed by synthesis strategies. We subsequently highlight recent developments in drug loading and controlled release, with an emphasis on the advantages, quantity capacity, and comparations. Furthermore, new opportunities for using vaterite in cell level and animal level are detailed. Finally, the possible problems and development trends are discussed.
2. Study on spleen strengthening effects and mechanisms of Atractylodes chinensis and Atractylodes coreana
Ming-Yang CUI ; Yi-Hui DING ; Yang QU ; Zhi-Li XU ; Qian CAI
Chinese Pharmacological Bulletin 2024;40(1):181-188
Aim To analyze the differences in plasma biomarkers and metabolic pathways between Atractylodes chinensis and Atractylodes coreana after intervention in spleen deficiency rats, and discuss the spleen strengthening mechanism of the two from a non targeted metabolomics perspective. Methods A spleen deficiency model was established in SD rats using a composite factor method of improper diet, excessive fatigue, and bitter cold diarrhea. To determine the content of gastrointestinal and immunological indicators, UHPLC-QE-MS technology was used, combined with principal component analysis (PC A) and orthogonal projections to latent structures-discriminant analysis (OPLS-DA) methods to search for biomarkers in plasma of spleen deficiency rats, and metabolic pathways were induced using the Pathway database. Results After administration of Atractylodes chinensis and Atractylodes coreana, various indicators in plasma of spleen deficiency rats showed varying degrees of regression. Metabolomics analysis showed that Atractylodes chinensis and Atractylodes coreana respectively recalled 70 and 82 plasma differential metabolites. Atractylodes chinensis mainly regulated two metabolic pathways : "Glycine, serine, and threonine metabolism, and "Thiamine metabolism". Atractylodes coreana mainly regulated five metabolic pathways, "Glycine, serine, and threonine metabolism", "Thiamine metabolism, "Pyrimidine metabolism", "Butanoate metabolism", and "Riboflavin metabolism". Conclusions Both Atractylodes chinensis and Atractylodes coreana have certain regulatory effects on spleen deficiency rats, and their mechanism of action may be related to regulating metabolic pathways such as "Glycine, serine, and threonine metabolism, and "Thiamine metabolism"in spleen deficiency.
3.Study on fluvoxamine maleate sustained-release pellets and its compression technology
Ming-hui XU ; Xing-yue ZHANG ; Qiao DONG ; Xia ZHAO ; Yu-ru BU ; Le-zhen CHEN
Acta Pharmaceutica Sinica 2024;59(2):439-447
In this study, fluvoxamine maleate sustained-release pellet system tablets were prepared and were used to evaluate their release behaviors
4.Investigation on the Correlation Between Traditional Chinese Medicine Constitution and Pathogenic Factors in Patients with Ankylosing Spondylitis
Shui-Ying LYU ; Ji-Chao YIN ; Peng-Gang XU ; De-Yu LIU ; Bao-Di REN ; Ying WANG ; Ming-Hui DING ; Jun-Li ZHANG
Journal of Guangzhou University of Traditional Chinese Medicine 2024;41(3):545-549
Objective To study the correlation between traditional Chinese medicine(TCM)constitution and pathogenic factors in patients with ankylosing spondylitis(AS).Methods One hundred patients of AS and their family members who had medical consultation in the Fifth Hospital of Xi'an(i.e.,Shaanxi Hospital of Integrated Traditional Chinese and Western Medicine)in August 2019 and September 2020 were selected as the study subjects.The guidelines of Classification and Determination of Traditional Chinese Medicine Constitution issued by the China Association of Chinese Medicine were adopted to determine the traditional Chinese medicine(TCM)constitution types of the study subjects.The sociodemographic information,living habits,clinical symptoms,and TCM constitution types of the AS patients and their family members were collected by means of questionnaires and clinical investigations,and then the pathogenic factors of the patients with AS were investigated.The binomial Logistic regression model was used to analyze the correlation between TCM constitution types and pathogenic factors in patients with AS.Results(1)Among the 100 AS patients,the majority of them had the biased constitutions,and the biased constitutions with the occurrence frequency in descending order were yang deficiency constitution,qi deficiency constitution,and damp-heat constitution,which accounted for 33.00%,14.00%,and 18.00%,respectively.(2)The prevalence rates of AS in the first-,second-,and third-degree relatives of AS patients were 56.25%,40.00%and 25.00%,respectively.For the positive rates of human leukocyte antigen B27(HLA-B27)in AS patients and their family members,HLA-B27 in AS patients was all positive,while the positive rates of HLA-B27 in the first-,second-,and third-degree relatives of AS patients were 44.31%,30.67%and 15.63%,respectively.(3)The results of regression analysis showed that the disease duration of AS patients was significantly correlated with qi deficiency constitution,the grading of sacroiliac arthritis was correlated with qi stagnation constitution,and age was correlated with blood stasis constitution(P<0.05 or P<0.01).The results indicated that disease duration and age were the important factors affecting the constitution types of AS patients,and disease duration was closely related to qi deficiency while age was closely related to blood stasis.Conclusion AS is a highly hereditary autoimmune disease,and its onset is associated with HLA-B27.Yang deficiency is the basic constitution type of AS,and damp-heat constitution is the main constitution type in the progression of AS(especially in the active stage of the disease).The prolongation of the disease will exacerbate the illness condition of AS and then the manifestations of qi deficiency will be more obvious.
5.Analysis of HPV infection and genotype distribution among 1 658 male reproductive health outpatients
Nazhakaiti ABUDUKELIMU ; Jian-Hui LI ; Tian-Cheng ZHANG ; Xin WANG ; Zhi-Ming XU ; Qian-Xi ZHU
Fudan University Journal of Medical Sciences 2024;51(1):69-75
Objective To investigate the human papillomavirus(HPV)infection and genotype distribution characteristics among male reproductive health outpatients,and to compare the differences among different age groups of outpatients.Methods A total of 1 658 males,visited in the Affiliated Hospital of Shanghai Institute of Planned Parenthood Research from 2018 to 2022,were selected and 23 HPV genotypes were detected by PCR-reverse dot hybridization.Results Among the 1 658 subjects,the overall HPV infection rate was 22.50%.Single infection accounted for 66.76%,which was the main infection type.HPV infection among different age groups were statistically significant(P<0.001),with HPV infection of 16.83%,22.87%,34.63%,and 29.35%for 18-30,31-40,41-50,and≥51 years,respectively.The top 5 high risk HPV genotypes were HPV52(3.56%),HPV16(3.26%),HPV39(2.41%),HPV51(2.17%),HPV58(2.17%),and the top 1 low risk HPV genotype was HPV81(2.90%).The proportions of infected individuals in this study that could be completely covered by bivalent,quadrivalent,and nine-valent HPV vaccines were 7.77%,12.33%,and 26.27%,respectively.Conclusion The predominant infection type among male reproductive health outpatients was single infection type.HPV 52,16,39,51 and 58 were the most common high risk genotypes,while HPV 81 was the most common low risk genotype.Individuals aged 41-50 years had the highest HPV infection rate.
6.Drug metabolism and excretion of14Cbirociclib in Chinese male healthy subjects
Quan-Kun ZHUANG ; Hui-Rong FAN ; Shi-Qi DONG ; Bin-Ke FAN ; Ming-Ming LIU ; Ling-Mei XU ; Li WANG ; Xue-Mei LIU ; Fang HOU
The Chinese Journal of Clinical Pharmacology 2024;40(14):2118-2123
Objective To evaluate the characteristics of the mass balance and pharmacokinetics of[14 C]birociclib in Chinese male healthy volunteers after a single oral administration.Methods This study used a 14 C labeled method to investigate the mass balance and biological transformation of birociclib in human.Subjects were given a single oral dose of 360 mg/50 pCi of[14 C]birociclib suspension after meals.The blood,urine,and fecal samples were collected at specified time points/intervals after administration.The radiation levels of 14 C labeled birociclib-related compounds in the blood,plasma,urine,and feces were analyzed using liquid scintillation counting.In addition,a combination of high-performance liquid chromatography and on-line/off-line isotope detectors was used to obtain radioactive isotope metabolite spectra of plasma,urine,and fecal samples,and high-resolution mass spectrometry was used to identify the main metabolites.Results A total of 6 healthy male subjects were enrolled in this study.The median peak time of radioactive components in plasma was 5.00 h and the average terminal elimination half-life was 43.70 h after administration.The radioactive components were basically excreted and cleared from the body within 288.00 hours after administration,and average cumulative recovery rate of radioactive drugs was(94.10±8.19)%.The radioactive drugs were mainly excreted through feces,accounting for(84.60±7.10)%of the dose of radioactive drugs administered.Urine was the secondary excretory pathway,accounting for 9.41%of the dose of radioactive drugs administered.Metabolic analysis indicated that the prototype drug was the main radioactive components in plasma samples.The main metabolites in plasma were RM4(XZP-5286),RM6(XZP-3584),and RM7(XZP-5736).The drugs were mainly cleared from the body in the form of prototype drugs and metabolites.In addition to prototype drugs,a total of 9 metabolites were identified and analyzed in plasma,urine,and fecal samples,all of which were phase 1 metabolites.The main metabolic and clearance pathways of drugs in the body were deethylation,diisopropylat ion,oxidation,etc.Conclusion After a single oral administration of[14C]birociclib suspension to healthy subjects,it was mainly cleared from the body in the form of prototype drugs and metabolites,with feces as the main excretory pathway and urine as the secondary excretory pathway.Drugs mainly undergo metabolic reactions in the body,such as deethylation,diisopropylation,and oxidation.The subjects were well tolerance after administration.
7.Clinical characteristics and drug resistance analysis of Pantoea agglomerans infection
Ming-Ming XIN ; Xu-Zhu MA ; Xiao-Hui WANG ; Ming-Gui LIN
The Chinese Journal of Clinical Pharmacology 2024;40(19):2763-2765
Objective To analyze the clinical characteristics of patients infected with Pantoea agglomerans and the drug resistance of the strains,providing corresponding reference for the rational use of antibiotics in clinical practice.Methods The clinical characteristics,treatment outcomes of patients infected with Pantoea agglomerans,and the drug resistance of Pantoea agglomerans were analyzed.Results Among the 22 patients infected with Pantoea agglomerans,16 were male(72.7%),and 6 were female(27.3%).Patients over 60 years old were the main infected population(72.7%),and 11 patients had underlying diseases that caused low immune function(50.0%).Lung,urinary system,and blood were the most common sites of infection,and 59.1%were nosocomial infections.Pantoea agglomerans showed good sensitivity to commonly used clinical antibiotics.The sensitivity rates of piperacillin/tazobactam,ertapenem,amikacin,and cefoperazone/sulbactam were 100.0%,and the sensitivity rate of levofloxacin was 94.4%,and the sensitivity rate of ceftriaxone was 81.3%.Conclusion Infections caused by Pantoea agglomerans are mostly nosocomial infections,and the main infected population is the elderly.Although most Pantoea agglomerans are sensitive to commonly used clinical antibiotics,some strains have shown multiple drug resistance.
8.Clinical trial of sindilizumab combined with albumin-bound paclitaxel chemotherapy in the treatment of advanced gastric cancer patients
Zheng-Dong WANG ; Cheng PAN ; Ai-Ming ZHOU ; Guang-Hui XU
The Chinese Journal of Clinical Pharmacology 2024;40(20):2968-2972
Objective To analyze the therapeutic effects and survival benefits of sintilimab combined with albumin-bound paclitaxel chemotherapy in the treatment of patients with advanced gastric cancer.Methods Patients with advanced gastric cancer were divided into the treatment group and the control group by cohort method.The control group was treated with albumin-bound paclitaxel-based chemotherapy[intravenous infusion of albumin-bound paclitaxel at 125 mg·m-2 from day 1 to day 8,for a cycle(21 days as a cycle);Tiggio capsule 40 mg·m-2·d-1 was taken orally for 1-14 days for 1 consecutive cycle;Trastuzumab was administered once every 3 weeks at an initial loading dose of 8 mg·kg-1,followed by maintenance treatment at a dose of 6 mg·kg-1 every 3 weeks].On this basis,the treatment group was treated with intravenous infusion of sintilimab injection at a dose of 200 mg·time-1 on the first day of each cycle,with 21 d as a cycle.After 6 cycles of continuous treatment,both groups were given maintenance treatment and were followed up for 8 months.The two groups were compared in terms of clinical efficacy,the levels of serum tumor markers[carbohydrate antigen 242(CA242),carbohydrate antigen 724(CA724),carcinoembryonic antigen(CEA),tissue polypeptide-specific antigen(TPS),soluble intercellular cell adhesion molecule-1(sICAM-1)and E-cadherin],survival and evaluated the safety.Results In this study,39 and 41 patients were enrolled in the control group and the treatment group,respectively.At the end of treatment,the objective response rates(ORR)in the treatment group and the control group were 56.10%and 33.33%;the disease control rates(DCR)were 78.05%and 48.71%.The differences were statistically significant(all P<0.05).After treatment,serum CA242 levels in the treatment group and the control group were(57.64±5.82)and(68.95±7.23)mg·L-1;CA724 levels were(36.58±3.79)and(43.65±4.48)U·mL-1;CEA levels were(17.33±1.78)and(20.16±2.35)ng·mL-1;TPS levels were(21.35±2.44)and(37.65±3.84)U·L-1;sICAM-1 levels were(216.77±22.53)and(275.34±28.63)ng·mL-1;E-cadherin levels were(12.15±1.36)and(9.87±1.45)ng·mL-1.The differences were statistically significant(all P<0.05).The average progression free survival(PFS)of the treatment group and the control group was 7.55 months and 7.17 months;PFS rates were 65.78%and 56.42%.The differences were statistically significant(P<0.05).The adverse drug reactions in the treatment group and the control group were mainly bone marrow suppression,nausea and vomiting,liver function damage,peripheral nerve paresthesia,and hypothyroidism.There was no statistically significant difference in the above adverse drug reactions between the treatment group and the control group(all P>0.05).Conclusion Sintilimab combined with albumin-bound paclitaxel chemotherapy is effective in the treatment of patients with advanced gastric cancer,which can significantly improve serum tumor markers and prolong PFS,with good safety.
9.Relationship between Phenotypic Changes of Dendritic Cell Subsets and the Onset of Plateau Phase during Intermittent Interferon Therapy in Patients with CHB
Liu YANG ; Yu Shi WANG ; Ting Ting JIANG ; Wen DENG ; Min CHANG ; Ling Shu WU ; Hua Wei CAO ; Yao LU ; Ge SHEN ; Yu Ru LIU ; Jiao Yuan GAO ; Jiao Meng XU ; Ping Lei HU ; Lu ZHANG ; Yao XIE ; Hui Ming LI
Biomedical and Environmental Sciences 2024;37(3):303-314
Objective This study aimed to evaluate whether the onset of the plateau phase of slow hepatitis B surface antigen decline in patients with chronic hepatitis B treated with intermittent interferon therapy is related to the frequency of dendritic cell subsets and expression of the costimulatory molecules CD40,CD80,CD83,and CD86. Method This was a cross-sectional study in which patients were divided into a natural history group(namely NH group),a long-term oral nucleoside analogs treatment group(namely NA group),and a plateau-arriving group(namely P group).The percentage of plasmacytoid dendritic cell and myeloid dendritic cell subsets in peripheral blood lymphocytes and monocytes and the mean fluorescence intensity of their surface costimulatory molecules were detected using a flow cytometer. Results In total,143 patients were enrolled(NH group,n = 49;NA group,n = 47;P group,n = 47).The results demonstrated that CD141/CD1c double negative myeloid dendritic cell(DNmDC)/lymphocytes and monocytes(%)in P group(0.041[0.024,0.069])was significantly lower than that in NH group(0.270[0.135,0.407])and NA group(0.273[0.150,0.443]),and CD86 mean fluorescence intensity of DNmDCs in P group(1832.0[1484.0,2793.0])was significantly lower than that in NH group(4316.0[2958.0,5169.0])and NA group(3299.0[2534.0,4371.0]),Adjusted P all<0.001. Conclusion Reduced DNmDCs and impaired maturation may be associated with the onset of the plateau phase during intermittent interferon therapy in patients with chronic hepatitis B.
10.Association of Cytokines with Clinical Indicators in Patients with Drug-Induced Liver Injury
Hua Wei CAO ; Ting Ting JIANG ; Ge SHEN ; Wen DENG ; Yu Shi WANG ; Yu Zi ZHANG ; Xin Xin LI ; Yao LU ; Lu ZHANG ; Yu Ru LIU ; Min CHANG ; Ling Shu WU ; Jiao Yuan GAO ; Xiao Hong HAO ; Xue Xiao CHEN ; Ping Lei HU ; Jiao Meng XU ; Wei YI ; Yao XIE ; Hui Ming LI
Biomedical and Environmental Sciences 2024;37(5):494-502
Objective To explore characteristics of clinical parameters and cytokines in patients with drug-induced liver injury(DILI)caused by different drugs and their correlation with clinical indicators. Method The study was conducted on patients who were up to Review of Uncertainties in Confidence Assessment for Medical Tests(RUCAM)scoring criteria and clinically diagnosed with DILI.Based on Chinese herbal medicine,cardiovascular drugs,non-steroidal anti-inflammatory drugs(NSAIDs),anti-infective drugs,and other drugs,patients were divided into five groups.Cytokines were measured by Luminex technology.Baseline characteristics of clinical biochemical indicators and cytokines in DILI patients and their correlation were analyzed. Results 73 patients were enrolled.Age among five groups was statistically different(P=0.032).Alanine aminotransferase(ALT)(P=0.033)and aspartate aminotransferase(AST)(P=0.007)in NSAIDs group were higher than those in chinese herbal medicine group.Interleukin-6(IL-6)and tumor necrosis factor alpha(TNF-α)in patients with Chinese herbal medicine(IL-6:P<0.001;TNF-α:P<0.001)and cardiovascular medicine(IL-6:P=0.020;TNF-α:P=0.001)were lower than those in NSAIDs group.There was a positive correlation between ALT(r=0.697,P=0.025),AST(r=0.721,P=0.019),and IL-6 in NSAIDs group. Conclusion Older age may be more prone to DILI.Patients with NSAIDs have more severe liver damage in early stages of DILI,TNF-α and IL-6 may partake the inflammatory process of DILI.

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