1.Preparation and performance evaluation of dissolving microneedles with a single matrix of Pterocarya hupehensis total flavonoids
Xingxing GAO ; Dan CHEN ; Yan XIA ; Lin DING ; Xingyue CHEN ; Yang XIANG ; Lunzhi LIU ; Lin YUAN
China Pharmacy 2026;37(16):2097-2104
OBJECTIVE To screen a single matrix, prepare dissolving microneedles of Pterocarya hupehensis total flavonoids(PHTF-MN), and characterize it while evaluating its analgesic effects.METHODS Using microneedle morphology and puncture rate as evaluation indicators, the matrix was screened from polyvinyl alcohol (PVA), polyvinylpyrrolidone K30 (PVP K30), PVP K90, and sodium hyaluronate with relative molecular weights of 15 000 and 60 000 (HA 1.5w and HA 6w ). PHTF-MN was prepared by the layer-by-layer casting method with the selected matrix, and the appearance and morphology, total flavonoid content, mechanical properties, puncture performance, dissolution properties, and drug release behavior of the obtained PHTF-MN were characterized. Using male BALB/c mice as test subjects and aspirin (ASA) as a positive control, the analgesic effects of the microneedles were evaluated using a formalin-induced pain model.RESULTS Blank microneedles prepared with 30% HA 1.5w exhibited optimal surface flatness and the membrane puncture rate (through 4 layers of parafilm membrane) reaching 78%. The PHTF-MNs (with PHTF contents of 10, 20, 30, 40, and 50 mg/g in the matrix) exhibited uniform arrays and intact tips, with RSDs for total flavonoid contents all below 7% ( n =8). The single-needle puncture forces were 1.46 and 1.07 N (with PHTF contents of 30 and 50 mg/g in the matrix, respectively). The skin penetration rate approached 100%, with visible puncture marks in the stratum corneum and drug residue (with a PHTF content of 50 mg/g in the matrix). After 30 min of fixation, the needles had almost completely dissolved, and the skin retention rates all exceeded 90% (with PHTF contents of 10, 30, and 50 mg/g in the matrix, respectively). The cumulative release within 8 h was (134.64±2.03) μg/cm 2 , and the fit to the first-order kinetic equation ( R 2 =0.950 1) was highest (with a PHTF content of 50 mg/g in the matrix). Low- and high-dose PHTF-MN (containing 85.26 and 145.03 μg of total flavonoids per patch, respectively; 1 patch/day) significantly shortened the cumulative time of phase Ⅱ pain response in mice ( P <0.05), with pain inhibition rates (43.67% and 59.78%) comparable to those of ASA (53.70%).CONCLUSIONS PHTF-MN using HA 1.5w as a single matrix was successfully prepared. This formulation features a simplified preparation process, uniform drug loading, favorable mechanical properties, resistance to fracture, and rapid dissolution. Its drug release behavior conforms to a first-order kinetic model, and its analgesic effect is comparable to that of ASA.
2.Effect and mechanism of melatonin on the epithelial-mesenchymal transition of human peritoneal mesenchymal cells
Shan LIU ; Mingxia ZHANG ; Lunzhi LIU
Journal of China Medical University 2024;53(3):235-239
Objective To investigate the effect and mechanism of melatonin on the epithelial-mesenchymal transition(EMT)of human peritoneal mesothelial cells.Methods A human peritoneal mesoepithelial cell line(HMrSV5)was cultured.Decorin(DCN)overex-pression and knockout plasmids were constructed.The cells were divided into the normal,TGF-β1,TGF-β1+melatonin,TGF-β1+mela-tonin+siDCN,TGF-β1+melatonin+siNC,and TGF-β1+DCN groups.The cell proliferation and survival rates were determined using Cell Counting Kit-8(CCK-8).The protein and mRNA expression levels of DCN,TGF-β1,Smad2,and E-cadherin were detected by Western blotting and real-time polymerase chain reaction(PCR),respectively.Results The CCK-8 assay showed that the cell survival rates were higher in the TGF-β1+melatonin,TGF-β1+melatonin+siDCN,and TGF-β1+DCN groups than the TGF-β1 group(P<0.05).The cell sur-vival rate was higher for the TGF-β1+melatonin group than the TGF-β1+melatonin+siDCN group(P<0.05).Western blotting and real-time PCR showed DCN and that E-cadherin were significantly down-regulated in the TGF-β1 group compared with the control group(P<0.05).Compared with the TGF-β1 group,the TGF-β1+melatonin and TGF-β1+melatonin+siDCN groups showed up-regulated E-cadherin and DCN expression levels and down-regulated TGF-β1 and Smad2 expression levels(P<0.05).Compared with the TGF-β1+melato-nin+siDCN group,the TGF-β1+melatonin+siDCN group showed up-regulated E-cadherin and DCN expression levels and down-regulated TGF-β1 and Smad2 expression levels(P<0.05).Conclusion Melatonin can delay the EMT of human peritoneal mesoepithelial cells,and the DCNgene may be an important target to inhibit the EMT of these cells.
3.Analyse curative effect and immune indices of tripterygium glycosides on aged glomerulonephritis rats
Shan LIU ; Lunzhi LIU ; Zhihui TAN ; Xiaofen YANG
Chinese Journal of Immunology 2014;(5):627-629
Objective:To analyse the curative effect and immune indices of tripterygium glycosides on glomerulonephritis rats . Methods:Aged Wistar rats were randomly divided into 3 groups , Group A:glomerulonephritis model rats received tripterygium glyco-sides treatment;Group B:healthy Wistar rats received no treatment; Group C: glomerulonephritis model rats received no treatment . Results:12 weeks after experiment , Group A and Group C had higher levels of 24-hour urine protein than Group B and these of pre-experiment(P<0.05).Group A had a lower level of 24-hour urine protein than Group C(P<0.05).Group A and Group C had high-er levels of TG, TC than Group B, with lower levels of ALB than Group B (P<0.05).Group A had lower levels of TG, TC than Group C, but a higher level of ALB than Group C (P<0.05).Group A had a higher rate of 0-1 grades in pathology grade than group C(χ2 =6.667,P=0.010).Group C had higher levels of TNF-αand IL-6 than Group B and Group A (P<0.05).Conclusion:Tripterygium glycosides can reduce the urine protein excretion of rats that with mesangial proliferative glomerulonephritis , rectify dyslip-idosis, raise plasma-albumin, decrease the protein expression of TNF-αand IL-6 in glomerulus.
4.Clinical observation on the efficiency of intravenous sucrofer combined with erythropoiesis stimulating factor in treatment of patient with refractory renal anemia
Chinese Journal of Primary Medicine and Pharmacy 2012;19(14):2133-2134
Objective To investigate the clinical efficiency and security of Fe(OH) 3-sncrose-compond combined with erythropoietin on renal anemia.Methods 30 cases of oral iron combined with erythropoietin in the unsatisfactory uremia patients undergoing maintenance hemodialysis,the cases were randomly divided into two groups:the treatment group(n =16) using intravenous sucrose iron 100mg,twice a week,after a total of 1000mg,then l00mg,once 1 -2 weeks;the control group(n =14) continue to oral:ferrous succinate 0.2g,three times everyday,erythropoietin dose was the same in lothgroups for g weeks.Results Hemoglobin was significantly higher(P < 0.01) and hematocrit was significantly higher(P <0.01),and serum ferritin significant increased(P <0.0l) in sucrose iron treatment group than these of the control group;the patients of treatment group have obviously improved in spirit,appetite,physical and life quality and so on.Sometimes,nausea,vomiting,skin itching were complained lut without significant side effects.While in the control group limited increase in the level of hemoglobin was seen,the majority had nausea,abdominal discomfort,poor appetite.Conclusion The efficiency of intravenous sucmfer combined with erythropoietin in treatment of renal anemia was effective than conventional oral iron combined with erythropoietin and with fewe adverse reactions.

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