OBJECTIVE: To develop phospholipid vehicle to improve the bioavailability of curcumin after oral administration. METHODS: Two phospholipid vehicles, including phospholipid complex and liposome, were prepared. The characteristics, such as entrapment efficiency, shape, size, and structure, were compared. An in situ recirculation method was used to investigate the intestinal absorption of both phospholipid vehicles. RESULTS: Spherical or elliptical vesicles were observed under transmission electron microscope and atomic force microscope after the phospholipid vehicles were dispersed in water. The average entrapment efficiencies of phospholipid complex and liposome were (90.81 ± 1.32)% and (81.59 ± 2.41)% respectively. The mean sizes and zeta electric potentials were (91.69 ± 12.26) nm and (-13.73 ± 4.37) for the phospholipid complex, and (76.39 ± 8.58) nm and (-11.27 ± 1.26) for the liposomes. DSC, IR and Raman spectrum verified that there was reaction between curcumin and the phospholipid polar group around phosphorus atom in the complex but not in the liposomes. The apparent permeability coefficients (Papp) in the whole intestine were (1.1312 ± 0.0498) and (0.4780 ± 0.0120) 10 -6 cm-2 · s-1 for the complex and liposome respectively, which were 17.60 times and 5. 90 times higher than the crude drug. The absorption rate constants (Ka) and Papp of the complex were higher than the liposomes at duodenum, colon and ileum significantly. There was no difference at jejunum. CONCLUSION: Phospholipid complex can promote the absorption of curcumin in a larger degree than liposomes.

Objective To comprehensively analyze the nursing measures of early thrombolytic therapy for acute myocardial infarction. Methods 140 patients with acute myocardial infarction admitted in our hospital from October 2013 to October 2016 were randomly divided into control group (70 cases) and experimental group (apply early thrombolytic care on the basis of routine nursing method, 70 cases) according to different nursing methods. SPSS20.0 statistical software was used to analyze the incidence of complications, mean hospitalization time, average bedridden time and total satisfaction. Results The average hospital stay and the average length of stay in the experimental group were much shorter than those in the control group (P<0.05). The total score of the experimental group was much higher than that of the control group (P<0.05). The complication rate of the experimental group was much lower than that of the control group (P<0.05). Conclusion Nursing measures for early thrombolytic therapy in patients with acute myocardial infarction can significantly reduce the incidence of complications in patients.

To study the interaction of drugs of different properties, namely puerarin, borneol and catalpol in the process of in- clusion, in order to explore the inclusion regularity of multi-component and multi-property traditional Chinese medicine compound in- clusions. With HP-β-CD as the inclusion material, the freeze-drying method was used to prepare the inclusion. The inclusion between puerarin, borneol and catalpol was tested by measuring the inclusion concentration, DSC and X-ray diffraction. According to the find- ings, when insoluble drugs puerarin and borneol were included simultaneously, and puerarin was overdosed, puerarin included was almost equal to puerarin included, and borneol was not included. When puerarin was under-dosed, and HP-β-CD was overdosed, borne- ol was included, and the simultaneous inclusion was lower than the separate inclusion of borneol. When water-soluble drug catalpol was jointly included with puerarin or borneol, the simultaneous inclusion was almost the same with their separate inclusion, without charac- teristic peak of catalpol in DSC and X-ray diffraction patterns. There is a competition in the simultaneous inclusion between water-solu- ble drugs puerarin and borneol and a stronger competition in puerarin. The water-soluble drug catalpol could be included with HP-β-CD with no impact on the inclusion of puerarin or borneol.
2-Hydroxypropyl-beta-cyclodextrin ; Bornanes ; chemistry ; therapeutic use ; Brain Ischemia ; drug therapy ; Drug Compounding ; methods ; Freeze Drying ; Iridoid Glucosides ; chemistry ; therapeutic use ; Isoflavones ; chemistry ; therapeutic use ; Solubility ; beta-Cyclodextrins ; chemistry

To investigate the effect of Jiawei Foshou San and its various combined administration on hepatic P450 enzyme activity and hepatocyte morphology in rats. Rats were orally administered with drugs for four weeks and then sacrificed to prepare liver microsomes. The liver microsomes were incubated with the cocktail method; The metabolites were determined with the rapid liquid chromatography with tandem mass spectrometry (LC-MS/MS) to investigate the hepatocyte P450 enzyme activity. In addition, the hepatic pathological changes were observed by using the hematoxylin and eosin (HE) staining. Compared with the control group, the enzyme activity of CYP1A2 and CYP3A4 in the Jiawei Foshou san group showed a significant rise (P < 0.05); the enzyme activity of CYP1A2, CYP2C9, CYP2D6, CYP2E1 and CYP3A4 in the ferulic acid + ligustrazine group and the ligustrazine + tetrahydropalmatine group showed a significant rise (P < 0.05) ; the enzyme activity of CYP1A2, CYP2D6 and CYP2E1 in the ligustrazine group showed a significant rise (P < 0.05); the enzyme activity of CYP3A4 in the ferulic acid group showed a significant reduction (P < 0.05). After the administration with various drugs, the hepatocyte morphologies in the ferulic acid group and the ligustrazine group were normal. The pathological changes were observed in the tetrahydropalmatine group, such as unclear boundary of hepatic lobules, disordered hepatic cell arrangement, blurred edge, anisokaryosis and infiltration of inflammatory cells. The ferulic acid + tetrahydropalmatine group, the ligustrazine + tetrahydropalmatine group and the Jiawei Foshou San group also showed inflammatory infiltration, but with less pathological changes, particularly the Jiawei Foshou San group. The study result shows that Jiawei Foshou San can induce the enzyme activity of CYP1A2 and CYP3A4, and ligustrazine may be the effective substance for inducing CYP1A2. Its combination with ferulic acid and ligustrazine can significantly reduce the liver toxicity of tetrahydropalmatine.
Animals ; Cytochrome P-450 Enzyme System ; metabolism ; Drugs, Chinese Herbal ; administration & dosage ; Female ; Hepatocytes ; drug effects ; enzymology ; Microsomes, Liver ; drug effects ; enzymology ; Rats ; Rats, Sprague-Dawley

This paper introduced an experimental study of polylacticacid (PLA) nanoparticles of lipophilic anti-cancer herb drug using a precipitation method. Cucurbitacins (Cu) and Curcuminoids (Cur) were selected to be model drugs. They had similar solubility but their incorporation effects were significantly different: the average drug entrapment ratio, the average drug loading and the average drug recovery were 38.53%, 2.21% and 27.02% respectively; while those of Cur-PLA-NP were 94.36%, 14.35% and 91.23% respectively. To analyse the reason, drug incorporation process was investigated. By measuring solvent evaporation rate, ratio of drug PLA precipitates, drug distribution in system and entrapping ratio at different time of preparation, we found the difference of precipitation velocity of drug was the main reason. We also concluded that not all lipophilic drug can be well entrapped into PLA nanoparticle by nanoprecipitation method. The drug incorporation depended on the interations among drug, PLA and organic solvents, in addition to the solubility of the drug.
Antineoplastic Agents, Phytogenic ; chemistry ; Chemical Precipitation ; Cucurbitacins ; chemistry ; Curcumin ; chemistry ; Drug Compounding ; methods ; Drugs, Chinese Herbal ; chemistry ; Lactic Acid ; chemistry ; Nanoparticles ; Nanotechnology ; methods ; Particle Size ; Polyesters ; Polymers ; chemistry

The association rate constant and dissociation rate constant are important parameters of the drug-cyclodextrin supermolecule systems, which determine the dissociation of drugs from the complex and the further in vivo absorption of drugs. However, the current studies of drug-cyclodextrin interactions mostly focus on the thermodynamic parameter of equilibrium constants (K). In this paper, a method based on quantitative high performance affinity chromatography coupled with mass spectrometry was developed to determine the apparent dissociation rate constant (k(off,app)) of drug-cyclodextrin supermolecule systems. This method was employed to measure the k(off,app) of meloxicam and acetaminophen. Firstly, chromatographic peaks of drugs and non-retained solute (uracil) on β-cyclodextrin column at different flow rates were acquired, and the retention time and variance values were obtained via the fitting the peaks. Then, the plate heights of drugs (H(R)) and uracil (H(M,C)) were calculated. The plate height of theoretical non-retained solute (H(M,T)) was calculated based on the differences of diffusion coefficient and the stagnant mobile phase mass transfer between drugs and uracil. Finally, the k(off,app) was calculated from the slope of the regression equation between (H(R)-H(M,T)) and uk/(1+k)2, (0.13 ± 0.00) s(-1) and (4.83 ± 0.10) s(-1) for meloxicam and acetaminophen (control drug), respectively. In addition, the apparent association rate constant (k(on,app)) was also calculated through the product of K (12.53 L x mol(-1)) and k(off,app). In summary, it has been proved that the method established in our study was simple, efficiently fast and reproducible for investigation on the kinetics of drug-cyclodextrin interactions.
Acetaminophen ; chemistry ; Chromatography, Affinity ; Drug Interactions ; Kinetics ; Mass Spectrometry ; Thermodynamics ; Thiazines ; chemistry ; Thiazoles ; chemistry ; beta-Cyclodextrins ; chemistry

Objective To construct a eukaryofic expression vector for A PP695 gene carrying green fluorescence protein (GFP) gene. Methods RT-PCR was used to amplify the full-length APP695 cDNA. The PCR products and the eukaryotic expression vector pIRES2-EGFP were digested by restriction endonueleases, and the digested APP695 gene was inserted into the digested eukaryotic expression vector. The positive recombinants were identified by PCR analysis, Nhe Ⅰ and Hind Ⅲ digestion and sequence analysis. Results The 2088-bp DNA fragment was amplified by PCR from the plasmid pCB6, and an identical DNA fragment was also amplified from the recombinants. The products of double restriction enzyme digestion were A PP695 gene with a 5.3-kb DNA fragment. Sequence analysis confirmed successful insertion of A PP695 gene into pIRES2-EGFP vector. Conclusion The eukaryotie expression vector pIRES2/APP695-EGFP has been successfully constructed.

Objective To evalute the efficacy of high-resolution CT(HRCT) in differential diagnosis and treatment of chronic suppurative otitis media and cholesteatoma otitis media by soft-tissue shadows. Methods HRCT scanning was performed in 120 cases, 153 ears, with chronic otitis suppurative media and cholesteatoma otitis media, of which original data were processed with multi-planar reconstructtion (MPR) and maximum intensity projection ( MIP) , the characteristics of the soft-tissue shadows' growth, window width or window leveling and bony destruction were respectively observed, as well as compared with the surgery findings. Results In 120 patients (133 ears), 109 ears were diagnosed as cholesteatoma otitis media, and 44 ears were diagnosed as chronic suppurative otitis media, among which 33 ears had granulation tissue and 11 ears had secretion. One hundred and seven ears were postoperatively diagnosed as cholesteatoma otitis media, among which 25 ears had granulation tissue. Among 46 ears of chronic suppurative otitis media, 35 ears had granulation tissue, and only 11 ears had secretion. A 98. 6% diagnostic accuracy can be reached with HRCT in diagnosing cholesteatoma otitis media and chronic suppurative otitis media. The Youden's index was 0. 98, 0. 98 and 1. 00 respectively with HRCT in diagnosing cholesteatoma, granulation tissue and secretion. Conclusions Combination of the three different imaging methods, axial images, coronal MPR images and MIP images, can improve the efficacy of the HRCT diagnosis and definite chronic otitis media, which can be routinely used for surgery plan.

OBJECTIVETo study the changes of peripheral plasmacytoid dendritic cells and lymphocyte subsets in patients with chronic hepatitis B (CHB) during consensus interferon (CIFN) treatment.

METHODSTwenty-three patients with CHB were treated with CIFN for 24 weeks and followed up for another 24 weeks. Peripheral plasmacytoid dendritic cells and lymphocyte subsets were measured throughout the treatment and follow-up periods.

RESULTSAfter CIFN treatment, 43.5% of the patients had virological and biochemical responses. The percentage and absolute number of peripheral plasmacytoid dendritic cells decreased significantly (P less than 0.05), the number of CD3+ cells, CD4+ T cells, B cells and the ratio of CD4+/CD8+ cells decreased also (P less than 0.05), but the number of CD8+ T cells and NK cells increased (P less than 0.05).

CONCLUSIONSConsistent virological and biochemical responses can be seen in some patients with CHB virus infection after CIFN treatment, and the percentage and number of their peripheral plasmacytoid dendritic cells greatly decreased, but the number of CD8+ T cells and NK cells increased.

Adult ; Antiviral Agents ; therapeutic use ; CD8-Positive T-Lymphocytes ; immunology ; Dendritic Cells ; immunology ; Female ; Hepatitis B, Chronic ; drug therapy ; immunology ; Humans ; Interferon-alpha ; therapeutic use ; Killer Cells, Natural ; immunology ; Male ; Young Adult

OBJECTIVETo explore the effects of ICAM-1 gene transfection on the differentiation of MSCs to adipocytes.

METHODSThe recombinant retroviral expression plasmid MIGR1-ICAM-1 containing full length of mouse ICAM-1 gene was constructed. The constructed plasmid MIGR1-ICAM-1, empty plasmid MIGR1 and packaging plasmid ECOS were transfected into T293 cell lines and then the supernatant generated from T293 cells were used to infect mouse MSCs cell line C3H10T 1/2. The transfective efficiency was determined by inverted fluorescence microscope, real-time PCR and flow cytometry. Furthermore, ICAM-1 overexpressing MSCs (C3H10T 1/2-ICAM-1) and empty vector transfection MSCs (C3H10T 1/2-MIGR1) were cultured in medium with or without induction reagents, Oil-red-O staining was used to detect the lipid accumulation, and the expression of transcriptional factors C/EBPα and PPARγ, which were key factors in the differentiation of MSCs to adipocytes, were tested by real-time-PCR.

RESULTSThe recombinant retrovirus vector containing mouse ICAM-1 gene was successful constructed. After transfection into MSCs cell line C3H10T 1/2, the overexpression ICAM-1 MSCs cell line (C3H10T 1/2-ICAM-1) and control cell line (C3H10T 1/2-MIGR1) were obtained. Furthermore, these two cell lines were treated without or with adipocytic induction reagents, C3H10T 1/2-ICAM-1 showed significantly lower mRNA expression level for C/EBPα [(1.2 ± 0.7), (2.9 ± 0.9)] and PPARγ [(1557.6 ± 70.2), (7547.0 ± 442.2)] when compared with C3H10T 1/2-MIGR1 [(5.8 ± 0.5), (23.0 ± 2.3) and (2453.0 ± 215.6), (9856.3 ± 542.2)](P < 0.05). Moreover, little lipid droplet and decreased quantity of adipocytes were detected in C3H10T 1/2-ICAM-1 [(3.2 ± 0.5)/well, (12.2 ± 3.8)/well] than that in C3H10T 1/2-MIGR1 [(11.2 ± 0.4)/well, (51.3 ± 2.8)/well] (P < 0.05).

CONCLUSIONOverexpression of ICAM-1 in MSCs can inhibit its adipocytic differentiation.

Adipocytes ; cytology ; Animals ; Cell Differentiation ; Cell Line ; Intercellular Adhesion Molecule-1 ; genetics ; Mesenchymal Stromal Cells ; cytology ; Mice ; Transfection