Objective To study the characteristics of the inpatients with cancer pain, the application of WHO three steps analgesic solution (three steps analgesic) and the application of traditional Chinese analgesic (TCM). Methods Retrospective investigation of distribution of cancer pain, situation of pain, application of TCM, and the application of conbination of three steps analgesic and TCM treatment, by using, clinical data from the oncology department of afflicated hospital of Liaoning university of TCM ranging from May, 2009 to June, 2010. Results 47.4% (517/1 090) of patiens were combined with cancer pain. Among the patients, majority were the middle-aged and old (59.19%) and male patients (57.63%). The abdominal pain (57.45%) and chest pain (37.91%) were topranks, and the distributions of pain period such assustainability (65.37%), moderately (53.38%), bloated pain (49.71%) and dull pain (29.98%) had larger proportion. The TCM excessive patterns(50.87%) were more than the TCM deficiency patterns (28.63%) or mixed TCM patters of excessive and deficiency patterns (20.50%). A total of 46 patients had mild pain, 76.09% of whom used TCM, 15.22% used first step drugs, and 8.69% used combination treatment, while 276 patients with moderate pain used second step analgesic, and 91.67%of them also used TCM, the rest195 patients with severe pain used third step analgesic, and 55.38%of them also used TCM. The time of pain release of TCM alone or combination of TCM and three steps analgesic were longer than the three steps analgesic alone. Conclusions Early intervention of traditional Chinese medicine on the patients with mild pain could reduce the dose of first step analgesic drugs, and TCM application at the second step could delay the speed of transtformfrom second to third step pain, and TCM could prevent the side effects of morphine when patients were with severe pain.

Objective: To optimize the formula and preparation process of docetaxel-loaded pluronic P123 micelles. Methods:Docetaxel-loaded pluronic P123 micelles were prepared by a thin-film hydration method and optimized by central composite design and response surface methodology. The influencing factors including the quantity of docetaxel, volume of organic phase, volume of hydra-tion and temperature of hydration were investigated with the entrapment efficiency as the index. The morphology of micelles was ob-served under a transmission electron microscope. The particle diameter and zeta potential were determined. The in vitro release property was measured by a dialysis method. Results:The relationship between the influencing factors and the evaluation parameter was fitted by multi-linear equation, quadratic polynomial equation and cubic polynomial equation, respectively. The results showed that the cubic polynomial equation was superior to the others according to the correlation coefficient. Docetaxel-loaded pluronic P123 micelles were spherical with the mean diameter, zeta potential, polydispersity index, encapsulation efficiency and drug loading of 108. 3 nm,-3. 99 mV, 0. 265, (97. 91 ± 0. 28)% and (3. 72 ± 0. 12)%, respectively. The cumulative release in vitro reached 95. 03% in 120 h, and docetaxel-loaded pluronic P123 micelles had notable sustained-release property. Conclusion: The technical process for do-cetaxel-loaded pluronic P123 micelles is simple and usable, and docetaxel-loaded pluronic P123 micelles show high encapsulation effi-ciency and notable sustained-release property.

Objective To analyze the distributional characteristics of NPC1L1 1 735 C>G polymorphism and the relation-ship between serum lipid levels and obesity in Guangxi Han population.Methods Genotyping of the NPC1L1 1 735 C>G poly-morphism of 409 cases of Han was performed by polymerase chain reaction and restriction fragment length polymorphism combined with gel electrophoresis in all subjects.The relationship of different genotypes in blood lipid levels and obesity were evaluated.Re-sults The frequency of CC,CG and GG genotypes was 39.40%,46.00% and 14.60% in Han.The frequency of C and G alleles was 62.35% and 37.65% in Han.The levels of BMI,LDL-C,ApoB was different among the three genotypes (P <0.05).The G al-lele carriers had higher serum LDL-C and ApoB levels than the G allele noncarriers (P <0.05 ).Serum lipid parameters and BMI were also correlated with some environmental factors.Conclusion The 1 735 C>G polymorphism in NPC1L1 gene may be correla-ted with serum lipid profiles and obesity,the G allele might increase the risk of hyperlipemia and obesity.

Objective:To explore the effect of oxycontin combined with gabapentin on the clinical cure and immunity for patients with neuropathic cancer pain.Methods:80 patients with neuropathic cancer pain were enrolled in our hospital from June to 2016 July,of which patients divided into two groups randomly,Group A(n=40) accepted oxycontin treatment,and Group B (n=40) adopted gabapentin based on the patients in Group A.The VAS score and curative effect of the patients were compared between two groups;The quality of life of all patients were evaluated post-treatment,and the change of immunity indexes were compared and analyzed.Results:The VAS score of all patients was decreased significantly compared with pre-treatment (P＜0.05),and the score of Group B was lower than those patients in Group A (P＜0.05);The total remission rate of Group B was significantly higher than those of Group A (P＜0.05);after treatment,the score of appetite,emotion,sleep,daily activities,social communications of all patients decreased significantly compared with pre-treatment (P＜0.05),and the change of Group B was decrease significantly higher than those patients in Group A (P＜0.05);the immune index of two groups was significantly increased (P＜0.05),and the level of the indexes including IgG,IgA,IgM,CD4+,CD4+/CD8+ and circulating immune complex (CIC) increased compared with pre-treatment remarkably (P＜0.05),and which change in Group B was significantly higher than Group A (P＜0.05).Conclusions:Oxycontin combined with gabapentin for patients with neuropathic cancer pain deserved popularization in clinical,and which not only possessed well clinical effect,but also increased the quality of life.

Objective:To observe the stability of thymosin ?_1 microspheres under preparation conditions.Methods: Using HPLC method,we investigated the influence of different temperatures(-20 ℃, 6-8℃,60℃),sonification time(10-60 s) and pH values (pH 4.0,7.0 and 10.0) on thymosin ?_1 stability.Results: Under the conditions of frozen environment(-20℃) and refrigeration(6-8℃), thymosin ?_1 remained stable for 30 d.Thymosin ?_1 did not degrade in 60℃ water bath for 12 h or in phosphate buffer solution(PBS,pH 4.0) under 37℃ for 14 h.The sonification time within 60 s was found to be safe for the preparation.Conclusion: Thymosin ?_1 is stable under these preparation conditions.

Objective:To prepare injectable interferon ?-2b(IFN-?-2b) loaded microsphere and develop a long-acting dosage form.Methods: IFN-?-2b loaded microspheres were prepared with poly(lactic-co-glycolic acid)(PLGA) as carrier material by double emulsion(w/o/w) method and solid in oil in oil(s/o/o) method separately.Physical and chemical characteristics of microspheres(mean diameter,morphology and drug entrapment efficiency) were evaluated;the in vitro release behavior and influencing factors of the microspheres were determined by micro-BCA(bicinchoninic acid) method;and IFN-?-2b stability during encapsulation and in vitro release was evaluated by sodium dodecyl sulfate polyacrylamide gel electropheresis.Results: The 2 types of microspheres produced had good shape and dispersive quality and a drug entrapment efficiency of more than 80%.IFN-?-2b bulk ultrafitration can significantly influence the mean diameter and in vitro release behavior of microspheres prepared by w/o/w method.The accumulated release(within 1 month) of the microspheres prepared by both methods was significantly improved when using PLGA with lower inherent viscosity.SDS-PAGE test showed aggregation of IFN-?-2b with s/o/o method,while there was no difference between the electrophoretic behavior of bulk IFN-?-2b and IFN-?-2b in microspheres prepared by w/o/w method.Conclusion: IFN-?-2b can be encapsulated into injectable microspheres to yield a one-month continuous release by both w/o/w method and s/o/o method.

OBJECTIVE:To study the cytotoxicity of the graft polymer after polyethyleneimine (PEI) had been modified by polyoxyethylene stearate (POES) and the property of the carrier,grafted-polymer/DNA complexes. METHODS: To modify PEI by conjugating PEI to POES with succinimidyl carbonate method. Structural analysis of synthesized polymer was performed by using 1H-NMR. Agarose gel electrophoresis (AGE) behavior of the graft polymer/DNA complexes was observed with particle size and zeta potential measured. The cytotoxicity of the graft polymer was evaluated by MTT method. The pGL3-lus served as a reporter gene,and the luciferase activity was determined to evaluate the transfection efficiency of grafted-polymer/DNA on Hela cells. RESULTS: 1H-NMR showed that the graft polymer had high purity. AGE showed that the DNA-wrapping ability of the graft polymer were increased with the increase of N/P ratios,and decreased with the increase of the POES graft number. The size of complexes was below 300 nm,and the zeta potential of the complexes increased with the increase of N/P ratios. The graft polymer showed significantly lower cytotoxicity than PEI. The graft polymer with lower POES graft number had higher transfection efficiency. CONCLUSIONS: The POES-modified PEI can be used as an effective non-viral genetic carrier.

The aim of this paper is to compare the cytotoxicity and cellular uptake efficiency of three kinds of poly(b-benzyl-L-amino) block-poly(ethylene glycol) nanoparticles (PXA-PEG-NPs) using Calu-3 cells, and select one as a nasal drug delivery vector for curcumin (Cur). Poly(gamma-benzyl-L-glutamate) block-poly(ethylene glycol) nanoparticles (PBLG-PEG-NPs), poly(gamma-benzyl-L-lysine) block-poly(ethyleneglycol) nanoparticles (PZLL-PEG-NPs) and poly(gamma-benzyl-L-aspartate) block-poly(ethylene glycol) nanoparticles (PBLA-PEG-NPs) were prepared by emulsion-solvent evaporation method. MTT assays were used to evaluate the cytotoxicity of PXA-PEG-NPs against Calu-3 cells. The cellular uptake of nanoparticles was visualized by an inverted fluorescence microscope and quantified by a flow cytometer. The results indicated that even at high concentration of 2 mg x mL(-1) the three nanoparticles had no cytotoxicity on Calu-3 cells. Compared to the curcumin solution, the three curcumin-loaded PXA-PEG-NPs showed significantly higher cellular uptake efficiency on Calu-3 cells (at equal concentration of curcumin with 5 microg x mL(-1) Cur solution), PBLG-PEG-NPs group was the highest. The cellular uptake increased with incubation time, and has positive correlation with nanoparticle concentration. In brief, PXA-PEG-NPs are conducive to delivery Cur into cells, and PBLG-PEG-NPs might be provided as a good nasal drug delivery carrier.

A series of novel riminophenazine derivatives bearing an alkyl substituent attached to N-5 and imino nitrogen at C-3 position of the phenazine ring were obtained through rational drug design, aiming to maintain high anti-tubercular activity, lower toxicity and reduce lipophilicity. All target compounds were prepared by utilizing simple and flexible synthetic route and evaluated against Mycobacterium tuberculosis H37Rv and screened for mammalian cytotoxicity. The results demonstrated that compounds with a cyclopropyl substituent at N-5 position were more active than the reference compound clofazimine. In particular, 2-(4-chloroanilino)-5-cyclopropyl-3-(4-methoxycyclohexyl) imino-3, 5-dihydrophenazine (25) was found to be the most potent compound with low cytotoxicity and lipophilicity. This compound could serve as a valuable lead molecule for further optimization.

Objective To modify polyethyleneimine (PEI) by using Poloxamer 188 (P188) , and evaluate its related feature as carriers of genes in vitro. Methods PEI was modified through conjugating one hydroxyl group of P188 to the amino group of PEI by carbonate method. Structural analysis of synthesized polymer was performed by using 1H-NMR. The particle size and Zeta potential of synthesized polymer /DNA complexes were measured. The cytotoxicity of the complexes was evaluated using MTT method in MCF-7 cells, HeLa cells and HepG2 cells. The pGL3-lus was used as a reporter gene, and the transfection efficiency of complexesat HeLa cells was evalutated by measuring activity of luciferase. Results The result of 1H-NMR showed the purity of these synthesized polymers was high. The particle size of complexes were decreased with the increment of N /P ratios. The Zeta potential of complexes increased with the increment of N /P ratios. The cytotoxicity of the complexes increased with the increment of N /P ratios. The synthesized polymers showed lower cytotoxicity than unmodified PEI. The new synthesized polymers had maintained the high transfection efficiency at high N /P ratios. In particular, the optimal transfection efficiency of (P188) 1- PEI (N /P = 24) was significantly higher than that of PEI (N /P = 6) . Conclusion The P188 modifed PEI can serve as a effective non-viral gene carriers to transfect Hela cells.