Improvement of in vitro dissolution and physical stability for spironolactone solid dispersion formulated with Soluplus / 药学学报

Spironolactone, a class II drug of the biopharmaceutics classification system, has low oral bioavailability due to poor solubility. Spironolactone solid dispersions were prepared using the solvent method in order to improve its aqueous solubility. Optimization studies of spironolactone solid dispersions were performed using in vitro dissolution tests. Differential scanning calorimetry, X-ray diffraction and Fourier transform infrared were used to investigate the physical state of the drug in carrier materials and to detect the possible interactions between the drug and carrier materials in the solid dispersions. In addition, stress tests were employed to elucidate the key factors which have influence on the stability of the spironolactone solid dispersions. Results showed that spironolactone in the solid dispersions formulated with Soluplus and HPMC-E5 were both in amorphous state and the hydrogen bonds between the drug and carrier materials were formed in the solid dispersion. Therefore, the in vitro dissolution of spironolactone was also significantly enhanced. Stress tests demonstrated that the physical stability of spironolactone solid dispersions prepared with Soluplus was greatly improved compared to those formulated with HPMC-E5. Thus, spironolactone solid dispersion formulated with Soluplus using the solvent method could be used to improve the in vitro dissolution and stability of poorly soluble drugs.

Suppressing the growth of Hep-2 human laryngeal cancer cells by silencing survivin gene in vitro and in vivo / 中华耳鼻咽喉头颈外科杂志

<p><b>OBJECTIVE</b>To study the effect of silencing survivin on the growth of Hep-2 human laryngeal cancer cells in vitro and in vivo.</p><p><b>METHODS</b>Hep-2 cells were transfected with pGCsilencer-siRNA-survivin (psi-survivin)by Lipofectamine 2000. The mRNA and protein expressions of survivin were detected by semi-quantitative RT-PCR and Western blot, respectively. Cell proliferation activity was measured by MTT assay. Apoptosis was assessed by flow cytometry. The implanted tumors were formed from injected Hep-2 cells in nude mice. After the tumor formation, psi-survivin was injected into peritumor tissues. The growth of tumor were observed. The tumor volume was calculated and the tumor growth curve was plotted. The expression of survivin in tumor tissues was detected by Western blot. The tumor cell apoptosis was observed by Tunel staining.</p><p><b>RESULTS</b>The sequence-specific siRNA of survivin inhibited the expressions of survivin mRNA and protein. The inhibition rates of survivin mRNA and protein expression were 54.4% and 37.0% respectively. Also the growth of Hep-2 cells was inhibited significantly, with a decrease by 71.7%. By the day 32 of tumor growth, the mean tumor volumes were (1443.9 ± 230.5) mm(3) (x(-) ± s) in saline control group, (1348.5 ± 198.4) mm(3) in plasmid-negative control group, and (624.6 ± 188.4) mm(3) in psi-survivin group, respectively (t = -5.917, P < 0.01). In the implanted tumors injected with psi-survivin, survivin protein expression was down-regulated significantly, with a inhibition rate of 41.8%. Tunel staining showed the apoptosis occurred in the implanted tumors.</p><p><b>CONCLUSION</b>Silencing survivin could significantly inhibit the growth of Hep-2 human laryngeal cancer cells in vitro and in vivo.</p>

Systematic evaluation on treatment of sub-health with acupuncture-moxibustion and Tuina in clinical researches / 中国针灸

<p><b>OBJECTIVE</b>To evaluate the therapeutic effect of acupuncture-moxibustion and Tuina massage for treatment of sub-health.</p><p><b>METHODS</b>A systematic evaluation on randomized controlled trial, quasi-randomized control trial or controlled clinical trial of treatment of sub-health with acupuncture-moxibustion and Tuina was carried out according to the assessment methods recommended by the Cochrane Collaboration.</p><p><b>RESULTS</b>There are totally 9 articles and 937 subjects met the inclusion criteria and are included into the assessment system. The average quality of methodologies adopted is not so high, and with many limitations. Meta-analysis or descriptive analysis on the data collected: (1) General effect: Tuina massage therapy is better than auricular-point-pressing therapy; acupuncture is better than self health care; acupoint injection is better than intramuscular injection, Tuina is similar to Chinese herb. (2) Quality of life and pain score: Tuina is better than blank control. (3) Individual effect: the effect of Tuina massage on lassitude is better than acupuncture. (4) Effect on sleep quality index: Tuina massage is better than acupuncture.</p><p><b>CONCLUSION</b>There are not enough evidences to approve that the effect of acupuncture-moxibustion and Tuina massage on sub-health is better than that of other therapies. Therefore, more high quality randomized controlled trials with strict and scientific designation are necessary for obtaining more and better evidences.</p>

Randomized controlled trial on effect of Tuina for treatment of sub-health people of somatic pain / 中国针灸

<p><b>OBJECTIVE</b>To evaluate the clinical effect and safety of Tuina for treatment of somatic pain of sub-health.</p><p><b>METHODS</b>A randomized, double-blind and blank parallel controlled trial was done. The experiment group was treated with Tuina and the control group lied down for rest, 45 minutes each time, twice each week for three weeks.</p><p><b>RESULTS</b>Tuina treatment could improve more on sensory, affective, evaluation, pain rating index and extant pain intensity of the pain index, and score of subjective sensation of life quality and health status together with physiology and psychology field of life quality.</p><p><b>CONCLUSION</b>Massage is an effective therapy for treatment of somatic pain of sub-health without adverse reactions and it should be generalized to application.</p>

Biological characteristics of highly tumorigenic CD44+CD133+ subpopulation of laryngeal carcinoma cells / 中华肿瘤杂志

<p><b>OBJECTIVE</b>To separate the cell subpopulation with high tumorigenic ability and study the biological characteristics of this subpopulation in laryngeal carcinoma cells.</p><p><b>METHODS</b>Human laryngeal carcinoma cells were obtained by primary tissue culture technique. CD44 and CD133 molecules were used as markers to isolate the CD44(+), CD133(+), CD44(+)CD133(+) and CD44(+)CD133(-) cell subpopulations from the laryngeal carcinoma cells by flow cytometry. A nude mouse tumor xenograft model was developed for the study of the tumorigenic effects of the different cell populations. 1 x 10(6), 1 x 10(5), 1 x 10(4) and 1 x 10(3) cells were injected into the left flank of the mice, respectively. The mice were observed for palpable tumor formation and were sacrificed at 4 weeks later to assess the tumor formation rate, tumor volume and tumor weight. Boyden chamber migration assay was used to determine the migration ability and immunochemistry was used to detect the expression of stem cell antigen SCA-1 and beta1-integrin. Semi-quantities RT-PCR and Western blot analysis were performed to detect the expression level of Bmi-1 in the different cell subpopulations.</p><p><b>RESULTS</b>The growth of subcutaneous tumors in nude mice showed that a tumor can be generated with 1 x 10(3) CD44(+)CD133(+) cells. When the same dose of 1 x 10(6) CD44(+)CD133(+) cells was injected into the mice, both the average weight and volume of the tumors were significantly higher than those generated from other cell subpopulations. Boyden chamber migration assay showed that the invasion ability of CD44(+)CD133(+) cells was significantly higher than that of other cell subsets. The results of immunochemical analysis showed an abundant expression of stem cell antigen SCA-1 and beta1-integrin in the CD44(+)CD133(+) cells. Semi-quantitative RT-PCR and Western blot analysis provided strong evidence that the Bmi-1 expression in CD44(+)CD133(+) and CD133(+) cells was very significantly higher than that in CD44(+), CD44(+)CD133(-) and control cells (P < 0.01).</p><p><b>CONCLUSION</b>Our findings demonstrate that CD44(+)CD133(+) subset cells in laryngeal carcinoma posses some biological characteristics of tumor stem cells, which may be the original cells of laryngeal carcinoma and may become a new target of tumor therapy.</p>

Knockdown of STAT3 expression using siRNA inhibits the growth of prostate cancer cell lines / 中华男科学杂志

<p><b>OBJECTIVE</b>To study the effects of pSilencer 1.0-U6-siRNA-STAT3 on the growth of PC3 and LNCaP cells.</p><p><b>METHODS</b>Three pairs of DNA template coding siRNA were synthesized against STAT3 to reconstruct pSilencer 1.0-U6-STAT3-siRNA, which was transfected into PC3 and LNCaP cells. The STAT3 expression in PC3 cells and LNCaP were transfected with pSilencer 1.0-U6-siRNA-STAT3, and it was detected by Western blot and Northern blot. MTT and FCM were used to observe the growth-inhibiting ratio and apoptosis in PC3 cells.</p><p><b>RESULTS</b>Western blot and Northern blot analyses demonstrated that pSilencer 1.0-U6-siRNA-STAT3 could significantly inhibit the expression of STAT3 in PC3 and LNCaP cells; MIT and FCM results showed that it could suppress the growth of PC3 cells and LNCaP and induce apoptosis of PC3 cells in vitro.</p><p><b>CONCLUSION</b>PSilencer 1.0-U6-siRNA-STAT3 could significantly inhibit STAT3 expression, suppress the growth of PC3 and LNCaP cells and induce the apoptosis of PC3 cells.</p>