Targeting drug delivery system (TDDS) is one of the most concerned research fields in cancer treatment because it can bind selectively and react with the target diseased sites at the cellular or sub-cellular level, making distribution and release of drugs in a controlled manner, thus enhance therapeutic effects and reduce toxic and side-effects on normal cells. Polyamidoamine dendrimer (PAMAMD) is a kind of newly developed polymer in nanometer degree. Hyper-branched, monodispersity, three-dimensional structure and host-guest entrapment ability make it used as drug carrier, gene delivery system and imaging agent. Various targeting ligands, which have high affinity to specific organs, tissues or cells in human body, can be linked to surface functional groups of PAMAMD. And drugs and theoretical gene are carried by encapsulation or chemical conjugation. Finally, PAMAMD targeting drug delivery system can carry drugs and theoretical gene to diseased sites and then release them for targeted therapy. The PAMAMD-based conjugates have small size, ligh permeability and retention effect (EPR), low toxicity and so on. The research progress of PAMAMD modified by different ligands in targeting drug delivery system is reviewed, and research direction of the PAMAMD targeting delivery system in the future is also suggested.

0.05).(3)The levels of CRH and DHEA-S in umbilical cord blood of PL(7.8?3.3)ng/L,and(514?295)?g/L,respectively and of TL (7.7?4.1)ng/L,and(483?207)?g/L,were higher than that in term not in labor(4.8?2.4)ng/L, and(360?80)?g/L,respectively(P 0.05).In PL,the level of CRH in umbilical cord blood and the expression of CRH mRNA in placentas and fetal membranes were correlated with each other(r=0.935 and 0.853,P

Objective To explore the related factors of hepatitis B virus(HBV) drug resistance and their clinical significance . Methods The retrospective analysis was performed on the dinical data in 153 cases of CHB in our hospital during 2011-2013 .The 8 viral drug resistance loci of 4 known nucleosides analogues lamivudine ,adefovir ester ,entecavir and telbivudine were performed the direct sequencing by using the double DNA end termination method(Sanger method);the related clinical factors of drug‐resist‐ant virus genotypes were statistically analyzed and the correlation between prognosis and drug resistance was analyzed .Results A‐mong 153 patients with CHB ,47 cases(29 .8% ) appeared virus genotype drug‐resistant ,the common sites were 204M‐I(18 cases) , 204M‐V(8 cases) ,followed by 181A‐T(10 cases) ,181A‐V(5 cases) ,then 180L‐M (14 cases) .The proportion of viral drug resist‐ance in the patients with family history ,HBeAg positive ,using the nucleotide analogues in the past and the baseline ALT≥5 times was significantly increased ,the incidence rates were 38 .8% ,34 .8% ,34 .6% and 50 .0% respectively .The multivariable COX re‐gression found that HBV‐DNA genetic drug resistance increased the risk of progression to cirrhosis of the liver ,the OR value was 4 .704(95% CI:1 .199 -18 .454) .Conclusion the Sanger method for direct sequencing is reliable and accurate method of HBV‐DNA genotype drug resistance .The proportion of viral drug resistance in the patients with a family history of hepatitis B ,HBeAg positive ,using nucleotide analogues and baseline ALT≥5 times is significantly increased;HBV‐DNA genotype drug resistance also increases the risk of progression to cirrhosis of the liver .

AIM To study the effects of different kinds of chloride channel blockers on KCl and 5 HT induced contractile responses in cerebrovascular smooth muscle. METHOD The tension of rabbit basilar artery rings was measured. RESULTS ① DIDS, furosemide and NPPB inhibited the responses to KCl and 5 HT in a concentration dependent manner. The effects of DIDS, furosemide and NPPB on the response to 5 HT were stronger than that to KCl. ②When SK&F 96365 evoked a maximum inhibitory effect on 5 HT induced response, subsequent additions of DIDS, furosemide and NPPB could further produced vascular relaxation. CONCLUSION The chloride channel participates KCl and 5 HT induced contractile responses in cerebral basilar artery.

AIM To study the effects of protein tyrosine kinase inhibitor and protein tyrosine phosphatase inhibitor on cultured bovine cerebrovascular smooth muscle cells (CSMC) Ca 2+ store operated Ca 2+ influx. METHODS Cell culture and single intracellular free Ca 2+ concentration was measured in fura 2/Am flueorescence probe by MetaFluor Fluorescence ratio imaging system. RESULTS (1) protein tyrosine kinase inhibitor (genistein,2.5,5,10 ?mol?L -1 )decreased Ca 2+ influx significantly induced by endothelin 1(ET 1),ATP,cyclopiazonic acid(CPA) in concentration dependent manner; (2) Protein tyrosine phosphatase inhibitor (vanadate,2,4,8 ?mol?L -1 ) increased Ca 2+ influx significantly induced by ET 1,ATP,CPA in concentration dependent manner. CONCLUSION Protein tyrosine kinase inhibitor and protein tyrosine phosphatase inhibitor have effects on Ca 2+ store operated Ca 2+ influx induced by ET 1, ATP, CPA. Protein tyrosine phosphorylation participats in the signal transduction of Ca 2+ store operat Ca 2+ influx in cerebrovascular smooth muscle cells.

Objective To study the diagnostic value of pencilliosis marneffei (PM)in a non-HIV-infected child with the com-bined detection of aspergillosis galactomannan,fungus Glucan(1-3)-β-D and boold culuture.Methods The venous blood specimen from the child was collected for the quantified detection of aspergillosis galactomannan,fungus Glucan(1-3)-β-D. The growth and colonial morphology of fungus was inspected with the positive blood culture and the characteristics of fun-gus smear were observed under microscope.Results The result of aspergillosis galactomannan was 14.45 μg/L and fungus Glucan (1-3)-β-D 77.14 pg/ml.Penicillium marnrffei was identified using blood culture.It was mycelia form under 25℃ and the salouraud medium produced water soluble claret-red pigment produced.It was mycelia form under 35℃ and the colony was gyri creases,the characteristic broom-like hypha and separation hypha could be found under microscope.Conclusion It is effective for the early diagnosis and therapy of PM with the combination detection of aspergillosis galactomannan,fungus Glucan (1-3)-β-D and boold culuture and have better clinical diagnosis value.

OBJECTIVETo study clinical effects of unilateral pedicle screw-rod system fixation combined with the single the cage of interbody fusion in the treatment of lumbar degenerative instability via paraspinal intermuscular approach under MAST Quadrant retractor.

METHODSFrom February 2010 to December 2011, 39 patients with lumbar degenerative instability after invalid conservative treatment were treated with unilateral fixation combined with interbody fusion via the paraspinal intermuscular approach under MAST Quadrant retractor. The indexes such as the operative time, blood loss, complications, VAS pain scores, JOA (subjective symptoms of low back pain,lower limb pain and numbness, sensory disturbance, movement disorders) scores, modified Macnab criteria for curative effect evaluation were observed before treatment, at the 1st month after treatment and the latest follow-up. The intervertebral fusion was studied on the X-ray at the latest follow-up.

RESULTSAll the patients were followed up, and the mean during was (22.3 +/- 8.6) months. The operation time was (138 +/- 46) min, and the amount of bleeding was (335 +/- 152) ml. There were no complications such as cerebrospinal fluid leakage and spinal nerve injury during operation, and no incision infection after operation. The VAS pain score was reduced from preoperative 7.93 +/- 1.27 to 2.05 +/- 1.18 on the 1st month after operation and 1.89 +/- 0.42 at the latest follow-up. The JOA total score was improved from preoperative 1.59 +/- 0.42 to 8.86 +/- 0.37 on the 1st month and 9.02 +/- 0.29 at the latest follow-up. According to modified Macnab criteria, there were 17 cases got an excellent result, 19 good, 3 case fair. Thirty-five patients got intervertebral bony fusion at the latest follow-up.

CONCLUSIONUnilateral pedicle screw-rod system fixation combined with single cage interbody fusion in the treatment of lumbar degenerative instability via paraspinal intermuscular approach under MAST Quadrant retractor is a safe, minimally invasive, satisfactorily effective methods to treat lumbar degenerative instability.

Adult ; Aged ; Female ; Follow-Up Studies ; Fracture Fixation, Internal ; Humans ; Intervertebral Disc Degeneration ; surgery ; Intervertebral Disc Displacement ; surgery ; Lumbar Vertebrae ; surgery ; Male ; Middle Aged ; Pedicle Screws ; Reconstructive Surgical Procedures ; Spinal Fusion ; Treatment Outcome

Objective:To analysis the appearances and to evaluate the diagnostic value of X-ray CT and MR imaging in osteoid osteoma.Methods:22 cases 19 females and 3 males of osteoid osteoma proved by surgical pathology and their X-ray,CT and MRI were reviewed.The ability of X-ray,CT and MRI to demonstrate the nidus and surrounding reaction were analyzed.Results:The nidus were appeared as round or oval shape and the diameter was less than 2 cm.It was fomd in 17 cases of X-ray film，22 CT and 20 of MRI .There were different degree of bone sclerosis,periosteal reaction and soft tissues or bone marrow edema around the nidus.The diagnostic accuracy was 77.3% for X-ray，100% for CT and 90.9% for MRI.Conclusion:Most of osteoid osteoma have the typical appearances and is no difficult to make diagnosis.CT scan is the most accuracy method to demonstrate the nidus.It is possible to make misdiagnosis only with X-ray or MRI for the case that the hidus not be demonstodted.

Aim To study absorption characteristics of SM-1 , a novel anti-tumor agent , to provide a research basis for the druggability evaluation of SM-1 and formu-lation design. Methods Caco-2 cell monolayer model and in situ single-pass intestinal perfusion rat model were used to study the absorption characteristics of SM-1 , and the absorption of SM-1 in vivo was evaluated through absolute bioavailability study in rats. Results The results of cell monolayer model showed that cu-mulative absorption and efflux of SM-1 increased line-arly with concentration ( 10 ~40 mg · L-1 ) . There were no significant differences in Papp with different concentrations ( P>0. 05 ) . SM-1 was absorbed mainly through passive diffusion. The intestinal perfusion re-sults showed that Ka and Pef of SM-1 had no significant differences ( P > 0. 05 ) , when the concentrations ranged from 25 to 100 mg · L-1 . SM-1 entered the systemic circulation mainly via on passive diffusion, indicating it is a compound with high permeability. The absorption of SM-1 in duodenum was superior to other intestinal segments ( P <0. 05 ) , there were no significant differences in the jejunum, ileum and colon ( P >0. 05 ) . The absolute bioavailability of SM-1 in rats was 29. 3%. Conclusion The membrane perme-ability of SM-1 is high and it can be absorbed by intes-tine well. The absorption mechanism of SM-1 is pas-sive diffusion, and it possibly escapes from the efflux transporter protein. The absolute bioavailability of SM-1 in rats is low.

Targeting drug delivery system (TDDS) is one of the most concerned research fields in cancer treatment because it can bind selectively and react with the target diseased sites at the cellular or sub-cellular level, making distribution and release of drugs in a controlled manner, thus enhance therapeutic effects and reduce toxic and side-effects on normal cells. Polyamidoamine dendrimer (PAMAMD) is a kind of newly developed polymer in nanometer degree. Hyper-branched, monodispersity, three-dimensional structure and host-guest entrapment ability make it used as drug carrier, gene delivery system and imaging agent. Various targeting ligands, which have high affinity to specific organs, tissues or cells in human body, can be linked to surface functional groups of PAMAMD. And drugs and theoretical gene are carried by encapsulation or chemical conjugation. Finally, PAMAMD targeting drug delivery system can carry drugs and theoretical gene to diseased sites and then release them for targeted therapy. The PAMAMD-based conjugates have small size, ligh permeability and retention effect (EPR), low toxicity and so on. The research progress of PAMAMD modified by different ligands in targeting drug delivery system is reviewed, and research direction of the PAMAMD targeting delivery system in the future is also suggested.
Amino Acids ; administration & dosage ; chemistry ; Animals ; Antibodies, Monoclonal ; administration & dosage ; chemistry ; Antineoplastic Agents ; administration & dosage ; therapeutic use ; Biotin ; administration & dosage ; chemistry ; Dendrimers ; administration & dosage ; chemistry ; Drug Carriers ; administration & dosage ; chemistry ; Drug Delivery Systems ; Folic Acid ; administration & dosage ; chemistry ; Gene Transfer Techniques ; Humans ; Ligands ; Neoplasms ; drug therapy ; Polyamines ; administration & dosage ; chemistry ; pharmacokinetics ; Polyethylene Glycols ; administration & dosage ; chemistry ; Transferrin ; administration & dosage ; chemistry