OBJECTIVE: To explore targeting of nanometer drugs and the adverse reaction during disease treatment. METHODS: The first author retrieved China National Knowledge Infrastructure with the key words of "nanometer drug, nanometer particle, drug carrier, targeting, adverse reaction" for articles published from 2001 to 2009 in Chinese. The articles addressing close content of targeting and adverse reactions of nanometer drugs were included, and Meta analysis, irrelevant or duplicated articles were excluded. Finally, 18 articles were included. We summarized the present studies concerning targeting and adverse reactions of nanometer drugs. RESULTS: Compared with common drugs, nanometer drugs had great surface area, strong chemical activity, and rapid rate of absorption. Nanometer drugs process a superiority compared with common drugs in aspects of traversing various barriers of the body, controlling release speed of drugs, and setting drug targeting. CONCLUSION: Compared with previous drugs, the targeting nanometer drugs present significant targeting, i.e. it can bring drugs to the targeting site. It not only can elevate curative effects, but decrease adverse reactions. Nanometer drugs as a new preparation provide a new thought for treating some refractory diseases, and bring a reformation for medical research. However, some nanometer materials show toxic properties, and especially the outcomes of interaction of nanometer materials to human or environment are still unclear. Therefore, the biological effects, action mechanism and elimination measures of toxicity of nanometer materials should be completely studied prior to the nanometer materials are made into commercialization products, which will bring a basic rationale for reasonable application of nanometer materials.

OBJECTIVE:To compare cost-effectiveness of 3 kinds of statins in the treatment of hyperlipidemia. METHODS:180 hyperlipidemia patients were randomly divided into 3 group,with 60 cases in each group. Group A was given Atorvastatin tablet 20 mg/time,once a day;group B received Simvastatin tablet 20 mg/time,once a day;group C was given Rosuvastatin tablet 10 mg/time,once a day. Therapeutic efficacy was evaluated in 3 groups,and cost-effectiveness analysis was conducted. RESULTS:The ef-fective rate was 85.0% in group A,83.3% in group B and 81.7% in group C,there was no statistical significance(P>0.05). Total cost of 3 groups were 610.40 yuan,193.60 yuan and 408.00 yuan;the cost-effectiveness ratio of group B was 2.32,which was sig-nificantly lower than 7.18 of group A and 4.99 of group C,with statistical significance(P<0.05). The results of sensitivity analysis was consistent with it. CONCLUSIONS:Simvastatin is effective and economical medication in the treatment of hyperlipidemia.

Microsphere of diameter 1-300 ?m is a biophysical target drug-loading reagent. Loading material of microspheres is classified into natural polymer,semisynthetic macromolecule,and synthetic macromolecule. Based on proper preparation technique and prescription,drug-loading microspheres made by synthetic macromolecule can release drug to a certain velocity during several weeks or months,reduce administration times,and enhance complaisance. Moreover,microspheres are ideal drug-loading system for protein and polypeptide drug. Research of microspheres is a hot topic at recent,thus more and more drugs are developed into microspheres. Poly(lactic-co-glycolic acid) (PLGA) characterizing by great security,good biocompatibility,and alterable biodegradation is a common material to make microspheres. There are three ways to establish PLGA sustained-release microspheres,including solvent evaporation method,spray drying method,and phase separation method. In particular,solvent evaporation method is frequently used to make PLGA microspheres loading polypeptide and protein in various medical fields of immunology,gene therapy,tumor therapy,bone defect repairing,and ophthalmology.

Objective To establish a reversed HPLC method to determine the contents of gatifloxacin and tinidazole simultaneously. Methods ODS C_ 18 column (4.6mm?250mm,5?m) was used as an analytical column. The mobile phase consisted of 15% acetonitrile, 25% of methanol and 60% of 0.05mol/L KH_2PO_4 buffer,which contained 0.5% triethylamine and was adjusted to pH 3.5 by phosphoric acid. The flow rate was 1ml/min. The detection wavelength was 318nm. The column temperature was 30℃. 20?l of diluted sample solution was injected to the sampler. Results The calibration curve of gatifloxacin was linear in the range of 2~20?g /ml (r=0.999 6) ,and that of tinidazole was 2~20 ?g /ml (r=0.999 9). The recovery rates of them were 100.1% and 100.4%,respectively. RSDs of both drugs were less than 1.1 %. Conclusions The method is simple,accurate and sensitive and can be used to determine the two components simultaneously.

Background and purpose:The epidermal growth factor receptor (EGFR) is commonly overexpressed in a variety of solid tumors, and has important roles in cancer pathogenesis and progression. EGFR thus provides a rational target for cancer therapy. We studied siRNA-mediated inhibition of epidermal growth factor receptor expression and its biologic effects in different human cancer cell lines (A431, HeLa and SPC-A-1). Methods:Cells were transfected with chemically synthesized siRNA-EGFR. EGFR mRNA was quantified by real-time PCR and was detected by immunofluorescence staining and flow cytometry. The biologic effects on cell growth were assessed by colony-formation assay.Results:siRNA-EGFR significantly decreased mRNA level of EGFR by 73.9 %, 44.6 % and 57.7 %, protein expression of EGFR by 77.0 %, 61.3 % and 65.2 %, and reduced colony number by 27.2 %, 53.9 % and 59.1 % in A431, HeLa and SPC-A-1, respectively.Conclusions:Our data suggested that RNA interference could downregulate EGFR and inhibit colony forming ability and EGFR expression at mRNA/protein levels in human cancer cell lines with different pathological types. siRNA could be one of the promising strategies in future targeted cancer therapy.

Objective To investigate the effect of tadpole extract(T871 3) on tumor cells and its mechanism. Methods We studied the effects of T871 3 on proliferation, differentiation and apoptosis of HL 60 cells by cytomorphological observation, cytochemistry and TUNEL method. We also examined gene expression during the induction of apoptosis and differentiation in tadpole extract treated HL 60 cells by in situ hybridization and intact cell mRNA dot blot techniques. Results 1 T871 3 was able to inhibite HL 60 cells proliferation. 2 T871 3 was able to induce HL 60 cells to differentiate along monocyte macrophage lineage at low concentration, and apoptosis at higher concentration. 3 The differentiation of HL 60 cells was accompanied by downregulations of c myc,c myb gene expression, The apoptosis of HL 60 cells was accompanied by downregulations of c\|myc bcl 2 gene expression, suggesting that these genes may be involved in the apoptosis and differentiation process. Conclusion Tadpole extract may have effects on HL 60 cells through changing the oncogene expression. [

Heart Failure ; Humans ; Models, Cardiovascular ; Prognosis

Background Identifying and testing of pain is very necessary for the care and decrease of the suffering of experimental animal in medical experiment.Effective method for testing the pain and distress status of experimental animal with eye disease is still absent in China.Objective This pilot study was to establish an evaluating system for assessing the pain and distress status of bullous keratopathy rabbit model.Methods This study was approved by the Ethic Committee of Beijing University First Hospital.Twelve healthy New Zealand rabbits were selected in this experiment.Bullous keratopathy model was established in the left eyes of 9 rabbits by scraping corneal endothelium as the experimental team,and other 3 rabbits were served as the control team.The cornea lesion was examined by manipulate slit lamp,and the central cornea thickness (CCT) was measured by ultrasound biomicroscopy (UBM).Weight+20 Indexes For Pain and Distress Status Referring Guidelines for Pain and Distress in Laboratory Animals made by International Animal Care and Use Committee (IACUC) were assessed and measured as well.Results Corneal edema and opacity were obvious 1 day after surgery.Corneal bullous appeared from the third day after surgery,and cornea erosion was seen at the location of bullous breakage.The corneal lesions remained until 14 days after surgery.CCT value was (1468±100),(2313±588),(2391±271) and (2362±151) μm,respectively in day 1,3,7 and 14 after the establishment of models,which showed significant increase in comparison with the preoperative CCT (390±6)μm (all P=0.000).However,no significant difference was seen in the CCT between day 3,7 and 14 (P＞0.05).Body weight of the rabbits was (3.29±0.20),(3.20-0.17),(2.77±0.25) and (3.10±0.30)kg respectively in day 1,3,7 and 14 after operation,with significant decrease in comparison with the pre-operative weight (3.52-0.18)kg in the experimental team (P=0.008,0.007,0.003,0.004).The scores for pain and distress status of all rabbits in pre-operation of the experimental team and in the control team were zero,and the score was 7 (7,7),11 (10,12),9 (8,10),9 (9,9)in day 1,3,7 and 14 in the experimental team after surgery,with the highest score in day 3,which was bullous and bullous breakage duration.Seven of twenty indexes,including the reduce of diet and drinking,self-imposed isolation/hiding,grinding teeth,aggression,deceased movement,abnormal posture,vocalization occurred in the model animals after surgery.Conclusions Weight+20 Indexes For Pain and Distress Status is an effective,impersonal and quantitative method for observing and evaluating the pain and stress status in bullous keratopathy rabbit.

Antibody drug conjugates (ADCs) are an emerging class of targeted therapeutics with the potential to improve therapeutic index over the traditional chemotherapy. However, it is difficult to control the site and stoichiometry of conjugation in mAb, typically resulting in heterogeneous mixtures of ADCs that are difficult to optimize. New methods for site-specific drug attachment allow development of more homogeneous conjugates and control of the site of drug attachment. In this article, the new literature on development of ADCs and site-specific ADCs is reviewed. In addition, we summarized the various strategies in production of site-specific ADCs.
Antibodies, Monoclonal ; chemistry ; Antibody Specificity ; Binding Sites, Antibody ; Immunoconjugates ; chemistry

Objective To investigate the value of a new index - Tei index for estimating left ventricular global function in patients with acute myocardial infarction.Methods The study population included 95 patients with acute myocardial infarction.They were divided into two groups according to EF measured by echocardiography in apical four chamber view:one group with normal EF(EF≥50%,n=52)(group A),the other with abnormal EF(EF