The objective of this study was to develop a method for the determination of taxol injection using near infrared transmission spectroscopy, turning out redetermination for injection from hospital pharmacy before using. Near infrared spectra (NIR) in the range of 12 000 approximation 4 000cm(-1) were recorded for the taxol injection manufactured during recent 24 months with different time. Calibration models were established using the partial least squares (PLS). Comparing different spectra pretreatments methods, dimension and spectra range, The study showed that spectra information cab be extracted thoroughly by delete a line method with dimension 6, spectra range 9002.5 approximately 4597.7cm(-1) ,standard error of the calibration sets(SEC) 0.035 and standard error of the prediction sets(SEP) 0. 059. Percent of prediction sets sample is less than +/- 2%. Results indicate that near infrared transmission spectroscopy method can be used to rapidly analyze the frequent and important drugs from hospital pharmacy.
Antineoplastic Agents, Phytogenic ; administration & dosage ; analysis ; Calibration ; Injections ; Paclitaxel ; administration & dosage ; analysis ; Spectroscopy, Near-Infrared ; methods

OBJECTIVETo inspect the effect of activated carbon with different dosage and temperature on quality of paclitaxel injection.

METHODDeterminations in WS1-(X-026)-2001Z-paclitaxel injection were refered to compare the effect of different dosage and temperature for activated carbon on the taxol content, related material, clarity and bacterial endotoxin.

RESULTWhen used with 0.25% and 35 degrees C, activated carbon will ensure the quality of paclitaxel injection.

CONCLUSION0.25% and 35 degrees C are the best condition when activated carbon is used in paclitaxel injection.

Antineoplastic Agents, Phytogenic ; administration & dosage ; Charcoal ; administration & dosage ; analysis ; Drug Compounding ; methods ; Injections ; Paclitaxel ; administration & dosage ; Quality Control ; Temperature

MicroRNAs (miRNAs) are a set of non-coding small RNA molecules that play a critical role in regulation of protein coding genes in cells. MiRNAs have been extensively studied as novel biomarkers, therapeutic targets, and new drugs in various human diseases. Breast cancer is a one of the leading tumor types significantly affecting women health worldwide. Over the past decade, a number of natural agents, such as paclitaxel and curcumin, have been applied for treatment and prevention of breast cancer due to their relatively low toxicity. However, the mechanisms of action have not been completely understood. Investigation on miRNAs is able to potentially provide a novel insight into better understanding the anticancer activities of these natural products. Given that a single miRNA can target multiple genes, theoretically, those genes involved in a certain phenotype can be clustered with one or a few miRNAs. Therefore, pleiotropic activities of natural agents should be interpreted by interactions between selected miRNAs and their targets. In this review, we summarize the latest publications related to the alterations of miRNAs by two natural agents (paclitaxel and curcumin) that are currently used in intervention of breast cancer, and conclude that the mechanism involving the regulation of miRNA expression is one of the keys to understand pleiotropic activities of natural agents.
Animals ; Antineoplastic Agents ; administration & dosage ; Biological Products ; administration & dosage ; Breast Neoplasms ; drug therapy ; genetics ; metabolism ; prevention & control ; Curcumin ; administration & dosage ; Female ; Humans ; MicroRNAs ; genetics ; metabolism ; Paclitaxel ; administration & dosage

OBJECTIVETo prepare carbon nanoparticle-paclitaxel suspension(CNPS) and to study the pharmacokinetics of intraperitoneal chemotherapy with CNPS.

METHODSSaturated absorption capacity of carbon nanoparticle suspension (CNS) and paclitaxel were detected by high performance liquid chromatography in order to prepare the above suspension. Wistar rats were randomly divided into the experimental group (A) and the control group (B), to which intraperitoneal injections of CNPS and paclitaxel were given respectively. At different time points, measure the blood samples, mesenteric lymph nodes, and intraperitoneal lavage fluid were collected to measure the concentration of paclitaxel.

RESULTSOne ml CNS could absorb 7 mg paclitaxel by maximum. The ratio of area under the curve (AUC) in the plasma of group A to group B was 0.63. The ratio of AUC in lymph nodes of group A to group B was 0.75 and that in intraperitoneal lavage fluid was 1.25. The metabolic half-life (t1/2) of paclitaxel in the plasma of group A was 1.61 times as long as that of group B. The t1/2 of paclitaxel in intraperitoneal lavage fluid of group A was 0.88 as long as that of Group B. The t1/2 of paclitaxel in lymph nodes of group A was 1.10 as long as that of Group B.

CONCLUSIONSCNS has a high absorption capacity with paclitaxel. Intraperitoneal chemotherapy by CNPS is characterized by low drug concentration in the blood, high drug concentration in the peritoneal cavity and high safety. However, the targeting and lymphatic retention effect are not significant. The mechanism warrants further investigation.

Albumin-Bound Paclitaxel ; Albumins ; chemistry ; pharmacokinetics ; Animals ; Area Under Curve ; Carbon ; chemistry ; Injections, Intraperitoneal ; Lymph Nodes ; Nanoparticles ; administration & dosage ; Paclitaxel ; chemistry ; pharmacokinetics ; Rats ; Rats, Wistar

Drug-coated stent play an important role in percutaneous transluminal coronary angioplasty (PTCA), and it constitutes an innovation to further reduce the incidence of restenosis. In this paper, the mechanisms and the process of endovascular stent implantation,and the principles of drug release of drug-coated stent are reviewed. Especially, polymer coated design and the further development of drug eluting stents are discussed.
Angioplasty, Balloon, Coronary ; instrumentation ; Coronary Restenosis ; prevention & control ; Drug Delivery Systems ; Drug-Eluting Stents ; Heparin ; administration & dosage ; Humans ; Paclitaxel ; administration & dosage ; Sirolimus ; administration & dosage

Mesenchymal stem cells (MSCs) have the inherent tumor-homing ability with the attraction of multiple chemokines released by tumor tissues or tumor microenvironments, which can be utilized as promising cellular carriers for targeted delivery of anti-tumor drugs and genes. In most circumstances, large amount of systemicly administrated MSCs will be firstly trapped by lungs, following with re-distribution and homing to tumor tissues after lung clearance. Several approaches like enhanced interactions between chemokines and receptors on MSCs or reducing the retention of MSCs by changes of administration methods are firstly reviewed for improving the homing of MSCs towards tumor tissues. Additionally, the potentials and gains of utilizing MSCs to carry several chemotherapeutics, such as doxorubicin, paclitaxel and gemcitabine are summarized, showing the advantages of overcoming the short half-life and poor tumor targeting of these chemotherapeutics. Moreover, the applications of MSCs to protect and deliver therapeutic genes to tumor sites for selectively tumor cells eliminating or promoting immune system are highlighted. In addition, the potentials of using MSCs for tumor-targeting delivery of diagnostic and therapeutic agents are addressed. We believed that the continuous improvement and optimization of this stem cells-based cellular delivery system will provide a novel delivery strategy and option for tumor treatment.
Antineoplastic Agents ; administration & dosage ; Doxorubicin ; administration & dosage ; Drug Delivery Systems ; Gene Transfer Techniques ; Humans ; Mesenchymal Stem Cells ; Neoplasms ; therapy ; Paclitaxel ; administration & dosage ; Research ; trends

Paclitaxel-loaded methoxy poly (ethylene glycol )-b-poly (L-lactic acid) diblock copolymer nanoparticles (PMT) were prepared by a self-emulsification/solvent evaporation method. The PMT morphology, size and its distribution, and drug release in vitro were investigated by DLS, UV, TEM and HPLC. The results indicate that PMT show a spherical morphology with inner core and outer shell. The diameter (nm) of PMT increases with the increase of the drug-loaded amount. The initial burst release is not observed, the drug releasing rate in vitro is lower, and the accumulated release increases with the increase of replacement amout of the pH7. 4 medium. This study develops a new formulation for paclitaxel and provides an experimental basis for the intravenous administration of paclitaxel.
Antineoplastic Agents, Phytogenic ; administration & dosage ; Delayed-Action Preparations ; Drug Carriers ; administration & dosage ; chemistry ; Humans ; Injections, Intravenous ; Nanoparticles ; Paclitaxel ; administration & dosage ; Polyesters ; administration & dosage ; chemistry ; Polyethylene Glycols ; administration & dosage ; chemistry ; Polymers ; administration & dosage ; chemistry

OBJECTIVETo observe the incidence rate of stent thrombosis after implantation of drug-eluting stents (DES) in patients with coronary artery disease (CAD) in the real world.

METHODSA total of 8190 consecutive CAD patients underwent implantation with Cypher or Cypher Select stents (Cordis, USA, n = 2986), TAXUS stents (Boston Scientific Corp., USA, n = 1587) and Chinese Rapamycin eluting stents (Firebird, Microport Medical Company, China, n = 3617) for enrolled in this single center registry study from Dec.2001 to April 2007. One-year follow-up was completed in 5412 patients (2210 Cypher or Cypher select stents, 1238 TAXUS stents and 1964 Firebird stents). Two-year follow-up was finished in 2176 patients (1245 Cypher or Cypher Select stents, 558 TAXUS stents and 373 Firebird stents). 80.1% of all the lesions were the type B2 and type C lesions. All patients were treated with aspirin plus clopidogrel for at least 9 months post DES.

RESULTSAmong 8190 patients, 17 patients had acute stent thrombosis (0.21%): 7 in the Cypher group, 4 in the TAXUS group, 6 in the Firebird group; 23 patients had subacute stent thrombosis (0.28%): 8 in Cypher group, 6 in TAXUS group and 9 in Firebird group. The incidence rate of acute and subacute thrombosis was 0.49% (40/8190) and incidence of thrombosis was similar among the three groups (0.50% in Cypher group, 0.63% in TAXUS group and 0.41% in Firebird group, P > 0.05). One-year follow-up showed that late thrombosis rate was 0.63 % (34/5412) and similar among the groups (0.63% in Cypher group, 0.89% in TAXUS group and 0.46% in Firebird group, P > 0.05). Two-year follow-up showed that late thrombosis rate was 0.74 % (16/2176) and was similar among the 3 groups (0.72% in Cypher group, 0.90% in TAXUS group and 0.54% in Firebird group, P > 0.05).

CONCLUSIONThis study indicates that using the first-generation DES to treat complex coronary lesions is safe and effective and the incidence of late thrombosis remains low (< 1%) under double antiplatelet treatment.

Coronary Artery Disease ; therapy ; Drug-Eluting Stents ; adverse effects ; Follow-Up Studies ; Humans ; Incidence ; Male ; Paclitaxel ; administration & dosage ; Thrombosis ; etiology

OBJECTIVETo evaluate the safety and efficiency of local paclitaxel delivery using the double-balloon perfusion catheter to prevent restenosis in the canine coronary artery.

METHODSTwenty domestic canines underwent bare-mental stent implantation after balloon injure of the left coronary artery. A novel double-balloon perfusion catheter was used to deliver the drug locally in the canine coronary artery. In the treatment group (n = 15), paclitaxel (10 ml, 20 micromol/L) was delivered using the double-balloon perfusion catheter before stent implantation. In the control group (n = 5), 10 ml saline was delivered using the double-balloon perfusion catheter before stent implantation. The perfusion time in both groups was (26.45 +/- 5.18) s. Animals underwent coronary angiography and optical coherence tomography (OCT) 90 days after stent implantation and were sacrificed. Vessels were perfusion-fixed and morphometric analysis was performed using conventional techniques.

RESULTSCoronary angiography results showed restenosis rate in control group was significantly higher than that in treatment group (60% vs. 33.33%, P < 0.05). The parameters of OCT showed in treatment group and control group: the neointimal thickness was (0.19 +/- 0.08) mm and (0.38 +/- 0.03) mm, the neointimal area was (1.52 +/- 0.49) mm2 and (2.51 +/- 0.47) mm2, the lumen area was (3.50 +/- 0.66) mm2 and (2.78 +/- 0.57) mm2, the extent of stenosis was (30.13 +/- 8.56)% and (47.40 +/- 4.50)%, and all the variances above were significantly different between the two groups (P < 0.05). The histologic parameters showed in treatment group and control group: the neointimal thickness was (0.22 +/- 0.10) mm and (0.47 +/- 0.05) mm, the neointimal area was (1.85 +/- 0.78) mm2 and (3.43 +/- 0.25) mm2, the lumen area was (3.15 +/- 0.43) mm2 and (1.85 +/- 0.55) mm2, the extent of stenosis was (36.00 +/- 10.97)% and (65.40 +/- 8.23)%, and all the variances above were also significantly different between the two groups (P < 0.05). The stents of both the groups were fully endothelialized. No thrombus or aneurysm was found in stents.

CONCLUSIONLocal delivery of paclitaxel with the double-balloon perfusion catheter to prevent restenosis in coronary stents is safe and efficient.

Angioplasty, Balloon, Coronary ; Animals ; Catheters ; Coronary Restenosis ; prevention & control ; Disease Models, Animal ; Dogs ; Injections ; Paclitaxel ; administration & dosage ; therapeutic use ; Stents

OBJECTIVETo evaluate the effect of different preparation methods on the encapsulation efficiency (EE) and drug loading (DL) of paclitaxel-loaded polybutylcyanoacrylate nanoparticles (PTX-PBCA-NPs) and optimize the preparation of PTX-PBCA-NPs.

METHODSWith DL and EE as the major indexes, the qualities of PTX-PBCA-NPs produced by the interfacial polymerization and emulsion polymerization method were compared. The optimized prescription was obtained by orthogonal design.

RESULTSThe ranges of EE of PTX-PBCA-NPs with the two methods were both 94.39%-99.23%. The highest DL with interfacial polymerization was (1.07-/+0.03)%, as compared to (0.86-/+0.01)% with emulsion polymerization. The optimized preparation conditions resulted in the mean size of PTX-PBCA-NPs of 235.6 nm, DL of 0.80%, and EE of 95.71%.

CONCLUSIONThe EE of PTX-PBCA-NPs prepared by the above two methods is consistent with the requirement of the Pharmacopoeia of China, and PTX-PBCA-NPs containing higher DL can be obtained via interfacial polymerization.

Delayed-Action Preparations ; chemical synthesis ; Drug Carriers ; chemistry ; Drug Delivery Systems ; Enbucrilate ; chemistry ; Nanoparticles ; chemistry ; Paclitaxel ; administration & dosage ; Polymerization