Traditional chemotherapy has become one of the essential treatments of cancer. However, cytotoxic agents are not tumor specific, which would cause serious side effects. Antibody-drug conjugates (ADCs), also called immunoconjugates, belong to the "targeted chemotherapeutics" category of anti-cancer drugs. ADCs are composed of three components including the cytotoxic drug, the monoclonal antibody, and the linker connecting the drug to the antibody. With the special-binding between antibody and antigen expressed on the surface of targeted cancer cells, ADCs provide a method to achieve excellent localization of the drug at the desired site in the body. The internalization and formation of ADCs are crucial in designing and applying an antibody conjugate to a particular disease model. In this review, we summarize three distinct internalization routes of ADCs and analysis the structure of ADCs. We also discuss in detail the categories and interaction of every component, as well as their influence to targeting property, liability and activity.
Antibodies, Monoclonal ; administration & dosage ; Antineoplastic Agents ; administration & dosage ; Drug Delivery Systems ; Immunotoxins ; chemistry ; therapeutic use

Aspargine-glycine-arginine (NGR)-containing peptides are targeted peptides which can be integrated with CD13 receptors on tumor vascular endothelial cells. NGR peptides are connected to liposomes to obtain NGR peptide-modified liposomes. By intravenous injection of these liposomes, NGR peptides can be combined with CD13 receptors on tumor vascular endothelial cells, position liposomes in tumor tissues, and concentrate drug in liposomes in tumor, so as to enhance the antitumor effect. The article starts with NGR peptides, summarizes definition of NGR, NGR peptide-modified liposomes, strengths and weaknesses of NGR peptide-modified liposomes in antitumor and the latest study orientation of NGR peptide-modified liposomes, and looks into the future of studies on NGR peptide-modified liposomes.
Animals ; Antineoplastic Agents ; pharmacology ; CD13 Antigens ; administration & dosage ; pharmacology ; Humans ; Liposomes ; Oligopeptides ; administration & dosage ; pharmacology

OBJECTIVETo optimize the preparation of genistein chitosan microspheres with central composite design (CCD).

METHODThe chitosan microspheres were prepared by the O/W/O multiple emulsion method. Second-order polynomial and linear equations were fitted to the data, and the resulting equations were used to produce response surface graphs and the best experiment conditions.

RESULTThe theoretical drug content was 13%-15%, the concentration of organic phase was 30%-40% and the concentration of oil phase was 68%-72%.

CONCLUSIONThe best experiment conditions can be obtained by central composite design and response surface methodology. The observed values agree well with model predicted values.

Antineoplastic Agents ; administration & dosage ; Chitin ; analogs & derivatives ; Chitosan ; Delayed-Action Preparations ; Genistein ; administration & dosage ; Mathematics ; Microspheres

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

This study evaluated the effects of prolonged primary chemotherapy in retinoblastoma. The data for 27 eyes in 22 children who were treated for retinoblastoma with up to 13 cycles of primary chemotherapy was reviewed. The chemotherapy consisted of etoposide, vincristine, and either carboplatin or ifosfamide. In bilateral retinoblastoma, 1 eye was in each Ia, Ib, and Va, according to the Reese-Ellsworth classification, 2 in each IIa, IIIa, and IIIb, 4 in IIb, and 5 in IVa. Enucleation was performed in 1 in IIa and 1 in Va. In unilateral, 1 was in each IIa, IIIa, IVa, IVb, and Vb, and 4 in Va. Enucleation was performed in 8 with the exception of 1 in IIa. Complete regression was observed in 17 eyes (12 patients). There was no toxicity severe enough to delay treatment. Prolonged primary chemotherapy can be considered as an alternative treatment for retinoblastoma in III or less.
Antineoplastic Agents/administration& dosage ; Antineoplastic Agents, Alkylating/administration& dosage ; Antineoplastic Agents, Phytogenic/administration& dosage ; Antineoplastic Combined Chemotherapy Protocols/*administration& dosage ; Carboplatin/administration& dosage ; Child, Preschool ; Drug Administration Schedule ; Etoposide/administration& dosage ; Eye Enucleation ; Human ; Ifosfamide/administration& dosage ; Infant ; Retinal Neoplasms/*drug therapy/surgery/ultrasonography ; Retinoblastoma/*drug therapy/surgery/ultrasonography ; Retrospective Studies ; Vincristine/administration& dosage

Electrochemotherapy (ECT) is a novel cancer treatment in which electric pulses (EPs) inducing cell membrane pored (electroporation) are used as a means of delivering antitumor drugs to the cytoplasm of cancer cells. The minimal thresholds of electric field strength of in vitro tumor cell line and tumor tissue are 450-650 V/cm and 400-600 V/cm, respectively. The typical electrical requirement is 600-1300 V/cm, pulse width of 100 micros, 8 pulses, 1 Hz. More than 10 kinds of antitumor drugs have been applied to ECT, in which the most efficacious drug is Bleomycin, and then Cisplatin. Some exciting inhibitory effects on cells in vitro and on solid tumors in clinical trials have been noticed. The factors influencing ECT effects include the electric parameters, diameter of electrode, distribution of electric field lines, size of tumor, model of drugs injection and kinds of drugs. Some questions of ECT are still open, such as the dosages and kinds of drugs for clinical trials, model of drug injection, influence on normal tissues, therapeutic mechanism.
Antibiotics, Antineoplastic ; administration & dosage ; Antineoplastic Agents ; administration & dosage ; Bleomycin ; administration & dosage ; Cisplatin ; administration & dosage ; Electric Stimulation Therapy ; methods ; Electrochemistry ; Electroporation ; methods ; Humans ; Neoplasms ; therapy

OBJECTIVETo investigate the influence of drug properties on the encapsulation effiency (EE) and drug release of transfersomes for a proper transfersome preparation.

METHODTo prepare the transfersomes of colchicines (CLC), vincristine sulfate (VCR) and mitoxantrone hydrochloride (DHAD) with the same materials and methods, and then measure their EE. To find out the relationship between drug properties like solubility, molecular weight and charges, and EE. To performe the drug release experiments of various types of transfersomes in vitro, and compare their differences.

RESULTVCR and DHAD are lipophilic or hydrophilic, owing positive charges and large molecular weight, as a result, their EE are high, while CLC is amphipathic, neutral, and of small molecular weight, its EE is very low. As DHAD can insert into the membrane of transfersome, the drug release of DHAD-T in vitro is much slower than that of VCR-T.

CONCLUSIONTo prepare transfersomes with high EE, drugs that are lipophilic or hydrophilic, high molecular weight and opposite charges to the membrane should be chosen. Interaction between drugs and membrane will influnce the rate of drug release.

Antineoplastic Agents ; administration & dosage ; chemistry ; Antineoplastic Agents, Phytogenic ; administration & dosage ; chemistry ; Colchicine ; administration & dosage ; chemistry ; Deoxycholic Acid ; Drug Carriers ; Gout Suppressants ; administration & dosage ; chemistry ; Mitoxantrone ; administration & dosage ; chemistry ; Particle Size ; Phosphatidylcholines ; Solubility ; Technology, Pharmaceutical ; methods ; Vincristine ; administration & dosage ; chemistry

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

BACKGROUNDLiver targeting drug delivery systems can improve the curative effects and relieve the cytotoxicity of the chemotherapy drugs in the treatment of liver diseases. Nanoparticles carrying therapeutic drugs are currently under hot investigation with great clinical significance. This study was aimed to investigate the different tissue distribution of the adriamycin polybutylcyanoacrylate nanoparticle (ADM-PBCA-NP) in the mice body after an injection via lateral tail vein, and to study the liver targeting effects of ADM-PBCA-NP in different diameters on normal mice liver.

METHODSOne hundred and eighty Kunming mice were randomly divided into 6 groups with 30 mice in each group (5 treatment groups of ADM-PBCA-NP in the different diameter ranges, non-conjugated free adriamycin injection was employed as the control group). A single dose of either conjugated or free adriamycin equaled 2 mg/kg of body weight was delivered via the tail vein. Five mice in each trail were sacrificed at 5, 15, 30 minutes, 1, 5 and 12 hours postinjection, respectively. The adriamycin concentrations in the respectively collected liver, kidney, spleen, heart, lung and plasma were demonstrated using a high performance liquid chromatography with fluorescence detector.

RESULTSCompared with the control group, adriamycin was hardly detected in the heart muscle of the treatment groups (P < 0.05). The nanoparticle-conjugated adriamycin was cleaned up quickly from the kidney tissue. The adriamycin concentrations of the mice liver and spleen in the experimental groups were significantly higher than that in the control group, except for the group with the nanoparticles diameters of (22.3 +/- 6.2) nm (P < 0.05). The ADM-PBCA-NP in (101.0 +/- 20.3) nm diameter had the highest liver distribution, and the second highest adriamycin distribution in liver was the group of (143.0 +/- 23.5) nm diameter (P < 0.05). Moreover, adriamycin was released slowly in the liver during the detection period in the experimental groups. ADM-PBCA-NP in (22.3 +/- 6.2) nm diameter was not distributed in the tissue of the liver, kidney, heart, spleen, and lung.

CONCLUSIONSADM-PBCA-NP in 100 - 150 nm diameter range has the best liver targeting with a characteristic of slow medicine release. It also decreases the medicine distribution in the heart, kidney and lung. In the treatment of liver cancer, the polybutylcyanoacrylate nanoparticles system has a good liver targeting ability, which increases the anticancer activity and markedly decreases the toxicity of adriamycin.

Animals ; Antineoplastic Agents ; administration & dosage ; Doxorubicin ; administration & dosage ; Drug Delivery Systems ; Enbucrilate ; administration & dosage ; Liver ; metabolism ; Mice ; Nanostructures ; Tissue Distribution

Antineoplastic Agents ; administration & dosage ; pharmacology ; Drug Delivery Systems ; Humans ; Liposomes ; administration & dosage ; pharmacology ; Sesquiterpenes ; administration & dosage ; pharmacology