To evaluate the efficacy and safety of drug-eluding beads transarterial chemoembolization (DEB-TACE) in treatment of unrecectable hepatocellular carcinoma (HCC).The clinical data of 42 consecutive HCC patients undergoing TACE were retrospectively analyzed, including 20 cases received conventional TACE (cTACE group) and 22 cases received TACE with epirubicine-loaded microspheres (CalliSpheres) (DEB-TACE group). MRI scans were performed 1 week before and 1, 3 and 6 months after initial therapy. The response to treatment, disease recurrence, complications and adverse effects were documented and compared between two groups.There were no significant differences in 1-month, 3-month and 6-month objective response rate (CR+PR) and disease control rate (CR+PR+SD), disease recurrence, complications and adverse effects of interventional therapy between cTACE group and DEB-TACE group. Additionally, there were no significant differences about locoregional biliary injuries, intrahepatic biloma, and newly detected intra- or extrahepatic HCC on MRI between cTACE group and DEB-TACE group.There were no statistically significant differences between cTACE group and DEB-TACE group with regard to the short-term response, disease recurrence, complications and side effects. Hepatic-locoregional complications may be more frequent in DEB-TACE group than those in cTACE group.
Carcinoma, Hepatocellular ; diagnostic imaging ; therapy ; Chemoembolization, Therapeutic ; adverse effects ; instrumentation ; methods ; Comparative Effectiveness Research ; Drug Delivery Systems ; instrumentation ; methods ; Epirubicin ; administration & dosage ; therapeutic use ; Humans ; Liver Neoplasms ; Magnetic Resonance Imaging ; Microspheres ; Neoplasm Recurrence, Local ; Retrospective Studies ; Treatment Outcome

New enrofloxacin microspheres were formulated, and their physical properties, lung-targeting ability, and tissue distribution in rats were examined. The microspheres had a regular and round shape. The mean diameter was 10.06 microm, and the diameter of 89.93% of all microspheres ranged from 7.0 microm to 30.0 microm. Tissue distribution of the microspheres was evaluated along with a conventional enrofloxacin preparation after a single intravenous injection (7.5 mg of enrofloxacin/kg bw). The results showed that the elimination half-life (t(1/2beta)) of enrofloxacin from lung was prolonged from 7.94 h for the conventional enrofloxacin to 13.28 h for the microspheres. Area under the lung concentration versus time curve from 0 h to infinity (AUC(0-infinity)) was increased from 11.66 h.microg/g to 508.00 h.microg/g. The peak concentration (Cmax) in lung was increased from 5.95 microg/g to 93.36 microg/g. Three lung-targeting parameters were further assessed and showed that the microspheres had remarkable lung-targeting capabilities.
Animals ; Anti-Bacterial Agents/*adverse effects ; Drug Delivery Systems/instrumentation/*methods ; Female ; Fluoroquinolones/*adverse effects ; Half-Life ; Humans ; Injections, Intravenous ; Lung/*drug effects ; Male ; *Microspheres ; Rats ; Rats, Sprague-Dawley ; Tissue Distribution

The present study was designed to develop and evaluate glycyrrhetinic acid-graft-hyaluronic acid (HGA) conjugate for intravenous paclitaxel (PTX) delivery. Lyophilized PTX-loaded self-assembled HGA nanoparticles (PTX/HGAs) were prepared and characterized by dynamic light scattering measurements. Hemolysis test, intravenous irritation assessment, and in vitro and in vivo pharmacodynamic studies were carried out. B16F10 and HepG2 cells were used in the cell apoptosis analysis. The mouse MDA-MB-231 xenograft model was used for the evaluation of in vivo anticancer activity of the drugs, by the analysis of tumor growth and side effects on other tissues. PTX/HGAs showed high stability and good biocompability. Compared with PTX plus GA plus HA solution, PTX/HGAs displayed obvious superiority in inducing the apoptosis of the cancer cells. Following systemic administration, PTX/HGAs efficiently suppressed tumor growth, with mean tumor inhibition ratio (TIR) being 65.08%, which was significantly higher than that of PTX plus GA plus HA treatment. In conclusion, PTX/HGAs demonstrated inhibitory effects tumor growth without unwanted side effects, suggesting that HGA conjugates hold a great potential as a delivery carrier for cancer chemotherapeutics to improve therapeutic efficacy and minimize adverse effects.
Animals ; Antineoplastic Agents ; administration & dosage ; adverse effects ; chemistry ; Apoptosis ; drug effects ; Drug Carriers ; chemistry ; Drug Delivery Systems ; instrumentation ; methods ; Drug Synergism ; Female ; Glycyrrhetinic Acid ; chemistry ; Hep G2 Cells ; Humans ; Hyaluronic Acid ; chemistry ; Male ; Mice ; Paclitaxel ; administration & dosage ; adverse effects ; chemistry

Paracetamol was used as a model drug in this study to investigate the synergetic effects of lipid coating and beta-cyclodextrin (beta-CD) inclusion for masking the bitter taste of poorly soluble drugs. To control the concentration as low as possible of the free drug which produced a bitter taste, a kinetic model was established to calculate the drug distribution theoretically among the free drug in medium, lipid coated particles and molecular inclusion on the basis of the preparation and characterization of the lipid microspheres, so as to select the proper amount of beta-CD. Finally, the synergetic drug delivery systems were prepared and characterized by 1H nuclear magnetic resonance (1H NMR), molecular simulation and the electronic tongue. As a result, the drug release rate constant (k) of the lipid microspheres coated with octadecanol was determined as 0.001 270 s(-1). Then, the synergetic drug delivery systems were prepared with the ratio of 6.74 : 1 (w/w) for beta-CD and paracetamol. The chemical shift values for the fingerprint peaks of paracetamol all increased and hydrogen bonds were formed between the oxygen on the phenolic hydroxyl group, the nitrogen on the imino in paracetamol and the hydrogens on the hydroxyl groups in beta-CD. The results tested by the electronic tongue indicated that the paracetamol, lipid microspheres, beta-CD inclusion and their mixture showed different taste characteristics, with the bitterness order of the synergetic drug delivery systems approximately lipid microspheres < beta-CD inclusion < paracetamol, which confirmed the synergetic taste masking effects of lipid coating and beta-CD molecular inclusion. In summary, the synergetic taste masking was jointly achieved through the retard of the drug release by the lipid coating and the inclusion of the free paracetamol by beta-CD through hydrogen bonds.
Acetaminophen ; administration & dosage ; chemistry ; Administration, Oral ; Drug Delivery Systems ; Electrical Equipment and Supplies ; Electrochemical Techniques ; instrumentation ; methods ; Hydrogen Bonding ; Kinetics ; Lipids ; chemistry ; Microspheres ; Solubility ; Taste ; drug effects ; beta-Cyclodextrins ; chemistry

The paeonol proniosomes ointment and ordinary ointment were administered to rats. Physiological saline served as perfused solution. The perfusion rate was 5 mL x L(-1) and the microdialysis samples were collected every 20 min intervals. The paeonol concentration in perfused solution was determined by HPLC. Investigation of the pharmacokinetics of paeonol proniosomes ointment and ordinary ointment by the skin-blood synchronous microdialysis coupled with HPLC is reported in this study. The results show that the recovery was (54.80 +/- 1.50)% in vitro and (54.58 +/- 4.61)% in vivo. The results showed that paeonol proniosomes ointment significantly raised the drug concentrations in skin more than the paeonol ordinary ointment. The paeono proniosomes ointment has less drugs into the blood as the ordinary ointments in blood, but its blood drug concentrations were steadier. The paeonol proniosomes ointment may be developed into a new preparation.
Acetophenones ; administration & dosage ; blood ; chemistry ; pharmacokinetics ; Animals ; Drug Delivery Systems ; instrumentation ; methods ; Drugs, Chinese Herbal ; administration & dosage ; chemistry ; pharmacokinetics ; Male ; Microdialysis ; Ointments ; administration & dosage ; chemistry ; pharmacokinetics ; Paeonia ; chemistry ; Rats ; Rats, Wistar ; Skin ; metabolism

Responsive drug delivery system can release drug at specific time and sites, and effectively overcome the drug resistance of organisms. With such advantages as drug protection, local targeting, inhibition of enzymatic activity, memory and expression, it has good prospect of application. So far, many chemical preparations have been launched in the market. This article mainly summarizes the advance in studies on establishment methods of responsive drug delivery system, while proposing research ideas for the traditional Chinese medicine component-based responsive drug delivery system according to the multi-component, multi-link and multi-target characteristics, in the expectation of providing reference and thought for the development of the drug delivery system.
Animals ; Drug Delivery Systems ; instrumentation ; methods ; trends ; Drugs, Chinese Herbal ; administration & dosage ; chemistry ; Humans

The development of automatic drug delivery is reviewed in this paper. The control-relevance of models, the relevant algorithm, the system running and the simulation effect are introduced. The value for clinical application of each case is assessed. The new advances and high-lights of researches are discussed.
Algorithms ; Drug Delivery Systems ; instrumentation ; Drug Therapy, Computer-Assisted ; instrumentation ; Humans ; Infusion Pumps ; Monitoring, Physiologic ; methods

OBJECTIVETo prepare ginkgolide B-loaded self microemulsifying drug delivery system (SMEDDS) and evaluate its quality.

METHODThe solubility of ginkgolide B in different oil, surfactant and co-surfactant were measured by HPLC-ESI-MS. The GB-SMEDDS formulation was optimized by the self emulsifying efficiency of various combinations of oil and mix-surfactant evaluated by using pseudo-temary phase diagram. The preliminary stability of GB-SEMEDDS was evaluated by the variety of loading rate of GB and dispersed medium. The morphology, the particle size and the formulation stability were evaluated after diluting by 0.1 mol x L(-1) HCl.

RESULTThe blank self microemulsified system was composed of ethyl oleate-( cremophor EL-lecithin-ethanol, 4: 1:2) (40: 60), the loading dosage was 2.5%. Little influence of GB and emulsified medium was observed on the stability of GB-SEMDDS. After diluted with 0.1 mol x L(-1) HCl, the morphology of the microemulsion was homogeneous small spherical drops observed under electro-microscope. The particle size was (41.6 +/- 1.11) nm, the self microemulsifing time was around 2 min. The formulation was stable within 8 h, without significant changes in particle size and separation of drugs.

CONCLUSIONGB-SMEDDS is easy to prepare and its quality is stable. The solubility of GB was significantly improved by SMEDDS.

Chemistry, Pharmaceutical ; instrumentation ; methods ; Drug Delivery Systems ; instrumentation ; methods ; Emulsions ; chemistry ; Ginkgolides ; chemistry ; pharmacokinetics ; Lactones ; chemistry ; pharmacokinetics ; Particle Size ; Solubility ; Surface-Active Agents ; chemistry

The recent fast development in biotechnology has resulted in a large number of therapeutic biologicals coming in the foreground for clinical application. Transdermal drug delivery (TDD) is designed for patching the drug on the skin, and then the drug molecules permeate through the skin into the subcutaneous capillary vessels. However,very few drugs can be administered transdermally at the therapeutic levels to pass through the barrier of stratum corneum. Several physical and chemical methods are applied to improve the permeability of skin. Research result shows that the low-frequency ultrasonic technique can extraordinarily increase the rate of permeation. As a result, it is becoming one of the potential methods that serve as the substitutes for traditional methods. In this paper is presented a type of equipment based on MSP430. The principle of design, the structure of hardware, and the applied function in this area are described.
Administration, Cutaneous ; Drug Delivery Systems ; instrumentation ; methods ; Equipment Design ; Humans ; Pharmaceutical Preparations ; administration & dosage ; Skin Absorption ; radiation effects ; Ultrasonics

Ultrasonic beam can be focused on a particular tissue. As ultrasound contrast agents for medical ultrasound imaging, gas-filled microbubbles can also be used as drugs or gene carriers. Therefore, ultrasonic microbubbles become a topic of intense interest in drug delivery because they can be used as gene targeting delivery systems. Based on the relevant materials, the applications of ultrasonic microbubbles as gene delivery systems in various tissues in vivo were reviewed, such as cardiac, vascular, skeletal muscle and tumor. Their potential problems in future use were also discussed.
Animals ; Colonic Neoplasms ; therapy ; Coronary Disease ; therapy ; Drug Delivery Systems ; instrumentation ; methods ; trends ; Genetic Therapy ; instrumentation ; methods ; trends ; Humans ; Lipids ; chemistry ; Microbubbles ; Ultrasonics