Design and Evaluation of Folate-Appended α-, β-, and γ-Cyclodextrins Having a Caproic Acid as a Tumor Selective Antitumor Drug Carrier in Vitro and in Vivo

2013 ◽  
Vol 14 (12) ◽  
pp. 4420-4428 ◽  
Author(s):  
Ayaka Okamatsu ◽  
Keiichi Motoyama ◽  
Risako Onodera ◽  
Taishi Higashi ◽  
Takahiro Koshigoe ◽  
...  
Keyword(s):  
Drug Carrier ◽  
Caproic Acid ◽  
Antitumor Drug ◽  
Tumor Selective

Accumulation of Macromolecular Particles in the Reticuloendothelial System (RES) Mediated by Platelet Aggregation and Disaggregation

1969 ◽  
Vol 22 (03) ◽  
pp. 496-507 ◽  
Author(s):  
W.G van Aken ◽  
J Vreeken
Keyword(s):  
Platelet Aggregation ◽  
Degradation Products ◽  
Reticuloendothelial System ◽  
Caproic Acid ◽  
Carbon Particles ◽  
Carbon Clearance ◽  
Aggregation And Disaggregation ◽  
Platelet Aggregates

SummaryCarbon particles cause platelet aggregation in vitro and in vivo. Prior studies established that substances which modify thrombocyte aggregation also influence the rate at which carbon is cleared from the blood.This study was performed in order to elucidate the mechanism by which the carbon-platelet aggregates specifically accumulate in the RES.Activation of fibrinolysis by urokinase or streptokinase reduced the carbon clearance rate, probably due to generated fibrinogen degradation products (FDP). Isolated FDP decreased the carbon clearance and caused disaggregation of platelets and particles in vitro. Inhibition of fibrinolysis by epsilon-amino-caproic acid (EACA), initially accelerated the disappearance of carbon and caused particle accumulation outside the RES, predominantly in the lungs. It is supposed that platelet aggregation and locally activated fibrinolysis act together in the clearance of particles. In the normal situation the RES with its well known low fibrinolytic activity, becomes the receptor of the particles.

scholarly journals Folate-Functionalized Mesoporous Hollow SnO2 Nanofibers as a Targeting Drug Carrier to Improve the Antitumor Effect of Paclitaxel for Liver Cancer Therapy

2018 ◽  
Vol 2018 ◽  
pp. 1-11
Author(s):  
Huiling Lv ◽  
Chao Wu ◽  
Xuan Liu ◽  
Andi Bai ◽  
Yue Cao ◽  
...  
Keyword(s):  
Cancer Therapy ◽  
Liver Cancer ◽  
Drug Carrier ◽  
In Vitro Release ◽  
Hollow Structure ◽  
Amorphous State ◽  
Outer Diameter ◽  
Drug Delivery Carrier

In this study, we prepared PTX-loaded mesoporous hollow SnO2 nanofibers conjugated with folic acid (SFNFP) for liver cancer therapy. According to SEM and TEM characterization, SFNF showed a mesoporous hollow structure. The average outer diameter was 200 nm, and the wall thickness was 50 nm. The DSC and XRD study showed that PTX in the channels of nanofibers was present in an amorphous state. The in vitro release experiments demonstrated that SFNF could efficiently improve the dissolution rate of PTX. Both in vitro cell experiments and in vivo antitumor experiments showed that SFNFP could efficiently inhibit the growth of liver cancer cells. Therefore, SFNF is a promising targeting antitumor drug delivery carrier.

scholarly journals DEVELOPMENT OF RITONAVIR LOADED NANOPARTICLES: IN VITRO AND IN VIVO CHARACTERIZATION

2018 ◽  
Vol 11 (3) ◽  
pp. 284
Author(s):  
Pravin S Patil ◽  
Shashikant C Dhawale
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Dissolution Rate ◽  
Drug Carrier ◽  
Entrapment Efficiency ◽  
Significant Rise ◽  
Scanning Calorimetry ◽  
In Vitro Drug Release

 Objective: The purpose of the present investigation was to develop a nanosuspension to improve dissolution rate and oral bioavailability of ritonavir.Methods: Extended-release ritonavir loaded nanoparticles were prepared using the polymeric system by nanoprecipitation technique. Further, the effect of Eudragit RL100 (polymeric matrix) and polyvinyl alcohol (surfactant) was investigated on particle size and distribution, drug content, entrapment efficiency, and in vitro drug release from nanosuspension where a strong influence of polymeric contents was observed. Drug-excipient compatibility and amorphous nature of drug in prepared nanoparticles were confirmed by Fourier transform infrared spectroscopy, differential scanning calorimetry, and powder X-ray diffraction studies, respectively.Results: Hydrophobic portions of Eudragit RL100 could result in enhanced encapsulation efficiency. However, increase in polymer and surfactant contents lead to enlarged particle size proportionately as confirmed by transmission electron microscopy. Nanosuspension showed a significant rise in dissolution rate with complete in vitro drug release as well as higher bioavailability in rats compared to the pure drug.Conclusion: The nanoprecipitation technique used in present research could be further explored for the development of different antiretroviral drug carrier therapeutics.

scholarly journals Albumin coated liposomes: a novel platform for macrophage specific drug delivery

2011 ◽  
Vol 1 (1) ◽  
pp. 2 ◽  
Author(s):  
Clément Vuarchey ◽  
Sushil Kumar ◽  
Reto Schwendener
Keyword(s):  
Drug Delivery ◽  
Drug Carrier ◽  
Cell Types ◽  
Specific Drug ◽  
Splenic Macrophages ◽  
Peg Liposomes ◽  
Short Time ◽  
Liposome Surface

Here we report a new and efficient approach of macrophage specific drug delivery by coating liposomes with albumin. Activated albumin was reacted with liposomes containing polyethylene glycol (PEG) as hydrophilic spacers to create a flexible layer of covalently bound albumin molecules on the liposome surface. Albumin coated liposomes were taken up faster and more efficiently than uncoated liposomes by murine macrophages. Liposome uptake was significantly higher in macropha - ges as compared to other cell types tested (endothelial cells, fibroblasts, tumor cells), suggesting specificity for macrophages. In vivo, splenic macrophages phagocytosed BSA coated liposomes (BSA-L) at faster rates compared to conventional liposomes (L) and PEG liposomes (PEG-L). To prove the effectiveness of this new macrophage specific drug carrier, the bisphosphonates clodronate and zoledronate were encapsulated in BSA-L and compared with conventional liposomes. <em>In vitro</em>, treatment of macrophages with clodronate or zoledronate in BSA-L led to cytotoxic activity within a very short time and to up to 50-fold reduced IC50 concentrations. <em>In vivo</em>, clodronate encapsulated in BSA-L depleted splenic macrophages at a 5-fold lower concentration as conventional clodronate-liposomes. Our results highlight the pharmaceutical benefits of albumin-coated liposomes for macrophage specific drug delivery.

scholarly journals High in Vitro and in Vivo Tumor-Selective Novel Ruthenium(II) Complexes with 3-(2′-Benzimidazolyl)-7-fluoro-coumarin

2019 ◽  
Vol 10 (6) ◽  
pp. 936-940 ◽  
Author(s):  
Qi-Pin Qin ◽  
Zhen-Feng Wang ◽  
Xiao-Ling Huang ◽  
Ming-Xiong Tan ◽  
Bei-Bei Shi ◽  
...  
Keyword(s):  
Tumor Selective

scholarly journals Preparation, in vitro and in vivo evaluation of algino-pectinate bioadhesive microspheres: An investigation of the effects of polymers using multiple comparison analysis

2010 ◽  
Vol 60 (3) ◽  
pp. 255-266 ◽  
Author(s):  
Santanu Chakraborty ◽  
Madhusmruti Khandai ◽  
Anuradha Sharma ◽  
Nazia Khanam ◽  
Ch. Patra ◽  
...  
Keyword(s):  
Drug Release ◽  
Oral Delivery ◽  
Drug Carrier ◽  
Polymer Concentration ◽  
Multiple Comparison ◽  
Prolonged Release ◽  
Comparison Analysis ◽  
Significant Difference

Preparation,in vitroandin vivoevaluation of algino-pectinate bioadhesive microspheres: An investigation of the effects of polymers using multiple comparison analysisIonotropic gelation was used to entrap aceclofenac into algino-pectinate bioadhesive microspheres as a potential drug carrier for the oral delivery of this anti-inflammatory drug. Microspheres were investigatedin vitrofor possible sustained drug release and their usein vivoas a gastroprotective system for aceclofenac. Polymer concentration and polymer/drug ratio were analyzed for their influence on microsphere properties. The microspheres exhibited good bioadhesive property and showed high drug entrapment efficiency. Drug release profiles exhibited faster release of aceclofenac from alginate microspheres whereas algino-pectinate microspheres showed prolonged release. Dunnet's multiple comparison analysis suggested a significant difference in percent inhibition of paw edema when the optimized formulation was compared to pure drug. It was concluded that the algino-pectinate bioadhesive formulations exhibit promising properties of a sustained release form for aceclofenac and that they provide distinct tissue protection in the stomach.

Continued in vitro and in vivo release of an antitumor drug from albumin microspheres

1983 ◽  
Vol 39 (8) ◽  
pp. 913-916 ◽  
Author(s):  
S. Fujimoto ◽  
F. Endoh ◽  
Y. Kitsukawa ◽  
K. Okui ◽  
Y. Morimoto ◽  
...  
Keyword(s):  
Antitumor Drug ◽  
Albumin Microspheres ◽  
In Vivo Release

pH-Responsible fluorescent carbon nanoparticles for tumor selective theranostics via pH-turn on/off fluorescence and photothermal effect in vivo and in vitro

Nanoscale ◽  
2018 ◽  
Vol 10 (5) ◽  
pp. 2512-2523 ◽  
Author(s):  
Eun Bi Kang ◽  
Jung Eun Lee ◽  
Zihnil Adha Islamy Mazrad ◽  
Insik In ◽  
Ji Hoon Jeong ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Photothermal Therapy ◽  
Carbon Nanoparticles ◽  
Fluorescence Probes ◽  
Photothermal Effect ◽  
Turn On ◽  
Fluorescent Carbon Nanoparticles ◽  
Tumor Selective

Here we designed the functionalized FNP as “switch-on” fluorescence probes to sense intracellular cancer cells and controllable photothermal therapy (PTT) in vivo and in vitro.

scholarly journals THER-15. DEVELOPING TUMOR-HOMING CYTOTOXIC HUMAN INDUCED NEURAL STEM CELL THERAPY FOR BRAIN METASTASES

2019 ◽  
Vol 1 (Supplement_1) ◽  
pp. i13-i14
Author(s):  
Alison Mercer-Smith ◽  
Wulin Jiang ◽  
Juli Bago ◽  
Simon Khagi ◽  
Carey Anders ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Brain Metastases ◽  
Drug Carrier ◽  
Human Fibroblasts ◽  
Genetically Engineered ◽  
In Vivo Studies ◽  
Tumor Homing ◽  
The Brain

Abstract INTRODUCTION: Non-small cell lung cancer (NSCLC) and breast cancer are the most common cancers that metastasize to the brain. New therapies are needed to seek out and eradicate metastases. Genetically engineered neural stem cells (NSCs) have shown unique tumor-homing capacity, allowing them to deliver cytotoxic proteins directly to tumors. An ideal NSC drug carrier would be readily available and autologous. We have transdifferentiated human fibroblasts into induced NSCs (hiNSCs) that home to tumors and engineered the hiNSCs to release the cytotoxic protein TRAIL. Here we used intracerebroventricular (ICV) injections to deliver hiNSCs to metastatic foci. METHODS: We performed an in vitro efficacy co-culture assay, used in vivo studies to determine the migration, persistence, and efficacy of therapeutic hiNSCs against H460 NSCLC and triple-negative breast cancer MB231-Br tumors in the brain. Following the establishment of tumors in the brains of nude mice, hiNSCs were injected directly into the tumor or the ventricle contralateral to the site of tumor. The migration and persistence of hiNSCs was investigated by following the bioluminescence of the hiNSCs. The therapeutic efficacy of the hiNSCs was determined by following the bioluminescece of the tumor. RESULTS/CONCLUSION: Co-culture results demonstrated that hiNSC therapy reduced the viability of H460 and MB231-Br up to 75% and 99.8% respectively compared to non-treated controls. ICV-administered hiNSC serial imaging show that cells persisted for more than one week. Fluorescent analysis of tissue sections showed that hiNSCs co-localized with lateral and a contralateral tumors within 7 days. Using H460 and MB231-Br models, kinetic tracking of intracranial tumor volumes showed intratumoral or ICV-injected therapeutic hiNSCs reduced the growth rate of brain tumors by 31-fold and 3-fold, respectively. This work demonstrates for the first time that we can effectively deliver personalized cytotoxic tumor-homing cells through the ventricles to target brain metastases.

scholarly journals Improved In vivo Effect of Chrysin as an Absorption Enhancer Via the Preparation of Ternary Solid Dispersion with Brij®L4 and Aminoclay

2018 ◽  
Vol 16 (1) ◽  
pp. 86-92 ◽  
Author(s):  
Sang Hoon Lee ◽  
Yeo-song Lee ◽  
Jae Geun Song ◽  
Hyo-Kyung Han
Keyword(s):  
Drug Release ◽  
Drug Carrier ◽  
Solid Dispersions ◽  
Amorphous State ◽  
Absorption Enhancer ◽  
Cancer Resistance ◽  
Surface Acting ◽  
Strong Inhibitor

Background: Chrysin is a strong inhibitor of breast cancer resistance protein (BCRP) but it is practically insoluble in water. Effective solubilization of chrysin is critical for its pharmaceutical application as an absorption enhancer via inhibition of BCRP-mediated drug efflux. Objective: This study aimed to develop an effective oral formulation of chrysin to improve its in vivo effect as an absorption enhancer. Method: Solid dispersions (SDs) of chrysin were prepared with hydrophilic carriers having surface acting properties and a pH modulator. In vitro and in vivo characterizations were performed to select the optimal SDs of chrysin. Results: SDs with Brij&®L4 and aminoclay was most effective in increasing the solubility of chrysin by 13-53 fold at varying drug-carrier ratios. Furthermore, SDs significantly improved the dissolution rate and extent of drug release. SDs (chrysin: Brij&®L4: aminoclay=1:3:5) achieved approximately 60% and 83% drug release within 1 h and 8 h, respectively, in aqueous medium, while the dissolution of the untreated chrysin was less than 13%. XRD patterns indicated the amorphous state of chrysin in SDs. The SD formulation was effective in improving the bioavailability of topotecan, a BCRP substrate in rats. Following oral administration of topotecan with the SDs of chrysin, the Cmax and AUC of topotecan was enhanced by approximately 2.6- and 2-fold, respectively, while the untreated chrysin had no effect. Conclusion: The SD formulation of chrysin with Brij&®L4 and aminoclay appeared to be promising in improving the dissolution of chrysin and enhancing its in vivo effect as an absorption enhancer.

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