Free Drug Theory

2021 ◽  
pp. 1-6
Author(s):  
Alan Talevi ◽  
Carolina L. Bellera
Keyword(s):  
Free Drug

Free Drug Samples Are of Concern in Pediatric Population

2008 ◽  
Vol 42 (11) ◽  
pp. 33
Author(s):  
SHARON WORCESTER
Keyword(s):  
Pediatric Population ◽  
Free Drug ◽  
Free Drug Samples

Free Drug Samples Create Ethical Rift Among MDs

2007 ◽  
Vol 40 (2) ◽  
pp. 45
Author(s):  
PATRICE WENDLING
Keyword(s):  
Free Drug ◽  
Free Drug Samples

Poor, Uninsured Less Likely to Get Free Drug Samples

2008 ◽  
Vol 4 (2) ◽  
pp. 7
Author(s):  
Jane Anderson
Keyword(s):  
Free Drug ◽  
Free Drug Samples

Encapsulation of Imatinib in Targeted KIT-5 Nanoparticles for Reducing its Cardiotoxicity and Hepatotoxicity

2020 ◽  
Vol 20 (16) ◽  
pp. 1966-1980
Author(s):  
Jaleh Varshosaz ◽  
Saeedeh Fardshouraki ◽  
Mina Mirian ◽  
Leila Safaeian ◽  
Setareh Jandaghian ◽  
...  
Keyword(s):  
Controlled Release ◽  
Side Effects ◽  
Kinase Inhibitor ◽  
Lymphoblastic Leukemia ◽  
Drug Carrier ◽  
Free Drug ◽  
Jurkat Cells ◽  
Targeted Nanoparticles ◽  
Inhibitor Drug ◽  
Histopathological Results

Background: Using imatinib, a tyrosine kinase inhibitor drug used in lymphoblastic leukemia, has always had limitations due to its cardiotoxicity and hepatotoxicity side effects. The objective of this study is to develop a target-oriented drug carrier to minimize these adverse effects by the controlled release of the drug. Methods: KIT-5 nanoparticles were functionalized with 3-aminopropyltriethoxysilane and conjugated to rituximab as the targeting agent for the CD20 positive receptors of the B-cells. Then they were loaded with imatinib and their physical properties were characterized. The cell cytotoxicity of the nanoparticles was studied by MTT assay in Ramos (CD20 positive) and Jurkat cell lines (CD20 negative) and their cellular uptake was shown by fluorescence microscope. Wistar rats received an intraperitoneal injection of 50 mg/kg of the free drug or targeted nanoparticles for 21 days. Then the level of aspartate Aminotransferase (AST), alanine Aminotransferase (ALT), Alkaline Phosphatase (ALP) and Lactate Dehydrogenase (LDH) were measured in serum of animals. The cardiotoxicity and hepatotoxicity of the drug were also studied by hematoxylin and eosin staining of the tissues. Results: The targeted nanoparticles of imatinib showed to be more cytotoxic to Ramos cells rather than Jurkat cells. The results of the biochemical analysis displayed a significant reduction in AST, ALT, ALP, and LDH levels in animals treated with targeted nanoparticles, compared to the free drug group. By comparison with the free imatinib, histopathological results represented less cardiotoxicity and hepatotoxicity in the animals, which received the drug through the current designed delivery system. Conclusion: The obtained results confirmed that the rituximab targeted KIT-5 nanoparticles are promising in the controlled release of imatinib and could decrease its cardiotoxicity and hepatotoxicity side effects.

scholarly journals 1304. Characterization of Tebipenem Pivoxil Hydrobromide Pharmacokinetics-Pharmacodynamics (PK-PD) in a Neutropenic Murine Acute Pyelonephritis (AP) Model

2020 ◽  
Vol 7 (Supplement_1) ◽  
pp. S666-S666
Author(s):  
Brian D VanScoy ◽  
Steven Fikes ◽  
Christopher M Rubino ◽  
Sujata M Bhavnani ◽  
Nicole S Cotroneo ◽  
...  
Keyword(s):  
Acute Pyelonephritis ◽  
Free Drug ◽  
Research Support ◽  
Model Free ◽  
Drug Concentrations ◽  
Drug Plasma ◽  
Dose Ranging ◽  
Tebipenem Pivoxil ◽  
Tract Infections ◽  
The Relationship

Abstract Background Tebipenem pivoxil hydrobromide (tebipenem HBr), an orally (PO) bioavailable prodrug of tebipenem, is a carbapenem with broad-spectrum activity against Gram-positive and -negative bacteria that is being developed for the treatment of patients with complicated urinary tract infections, including AP. Data from a one-compartment in vitro infection model demonstrated that the ratio of free-drug plasma area under the curve (AUC) to MIC with adjustment for dosing interval (τ) (AUC:MIC ratio•1/τ) was the PK-PD index most associated with tebipenem HBr efficacy [VanScoy BD et al., IDWeek 2019, Poster 1565]. Studies were undertaken to characterize the magnitude of tebipenem HBr free-drug plasma AUC:MIC ratio•1/τ associated with efficacy for Enterobacteriaceae using a neutropenic murine AP model. Methods A single dose pharmacokinetic study was completed in neutropenic mice infected via intra-renal injection with 104 CFU/kidney of Escherichia coli NCTC 13441. Following PO administration of 4 tebipenem HBr doses (1, 15, 45 and 100 mg/kg), plasma samples were collected at 0.25, 0.5, 1, 2, 4, 6 and 8 hours post-treatment initiation and drug concentrations were determined using LC/MS/MS. Dose-ranging studies were completed using a panel of 7 Enterobacteriaceae isolates (tebipenem HBr MIC values of 0.015 to 0.5 mg/L). Mice were infected with 104 CFU/kidney via intra-renal injection. Two hours post-incubation, 8 total daily tebipenem HBr doses (0.3 to 135 mg/kg) were fractionated into regimens given every 8 hours. The relationship between change in log10 CFU/g from baseline at 24 hours and free-drug plasma AUC:MIC ratio•1/τ was fit using a Hill-type model. Free-drug plasma AUC:MIC ratio•1/τ values associated with net bacterial stasis and 1- and 2-log10 CFU/g reductions from baseline at 24 hours were determined. Results The relationship between change in log10 CFU/g from baseline at 24 hours and tebipenem HBr free-drug plasma AUC:MIC ratio•1/τ described the data well (r2 = 0.833). Free-drug plasma AUC:MIC ratio•1/τ values associated with net bacterial stasis and a 1-log10 CFU/g reduction from baseline were 26.2 and 54.1, respectively. A 2-log10 CFU/g reduction was not achieved. Relationship between change in log10 CFU/g from baseline at 24 hours and tebipenem HBr free-drug plasma AUC:MIC ratio•1/τ based on data for a panel of Enterobacteriaceae isolates evaluated in the dose-ranging studies conducted using a neutropenic murine acute pyelonephritis model Conclusion These data will be useful to support tebipenem HBr dose selection for clinical studies in patients with AP. Disclosures Brian D. VanScoy, B.S., Institute for Clinical Pharmacodynamics, Inc. (Employee)Spero Therapeutics (Grant/Research Support) Steven Fikes, BA, Institute for Clinical Pharmacodynamics, Inc. (Employee)Spero Therapeutics (Grant/Research Support) Christopher M. Rubino, PharMD, Institute for Clinical Pharmacodynamics, Inc. (Employee)Spero Therapeutics (Grant/Research Support) Sujata M. Bhavnani, PharMD, MS, FIDSA, Institute for Clinical Pharmacodynamics, Inc. (Employee)Spero Therapeutics (Grant/Research Support) Nicole S. Cotroneo, BS, Spero Therapeutics (Employee, Shareholder) Ian A. Critchley, PhD, Spero Therapeutics (Employee, Shareholder) Thomas R. Parr, PhD, Spero Therapeutics (Employee, Shareholder) Paul G. Ambrose, PharMD, FIDSA, Institute for Clinical Pharmacodynamics, Inc. (Employee)Spero Therapeutics (Grant/Research Support)

Monitoring free drug concentrations: challenges

Bioanalysis ◽  
2011 ◽  
Vol 3 (15) ◽  
pp. 1753-1768 ◽  
Author(s):  
Florin Marcel Musteata
Keyword(s):  
Free Drug ◽  
Drug Concentrations

scholarly journals Different Microfluidic Environments for In Vitro Testing of Lipid Nanoparticles against Osteosarcoma

2021 ◽  
Vol 8 (6) ◽  
pp. 77
Author(s):  
Oihane Mitxelena-Iribarren ◽  
Sara Lizarbe-Sancha ◽  
Jay Campisi ◽  
Sergio Arana ◽  
Maite Mujika
Keyword(s):  
Target Therapy ◽  
Treatment Options ◽  
Lipid Nanoparticles ◽  
Cell Number ◽  
Current Treatment ◽  
Drug Dose ◽  
Free Drug ◽  
Tumor Treatment ◽  
Equal Dose

The use of lipid nanoparticles as biodegradable shells for controlled drug delivery shows promise as a more effective and targeted tumor treatment than traditional treatment methods. Although the combination of target therapy with nanotechnology created new hope for cancer treatment, methodological issues during in vitro validation of nanovehicles slowed their application. In the current work, the effect of methotrexate (MTX) encapsulated in different matrices was evaluated in a dynamic microfluidic platform. Effects on the viability of osteosarcoma cells in the presence of recirculation of cell media, free MTX and two types of blank and drug-containing nanoparticles were successfully assessed in different tumor-mimicking microenvironments. Encapsulated MTX was more effective than the equal dose free drug treatment, as cell death significantly increased under the recirculation of both types of drug-loaded nanoparticles in all concentrations. In fact, MTX-nanoparticles reduced cell population 50 times more than the free drug when 150-µM drug dose was recirculated. Moreover, when compared to the equivalent free drug dose recirculation, cell number was reduced 60 and 100 points more under recirculation of each nanoparticle with a 15-µM drug concentration. Thus, the results obtained with the microfluidic model present MTX-lipid nanoparticles as a promising and more effective therapy for pediatric osteosarcoma treatment than current treatment options.

Apoptotic Bodies in the Pancreatic Tumor Cell Culture Media Enable Label‐Free Drug Sensitivity Assessment by Impedance Cytometry

2021 ◽  
pp. 2100438
Author(s):  
Carlos Honrado ◽  
Sara J. Adair ◽  
John H. Moore ◽  
Armita Salahi ◽  
Todd W. Bauer ◽  
...  
Keyword(s):  
Drug Sensitivity ◽  
Pancreatic Tumor ◽  
Culture Media ◽  
Free Drug ◽  
Label Free ◽  
Apoptotic Bodies ◽  
Cell Culture Media ◽  
Pancreatic Tumor Cell ◽  
Sensitivity Assessment ◽  
Tumor Cell Culture

scholarly journals Breast cancer drug delivery by novel drug-loaded chitosan-coated magnetic nanoparticles

2021 ◽  
Vol 12 (1) ◽  
Author(s):  
A. Taherian ◽  
N. Esfandiari ◽  
S. Rouhani
Keyword(s):  
Breast Cancer ◽  
Magnetic Nanoparticles ◽  
Free Drug ◽  
Pomegranate Peel ◽  
Vast Number ◽  
Therapeutic Method ◽  
Cytotoxicity Studies ◽  
Pomegranate Peel Extract ◽  
Novel Drug ◽  
Peel Extract

Abstract Background Breast cancer is one of the most challenging cancers among women which is considered one of the most lethal cancers to this date. From the time that cancer has been discovered, finding the best therapeutic method is still an ongoing process. As a novel therapeutic method, nanomedicine has brought a vast number of materials that could versatilely be used as a drug carrier. The purpose of this study is to develop a novel black pomegranate peel extract loaded with chitosan-coated magnetic nanoparticles to treat breast cancer cells. Results The morphology and size distribution of the nanoparticles studied by dynamic light scattering, atomic force microscopy, scanning, and transitional electron microscopy showed the spherical shape of the nanoparticles and their promising size range. Studies by Fourier transform infrared spectroscopy, X-ray diffraction, vibrating sample magnetometer, and zeta sizer confirmed the synthesis, substantial crystallinity, magnetic potential of the nanoparticles, and their satisfactory stability. The DPPH assay revealed that the obtained black pomegranate peel extract has 60% free radical scavenging activity. The cytotoxicity studies by MTT and LDH assay carried out on NIH/3T3, MBA-MB-231, and 4T1 cells confirmed that the magnetic nanoparticles had no significant cytotoxicity on the cells. However, the drug-loaded nanoparticles could significantly eradicate cancerous cells which had more efficiency comparing to free drug. Furthermore, free drug and drug-loaded nanoparticles had no toxic effect on normal cells. Conclusion Owing to the results achieved from this study, the novel drug-loaded nanoparticles are compatible to be used for breast cancer treatment and could potentially be used for further in vivo studies.

Synthesis, Chemical Characterisation, and DNA Binding Studies of Ferrocene-Incorporated Selenoureas

2013 ◽  
Vol 66 (6) ◽  
pp. 626 ◽  
Author(s):  
Raja Azadar Hussain ◽  
Amin Badshah ◽  
Muhammad Nawaz Tahir ◽  
Bhajan Lal ◽  
Inayat Ali Khan
Keyword(s):  
Cyclic Voltammetry ◽  
Dna Binding ◽  
Atomic Absorption Spectrophotometry ◽  
Free Drug ◽  
X Ray Diffraction ◽  
Peak Potential ◽  
Binding Studies ◽  
Vis Spectroscopy ◽  
Dna Binding Studies ◽  
And Diffusion

In this article we have presented the synthesis, chemical characterisation (by NMR and FTIR spectroscopy, atomic absorption spectrophotometry, elemental analysis, and single crystal X-ray diffraction), electrochemistry, and DNA binding studies (with cyclic voltammetry, viscometry, and UV-vis spectroscopy) of six new ferrocene incorporated selenoureas. All the six compounds interact electrostatically with DNA which was evident by a negative shift in the cyclic voltammetry peak potential of the drug–DNA adduct relative to the free drug. The drug–DNA binding constant was calculated by a decrease in peak current after the addition of DNA to the free drug. We have also reported binding site sizes and diffusion coefficients of the synthesised compounds.

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