In vivo pharmacokinetic studies and intracellular delivery of methotrexate by means of glycine-tethered PLGA-based polymeric micelles

Publication date: 15 March 2017 Source:International Journal of Pharmaceutics, Volume 519, Issues 1–2 Author(s): Madhwi, Rajendra Kumar, Pramod Kumar, Bhupinder Singh, Gajanand Sharma, Om Prakash Katare, Kaisar Raza Methotrexate (MTX) is a widely used drug for the management of various kinds of cancers. However, numerous challenges are associated with MTX like poor aqueous solubility, dose-dependent side effects and poor-bioavailability. With an aim to explore the potential benefits in drug delivery of MTX, it was intended to fabricate glycine-PLGA-based polymeric micelles. Glycine was chemically linked to PLGA and the linkage was confirmed by FT-IR, and NMR-Spectroscopy. The developed polymeric micelles offered substantial loading to MTX with a pH-dependent drug release profile. The drug was released maximally at the cancer cell pH vis-à-vis blood plasma pH. The cytotoxicity of drug against MDA-MB-231 cell lines was enhanced by approx. 100% and the confocal laser scanning microscopy confirmed the localization of dye-tagged nanocarriers in the interiors of cancer cells. The bioavailable fraction of the drug was increased by approx. 4-folds, whereas elimination half-life was enhanced by around two-folds in Wistar rats. The novel approach offers a biodegradable and promising carrier for the better delivery of anticancer agents with immense promises of efficacy enhancement, improved delivery and better pharmacokinetic profile. Graphical abstract
Source: International Journal of Pharmaceutics - Category: Drugs & Pharmacology Source Type: research

Related Links:

Publication date: Available online 8 December 2018Source: Biocatalysis and Agricultural BiotechnologyAuthor(s): S.P. Angeline Kirubha, Alankruti RajputAbstractMagnetic nanoparticles (MNP) have been developed in the recent years for various applications like cell separation, immunoassay, and drug delivery. The present study involves the synthesis of stable, biocompatible Iron oxide MNP by coprecipitation of ferric chloride and ferrous chloride with Polyethylene glycol (PEG) as a surfactant to coat the nanoparticles twice. Scanning electron microscopic (SEM) images confirm the formation of uniform MNPs of size 12–17&nb...
Source: Biocatalysis and Agricultural Biotechnology - Category: Biotechnology Source Type: research
Vicky Phelan exposed a health scandal in Ireland after discovering her smear test for cervical cancer had been misread.
Source: BBC News | Health | UK Edition - Category: Consumer Health News Source Type: news
BackgroundThe study was conducted to evaluate the performance of a state ‐of‐the‐art commercial deep learning‐based computer‐aided diagnosis (DL‐CAD) system for detecting and characterizing pulmonary nodules.MethodsPulmonary nodules in 346 healthy subjects (male: female  = 221:125, mean age 51 years) from a lung cancer screening program conducted from March to November 2017 were screened using a DL‐CAD system and double reading independently, and their performance in nodule detection and characterization were evaluated. An expert panel combined the results of the DL‐CAD system and doubl...
Source: Thoracic Cancer - Category: Cancer & Oncology Authors: Tags: ORIGINAL ARTICLE Source Type: research
PET imaging tracers that track breast cancer enzymes could help guide treatment...Read more on AuntMinnie.comRelated Reading: SNMMI: Fluciclovine-PET changes prostate treatment Mammi-PET finds tiny breast lesions -- but could improve Fused MRI and PET improve specificity of breast MRI PEM performs well against breast MRI, whole-body PET NCPIC to provide PET breast scans for uninsured
Source: AuntMinnie.com Headlines - Category: Radiology Source Type: news
Publication date: Available online 6 December 2018Source: Biochimica et Biophysica Acta (BBA) - BiomembranesAuthor(s): D. Sivaramakrishna, Muvva D. Prasad, Musti J. SwamyAbstractN‑Acylserinols (NASOHs) exhibit anti-cancer activity by elevating ceramide levels, and/or by activating proapoptotic effectors. In the present work we investigated the thermotropic phase behavior and supramolecular organization of a homologous series of NASOHs (number of C-atoms in the acyl chain, n = 8–18), and the interaction of N-myristoylserinol (NMSOH) with cholesterol, and characterized cationic niosomes made up of NMSOH, choleste...
Source: Biochimica et Biophysica Acta (BBA) Biomembranes - Category: Biochemistry Source Type: research
Conclusion Patients with normal diastolic function at baseline receiving trastuzumab±anthracycline adjuvant therapy may develop DD before SD, therefore offering an opportunity for early referral to cardiologists to optimize cardiovascular risk factors and manage cardiotoxicity.
Source: Nuclear Medicine Communications - Category: Nuclear Medicine Tags: ORIGINAL ARTICLES Source Type: research
Conclusion 18F-FDG PET/CT showed good diagnostic and prognostic utility in recurrent MBC. It was better than bone scan in evaluation of skeletal metastases. Most importantly, 18F-FDG PET/CT helped in early detection of second malignancy and their clinical management in studied patients.
Source: Nuclear Medicine Communications - Category: Nuclear Medicine Tags: ORIGINAL ARTICLES Source Type: research
Conclusion The spectrum of [18F]HX4 uptake in this small series of patients exemplifies the difference in oxygenation profiles between histologically similar tumours. Performing an additional PET scan with [18F]HX4 prior to chemoradiotherapy treatment was logistically challenging in a routine setting, and therefore validation of its clinical impact should be the focus of future studies [EudraCT number 2013-003563-58].
Source: Nuclear Medicine Communications - Category: Nuclear Medicine Tags: ORIGINAL ARTICLES Source Type: research
Purpose The intensity of prostate-specific membrane antigen (PSMA) expression increases as the tumor grade increases and the uptake of Ga-68-PSMA is higher in high-grade tumors. The aim of the present study was to evaluate the correlation of preoperative tracer uptake of primary tumor to Gleason Score in patients who underwent prostatectomy. Patients and methods We retrospectively evaluated 141 patients who had Ga-68-PSMA positron emission tomography/computed tomography (PET/CT) imaging and who underwent prostatectomy. All patients had a diagnosis of prostate cancer on the basis of 10–24 cores transrectal ultras...
Source: Nuclear Medicine Communications - Category: Nuclear Medicine Tags: ORIGINAL ARTICLES Source Type: research
Conclusions: Our workflow allows the quantification of simultaneously acquired PET, MRSI and DWI data in rodents on a clinical PET/MR scanner. The correlations and findings suggest that a major portion of consumed glucose is metabolized by aerobic glycolysis in the investigated tumor model. Furthermore, we conclude that variations in cell density affect PET and 13C-data in a similar manner and correlations of longitudinal metabolic data appear to reflect both biochemical processes and tumor cellularity.
Source: Theranostics - Category: Molecular Biology Authors: Tags: Research Paper Source Type: research
More News: Cancer | Cancer & Oncology | Chemistry | Drugs & Pharmacology | Methotrexate | Nanotechnology | PET Scan | Study