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Improved oral bioavailability and therapeutic efficacy of erlotinib through molecular complexation with phospholipid

Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Chander Parkash Dora, Varun Kushwah, Sameer S. Katiyar, Pradeep Kumar, Viness Pillay, Sarasija Suresh, Sanyog Jain The current study was aimed to prepare a molecular complex of erlotinib (ERL) with phospholipid (PC) for enhancement of solubility and thus bioavailability, therapeutic efficacy and reducing the toxicity of erlotinib. Phospholipid complex of drug was prepared by solvent evaporation method and characterized by differential scanning calorimetry (DSC), Fourier transform infra-red spectroscopy (FT-IR), proton and phosphorus nuclear magnetic resonance spectroscopy (1H NMR and 31P NMR), powder X-ray diffraction (P-XRD), scanning electron microscopy (SEM) and transmission electron microscopy (TEM), which all explained the interactions of two components, validating the complexation phenomenon. In silico study also supported the phase change and molecular interactions for the establishment of ERL-PC. Spherical shaped nanostructures with 183.37±28.61nm size, −19.52±6.94mV potential and 28.59±2.66% loading efficiency were formed following dispersion of ERL-PC in aqueous media. In vitro release study revealed the higher release of ERL-PC due to amorphization and solubilization of drug. Caco-2 cell uptake resulted in ∼2 fold higher uptake of ERL-PC than free drug. In vitro cell culture studies were performed using human panc...
Source: International Journal of Pharmaceutics - Category: Drugs & Pharmacology Source Type: research

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We present a patient with epidermal growth factor receptor (EGFR)-mutant-NSCLC who developed metastatic SCLC after initial therapy with second-generation EGFR-tyrosine kinase inhibitor, afatinib. A 65-year-old male non-smoker was diagnosed with adenocarcinoma of the right lung, stage IVA (M1a). Due to tumor positivity for EGFR-Exon 19 deletion, the patient was started on oral afatinib, which resulted in a partial response. After ten months of treatment, he presented in the office with abdominal pain, distension, weight loss and jaundice. He had diffuse skeletal and hepatic metastases on PET/CT scan with interval progressio...
Source: Cancer Biology and Therapy - Category: Cancer & Oncology Authors: Tags: Cancer Biol Ther Source Type: research
Conclusions Triple malignancy in a single patient is exceptional. The management depend on stages. Surgery is the standard of care in localized cancers.
Source: International Journal of Surgery Case Reports - Category: Surgery Source Type: research
AbstractPancreatic ductal adenocarcinoma (PDAC) remains a difficult disease to treat and continues to portend a poor prognosis, as most patients are unresectable at diagnosis. 18F-fluorodeoxyglucose (FDG) positron emission tomography (PET) combined with CT (PET/CT) has been a cornerstone in oncological imaging of different cancers; however, the role of PET/CT in PDAC is continually evolving and currently not well established. Studies have shown the potential of PET/CT in guiding the management of patients with PDAC, with possible added benefit over anatomic imaging with CT or MRI in certain scenarios. PET/CT may be useful ...
Source: Abdominal Imaging - Category: Radiology Source Type: research
AbstractPurposeThe purpose of this study is to evaluate the performance of material-specific iodine (MS-I) images generated by rapid kV-switching single-source dual-energy computed tomography (rsDECT) for distinguishing post-operative changes from local tumor recurrence in patients on follow-up for pancreatic adenocarcinoma after surgical resection.MethodsIn this IRB-approved HIPPA-compliant study, retrospective review of 51 patients who underwent surgical resection of pancreatic adenocarcinoma was conducted and were followed up using contrast-enhanced rsDECT (Discovery CT 750HD, GE Healthcare, Milwaukee, WI). Independent ...
Source: Abdominal Imaging - Category: Radiology Source Type: research
This study evaluated the relationship between the maximum standardized uptake value (SUVmax) of preoperative positron emission tomography/computed tomography (PET/CT) and the characteristics of lung adenocarcinoma featuring ground‐glass opacity nodules (GGN). MethodsThe association of the SUVmax of preoperative PET/CT with ground‐glass opacity (GGO) proportion on CT, subtypes of adenocarcinoma (minimally invasive adenocarcinoma, invasive adenocarcinoma), predominant types of invasive adenocarcinoma, and size of the total and invasive components of pathology were evaluated in 190 patients who underwent resection for lun...
Source: Journal of Surgical Oncology - Category: Cancer & Oncology Authors: Tags: RESEARCH ARTICLE Source Type: research
n Yen Gigin Lin We aim to characterize the metabolic changes associated with early response to radiation therapy in a prostate cancer mouse model by 2-deoxy-2-[18F]fluoro-d-glucose ([18F]FDG) and [11C]acetate ([11C]ACT) positron emission tomography, with nuclear magnetic resonance (NMR) metabolomics corroboration. [18F]FDG and [11C]ACT PET were performed before and following irradiation (RT, 15Gy) for transgenic adenocarcinoma of mouse prostate xenografts. The underlying metabolomics alterations of tumor tissues were analyzed by using ex vivo NMR. The [18F]FDG total lesion glucose (TLG) of the tumor significant incre...
Source: Molecules - Category: Chemistry Authors: Tags: Article Source Type: research
CONCLUSION: FDG PET/CT is accurate in detecting esophageal adenocarcinoma recurrence, especially within the first postoperative year when most recurrences occur, and is useful in identifying patients with a solitary metastasis. Advances in knowledge: FDG-PET/CT should be considered as a valuable tool in the routine follow-up of surgically treated esophageal cancer patients within the first two years after surgery. PMID: 29125331 [PubMed - as supplied by publisher]
Source: The British Journal of Radiology - Category: Radiology Authors: Tags: Br J Radiol Source Type: research
AbstractGastric duplication cysts are rare and mostly present in the first year of life. In adulthood presentation is in the form of obstruction, ulceration, bleeding, fistulization etc. Malignancy is extremely rare with only 12 cases reported to date. We came across a gastric duplication cyst with papillary adenocarcinoma in a 63 year old man. He underwent cyst excision with radical subtotal gastrectomy. The awareness of such a condition made it possible for us to have a suspicion of malignancy preoperatively based on imaging and thus a radical surgery was performed. High index of suspicion is necessary to diagnose this c...
Source: Indian Journal of Surgical Oncology - Category: Cancer & Oncology Source Type: research
Conclusions: The regions of decreased metabolism detected in the study are related to memory, learning and voluntary movement which is consistent with previous findings based on clinical studies and neuropsychological tests that report impairments on neurocognitive and motor skills associated to these therapies.
Source: Clinical Nuclear Medicine - Category: Nuclear Medicine Tags: Original Articles Source Type: research
AbstractBackgroundWe aimed to determine whether treatment should be stratified according to 18-fluorodeoxyglucose positron emission tomography/computed tomography (18F-FDG PET/CT) maximum standardized uptake values (SUVmax) in pancreatic ductal adenocarcinoma.MethodsPatients who underwent preoperative 18F-FDG PET/CT between 2006 and 2014 (n = 138) were stratified into high (≥ 4.85) and low (
Source: Journal of Gastrointestinal Surgery - Category: Surgery Source Type: research
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