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

Related Links:

In conclusion, putative lung adenocarcinoma presenting as CUP may involve ROS1 rearrangement, and ROS1 inhibitor therapy may be effective. PMID: 30443294 [PubMed]
Source: Oncotarget - Category: Cancer & Oncology Tags: Oncotarget Source Type: research
In this report, we present the medical history of a  30-year-old male patient with HER2- and PD-L1-negative metastasized adenocarcinoma of the gastric cardia, who received three cycles of pembrolizumab (200  mg every 2 weeks) after the failure of the first-line (1L) treatment with docetaxel, cisplatin, 5‑fluorouracil (DCF). A restaging compu ted tomography (CT) scan for the chest and abdomen revealed an apparent progressive disease; therefore, the treatment was terminated. Five months after the termination of the treatment, a new CT scan demonstrated a spontaneous treatment response...
Source: Memo - Magazine of European Medical Oncology - Category: Cancer & Oncology Source Type: research
Authors: Ostojić J, Brčić L, Hrabač P, Seiwerth S Abstract Lung cancer as the major cause of cancer mortality worldwide includes several histologic subtypes evolving from numerous genetic and epigenetic changes emerging in alveolar, bronchiolar and bronchial epithelium. The majority of cases are diagnosed in advanced stage (i.e. stages IIIB and IV), often with scanty amount of tissue in transbronchial biopsies or cytology specimens. The aim of the present study was to investigate the expression of the scaffolding protein neural precursor cell expressed, developmentally downregulated 9 (NEDD9) in small biopsies ...
Source: Acta Clinica Croatica - Category: General Medicine Tags: Acta Clin Croat Source Type: research
The diagnostic definition of indeterminate lung nodules as malignant or benign poses a major challenge for clinicians. We discovered a potential marker, the sodium-dependent glucose transporter 2 (SGLT2), whose activity identified metabolically active lung premalignancy and early-stage lung adenocarcinoma (LADC). We found that SGLT2 is expressed early in lung tumorigenesis and is found specifically in premalignant lesions and well-differentiated adenocarcinomas. SGLT2 activity could be detected in vivo by positron emission tomography (PET) with the tracer methyl 4-deoxy-4-[18F] fluoro-alpha-d-glucopyranoside (Me4FDG), whic...
Source: Science Translational Medicine - Category: Biomedical Science Authors: Tags: Research Articles Source Type: research
ConclusionsSurvival did not differ for PDAC patients with ILNs identified on staging chest CTs compared with those without ILNs. Furthermore, ILN identification did not lead to changes in management of the primary abdominal tumor, questioning the utility of staging chest CTs for PDAC patients.
Source: Annals of Surgical Oncology - Category: Cancer & Oncology Source Type: research
This study concludes that plant mediated biosynthesis of nanoparticles is the superior alternative compared to chemical and physical approaches, to utilize them as drug delivery tool and need to conjugate apoptosis inducing biological agents with silver nanoparticles to suppress the uncontrolled division of cancer cells. PMID: 30403594 [PubMed - in process]
Source: Cellular and Molecular Biology - Category: Molecular Biology Tags: Cell Mol Biol (Noisy-le-grand) Source Type: research
The objective of this work is to improve diagnosis of neoplastic and inflammatory conditions using pCLE. MATERIALS AND METHODS: The charts of all patients who underwent pCLE at a single referral center between 2009 and 2015 were reviewed. ERCP reports were reviewed for eleven Miami and Paris criteria. Primary outcome was the identification of neoplasia by histopathology (defined as high-grade dysplasia and/or adenocarcinoma). To model predictors of neoplasia, we fit a binary regression model incorporating data from pCLE operating criteria, pCLE impression, and PSC status. RESULTS: 97 patients were identified. In th...
Source: Scandinavian Journal of Gastroenterology - Category: Gastroenterology Tags: Scand J Gastroenterol Source Type: research
This study aimed to investigate the prognostic value of metabolic tumor volume (MTV) and total lesion glycolysis (TLG), which are volume-based PET parameters, using18F-2-fluoro-2-deoxy-d-glucose positron emission tomography/computed tomography (18F-FDG PET/CT) in patients with surgically resectable lung adenocarcinoma.MethodsWe retrospectively evaluated 149 patients with lung adenocarcinoma who underwent18F-FDG PET/CT before surgical resection. Maximum standardized uptake value (SUVmax), MTV, and TLG of the primary tumor with threshold value of SUVmax 30, 40, and 50% were calculated, respectively. To compare the predictive...
Source: Nuclear Medicine and Molecular Imaging - Category: Nuclear Medicine Source Type: research
In conclusion, pathological analysis and CASTIN analysis revealed that ORT models of OE19 cells have a more invasive character and enhanced interaction with stromal cells compared with SC models. PMID: 30393433 [PubMed]
Source: Journal of Toxicologic Pathology - Category: Toxicology Tags: J Toxicol Pathol Source Type: research
EGFR mutation decreases FDG uptake in non‑small cell lung cancer via the NOX4/ROS/GLUT1 axis. Int J Oncol. 2018 Nov 06;: Authors: Chen L, Zhou Y, Tang X, Yang C, Tian Y, Xie R, Chen T, Yang J, Jing M, Chen F, Wang C, Sun H, Huang Y Abstract [18F]fluoro‑2‑deoxyglucose (FDG) positron emission tomography (PET)‑computed tomography (CT) is a functional imaging modality based on glucose metabolism. The association between the maximum standardized uptake value (SUVmax) from 18F‑FDG PET‑CT scanning and epidermal growth factor receptor (EGFR) mutation status has, to the best of our knowledge, ...
Source: International Journal of Oncology - Category: Cancer & Oncology Authors: Tags: Int J Oncol Source Type: research
More News: Adenocarcinoma | Drugs & Pharmacology | Nanotechnology | Pancreas | PET Scan | Phosphorus | Study | Tarceva | Toxicology