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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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Source: Pathologica - Category: Pathology Tags: Pathologica Source Type: research
We report the unique case of synchronous advanced lung AC of the right upper lobe (stage IIIB) and typical endobronchial carcinoid tumor in the contralateral lower lobe in a 49-year-old white female who had never smoked. PET-computed tomography scan revealed a fluorine-18-fluorodeoxyglucose-avid AC lesion, whereas the carcinoid tumor was fluorine-18-fluorodeoxyglucose occult. After two lines of platinum-based combination chemotherapies and radiotherapy, the AC progressed, and oral tyrosine kinase inhibitor therapy with erlotinib was initiated in third line. On erlotinib, the AC remained stable for 50 months until disease p...
Source: Anti-Cancer Drugs - Category: Cancer & Oncology Tags: Case Report Source Type: research
Co-delivery approach has been recommended to reduce the amount of each drug and to achieve the synergistic effect for cancer treatment. CUR and SF have antitumor effects, but their application is limited because of their low water solubility and poor oral bioavailability. To improve the bioavailability and solubility of SF and CUR, we performed an innovative co-delivery of SF and CUR with magnetic nanoparticles to endorse SF and CUR maintenance as an effective and promising antitumor drugs. The structure of the synthesized nanocarrieris evaluated by X-ray diffraction, transmission electron microscopy, scanning electron mic...
Source: Iranian Journal of Pharmaceutical Research - Category: Drugs & Pharmacology Source Type: research
CONCLUSION: While New Zealand outcomes in colorectal cancer have historically compared unfavourably against international standards, the outcomes observed in this cohort are encouraging and may reflect advances in care, including multidisciplinary team discussion, increased use of adjuvant therapy, surgical subspecialisation and protocolled surveillance and follow-up. PMID: 29389929 [PubMed - in process]
Source: New Zealand Medical Journal - Category: General Medicine Tags: N Z Med J Source Type: research
We present an atypical case of a 69-year-old woman with recurrent episodes of acute pancreatitis and a background history of mucinous colorectal adenocarcinoma. It is emphasized that in the framework of biliary malignant obstruction, modern non-invasive techniques like Magnetic Resonance Imaging (MRI) with hepatospecific contrast agent and Positron Emission Tomography (PET) may help establish the specific cause of the obstruction before any biliary decompression procedure is carried out. This strategy has the potential to prevent from more important tumour spread and provide a greater chance for curative surgery when appli...
Source: Journal of the Belgian Society of Radiology - Category: Radiology Source Type: research
Cervical cancer recently has become more common among younger women in Japan. Diagnosing early-stage cancer is straightforward using cervical cytodiagnosis and histological diagnosis. However, postmenopausal endophytic cervical cancer and skip lesions in cervical adenocarcinoma are difficult to detect. We compared the maximum standardized uptake value (SUVmax) of 18F-fluorodeoxy-glucose positron emission tomography/computed tomography (PET/CT) for primary staging of cervical cancer and evaluated the relationship of the imaging findings to prognosis. This was a retrospective study of 38 patients with cervical cancer who un...
Source: Medicine - Category: Internal Medicine Tags: Research Article: Observational Study Source Type: research
Conclusion Quantitative CT histogram values and SUV assessment can differentiate solid lung adenocarcinomas from squamous cell carcinomas. Kurtosis and SUVmax values were strongly correlated. The addition of RG and further combination of the parameters improved the results.
Source: European Journal of Radiology - Category: Radiology Source Type: research
Abstract Alternative models such as three-dimensional (3D) cell cultures represent a distinct milestone towards capturing the realities of cancer biology in vitro and reduce animal experimentation in the preclinical stage of drug discovery. Significant work remains to be done to understand how substrates used in in vitro alternatives influence cancer cells phenotype and drug efficacy responses, so that to accurately link such models to specific in vivo disease scenarios. Our study describes how the morphological, mechanical and biochemical properties of adenocarcinoma (A549) cells change in response to a 3D enviro...
Source: Tissue and Cell - Category: Cytology Authors: Tags: Tissue Cell Source Type: research
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Source: Scandinavian Journal of Gastroenterology - Category: Gastroenterology Tags: Scand J Gastroenterol Source Type: research
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Source: Cancer - Category: Cancer & Oncology Authors: Tags: Original Article Source Type: research
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