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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Publication date: Available online 17 July 2018Source: The Lancet Respiratory MedicineAuthor(s): Zhijie Wang, Ying Cheng, Tongtong An, Hongjun Gao, Kai Wang, Qing Zhou, Yanping Hu, Yong Song, Cuimin Ding, Feng Peng, Li Liang, Yi Hu, Cheng Huang, Caicun Zhou, Yuankai Shi, Li Zhang, Xin Ye, Meizhuo Zhang, Shaokun Chuai, Guanshan ZhuSummaryBackgroundDetection of EGFR mutations in tumour tissue is the gold-standard approach to ascertain if a patient will benefit from treatment with an EGFR tyrosine kinase inhibitor. However, if tissue is scant, another strategy is to use circulating tumour DNA (ctDNA), but this method needs va...
Source: The Lancet Respiratory Medicine - Category: Respiratory Medicine Source Type: research
Abstract Background: It is important to distinguish the classification of lung adenocarcinoma. A radiomics model was developed to predict tumor invasiveness using quantitative and qualitative features of pulmonary ground-glass nodules (GGNs) on chest CT. Materials and Methods: A total of 599 GGNs [including 202 preinvasive lesions and 397 minimally invasive and invasive pulmonary adenocarcinomas (IPAs)] were evaluated using univariate, multivariate, and logistic regression analyses to construct a radiomics model that predicted invasiveness of GGNs. In primary cohort (comprised of patients scanned from August ...
Source: Biomed Res - Category: Research Authors: Tags: Biomed Res Int Source Type: research
CONCLUSION: This is the first case to our knowledge describing both such lesions in one patient and the first case describing the use of 2-(3-{1-carboxy-5-[(6-[18F]fluoro-pyridine-3-carbonyl)-amino]-pentyl}-ureido)-pentanedioic acid (18F-DCFPyL)-PSMA PET/CT to detect IPAS. Furthermore we highlight the value of nuclear medicine diagnostic work up in complex cases. PMID: 30006647 [PubMed - as supplied by publisher]
Source: Hellenic Journal of Nuclear Medicine - Category: Nuclear Medicine Tags: Hell J Nucl Med Source Type: research
BB, Altun GD Abstract Prostate adenocarcinoma (PCa) is the most frequently diagnosed malignancy in the male population, with the most common sites for secondary lesions being the lymph nodes, bones, and lungs. Testicular metastases from PCa are very rare and mostly identified incidentally after therapeutic orchiectomy for advanced PCa or during autopsy. Here we present a case involving a 64-year-old man with biochemical recurrence of castrated oligometastatic PCa that presented as solitary testicular metastasis on Ga-PSMA ligand positron emission tomography/computed tomography. PMID: 30015663 [PubMed - as supplied by publisher]
Source: Clinical Prostate Cancer - Category: Cancer & Oncology Authors: Tags: Clin Nucl Med Source Type: research
Conclusion: Diagnosing a metastasis to the thyroid is challenging. On FNA, a dual cell population should raise suspicion. Immunocytochemical and molecular analysis may be helpful. Clinical information is essential in guiding specific ancillary technique panels in scant cellular material.Acta Cytologica
Source: Acta Cytologica - Category: Cytology Source Type: research
We report an unusual case of uterine corpus metastasis from rectal adenocarcinoma detected using 18F-FDG PET/CT. A 47-year-old woman was diagnosed with rectal adenocarcinoma and treated with surgery and radiochemotherapy 3 years ago. During follow-up, she presented with lower abdomen pain and elevated tumor markers, but ultrasonography findings were unremarkable. We performed an 18F-FDG PET/CT scan, which showed intense 18F-FDG avidity in the myometrium of the uterine corpus. Uterine corpus metastasis was suspected, and complementary MRI and diagnostic curettage histopathology confirmed uterine metastasis from rectal adenocarcinoma.
Source: Clinical Nuclear Medicine - Category: Nuclear Medicine Tags: Interesting Images Source Type: research
CONCLUSIONS: PERCIST1.0 appears to increase the chance of detecting patients with progressive disease compared to the conventional anatomical-based assessment of RECIST1.1. The integration of these additional radiographic metrics in assessing treatment response to nCR for pancreatic adenocarcinoma may provide a promising strategy to better select patients that are most suitable for therapeutic intensification. PMID: 30015263 [PubMed - as supplied by publisher]
Source: Translational Oncology - Category: Cancer & Oncology Authors: Tags: Transl Oncol Source Type: research
In conclusion, we describe a family of putatively benign clonal proliferations with a spectrum of morphology recapitulating various levels of the bronchiolar tree, of which only a minor subset fits the classic description of CMPT. Comparable mutation profiles and partially overlapping morphologic features across the spectrum of these lesions support their nosological relationship. We propose designating this entire family of lesions as BAs, and that lesions currently designated CMPTs represent a subgroup of this family.
Source: The American Journal of Surgical Pathology - Category: Pathology Tags: Original Articles Source Type: research
ConclusionAdenosquamous carcinoma is a malignant tumor with poorer prognosis than adenocacinomas.
Source: International Journal of Surgery Case Reports - Category: Surgery Source Type: research
We report here a 16-year-old patient who presented initially with symptoms characteristic of appendicitis. Following a CT scan suggesting perforated appendicitis, the patient was treated with intravenous antibiotics with a scheduled interval appendectomy three months later. Pathology reports from the interval appendectomy showed that the specimen contained a well-to-moderately differentiated adenocarcinoma. The patient then underwent robot assisted right hemicolectomy as definitive management, which demonstrated that the tumor originated in the cecum with invasion into the submucosa and focally infiltrating the muscularis ...
Source: Journal of Pediatric Surgery Case Reports - Category: Surgery Source Type: research
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