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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
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Source: Anti-Cancer Drugs - Category: Cancer & Oncology Tags: Case Report Source Type: research
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Source: Iranian Journal of Pharmaceutical Research - Category: Drugs & Pharmacology Source Type: research
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Source: New Zealand Medical Journal - Category: General Medicine Tags: N Z Med J Source Type: research
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Source: Medicine - Category: Internal Medicine Tags: Research Article: Observational Study Source Type: research
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Source: European Journal of Radiology - Category: Radiology Source Type: research
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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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