Self-nano Emulsifying Formulations: An Encouraging Approach for Bioavailability Enhancement and Future Perspective

Currently lipid-based formulations are playing a vital and promising role in improving the oral bioavailability of poorly water-soluble drugs. Lipid based formulations mainly consist of a drug dissolved in lipids such as triglycerides, glycerides, oils and surface active agent. Self nanoemulsifying formulations (SNEF) are isotropic mixtures of lipids/oils, surfactants and co-surfactants. On mild agitation followed by dilution in aqueous media, such as GI fluids, SNEF can form fine oil-in-water (o/w) nanoemulsions. Present chapter summarizes different types of lipid formulations with special emphasis on SNEF, availability of dosage forms, different components with natural surfactants from medicinal plants, mechanism of SNEF, recent advancements in oral drug delivery, solid SNEDDS, patents on SNEF and future prospects. SNEF emerging as powerful technique to improve solubility and commercialization of solid SNEF is the future novel drug delivery to improve bioavailability of poorly water soluble drugs

Molecular docking, synthesis and biological evaluation of some Imidazo-thiadiazole based Chalcone derivatives as potent triple mutant T790M/C797S EGFR inhibitors

In present study, we have designed and developed some imidazo-thiadiazole based chalcone derivatives as potential EGFR inhibitors. The designed derivative were screened through molecular docking studies and subjected for synthesis followed by in vitro anticancer activity. Most interestingly many molecules had formed one Pi-donor hydrogen bond (Pi-sulfur) or conventional hydrogen bond with Cys797 which is mutated amino acid residue for the second generation EGFR inhibitors. Many molecules had formed Pi-sulfur bond with Met790 which is mutated amino acid residue and developed resistance to the third generation EGFR inhibitors. All the interaction results presented here suggest these molecule has potential to be developed as most potent 4th generation EGFR inhibitors which will might have effectiveness against triple mutant T790M/C797S EGFR. From this investigation, it was decided to synthesize all the designed molecules with their biological evaluation. In vitro cytotoxicity of synthesized compounds against MCF-7 (Breast cancer) and A549 (Lung cancer) cells were carried out using MTT assay. All the synthesized compounds induced the cytotoxicity to MCF-7 and A549 and displayed good range of IC50 values in between 4 to 59 µm/mL.&nbsp