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- W4294904518 abstract "<ns3:p><ns3:bold>Background: </ns3:bold>Vemurafenib (VEM) was a licensed drug for the treatment of skin melanoma and is available only in the market as oral tablets prescribed in huge doses (1920 mg/day). One reason for the high dose is vemurafenib's low oral bioavailability.</ns3:p><ns3:p> <ns3:bold>Methods: </ns3:bold>VEM-lipid complex (DLC) was predicted based on Conquest and Mercury programs and prepared using the solvent evaporation method using the lipid (phosphatidylethanolamine).<ns3:bold> </ns3:bold>DLC was subjected to characterization (FT-IR, Raman spectroscopy, DSC, TGA, P-XRD, and FESEM) to confirm complexation. DLC was used to prepare solid in oil nanodispersion (DLC-SON) and subjected to in vitro, ex vivo, and in vivo evaluation in comparison to our recently prepared conventional SON (VEM-SON) and DLC-control.</ns3:p><ns3:p> <ns3:bold>Results: </ns3:bold>Conquest and Mercury predict the availability of intermolecular hydrogen bonding between<ns3:bold> </ns3:bold>VEM and phosphatidylethanolamine (PE). All characterization tests of DLC ensure the complexation of the drug with PE. Ex vivo studies showed that the drug in DLC-SON has significantly (P<0.05) higher skin permeation than DLC-control but lower drug permeation than conventional SON but it has a higher % skin deposition (P<0.05) than others. The half-maximal inhibitory concentration (IC50) of the prepared DLC-SON is significantly high (P<0.05) in comparison to the conventional SON and pure VEM. In vivo permeation using confocal laser scanning microscopy (on the rat) results indicated that both conventional SON and DLC-SON can cross the SC and infiltrate the dermis and epidermis but DLC-SON has a higher luminance/gray value after 24 h in the dermis in comparison to the conventional SON.</ns3:p><ns3:p> <ns3:bold>Conclusion:</ns3:bold> The novel lipid complex for VEM prepared using PE as a lipid and enclosed in SON showed higher anticancer activity and topical permeation as well as sustained delivery and good retention time in the dermis that localize the drug in a sufficient concentration to eliminate early diagnosed skin melanoma.</ns3:p>" @default.
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- W4294904518 date "2022-09-07" @default.
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- W4294904518 title "Modified solid in oil nanodispersion containing vemurafenib-lipid complex-in vitro/in vivo study" @default.
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- W4294904518 doi "https://doi.org/10.12688/f1000research.123041.2" @default.
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