Enhancing mechanism of Labrasol on intestinal membrane permeability of the hydrophilic drug gentamicin sulfate

Development of optimized self-nano-emulsifying drug delivery systems (SNEDDS) of carvedilol with enhanced bioavailability potential

“…All these techniques yield limited fruition when the drug exhibits low bioavailability, owing to metabolism by the cytochrome P450 family of enzymes present in the gut enterocytes and liver hepatocytes, instability in gastrointestinal (GI) fluids, restricted intestinal permeability, and/ or P-glycoprotein (P-gp) efflux (de Smidt et al, 2004;Sha et al, 2005;Koga et al, 2006;Constantinides & Wasan, 2007;Hauss, 2007;Singh et al, 2009a). Self-emulsifying drug delivery systems (SEDDS), in this regard, have been gaining world-wide acceptance to improve the bioavailability potential of lipophilic drugs by augmenting their dissolution and permeation, and for bypassing hepatic first-pass effect (Humberstone & Charman, 1997;Porter & Charman, 2001;Sha et al, 2005;Koga et al, 2006). Also, the SEDDS have been documented to show a prominent role in surmounting the effects of Pgp efflux and intestinal metabolism by Cytochrome P450 isoforms (Sha et al, 2005;Koga et al, 2006).…”

“…Self-emulsifying drug delivery systems (SEDDS), in this regard, have been gaining world-wide acceptance to improve the bioavailability potential of lipophilic drugs by augmenting their dissolution and permeation, and for bypassing hepatic first-pass effect (Humberstone & Charman, 1997;Porter & Charman, 2001;Sha et al, 2005;Koga et al, 2006). Also, the SEDDS have been documented to show a prominent role in surmounting the effects of Pgp efflux and intestinal metabolism by Cytochrome P450 isoforms (Sha et al, 2005;Koga et al, 2006). The SEDDS, being an isotropic mixtures of lipids, emulsifiers, and co-emulsifiers, typically produce emulsions with a globule size ranging between a few nanometers and several microns (Charman et al, 1992;Joshi et al, 2008;Pouton & Porter, 2008;Singh et al, 2009b).…”

Enhancement of Stability, Release and in Vitro Digestibility of Mulberry Stem Extract Using Microemulsions

“…2A). It has been reported that the presence of hydrophilic molecules in the aqueous phase influences the optimal head group area of the surfactant by altering the solubility of the head group in the aqueous phase [26]. In this case, PEG 400 (MW 380-420 g/mole) has a higher molecular weight than PG (MW 76.09 g/mole), thus PEG 400 shows a higher negative effect on the formation of microemulsions than PG.…”

“…PEG-8 caprylic/capric glyceride is a well-defined mixture of 30% mono-, di-and triglycerides of saturated C6-C14 fatty acids (predominantly C8 and C10 fatty acids), 50% of mono-and di-fatty acid esters of polyethylene glycol and 20% of free PEG 400 [23], which was used as a surfactant given its effectiveness in enhancing the intestinal absorption of various drugs [24][25][26]. Polyglyceryl-3 di iso stearate was used as cosurfactant in this study.…”

Oral Delivery of Insulin: Novel Approaches

“…The nanoparticles were expected to translocate the intestinal epithelium, while the oily vehicle was intended to reduce proteolytic degradation and improve permeability [109,110]. In addition, Labrasol and oleic acid are known penetration enhancers [111,112]. Our expectation is that part of the chitosan will rest inside the water droplet of the inverted micelles where it forms PEC with insulin while the other part projecting near the surfactant head groups where it interacts with surfactants stabilizes the w/o microemulsion and resulted in smaller microemulsion sizes [97].…”