فهرست نشریات علمی دسترسی آزاد ایران

Linagliptin, a novel anti-diabetic drug, is a DPP-4 inhibitor used in the treatment of type II diabetes. One of the major disadvantages of Linagliptin is its low oral bioavailability of 29.5% due to first-pass metabolism and P-gp efflux. In an attempt to increase the oral bioavailability, Linagliptin nanostructured lipid carrier were developed with Glyceryl monostearate, Oleic acid and Tween 80 as P-gp inhibitors. Linagliptin nanostructured lipid carrier were formulated using Glyceryl monostearate, Oleic acid, Tween 80 and PEG-400 as solid lipid, oil, surfactant and co surfactant, respectively. Twenty-seven formulations were prepared by the hot emulsification-ultrasonication technique. Particle size, poly dispersity index, entrapment efficiency were evaluated as responses. An optimized formula was evaluated for intestinal transport of Linagliptin by the ex-vivo intestinal permeation study using the non-everted sac model of Male Sprague Dawley rats. The mean particle size, polydispersity index, entrapment efficiency and zeta potential of the optimized formula were found to be 46.13 ± 2.19 nm, 0.279 ± 0.026, 79.75 ± 0.87% and – 12.8 ± 4.3 Mv respectively. The permeation study showed of 2.97 and 2.98 times increment in the in the flux and permeability coefficient in comparison to Linagliptin suspension. The enhanced linagliptin permeation may be due to P-gp efflux inhibition and lymphatic targeting. Thus, Linagliptin nanostructured lipid carrier can be considered promising carriers for oral delivery.