Background:
Linagliptin (LNG) is an oral hypoglycemic agent that acts by inhibiting the enzyme dipeptidyl peptidase - 4 (DPP-4) and reduces blood sugar levels in type-II diabetic patients. To date, the literature presents few analytical methods for the determination of LNG. However, no reversed phase-high performance liquid chromatography (RP-HPLC) method has been reported for the determination of LNG in nanotransfersomes and in vitro skin permeation samples.Objective: The present study involves the development and validation of RP-HPLCmethod to quantify LNG in both nanotransfersomes and in vitro skin permeation and deposition samples.
Methods:
The chromatographic analysis was performed on Luna C18 (2) column (250 x 4.6 mm, 5µm particle size) with a mobile phase consisting of a mixture of methanol: 0.2% orthophosphoric acid (50:50, v/v) at a flow rate of 1.0 mL/min, detection wave length of 227 nm, and column temperature of 40 °C.
Results:
The method was found to be specific, linear (r2 ≥ 0.999; 2-12 µg/mL), precise at both intra and inter day levels (percentage relative standard deviation; % RSD < 2.00), accurate (percentage recovery 100.21 – 103.83%), and robust. The detection and quantification limits were 0.27 and 0.82 µg/mL, respectively. The mean % entrapment efficiency and cumulative amount of LNG permeated across the rat skin from different transfersomal formulations ranged between 40.78 ± 2.54 % to 52.26 ± 2.15 % and 79.54 ± 16.67 to 200.74 ± 35.13 µg/cm2 respectively.
Conclusion:
The method was successfully applied to determine the entrapment efficiency, in vitro skin permeation and deposition behavior of LNG-nanotransfersomes.
Usefulness of Rat Skin as a Substitute for Human Skin in the in Vitro Skin Permeation Study
