The core objective of nanoparticles is to control and manipulate biomacromolecular constructs and supramolecular assemblies that are critical to living cells in order to improve the quality of human health. By definition, these constructs and assemblies are nanoscale and include entities such as drugs, proteins, DNA/RNA, viruses, cellular lipid bilayers, cellular receptor sites and antibody variable regions critical for immunology and are involved in events of nanoscale proportions. The emergence of such nanotherapeutics/diagnostics will allow a deeper understanding of human longevity and human ills that include cancer, cardiovascular disease and genetic disorders. A technology platform that provides a wide range of synthetic nanostructures that may be controlled as a function of size, shape and surface chemistry and scale to these nanotechnical dimensions will be a critical first step in developing appropriate tools and a scientific basis for understanding nanoparticles.

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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.