Preparation and Evaluation of Gliptin Liposomes for Targetting Ocular Region in Neurodegeneration

Abstract

Background: Neurodegeneration shows the distressing effects of miscommunications between brain cells. Insulin signaling dysregulation and small vessel disease in the base of diabetes may be important contributing factors in Alzheimer’s disease and vascular dementia. Gliptins play a role in neurodegeneration due to its neuroprotective effects. Eye is an extension of the brain. Ocular route reduces drug’s adverse effects offering an advantage in minimizing risk by targeted delivery to the brain. Conventional ophthalmic formulations exhibit poor bioavailability. Liposomes serve as promising active carriers of drugs to posterior segment eye disorders due to improvement in intravitreal half-life and targeted sustained drug delivery to the retina. Liposomes act as drug carriers for entrapment of hydrophilic and hydrophobic drugs. Objective: The study aimed to formulate and evaluate sitagliptin liposomal formulation for sustained effect in individuals suffering from neurodegeneration owing to high patient compliance, especially in geriatric patients. Methods: Sitagliptin liposomes were prepared by the ethanol injection method and were evaluated for various physicochemical properties such as visual appearance, particle size distribution, zeta potential, % drug entrapment efficiency, % drug loading capacity and in vitro drug release studies. Results: The optimized formulation (L-3) showed round-shaped distinct particles with good stability. The L-3 shows average diameter (281.9 nm); zeta potential (-11.9 mV); % entrapment efficiency (82.7 ± 0.89%); % drug loading (33.11 ± 0.67%). L-3 followed Korsmeyer- Peppas model with fickian diffusion transport of drug release giving n’ (0.3094), r2 (0.9753), with 83.78 ± 0.97% of sustained drug release. The L-3 passes the sterility test indicating its safe use in ophthalmic purposes. Conclusion: Thus, liposomal drug delivery is a highly effective approach for sustained drug delivery and minimizing the side effects of gliptins for effective therapy in neurodegeneration.