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.