Background: Neurodegeneration show 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 shows role in neurodegeneration due to its
neuroprotective effects. Eye is an extension of the brain. Ocular route reduces
drug’s adverse effects offering advantage in minimizing risk by targeted delivery to
brain. Conventional ophthalmic formulations exhibit poor bioavailability. Liposomes
serves 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 individual suffering from neurodegeneration owing
to high patient compliance especially in geriatric patient.
Method: Sitagliptin liposomes were prepared by 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), r
(0.9753), with 83.78 ± 0.97 % of sustained drug release. The L-3
passes the sterility test indicating its safe use in ophthalmic purpose.
Conclusion: Thus, liposomal drug delivery is highly effective approach for sustained
drug delivery and minimizing the side effects of gliptins for effective therapy in