Abstract
AIM: Lutein exhibits poor aqueous solubility, chemical instability, and low bioavailability following oral administration, which restricts its therapeutic use in Alzheimer's disease (AD). Hence, a lutein-laden liposomal in situ gel was formulated to enhance bioavailability and brain targeting via nasal delivery. METHOD: Lutein-laden liposomes were fabricated using an ethanol injection method and studied for various parameters. RESULT AND CONCLUSIONS: The formulated lutein-laden liposomes showed a particle size, polydispersity index, and encapsulation efficiency of 71.8 ± 6.4 nm, 0.327 ± 0.007, and 95.59 ± 3.03%, respectively. The permeation studies on goat nasal mucosa revealed drug permeation from the lutein-laden liposomal in situ gel and fivefold higher permeation than the lutein solution-based in situ gel. The drug targeting efficiency of the developed formulation was 372.80%. The pharmacokinetic study of the developed formulation administered via the nasal route showed a twofold higher C(max) and a 1.7-fold higher AUC than the drug suspension administered via the oral route. The histopathological analysis indicated that the developed formulation was safe. Thus, intranasal delivery of lutein could surpass poor oral bioavailability and be studied for managing AD and its symptoms using an intranasal delivery-based brain-targeted approach.