Quality-by-Design-Based Development of n-Propyl-Gallate-Loaded Hyaluronic-Acid-Coated Liposomes for Intranasal Administration.
The present study aimed to develop n-propyl gallate (PG)-encapsulated liposomes through a novel direct pouring method using the quality-by-design (QbD) approach. A further aim was to coat liposomes with hyaluronic acid (HA) to improve the stability of the formulation in nasal mucosa. The QbD method was used for the determination of critical quality attributes in the formulation of PG-loaded liposomes coated with HA. The optimized formulation was determined by applying the Box-Behnken design to investigate the effect of composition and process variables on particle size, polydispersity index (PDI), and zeta potential. Physiochemical characterization, in vitro release, and permeability tests, as well as accelerated stability studies, were performed with the optimized liposomal formulation. The optimized formulation resulted in 90 ± 3.6% encapsulation efficiency, 167.9 ± 3.5 nm average hydrodynamic diameter, 0.129 ± 0.002 PDI, and -33.9 ± 4.5 zeta potential. Coated liposomes showed significantly improved properties in 24 h in an in vitro release test (>60%), in vitro permeability measurement (420 μg/cm2) within 60 min, and also in accelerated stability studies compared to uncoated liposomes. A hydrogen-peroxide-scavenging assay showed improved stability of PG-containing liposomes. It can be concluded that the optimization of PG-encapsulated liposomes coated with HA has great potential for targeting several brain diseases.
['Sabir|Fakhara|F|0000-0002-4369-1599', 'Katona|Gábor|G|0000-0003-1564-4813', 'Pallagi|Edina|E|', 'Dobó|Dorina Gabriella|DG|', 'Akel|Hussein|H|0000-0003-4453-9545', 'Berkesi|Dániel|D|', 'Kónya|Zoltán|Z|0000-0002-9406-8596', 'Csóka|Ildikó|I|']
D000281:Administration, Intranasal D000818:Animals D000975:Antioxidants D004337:Drug Carriers D016503:Drug Delivery Systems D065546:Drug Liberation D006820:Hyaluronic Acid D008081:Liposomes D051379:Mice D011435:Propyl Gallate
hyaluronic acid in vitro release study intranasal delivery risk assessment scavenging assay