Development of gelatinized-core liposomes for the oral delivery of EGCG with improved stability, release property, and cellular antioxidant activity.

Epigallocatechin gallate (EGCG) exhibits antioxidant, anti-cancer, and anti-inflammatory properties; however, low cellular permeability and stability limit its bioavailability. Liposomes have the potential for enhancing bioactive compounds' bioavailability. Yet, low entrapment efficiency (EE) and burst release of hydrophilic substances make them impractical for food industry use. Here, we incorporated gelatin into liposomes to overcome these limitations. EGCG-loaded conventional liposomes (EGCG/CLs) and gelatinized-core liposomes (EGCG/GLs) had small particle sizes and high absolute zeta potentials. Encapsulation in EGCG/GLs significantly improved the EE of EGCG compared to that in EGCG/CLs (p < 0.05). EGCG/GLs retained EGCG in the hydrophilic region, whereas EGCG/CLs exhibited significantly higher release of EGCG during storage (p < 0.05). Additionally, in comparison to EGCG/CLs, gelatin incorporation significantly enhanced the sustained release, cellular permeability, and cellular antioxidant activity of EGCG (p < 0.05). This study emphasizes the capability of gelatinized-core liposomes as a potent delivery system for enhancing the stability and bioavailability of EGCG/CLs, broadening the prospects for utilizing them in the food industry.

Augmented in vitro and in vivo Profiles of Brimonidine Tartrate Using Gelatinized-Core Liposomes.

Background: The low entrapment efficiency of the hydrophilic drugs such as brimonidine tartrate (BRT) in liposomes represents a challenge that requires interventions. Gelatinized core liposomes (GCLs) were fabricated to increase the drug entrapment, corneal penetration, and physical stability of the investigated molecule. Research Design and Methods: GCLs encapsulating BRT were prepared and optimized utilizing D-optimal design (DOD). The effect of plasticizer incorporation on the physicochemical characteristics and on the in vivo performance was studied. The optimized formulations were investigated for pH, rheological properties, morphological characteristics, in vitro release profiles, biological performance, safety profile. The effects of storage and gamma sterilization were also investigated. Results: The results revealed the great success of the prepared formulations to achieve high entrapment efficiency reaching 98% after a maturation period of 10 days. The addition of glycerol as plasticizer significantly minimized the particle size and shortened the maturation period to 7 days. The selected formulations were stable for 3 months after gamma sterilization. The formulations showed significant lowering of intra-ocular pressure (IOP) in glaucomatous rabbits with sustainment of the pharmacological effect for 24 hours compared to drug solution. Conclusions: Enhanced in vitro and in vivo profiles of brimonidine tartrate loaded gelatinized-core-liposomes were obtained.