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

Abstract

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.

Self-Healing Alginate Hydrogel Formed by Dynamic Benzoxaborolate Chemistry Protects Retinal Pigment Epithelium Cells against Oxidative Damage

“…These results were in accordance with previous reports that both alginate and BOB grafted polymers are bio-safe biomaterials for potential biomedical applications [41,44]. For further in vivo application, more detailed investigations including eye irritancy test and histopathological examination after intraocular administration should be conducted in our future study [54].…”

Physicochemical properties and micro-interaction between micro-nanoparticles and anterior corneal multilayer biological interface film for improving drug delivery efficacy: the transformation of tear film turnover mode

“…The IOP was measured at specified time points after drop administration using a tonometer (Tonovet plus, iCare, Finland). The area of IOP reduction curve was analyzed (Hathout et al., 2019 ; Abdel Azim et al., 2022 ). All measurements were evaluated by the same operator under the same environmental conditions.…”

Recent Advances of Ocular Drug Delivery Systems: Prominence of Ocular Implants for Chronic Eye Diseases

“…Thus, employment of nanocarriers into the formulation of prostaglandin analogues would reduce the dependence on the solubilization effect of the preservative and could lead to the development of preservative-free formulations [ 75 ]. Moreover, nanocarriers have been used effectively to enhance ocular bioavailability and therapeutic activity, as well as to reduce systemic toxicity of topically applied β blockers, α-adrenergic agonists, and carbonic anhydrase inhibitors [ 76 , 77 , 78 ]. A summary of the drug delivery systems used to enhance the therapeutic activity of anti-glaucomatous drugs is found in Table 1 .…”