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...

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Bibliographic Details
Published in:International journal of nanomedicine 2022-01, Vol.17, p.2753-2776
Main Authors: Azim, Engy A. Abdel, Elkheshen, Seham A, Hathout, Rania M, Fouly, Marwa A, El Hoffy, Nada M
Format: Article
Language:English
Subjects:
Brimonidine
brimonidine tartrate
Cholesterol
d-optimal design
Design optimization
Drug delivery systems
Drugs
Efficiency
gelatin
gelatinized core liposomes
Glaucoma
Glycerin
Glycerol
Hydration
intra-ocular pressure
Investigations
Morphology
ocular drug delivery
Original Research
Particle size
Pharmaceuticals
plasticizer
Rheology
Sympathomimetic agents
Thin films
Vehicles
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Summary: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. Keywords: gelatin, brimonidine tartrate, D-optimal design, glaucoma, gelatinized core liposomes, ocular drug delivery, plasticizer, intra-ocular pressure, BRT, IOP, DOD
ISSN:1178-2013
1176-9114
1178-2013
DOI:10.2147/IJN.S370192