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Statistically optimized liposomal formulation of dorzolamide hydrochloride for sustained ocular delivery: in vitro
Susanta Paul1, Anannya Bose2, Kunal Ray1
1Department of Pharmaceutical Technology, NSHM Knowledge Campus, Kolkata- Group of Institutions, Kolkata, West Bengal, India.
Significance:
The liposomal formulation reveals a safe, sustained, and efficient ocular drug delivery to improve the therapeutic potential of dorozolamide hydrochloride in glaucoma treatment.
Objective:
A liposomal formulation of Dorzolamide hydrochloride was developed and evaluated for sustained ocular delivery with improved permeation and safety.
Methods:
Liposomes were prepared using the thin-film hydration method and optimized through a 32 full factorial design, analyzing the effects of phosphatidylcholine and cholesterol on entrapment efficiency and drug release via response surface methodology.
Results:
The optimized formulation, containing 200 mg phosphatidylcholine and 40 mg cholesterol, exhibited a vesicle size of 98.22 ± 10.03 nm, zeta potential of -21.53 ± 1.02 mV, and high entrapment efficiency (97.5%). In vitro studies confirmed sustained drug release over 8 h, while ex vivo transcorneal permeation was 1.8 times greater than that of marketed eye drops. Safety assessments using Hen's Egg Test-Chorioallantoic Membrane(HET-CAM) and Draize tests established the formulation as nonirritant and isotonic.
Conclusion:
Overall, the liposomal system significantly enhanced ocular bioavailability and demonstrated potential as a safe and effective option for long-term glaucoma therapy.
