Statistically optimized liposomal formulation of dorzolamide hydrochloride for sustained ocular delivery: in vitro and allergic evaluation in rabbit.

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.