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January 20, 20263 citations

Statistically Optimized Liposomal Formulation of Dorzolamide Hydrochloride for Sustained Ocular Delivery: In vitro and Allergic Evaluation in Rabbit.

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SPSubrata PaulABAnannya BoseKRK. Ghosh Ray

Key Points

  • The research aims to create a liposomal formulation of dorzolamide hydrochloride for better ocular drug delivery and improved therapeutic safety.
  • Developed liposomes using thin-film hydration method.
  • Optimized formulation through 3² full factorial design.
  • Analyzed effects of phosphatidylcholine and cholesterol on drug release and entrapment efficiency.
  • Optimized formulation contained 200 mg phospatidylcholine and 40 mg cholesterol.
  • Vesicle size was 98.22 ± 10.03 nm with a zeta potential of -21.53 ± 1.02 mV.
  • Entrapment efficiency reached 97.5% with sustained release over 8 hours.
  • Transcorneal permeation was 1.8 times greater than marketed eye drops.
  • Demonstrated non-irritant and isotonic properties in safety assessments.

Abstract

SignificanceThe liposomal formulation reveals a safe, sustained, and efficient ocular drug delivery to improve the therapeutic potential of dorozolamide hydrochloride in glaucoma treatment.ObjectiveA liposomal formulation of Dorzolamide hydrochloride was developed and evaluated for sustained ocular delivery with improved permeation and safety.MethodsLiposomes were prepared using the thin-film hydration method and optimized through a 32 full factorial design, analysing the effects of phosphatidylcholine and cholesterol on entrapment efficiency and drug release via response surface methodology.ResultsThe 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 hours, 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 non-irritant and isotonic.ConclusionOverall, the liposomal system significantly enhanced ocular bioavailability and demonstrated potential as a safe and effective option for long-term glaucoma therapy.

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Cite This Study

Paul et al. (2026) studied this question.

synapsesocial.com/papers/696f1a9f9e64f732b51eedaahttps://doi.org/10.1080/03639045.2026.2618506
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