Abstract

Purpose: To prepare ocular inserts of timolol maleate using guar gum as a polymer for treatment of glaucoma. Methods: Timolol maleate ocular inserts were prepared by solvent casting method using guar gum in different proportions (0.25% w/v, 0.50% w/v , 75 % w/v and 1.0% w/v). The prepared formulations were evaluated for thickness, weight variation, percentage drug content, surface pH, folding endurance, percentage moisture absorption and loss, percentage swelling, mechanical strength and in vitro transcorneal permeation. In-vitro transcorneal permeation study was performed on goat cornea using modified Franz diffusion cell. Results: The inserts were found to be of uniform thickness (ranging from 41.12±0.04µm to 79.90±0.03µm) and weight (0.84±0.07 mg to 2.11±0.09 mg). The % drug content in the inserts was found to be varied between 98.69±0.58to 96.37±0.58. The cumulative % drug releases from the formulation ranged from 50.22±1.41 to 97.72±0.67over a period of 24 h. In-vitro transcorneal study revealed that an increase in concentration of polymer slows down the release of timolol maleate from the formulation. Conclusion: Ocular inserts using guar gum as a polymer were successfully prepared and can be effectively used for sustain ocular delivery over a period of 24 h.

Highlights

  • Timolol maleate ocular inserts were prepared by solvent casting method using guar gum in different proportions (0.25% w/v, 0.50% w/v, 75 % w/v and 1.0% w/v)

  • The prepared formulations were evaluated for thickness, weight variation, percentage drug content, surface pH, folding endurance, percentage mois ture absorption and loss, percentage swelling, mechanical strength and in vitro transcorneal permeation

  • In-vitro transcorneal permeation study was performed on goat cornea using modified Franz diffusion cell

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Summary

Research Article

Lachoo Memorial College of Science and Technology, Pharmacy Wing, Jodhpur-342 003, Rajasthan, India. ABSTRAC T The objective of this study was to prepare ocular inserts of timolol maleate using guar gum as a polymer. Timolol maleate ocular inserts were prepared by solvent casting method using guar gum in different proportions (0.25% w/v, 0.50% w/v , 75 % w/v and 1.0% w/v). The prepared formulations were evaluated for thickness, weight variation, percentage drug content, surface pH, folding endurance, percentage mois ture absorption and loss, percentage swelling, mechanical strength and in vitro transcorneal permeation. The cumulative % drug releases from the formulation ranged from 50.22±1.41 to 97.72±0.67over a period of 24h. In-vitro transcorneal study revealed that an increase in concentration of polymer slows down the release of timolol maleate from the formulation. Ocular inserts using guar gum as a polymer were successfully prepared and ca n be effectively used for sustain ocular delivery over a period of 24h

INTRODUC TION
MATERIALS AND METHODS
Preparation of ocular insert
Weight variation
Surface pH determination
Folding endurance value
Moisture absorption
Moisture loss
Swelling Study
Drug content
In vitro transcorneal permeation study Corneal preparation
Mechanical strength
Permeation experiment
Mechanism and kinetics of drug release
Thick ness
Mechanical strength Tensile strength
Best fit model
In vitro transcorneal permeation study
Drug release kinetics
REFE RE NC ES
Full Text
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