Abstract
<p><strong>Objective: </strong>The current work was attempted to formulate and evaluate a controlled-release matrix-type ocular inserts containing a combination of brimonidine tartrate and timolol maleate, with a view to sustain the drug release in the cul-de-sac of the eye.<strong></strong></p><p><strong>Methods: </strong>Initially, the infrared studies were done to determine the drug–polymer interactions. Sodium alginate-loaded ocuserts were prepared by solvent casting technique. Varying the concentrations of polymer—sodium alginate, plasticizer—glycerine, and cross-linking agent—calcium chloride by keeping the drug concentration constant, made a total of nine formulations. These formulations were evaluated for its appearance, drug content, weight uniformity, thickness uniformity, percentage moisture loss, percentage moisture absorption, and <em>in vitro </em>release profile of the ocuserts. Finally, accelerated stability studies and the release kinetics were performed on the optimised formulation.<strong></strong></p><p><strong>Results: </strong>It was perceived that polymer, plasticizer, and calcium chloride had a significant influence on the drug release. The data obtained from the formulations showed that formulation—F9 was the optimised formulation, which exhibited better drug release. The release data of the optimised formulation tested on the kinetic models revealed that it exhibited first-order release kinetics. <strong></strong></p><p><strong>Conclusion: </strong>It can be concluded that a natural bioadhesive hydrophilic polymer such as sodium alginate can be used as a film former to load water soluble and hydrophilic drugs like brimonidine tartrate and timolol maleate. Among all formulations, F9 with 400 mg sodium alginate, 2% calcium chloride and 60 mg glycerin were found to be the most suitable insert in terms of appearance, ease of handling, thickness, <em>in vitro</em> drug release and stability.</p>
Highlights
The conventional medications such as eye ointments and drops administered into the eye have various constraints such as poor bioavailability, reduced therapeutic efficiency due to the precorneal elimination of the drug, and frequent dosing of the medications may lead to reduced patient compliance
The current work is focused to design and evaluation of a controlledrelease ocuserts containing a combination of Brimonidine tartrate (BT) and TM to treat glaucoma
Studies had revealed that fixed dose combinations of both the drugs are well tolerated in patients with glaucoma with least side effects [15,16,17]
Summary
The conventional medications such as eye ointments and drops administered into the eye have various constraints such as poor bioavailability, reduced therapeutic efficiency due to the precorneal elimination of the drug, and frequent dosing of the medications may lead to reduced patient compliance All these limitations can be overcome by the continuous delivery of the medications into the eye, which could be accomplished by formulating an ocular insert [1, 2]. Brimonidine tartrate (BT) and timolol tartrate (TM) are the most widely used medications that lower the IOP [8, 9] These are the non-selective beta-adrenergic blocker and the selective alpha 2-adrenergic receptor, respectively. These drugs act by lowering the IOP in the eye by impeding the production of aqueous humour [10, 11]
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a call
