Development and Evaluation of Brimonidine Tartrate Nanoparticulate Ocular Insert

Glaucoma is the second leading cause of vision loss in the world after cataracts. It is estimated that the number of people with glaucoma will be nearly 79.6 million worldwide by 2023. This alarmingly high number of anticipated patients requires urgent improvement in the current therapeutic approaches adopted for the treatment of this disease. At present, Antiglaucoma agent brimonidine tartrate is commercially available in the form of eye drops and marketed under the name of Alphagan® (0.2%) or Alphagan® P (0.1% and 0.15%). For effective management of intraocular pressure, it needs to be administered 1 to 3 drops every 6 h. The drawbacks associated with the available eye drops are short pre-corneal retention time along with poor patient compliance. The present was conducted to formulate, optimize and<i> </i>evaluate a brimonidine tartrate nanoparticulate ocular insert to improve patient compliance.<br/>Nanoparticulate ocular inserts were prepared in two steps initially ionic gelation for nanoparticles and solvent casting method for the ocular insert. Release studies showed that the prepared insert releases brimonidine tartrate by zero-order kinetic up to 8 h. The inserts were evaluated for several parameters like drug-excipient interaction, thermal studies, the thickness of the insert, swelling index, and moisture studies, Furthermore, the in-vivo evaluation showed that the ocular insert has good therapeutic activity and fewer side effects as compared to other marketed formulations.