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Related Experiment Video

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Intraoperative Visualization of Subretinal Injection and Retinal Detachment in Rats

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Long acting betaxolol ocular inserts based on polymer composite.

Hitesh B Gevariya¹, Jayvadan K Patel

¹Faculty of Pharmacy, Dharmsinh Desai University, Nadiad, Gujarat, India. hitu.phd@gmail.com

Current Drug Delivery

|August 6, 2013

Summary

Novel ocular inserts containing betaxolol hydrochloride offer sustained drug release for glaucoma treatment. These inserts improve ocular bioavailability and duration of action compared to traditional eye drops.

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Area of Science:

Ophthalmology
Pharmaceutics
Materials Science

Background:

Conventional ocular drug delivery faces pre-corneal challenges, limiting bioavailability and therapeutic efficacy.
Developing controlled and sustained ocular drug delivery systems is crucial for modern pharmaceutical applications.

Purpose of the Study:

To investigate the drug release kinetics of betaxolol hydrochloride from a PMMA/PEO hydrophobic matrix.
To evaluate the potential of these ocular inserts for improved ocular bioavailability and extended duration of action.

Main Methods:

Ocular inserts were fabricated using a film casting technique with varying proportions of PMMA and polyethylene oxide (PEO).
In vitro drug release studies were conducted using a flow-through apparatus simulating ocular conditions.
In vivo efficacy was assessed in a rabbit model of steroid-induced glaucoma.

Main Results:

Polymer composition and concentration significantly influenced drug release kinetics through changes in diffusion path length and pore formation.
Drug release mechanisms included non-fickian diffusion, anomalous transport, and super case II transport.
An optimized formulation (F8) demonstrated superior in vivo intraocular pressure (IOP) lowering activity for 24 hours, compared to 10 hours for eye drops.

Conclusions:

The developed PMMA/PEO ocular inserts provide a promising once-a-day sustained release formulation for glaucoma management.
In vitro-in vivo correlation (IVIVC) confirmed the reliability of the in vitro release data for predicting in vivo performance.