Related Experiment Video
Updated: Sep 19, 2025
10:02
Use of Rabbit Eyes in Pharmacokinetic Studies of Intraocular Drugs
Published on: July 23, 2016
32.5K
Injectable PLGA-based In Situ Forming Subconjunctival Implant for Sustained Ocular Delivery of Ketotifen Fumarate:
Nur Mita1,2, Xuejia Kang1,3, Pengyu Chen3
1Department of Drug Discovery and Development, Harrison College of Pharmacy, Auburn University, Auburn, AL, 36849, United States of America.
AAPS Pharmscitech
|June 2, 2025
Summary
This study developed a novel injectable implant for ketotifen fumarate to treat allergic conjunctivitis in animals. The new formulation enhances drug delivery, improving bioavailability and reducing dosing frequency for sustained ocular therapy.
Area of Science:
- Ophthalmology
- Biomaterials Science
- Veterinary Medicine
Background:
- Ketotifen fumarate is effective for allergic conjunctivitis but limited by poor bioavailability and frequent dosing.
- Current treatments require frequent administration, impacting patient compliance and therapeutic outcomes.
Purpose of the Study:
- To develop a ketotifen fumarate-loaded in situ forming subconjunctival injectable implant (ISFSI).
- To evaluate the physicochemical properties, drug release kinetics, and biocompatibility of the ISFSI for ocular applications in large animals.
Main Methods:
- Formulation of ISFSIs using ketotifen fumarate dispersed in polylactide-co-glycolide (PLGA) with release retarders.
- Characterization included visual appearance, viscosity, solidification time, in vitro drug release, SEM, DSC, rheology, and cytotoxicity assays.
- Injectability was predicted using the power law for various syringe and needle dimensions.
Main Results:
- All ISFSIs showed good recovery (>95%) and solidified upon contact with the release medium.
- The optimized formulation (KFM5) exhibited a triphasic release profile with low burst release (4.91%) following Higuchi kinetics.
- SEM revealed a "hollow and sponge-like" structure, DSC confirmed drug crystallinity, and rheology indicated acceptable injectability with >90% cell viability.
Conclusions:
- The developed ketotifen fumarate ISFSI offers a promising sustained drug delivery system for ocular conditions in large animals.
- The formulation demonstrates favorable physicochemical properties, controlled drug release, and excellent biocompatibility.
- This injectable implant has the potential to improve therapeutic efficacy and reduce dosing frequency for veterinary ophthalmology.
