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Published on: September 17, 2014
Eudragit RL100 based microspheres for ocular administration of azelastine hydrochloride
Ujwala A Shinde1, Jaykumar N Shete, Hema A Nair
1Department of Pharmaceutics, Bombay College of Pharmacy, Kalina, Santacruz E, Mumbai 400098, India. ujwalas29@gmail.com
Journal of Microencapsulation
|March 2, 2012
Summary
Polymeric microspheres loaded with azelastine hydrochloride offer a promising approach for treating allergic conjunctivitis. These novel microspheres demonstrated prolonged drug release and superior in vivo efficacy compared to existing formulations.
Area of Science:
- Ophthalmology
- Materials Science
- Pharmaceutics
Background:
- Allergic conjunctivitis is a prevalent ocular condition requiring effective and sustained treatment.
- Current formulations may have limitations in drug delivery and patient compliance.
- Polymeric microspheres offer a potential platform for controlled drug release in ocular applications.
Purpose of the Study:
- To investigate the potential of Eudragit RL100 polymeric microspheres for the ocular delivery of azelastine hydrochloride.
- To characterize the influence of drug-polymer ratio on microsphere properties and drug release kinetics.
- To evaluate the in vivo efficacy of azelastine hydrochloride microspheres in a rat model.
Main Methods:
- Azelastine hydrochloride loaded Eudragit RL100 microspheres were prepared using the solvent evaporation technique.
- Microspheres were characterized for particle size, zeta potential, and entrapment efficiency.
- In vitro drug release studies were conducted over 6 hours.
- Scanning electron microscopy (SEM), Fourier transform infrared (FTIR) spectroscopy, and differential scanning calorimetry (DSC) were employed for structural and chemical analysis.
- In vivo studies were performed in a rat model to assess the reduction in eosinophil count.
Main Results:
- Microsphere size ranged from 4.18-7.36 µm with positive zeta potential.
- Entrapment efficiency increased with higher drug-polymer ratios, reaching a maximum of 14.56%.
- In vitro studies showed sustained drug release over 6 hours.
- SEM revealed spherical microspheres with a dense structure.
- FTIR and DSC indicated minimal changes in drug-polymer interactions.
- In vivo studies demonstrated a more pronounced reduction in eosinophil count with azelastine hydrochloride microspheres compared to the marketed formulation.
Conclusions:
- Eudragit RL100 microspheres are a viable system for the sustained ocular delivery of azelastine hydrochloride.
- The developed microspheres exhibit favorable physicochemical properties and enhanced in vivo therapeutic potential for allergic conjunctivitis.
- This formulation represents a promising alternative to conventional treatments for allergic conjunctivitis.
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