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Progesterone-loaded chitosan microspheres: a long acting biodegradable controlled delivery system
S R Jameela1, T V Kumary, A V Lal
1Division of Polymer Chemistry, Sree Chitra Tirunal Institute for Medical Sciences and Technology, Trivandrum, India.
Summary
Highly crosslinked chitosan microspheres offer controlled long-term progesterone delivery, releasing 35% over 40 days. This formulation maintained therapeutic plasma levels for up to 5 months in rabbits.
Area of Science:
- Biomaterials Science
- Drug Delivery Systems
- Polymer Chemistry
Background:
- Chitosan microspheres are promising for drug delivery.
- Controlled release of steroids requires advanced formulation strategies.
- Progesterone delivery systems are crucial for various therapeutic applications.
Purpose of the Study:
- To develop and characterize crosslinked chitosan microspheres for progesterone encapsulation.
- To investigate the in vitro drug release kinetics.
- To evaluate the in vivo bioavailability and long-term release of progesterone.
Main Methods:
- Preparation of chitosan microspheres using glutaraldehyde crosslinking in a non-aqueous medium.
- Characterization of microsphere size (45-300 microns) and morphology.
- In vitro drug release studies in phosphate buffer at 37°C.
- In vivo bioavailability study via intramuscular injection in rabbits.
Main Results:
- Smooth, spherical chitosan microspheres loaded with progesterone were successfully prepared.
- Drug release showed significant dependence on crosslinking density: highly crosslinked spheres released ~35% in 40 days, lightly crosslinked released ~70%.
- In vivo studies demonstrated sustained plasma concentrations (1-2 ng/ml) for up to 5 months with minimal burst effect.
Conclusions:
- Crosslinked chitosan microspheres provide an effective system for sustained progesterone delivery.
- Controlling crosslinking density allows modulation of drug release rates.
- The formulation shows potential for long-term steroid delivery applications.