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Development of Risperidone PLGA Microspheres
Susan D'Souza1, Jabar A Faraj2, Stefano Giovagnoli3
1Sunovion Pharmaceuticals Inc., Marlborough, MA 01752, USA.
Journal of Drug Delivery
|March 12, 2014
Summary
Biodegradable poly(lactic-co-glycolic acid) (PLGA) microspheres offer sustained Risperidone delivery for schizophrenia treatment. These formulations improve drug effectiveness and reduce the need for combination oral therapies.
Area of Science:
- Pharmaceutics
- Biomaterials Science
- Pharmacology
Background:
- Schizophrenia treatment often requires combination therapy.
- Risperidone is a key antipsychotic medication.
- Sustained drug delivery systems aim to improve patient compliance and therapeutic outcomes.
Purpose of the Study:
- To design and evaluate biodegradable poly(lactic-co-glycolic acid) (PLGA) microspheres for sustained Risperidone delivery.
- To explore the potential of these microspheres to avoid combination therapy for schizophrenia.
- To investigate the impact of PLGA copolymer composition on drug release kinetics and in vivo behavior.
Main Methods:
- Preparation of four Risperidone-loaded PLGA microsphere formulations using 50:50 and 75:25 PLGA copolymers.
- In vitro characterization of microsphere properties.
- In vivo pharmacokinetic studies in Sprague-Dawley rats at 20 and 40 mg/kg doses.
- Simulation of multiple dosing regimens (weekly and 15-day).
Main Results:
- All formulations demonstrated an initial burst release followed by sustained Risperidone release.
- Microspheres made with 75:25 PLGA exhibited longer duration of action and higher cumulative AUC compared to 50:50 PLGA formulations.
- Multiple dosing simulations showed pulsatile drug release, achieving steady state by the second dose.
- PLGA composition and molecular weight influenced in vivo drug release profiles.
Conclusions:
- Biodegradable PLGA microspheres are suitable for developing sustained-release Risperidone formulations.
- These formulations can potentially eliminate the need for combination oral therapy in schizophrenia treatment.
- PLGA microspheres offer tailored in vivo behavior, enhancing pharmacological effectiveness and reducing washout periods.
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