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An Accelerated Release Method of Risperidone Loaded PLGA Microspheres with Good IVIVC
Xiaoqin Hu1, Jianwei Zhang1, Xuemei Tang1
1Beijing Institute of Pharmacology and Toxicology, Beijing 100850. China.
Current Drug Delivery
|May 20, 2017
Summary
An accelerated in vitro release method for risperidone poly(lactic-co-glycolic acid) (PLGA) microspheres was developed. This method accurately predicts in vivo performance and aids in quality control for long-acting drug formulations.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Biomaterials
Background:
- Long-acting microsphere formulations require extensive testing for release profiles.
- Conventional in vitro release methods are time-consuming for extended-release products.
- Accelerated release testing is crucial for efficient formulation design and quality control.
Purpose of the Study:
- To develop an accelerated in vitro release method for risperidone-loaded poly(lactic-co-glycolic acid) (PLGA) microspheres.
- To establish a good in vitro/in vivo correlation (IVIVC) for the developed method.
- To facilitate formulation development and quality control of long-acting risperidone delivery systems.
Main Methods:
- Optimized accelerated release conditions by evaluating temperature, ethanol concentration, pH, and osmotic pressure.
- Determined in vitro accelerated release profiles under optimized conditions.
- Assessed in vivo risperidone absorption in rats and calculated cumulative absorption profiles using kinetic models.
- Evaluated IVIVC using the Least Square Method.
Main Results:
- Temperature and ethanol concentration significantly influenced risperidone release from PLGA microspheres.
- Optimized conditions involved PBS (pH 7.0, 300 mOsm) with 20% ethanol at 45°C.
- High correlation coefficients (R2 > 0.95) and favorable slope values (0.9564-1.1868) were achieved for IVIVC.
- Sustained and complete risperidone release was observed, demonstrating method robustness.
Conclusions:
- An effective in vitro accelerated release method for risperidone microspheres with strong IVIVC was successfully established.
- This method shows significant potential for predicting in vivo performance.
- The developed method is valuable for quality control of risperidone-loaded PLGA microspheres.
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