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Published on: February 9, 2019
Lurasidone hydrochloride-loaded microparticle-based long-acting injectable: formulation optimisation,
Gaurav Awasthi1, Parth Patel1, Keerti Jain1
1Drug Delivery and Nanomedicine Research Laboratory, Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER) - Raebareli, Lucknow, India.
Researchers developed a novel long-acting injectable formulation for lurasidone hydrochloride using poly(lactic-co-glycolic acid) microparticles. This new formulation significantly improves drug delivery, offering sustained release over 90 days.
Area of Science:
- Pharmaceutical Sciences
- Biomaterials Engineering
- Drug Delivery Systems
Background:
- Lurasidone hydrochloride is an effective antipsychotic, but its current formulation has poor bioavailability and requires frequent dosing.
- There is a need for improved drug delivery systems to enhance patient compliance and therapeutic efficacy of lurasidone hydrochloride.
Purpose of the Study:
- To develop and optimize a long-acting injectable formulation of lurasidone hydrochloride using poly(lactic-co-glycolic acid) (PLGA) microparticles.
- To characterize the physical, chemical, and in vitro release properties of the developed microparticle formulation.
Main Methods:
- Fabrication of lurasidone hydrochloride-loaded PLGA microparticles.
- Characterization including particle size analysis, entrapment efficiency, drug loading, surface morphology (using scanning electron microscopy), and differential scanning calorimetry (DSC).
- In vitro drug release studies under real-time and accelerated conditions, analyzed using the Hixon-Crowell kinetic model.
Main Results:
- Optimized microparticles exhibited a particle size of 32.81 ± 1.46 µm, high entrapment efficiency (95.74 ± 3.19%), and drug loading (27.68 ± 0.95%).
- Morphological analysis revealed a 'golf ball' like surface texture, and DSC confirmed amorphization and successful drug encapsulation.
- In vitro release studies demonstrated a triphasic release pattern, with 80.26 ± 3.84% drug release achieved within 90 days under real-time conditions.
Conclusions:
- The developed PLGA microparticle formulation offers a promising long-acting injectable alternative for lurasidone hydrochloride.
- The formulation exhibits favorable characteristics for sustained drug delivery, potentially improving patient outcomes.
- Results provide a strong foundation for large-scale development and clinical translation of this novel injectable formulation.
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