(W1230-03-15) Preparation of Lurasidone Hydrochloride Nanoparticles and Enhanced Bioavailability

Purpose: Lurasidone hydrochloride is a thiazole derivative and atypical antipsychotic agent. It is used in the treatment of schizophrenia and bipolar disorder. Polymeric nanoparticle-based drug delivery systems are one of the most developing areas within nanotechnology. The study aimed to develop lurasidone nanoparticles with reduced particle size, enhanced dissolution rate, and enhanced bioavailability.

Methods: Lurasidone nanoparticles were prepared by the nanoprecipitation-solvent displacement method. Measurement of Particle Size, Poly Dispersity Index (PDI), Zeta Potential Entrapment efficiency, and invitro dissolution studies. The optimized formulations carried out by the DSC, SEM, and Pharmacokinetic studies were estimated by using HPLC.

Results: This may be due to the presence of optimum polymer and optimum stabilizer concentrations, compared to other formulations. An increase in polymer concentration increased the drug entrapment efficiency. However, maintaining the particle size within the intended submicron range required a high concentration of the surfactant Poloxamer 188. Batch F7 had a noteworthy particle size of 979.4 nm, suggesting a proficient control over the distribution of particle sizes. The morphology of the nanoparticles was confirmed by SEM examination to be spherical and rather consistent. From various parameters determined for drug release from nanoparticles based on the Peppas Model, and Higuchi Model, it is evident that values of ‘R²’ for the Higuchi plot of optimized nanoformulation is 0.9061, for first-order plot 0.9679, zero-order plot 0.950 and those of Peppas equation are 0.9521 respectively. This data reveals that drug release follows first-order release kinetics. The pharmacokinetic data revealed a significant increase in Cmax and AUC0-∞ of lurasidone nanoparticulate formulation in comparison to that of pure drug.

Conclusion: The drug entrapment efficiency and in vitro dissolution of F7 were high when compared to other formulations.  In summary, the present study showcases the potential of Lurasidone-loaded PLGA nanoparticles as an effective strategy for enhancing the therapeutic efficacy of this atypical antipsychotic agent. This research advances polymeric nanoparticle-based drug delivery systems, providing innovative solutions to solubility and bioavailability limitations in pharmaceutical formulations.

References: Sunny Shah, Bhavin Parmar, Moinuddin Soniwala. ” Design, Optimization, and Evaluation of Lurasidone Hydrochloride Nanocrystals”. AAPS PharmSciTech, 2016;17 (5).1150-8


Figure 1. SEM of a. pure lurasidone b. Lurasidone nanoparticles


Figure 2: In vitro drug release of Lurasidone Hydrochloride nanoparticulate formulations a. (F1-F4) b.(F5-F8)


Table 1. Data of Particle size analysis, polydispersity index, zeta potential, and entrapment efficiency of Lurasidone Hydrochloride nanoparticulate formulations