ABIRATERONE ACETATE LOADED SODIUM ALGINATE NANOPARTICLES FOR IMPROVING AQUEOUS SOLUBILITY AND DISSOLUTION OF ABIRATERONE ACETATE: PREPARATION AND FORMULATION OPTIMIZATION BY CENTRAL COMPOSITE DESIGN, CHARACTERIZATION

NALLAMUTHU M.; UMADEVI S.

doi:10.22159/ijap.2025v17i4.53942

Authors

NALLAMUTHU M. Department of Pharmaceutics, School of Pharmaceutical Sciences, Vels Institute of Science, Technology and Advanced Studies (VISTAS), Pallavaram, Chennai-600117, Tamil Nadu, India https://orcid.org/0009-0002-5003-720X
UMADEVI S. Department of Pharmaceutics, School of Pharmaceutical Sciences, Vels Institute of Science, Technology and Advanced Studies (VISTAS), Pallavaram, Chennai-600117, Tamil Nadu, India

DOI:

https://doi.org/10.22159/ijap.2025v17i4.53942

Keywords:

Sodium alginate, Abiraterone acetate, Nanoparticles, Central composite design, Aqueous solubility, Dissolution, Oral bioavailability

Abstract

Objective: Abiraterone acetate is poorly soluble in water and is not effectively absorbed from the gastrointestinal tract. The oral bioavailability of abiraterone acetate in humans is predicted to be less than 10% due to these characteristics. The target of the present work was to construct Abiraterone Acetate Loaded Sodium Alginate Nanoparticles (ASNPs) to improve the abiraterone acetate aqueous solubility and dissolution.

Methods: The ASNPs were constructed by using the solvent desolvation method. For ASNPs optimization, the Central Composite Design (CCD) was selected. Particle size and Drug Entrapment Efficiency (DEE) were employed as responses to optimize the independent variable composition using CCD.

Results: According to CCD, 13 formulations were developed. The particle size of 219.5±0.92 nm and DEE of 89.21±0.54% originated from the optimal batch based on the desirability function (0.978). Optimized ASNPs were found with a zeta potential of-46.9±0.65 mV, and in vitro drug release of 95.43±0.87%. Optimized ASNPs demonstrated a 28.4-fold increase in the solubility in water compared to pure abiraterone acetate. The in vitro drug release evaluation suggests that optimized ASNPs exhibit improved dissolution and sustained drug release compared to the commercial product.

Conclusion: This study concludes that optimized ASNPs overcome the aqueous solubility and dissolution challenges of abiraterone acetate and possess most of the ideal properties required for an oral sustained-release dosage form. This can reduce the dosage, administration time, and systemic toxicity, and improve oral bioavailability compared to the commercial product.

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