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Polymer-Based Solid Dispersions to Improve the Solubility and Dissolution Rate of Ziprasidone Hydrochloride
* 1, 2, 3 , 2 , 3
1  Department of Pharmacy, Bharti Vishwavidyalaya, Durg, Chhattisgarh, 491001, India.
2  Department of Pharmaceutics, Royal College of Pharmacy, Raipur, Chhattisgarh, 492099, India.
3  Department of Pharmacology, Rungta College of Pharmaceutical Science and Research, Bhilai, Chhattisgarh, 490024, India.
Academic Editor: Kyriakos Kachrimanis

Abstract:

Ziprasidone Hydrochloride is an atypical antipsychotic drug commonly prescribed for the treatment of schizophrenia. Its clinical efficacy is significantly limited by its very low aqueous solubility (<0.1 mg/mL), which restricts oral absorption and systemic bioavailability. In the present study, we aimed to enhance the solubility and dissolution rate of Ziprasidone Hydrochloride through the formulation of solid dispersions using hydrophilic polymers, including polyethylene glycol 6000 (PEG6000), polyvinylpyrrolidone (PVP), hydroxypropyl methylcellulose (HPMC), and hydroxypropyl cellulose (HPC). Solid dispersions were prepared by the solvent evaporation technique in various drug-to-polymer ratios and subjected to comprehensive physicochemical characterization. The formulations were analyzed using Scanning Electron Microscopy (SEM), Fourier Transform Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), and X-Ray Diffraction (XRD) studies. The results revealed that incorporation of Ziprasidone into polymer matrices led to a reduction in particle aggregation, conversion from crystalline to amorphous form, and improved wettability and dispersibility. Optimized solid dispersions exhibited approximately a 50% increase in solubility compared to the pure drug. Dissolution studies demonstrated a significant improvement in release profiles, with drug release directly proportional to the polymer concentration. Among the polymers tested, PVP was the most effective in enhancing solubility and dissolution. These findings indicate that polymer-based solid dispersions are a promising strategy for improving the oral bioavailability and therapeutic efficacy of poorly water-soluble drugs like Ziprasidone Hydrochloride.

Keywords: Ziprasidone Hydrochloride; Solid dispersion; Solubility enhancement; Dissolution rate; Hydrophilic polymers

 
 
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