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Paliperidone Acid-Based Cocrystal for Improving Biopharmaceutical Properties: In Vitro and In Vivo Evaluation.
Mohammed Elmowafy1, Nabil K Alruwaili1, Omar Awad Alsaidan1
1Department of Pharmaceutics, College of Pharmacy, Jouf University, Sakaka 72388, Saudi Arabia.
ACS Omega
|September 29, 2025
Summary
Developing paliperidone cocrystals with oxalic acid significantly enhanced solubility and oral bioavailability. This cocrystal formulation offers a promising solution for improving the biopharmaceutical properties of paliperidone.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery
- Materials Science
Background:
- Paliperidone is an effective antipsychotic but has poor solubility and low oral bioavailability.
- Improving the biopharmaceutical properties of paliperidone is crucial for its therapeutic efficacy.
Purpose of the Study:
- To develop paliperidone cocrystals using short-chain acids as coformers.
- To enhance the solubility, dissolution rate, and oral bioavailability of paliperidone.
Main Methods:
- Cocrystal screening using various short-chain acids.
- Characterization using FTIR, DSC, PXRD, and SEM.
- In vitro dissolution and in vivo bioavailability studies in comparison to pure paliperidone.
Main Results:
- Paliperidone-oxalic acid cocrystal (1:2 molar ratio) showed the highest solubility (9831 ± 113 μg/mL).
- Cocrystal formation was confirmed by structural analysis, revealing hydrogen bonds and a less crystalline state.
- The cocrystal exhibited a significantly faster dissolution rate and a 2.66-fold increase in oral bioavailability compared to paliperidone suspension.
Conclusions:
- Paliperidone cocrystal formation with oxalic acid is a viable strategy to overcome poor biopharmaceutical properties.
- The developed cocrystal formulation demonstrates improved solubility, dissolution, and bioavailability, offering a promising therapeutic alternative.
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