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image of Soluplus Stabilized Amorphous Dispersions for Enhanced Oral Absorption of Felodipine

Abstract

Background

Overcoming the poor aqueous solubility of small-molecule drugs is a major challenge in developing clinical pharmaceuticals. Felodipine (FLDP), an L-type calcium calcium channel blocker, is a poorly water-soluble drug.

Objectives

The study aimed to explore the potential applications of polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol (Soluplus) stabilized amorphous dispersions for augmenting the oral delivery of poorly water-soluble drugs.

Methods

Soluplus-stabilized amorphous FLDP (FLDP-SSAs) was prepared using a two-phase mixing method. The samples were analyzed for their microscopic and macroscopic behavior using polarized light microscopy (PLM), differential scanning calorimetry (DSC), molecular simulation, and dissolution studies. Subsequently, the pharmacokinetics of FLDP-SSAs were evaluated.

Results

The maximum drug-to-Soluplus mass ratio of FLDP-SSAs was 50:50, with a drug concentration of 8.0 mg/mL. They exhibited an amorphous nature, as confirmed by PLM and DSC. FLDP-SSAs generated nanoparticles with a particle size of approximately 50 nm during dissolution. Compared to FLDP oral solution, FLDP-SSAs exhibited higher solubility due to their amorphous nature and the generation of nanoparticles. The area under the curve (AUC) for oral FLDP-SSAs was 16.7-fold larger than that of the FLDP suspension.

Conclusion

FLDP-SSAs could stabilize FLDP in an amorphous state and serve as drug carriers to enhance oral absorption.

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2025-01-16
2025-07-04

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Soluplus Stabilized Amorphous Dispersions for Enhanced Oral Absorption of Felodipine
Bentham Science Publishers ; https://doi.org/10.2174/0115672018363757241216061705
/content/journals/cdd/10.2174/0115672018363757241216061705
/content/journals/cdd/10.2174/0115672018363757241216061705
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  • Article Type:     Research Article
Keywords: soluplus ; Felodipine ; oral absorption ; nanoparticle ; pharmacokinetics ; amorphous dispersions

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