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Etoposide Amorphous Nanopowder for Improved Oral Bioavailability: Formulation Development, Optimization, in vitro and
Yue Wang1, Shuhang Wang1, Yingju Xu1
1School of Pharmacy, Jilin University, Changchun, People's Republic of China.
International Journal of Nanomedicine
|October 29, 2020
Summary
This study developed an amorphous nanopowder to improve etoposide
Area of Science:
- Pharmaceutical Sciences
- Materials Science
- Drug Delivery
Background:
- Etoposide, a podophyllotoxin derivative, is crucial in cancer treatment.
- Etoposide is a BCS Class IV drug with poor solubility and permeability, limiting oral absorption.
- Developing novel formulations is essential to enhance etoposide's oral bioavailability.
Purpose of the Study:
- To develop and optimize an amorphous nanopowder formulation of etoposide.
- To enhance the solubility, dissolution, and oral absorption of etoposide.
- To evaluate the in vivo pharmacokinetic performance of the etoposide amorphous nanopowder.
Main Methods:
- Exploration of stabilizers and preparation processes for etoposide nanosuspension.
- Optimization of formulation using Box-Behnken design, focusing on ultrasonication time, phase ratio, and stabilizer concentration.
- Characterization of the amorphous nanopowder via particle size, PDI, XRD, and DSC; assessment of solubility, dissolution, and oral bioavailability in rats.
Main Results:
- Optimized etoposide amorphous nanopowder exhibited spherical particles (211.7 ± 10.4 nm, PDI 0.125 ± 0.028).
- The nanopowder demonstrated significantly enhanced solubility and dissolution compared to coarse powder and physical mixtures.
- Oral administration in rats showed a 2.21-fold increase in Cmax and a 2.13-fold increase in AUC0-t for the nanopowder versus crude etoposide suspension.
Conclusions:
- The optimized etoposide amorphous nanopowder effectively enhances dissolution and oral absorption.
- This formulation represents a promising delivery system for improving etoposide's oral bioavailability.
- The study highlights the potential of amorphous nanopowder technology for poorly soluble drugs.
Keywords:
amorphous nanopowderbioavailability enhancementetoposideoral absorptionpoor aqueous solubilityMore Related Videos
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