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Inventory of oral anticancer agents: Pharmaceutical formulation aspects with focus on the solid dispersion technique
E Sawicki1, J H M Schellens2, J H Beijnen3
1Department of Pharmacy & Pharmacology, The Netherlands Cancer Institute/MC Slotervaart, Louwesweg 6, 1066 EC Amsterdam, The Netherlands.
Cancer Treatment Reviews
|October 25, 2016
Summary
Poor dissolution of oral anticancer drugs (oncolytics) can hinder absorption and treatment efficacy. Solid dispersion technology significantly enhances drug dissolution and bioavailability for these poorly soluble medications.
Area of Science:
- Pharmaceutical Sciences
- Pharmacokinetics
- Drug Delivery
Background:
- Oral anticancer agents (oncolytics) require adequate dissolution for effective absorption and consistent therapeutic outcomes.
- Poor drug dissolution is a significant factor contributing to low oral bioavailability and variable blood concentrations for many oncolytics.
- This can lead to suboptimal treatment efficacy or even therapeutic failure.
Purpose of the Study:
- To review pharmaceutical formulation strategies and absorption pharmacokinetics of orally administered oncolytics.
- To highlight the role of solid dispersion technology in overcoming dissolution-limited absorption of poorly soluble drugs.
- To evaluate the impact of solid dispersion formulations on the bioavailability of specific oncolytics.
Main Methods:
- Review of current literature on orally administered oncolytics and their formulation characteristics.
- Analysis of pharmacokinetic data related to drug dissolution and absorption.
- Examination of the principles and application of solid dispersion technology in pharmaceutical formulations.
Main Results:
- Nearly half of orally administered oncolytics likely suffer from poor dissolution, impacting absorption.
- Solid dispersion formulations significantly enhance drug dissolution, leading to super-saturation and improved in vivo absorption.
- Three licensed oncolytics (everolimus, vemurafenib, regorafenib) formulated as solid dispersions demonstrate markedly improved dissolution and absorption compared to conventional forms.
Conclusions:
- Solid dispersion technology is a viable and effective strategy to improve the oral absorption of poorly soluble oncolytics.
- The successful implementation of solid dispersions for everolimus, vemurafenib, and regorafenib supports their wider application.
- Further adoption of solid dispersion technology is encouraged for developing new oral oncolytic formulations with enhanced bioavailability.
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