Bioavailability enhancement strategies: basics, formulation approaches and regulatory considerations

Area of Science:

• Pharmaceutical Science
• Biomedical Research
• Drug Delivery Systems

Background:

• Poor solubility and bioavailability are significant hurdles for approximately 40% of new molecular entities (NMEs).
• Intestinal barriers, including tight junctions, transporters, and enzymes, limit oral drug absorption.
• Advanced drug design methods like combinatorial chemistry and computer-aided drug design (CADD) often yield poorly soluble compounds.

Purpose of the Study:

• To critically review the barriers affecting oral drug bioavailability.
• To explore novel formulation strategies for enhancing drug bioavailability.
• To provide an overview of in vitro/in vivo assessment methods and regulatory aspects.

Main Methods:

• Literature review of drug solubility and bioavailability challenges.
• Analysis of novel drug delivery systems, including lipid-based nanocarriers, dendrimers, and carbon nanotubes.
• Examination of formulation techniques like nanosizing and complexation with polymers.

Main Results:

• Novel nanocarriers and advanced formulations can effectively enhance oral bioavailability.
• Understanding and overcoming intestinal barriers are crucial for drug absorption.
• Various formulation approaches show promise in improving drug solubility and delivery.

Conclusions:

• Nanotechnology-based drug delivery systems offer a promising solution to solubility and bioavailability issues.
• Targeted formulation strategies are essential for improving oral drug absorption.
• Further research and regulatory evaluation are needed for novel delivery systems.