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Recent Advances in Oral Drug Delivery Systems for BCS III Drugs
Junpeng Yu1, Peng Wang1, Zishen Bei1
1Institute of Traditional Chinese Medicine Zhuang-Yao Medicine Research, Guangxi University of Chinese Medicine, Nanning 530200, China.
Current Issues in Molecular Biology
|January 30, 2026
Summary
Biopharmaceutics Classification System (BCS) Class III drugs have poor oral absorption due to low intestinal permeability. This review analyzes strategies to enhance oral bioavailability, highlighting the need for mechanism-guided selection for effective drug delivery systems.
Area of Science:
- Pharmacology
- Drug Delivery
- Biopharmaceutics
Background:
- Biopharmaceutics Classification System (BCS) Class III drugs exhibit high solubility but low intestinal permeability.
- This characteristic limits oral bioavailability, independent of dissolution rates, due to intestinal absorption barriers and inter-individual variability.
Purpose of the Study:
- To critically evaluate strategies for enhancing oral bioavailability of BCS Class III drugs.
- To analyze key determinants of oral absorption using the intestinal permeability barrier as a framework.
Main Methods:
- Literature review focusing on the intestinal permeability barrier.
- Comparative analysis of bioavailability enhancement strategies based on mechanism, efficacy, conditions, and feasibility.
Main Results:
- Identified intrinsic limitations and boundaries of various bioavailability enhancement strategies.
- Demonstrated that no single strategy universally overcomes absorption barriers for BCS Class III drugs.
Conclusions:
- Mechanism-guided selection of strategies is crucial for rational design of oral drug delivery systems.
- A foundational basis is provided for developing tailored oral delivery systems for BCS Class III drugs.
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