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Recent advances in improving oral drug bioavailability by cocrystals
Shahram Emami1,2, Mohammadreza Siahi-Shadbad3, Khosro Adibkia4
1Drug Applied Research Center and Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran.
Bioimpacts : BI
|November 7, 2018
Summary
Cocrystallization enhances oral drug bioavailability by improving solubility and permeability. This review covers supersaturation, membrane permeability, pharmacokinetic interactions, and the integration of nanocrystal technology for better drug absorption.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery
- Materials Science
Background:
- Oral drug delivery is preferred but limited by poor bioavailability.
- Low drug solubility and permeability hinder clinical efficacy.
- Cocrystallization offers a strategy to enhance oral absorption.
Purpose of the Study:
- To review recent advances in improving oral absorption via cocrystallization.
- To discuss supersaturation, membrane permeability, and pharmacokinetic interactions of cocrystals.
- To explore the integration of nanocrystal technology with cocrystal design.
Main Methods:
- Review of recent literature on cocrystallization for oral drug delivery.
- Analysis of factors influencing cocrystal oral absorption: supersaturation, permeability, PK interactions.
- Discussion on in vivo-in vitro correlations and nanocrystal-cocrystal integration.
Main Results:
- Cocrystals can improve drug solubility and permeability, enhancing oral absorption.
- Supersaturation and precipitation kinetics are critical for cocrystal bioavailability.
- Potential drug-coformer interactions and toxicity concerns require careful evaluation.
- Nanosized cocrystals show promise for poorly soluble drugs.
Conclusions:
- Cocrystallization is a viable strategy for improving oral bioavailability, with marketed products available.
- Consideration of supersaturation, precipitation, and PK interactions is essential for cocrystal development.
- Further research is needed to address safety, in vivo prediction, and the full potential of cocrystals in humans.
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