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Bioavailability Enhancement: Drug Permeability Enhancement

Bioavailability Enhancement: Drug Permeability Enhancement

After oral administration, poor permeability often limits the rate at which drugs are absorbed through the intestinal epithelium. Enhancing drug permeability is crucial for effective therapy, and several strategies have been developed to overcome this challenge.One effective strategy involves the use of lipid-based formulations. These formulations enhance dissolution and solubility, targeting physiological mechanisms to increase drug absorption. This includes stimulating bile salt secretion,...

Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry

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Orally administered drugs primarily enter the systemic circulation via passive diffusion through the intestinal membranes. The drug's absorption is influenced by drug stability in the gastrointestinal GI tract, membrane permeability, the surface area available for absorption, luminal drug concentration, and residence time in the lumen. Drug permeability can be enhanced by adjusting the lipophilicity, polarity, or molecular size of the drug, promoting its passive transport across intestinal...

Bioavailability Enhancement: Drug Solubility Enhancement

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Factors Influencing Drug Absorption: Drug Dissolution

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The pharmacokinetic journey of drugs from solid oral dosage forms into systemic circulation is multifaceted. It begins with disintegration, a prerequisite ensuring a solid dosage form's subdivision into minute particles. Dissolution occurs next as these granulated entities solubilize in gastrointestinal fluids. This solubilization is crucial for the succeeding stage, permeation, which describes the traversal of the drug across the intestinal membrane and its subsequent entry into the blood...

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Related Experiment Video

Updated: May 9, 2026

Self-Nanoemulsification of Healthy Oils to Enhance the Solubility of Lipophilic Drugs

Self-Nanoemulsification of Healthy Oils to Enhance the Solubility of Lipophilic Drugs

Published on: July 27, 2022

Oral delivery of lipophilic drugs: the tradeoff between solubility increase and permeability decrease when using

Avital Beig¹, Riad Agbaria, Arik Dahan

¹Department of Clinical Pharmacology, School of Pharmacy, Faculty of Health Sciences, Ben-Gurion University of the Negev, Beer-Sheva, Israel.

|July 23, 2013

Summary

Oral cyclodextrin formulations significantly enhance lipophilic drug solubility but decrease intestinal permeability. This study presents a model to balance this solubility-permeability tradeoff for optimal drug absorption.

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Area of Science:

Pharmaceutical Sciences
Drug Delivery Systems
Physical Chemistry

Background:

Lipophilic drugs often exhibit poor aqueous solubility, limiting their oral bioavailability.
Cyclodextrins are widely used excipients to improve drug solubility and dissolution.
Understanding the impact of cyclodextrins on drug permeability is crucial for formulation development.

Purpose of the Study:

To investigate the effect of hydroxypropyl-β-cyclodextrin (HPβCD) on the solubility and intestinal permeability of lipophilic drugs.
To evaluate the role of the unstirred water layer (UWL) in drug absorption.
To develop a mass-transport model for predicting the solubility-permeability interplay.

Main Methods:

Solubility and permeability of dexamethasone were measured with varying HPβCD concentrations.
In vivo (rat intestinal perfusion) and in vitro (Caco-2 cells, PAMPA) models were employed.
A simplified mass-transport analysis was developed and validated.

Main Results:

HPβCD significantly increased dexamethasone apparent solubility (K1:1 = 2311 M⁻¹).
Drug permeability was markedly reduced across all experimental models upon HPβCD complexation.
The UWL did not influence dexamethasone absorption.
The developed mass-transport model accurately predicted dexamethasone permeability as a function of HPβCD concentration.

Conclusions:

A critical tradeoff exists between enhanced solubility and reduced permeability when using cyclodextrins for lipophilic drugs.
This solubility-permeability tradeoff is independent of the unstirred water layer.
The presented transport model aids in optimizing the balance between solubility and permeability for improved oral absorption.