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Bioavailability Enhancement: Drug Solubility Enhancement

Bioavailability Enhancement: Drug Solubility Enhancement

Bioavailability is a critical factor in determining a drug's effectiveness. It refers to the proportion of a drug that enters the circulation when introduced into the body and is, as a result, able to have an active effect. Enhancing bioavailability is essential for drugs with poor solubility, as it can significantly impact their therapeutic efficacy. Various methods are employed to increase the solubility of drugs, thereby enhancing their bioavailability.Micronization and nanonization are...

Bioavailability Enhancement: Drug Stability Enhancement and GI Retention

Bioavailability Enhancement: Drug Stability Enhancement and GI Retention

Improving a drug's stability in the gastrointestinal (GI) tract is paramount for enhancing its bioavailability and therapeutic effectiveness. Various strategies are employed to protect the drug from the harsh gastric milieu and to ensure its release and absorption at the desired site within the GI tract.Polymer coatings are one such method used to shield drugs from the stomach's acidic environment. By preventing premature drug release, these coatings improve the bioavailability of unstable...

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: Particle Size and Effective Surface Area

Factors Affecting Dissolution: Particle Size and Effective Surface Area

Dissolution kinetics, an essential aspect of oral drug delivery, is significantly influenced by the drug's particle size. According to the Noyes-Whitney dissolution model, the dissolution rate correlates directly with the drug's surface area. The larger the surface area, the higher the drug's solubility in water, leading to a faster drug dissolution rate. Reducing particle size increases the effective surface area, enhancing the dissolution process. Micronization and nanosizing are employed to...

Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry

Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry

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...

Modified-Release Drug Delivery Systems: Bioavailability

Modified-Release Drug Delivery Systems: Bioavailability

Modified-release (MR) dosage forms are designed to extend drug release over time, thereby maintaining stable plasma concentrations and reducing dosing frequency. However, their bioavailability is typically below 100% due to incomplete drug release and presystemic metabolism, and limitations in drug permeability across the gastrointestinal epithelium, all of which can restrict the fraction of the drug reaching systemic circulation. Consequently, studying the in vivo bioavailability of MR...

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Updated: Jun 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

Self-microemulsifying drug delivery system improves curcumin dissolution and bioavailability.

Xuemei Wu¹, Jianhua Xu, Xiuwang Huang

¹Institute of Clinical Pharmacology, Fujian Medical University, Fuzhou, PR China.

Drug Development and Industrial Pharmacy

|August 27, 2010

Summary

This summary is machine-generated.

This study developed a self-microemulsifying drug delivery system (SMEDDS) to enhance curcumin

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Solubility of Hydrophobic Compounds in Aqueous Solution Using Combinations of Self-assembling Peptide and Amino Acid

Solubility of Hydrophobic Compounds in Aqueous Solution Using Combinations of Self-assembling Peptide and Amino Acid

Published on: September 20, 2017

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Last Updated: Jun 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

Solubility of Hydrophobic Compounds in Aqueous Solution Using Combinations of Self-assembling Peptide and Amino Acid

Solubility of Hydrophobic Compounds in Aqueous Solution Using Combinations of Self-assembling Peptide and Amino Acid

Published on: September 20, 2017

Area of Science:

Pharmacology
Drug Delivery Systems
Nanotechnology

Background:

Curcumin exhibits broad biological activities but faces limitations in therapeutic use due to poor solubility and low bioavailability.
Self-microemulsifying drug delivery systems (SMEDDS) offer a promising approach to overcome these challenges.

Purpose of the Study:

To develop and evaluate an SMEDDS formulation for curcumin to improve its solubility, dissolution, and oral bioavailability.
To optimize the SMEDDS composition using phase diagrams and orthogonal design.

Main Methods:

Formulation of SMEDDS using various oils, surfactants, and cosurfactants.
Construction of pseudoternary phase diagrams to identify microemulsion regions.
Orthogonal design to optimize oil, surfactant, and cosurfactant concentrations.
Assessment of curcumin solubility, in vitro release, and in vivo oral bioavailability in mice.

Main Results:

An optimized SMEDDS formulation containing ethanol, Cremophor RH40®, and isopropyl myristate achieved a high curcumin concentration (50 mg/mL).
Complete curcumin release from SMEDDS was observed within 10 minutes.
The developed SMEDDS significantly enhanced oral bioavailability, with a relative bioavailability of 1213% compared to curcumin suspension.

Conclusions:

SMEDDS effectively enhances the in vitro dissolution and in vivo oral bioavailability of curcumin.
This formulation strategy holds potential for improving the therapeutic efficacy of curcumin.