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Updated: Dec 27, 2025
Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles
Published on: August 28, 2015
Creation of an assessment system for measuring the bitterness of azithromycin-containing reverse micelles
Ri Huang1,2, Yadan Zhang1, Tao Wang1
1Institute of Pharmacology and Toxicology, Academy of Military Medical Sciences, Taiping Road No.27, Beijing 100850, China.
Abstract:
We aimed to develop a novel method for assessing the bitterness of azithromycin-containing reverse micelles (AM-containing RMs). Azithromycin-containing reverse micelles were prepared by processing Lipoid E80 and medium chain triglycerides via a freeze-drying method. The bitterness threshold of azithromycin was determined by human taste test, and an equation was derived to correlate the azithromycin concentrations and bitterness scores of standard solutions. Simulated salivary fluids and sampling times were fixed based on the drug release profile of AM-containing RMs, with Zithromax® (a commercial formulation of azithromycin) used as the control. The drug release concentrations from stimulated salivary fluids were then used to assess the bitterness of AM-containing RMs and Zithromax®. Afterward, the oral bioavailability of both formulations was evaluated by in vivo experiments in male Wistar rats. The results showed that the bitterness threshold of azithromycin standard solutions was between 25.3 µg/ml and 30.4 µg/ml. Thereafter, we calculated that the bitterness scores and the drug release concentrations of the azithromycin-containing reverse micelle formulation were similar to those of Zithromax® at each time point after 10 min of dispersal in simulated salivary fluid. In addition, the AUC0 - after oral administration of AM-containing RMs was 1.75-fold (P < 0.05) higher than that of Zithromax®. In conclusions, a system for assessing bitterness was developed using an in vitro drug release evaluation method and a human taste test panel. We found that the bitterness of azithromycin was successfully masked by reverse micelles, which also improved the oral bioavailability of azithromycin compared to that of Zithromax®.
Insights
A new method successfully masked azithromycin bitterness using reverse micelles (AM-containing RMs). This formulation also enhanced oral bioavailability compared to Zithromax®, showing improved drug delivery potential.
Area of Science:
- Pharmaceutical Technology
- Drug Delivery Systems
- Formulation Science
Background:
- Azithromycin is known for its bitter taste, which can negatively impact patient compliance.
- Developing palatable formulations is crucial for improving therapeutic outcomes.
Purpose of the Study:
- To develop a novel method for assessing the bitterness of azithromycin-containing reverse micelles (AM-containing RMs).
- To evaluate the bitterness masking and oral bioavailability of AM-containing RMs compared to a commercial azithromycin formulation.
Main Methods:
- Azithromycin-containing reverse micelles were prepared using freeze-drying.
- Bitterness threshold was determined via human taste tests and correlated with drug concentration.
- An in vitro drug release method using simulated salivary fluid was employed.
- Oral bioavailability was assessed in vivo using male Wistar rats.
Main Results:
- The bitterness threshold for azithromycin was established between 25.3–30.4 µg/ml.
- AM-containing RMs showed similar bitterness scores to Zithromax® after 10 minutes in simulated salivary fluid.
- Oral administration of AM-containing RMs resulted in a 1.75-fold higher AUC0-∞ compared to Zithromax®.
Conclusions:
- A reliable in vitro system for bitterness assessment was developed.
- Reverse micelles effectively masked the bitterness of azithromycin.
- The developed AM-containing RMs demonstrated enhanced oral bioavailability over the conventional formulation.
