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Updated: Jul 2, 2026

Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles
Published on: August 28, 2015
Evaluation and optimization of preparative variables for controlled-release floatable microspheres prepared by poor
Yasunori Miyazaki1, Shigeru Yakou, Fumiki Yanagawa
1Department of Pharmacy, Tokyo Women's Medical University Medical Center East, Nishiogu, Arakawa-ku, Tokyo, Japan. myph@dnh.twmu.ac.jp
Researchers optimized floatable theophylline microspheres for drug delivery. The study identified ideal parameters for maximizing buoyancy and controlling drug release, enhancing therapeutic potential.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
Background:
- Floatable microspheres offer advantages in drug delivery, improving patient compliance and therapeutic efficacy.
- Theophylline is a widely used bronchodilator requiring optimized delivery systems for sustained action.
Purpose of the Study:
- To optimize preparative parameters for floatable theophylline microspheres using the emulsion-solvent evaporation method.
- To achieve simultaneous optimization for maximum buoyancy and controlled drug release profiles.
Main Methods:
- Utilized a three-factor, three-level Box-Behnken design to investigate independent variables: poor solvent volume, temperature-increase rate, and drug loading.
- Employed a partitioned artificial neural network for simultaneous optimization of dependent variables: percentage floating at 3 hours and time for 50% drug release.
Main Results:
- Identified optimal preparative parameters: 27.6% drug loading, 0.29°C/min temperature-increase rate, and 1.7 mL poor solvent.
- These parameters were found to maximize microsphere buoyancy and sustain theophylline release.
Conclusions:
- The emulsion-solvent evaporation method, optimized via Box-Behnken design and artificial neural networks, is effective for producing floatable theophylline microspheres.
- The identified optimal conditions provide a robust formulation for enhanced theophylline delivery with improved buoyancy and controlled release characteristics.
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