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Generation of Alginate Microspheres for Biomedical Applications
Published on: August 12, 2012
Development of cloxacillin loaded multiple-unit alginate-based floating system by emulsion-gelation method
Jadupati Malakar1, Amit Kumar Nayak, Dilipkumar Pal
1Bengal College of Pharmaceutical Science and Research, Durgapur, West Bengal, India.
International Journal of Biological Macromolecules
|October 25, 2011
Summary
This study developed optimized alginate-based floating beads for gastroretentive delivery of cloxacillin. The novel system demonstrated sustained drug release and prolonged gastric residence time, enhancing therapeutic potential.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Materials Science
Background:
- Gastroretentive drug delivery systems aim to prolong drug residence time in the stomach, enhancing therapeutic efficacy.
- Alginate-based formulations offer biocompatibility and versatility for developing controlled-release systems.
- Cloxacillin, an antibiotic, requires optimized delivery to achieve effective concentrations at the site of action.
Purpose of the Study:
- To develop and optimize liquid paraffin-entrapped alginate beads for gastroretentive delivery of cloxacillin.
- To evaluate the physicochemical properties, drug entrapment efficiency, and in vitro drug release of the developed system.
- To investigate the floating characteristics and drug release kinetics for sustained cloxacillin delivery.
Main Methods:
- Utilized an emulsion-gelation method for preparing liquid paraffin-entrapped calcium alginate beads.
- Employed a 3(2) factorial design and response surface methodology for process optimization.
- Characterized the beads using SEM, FTIR, and evaluated drug entrapment, density, floating behavior, and in vitro drug release in simulated gastric fluid (pH 1.2).
Main Results:
- Optimized beads exhibited high drug entrapment efficiency (64.63±0.78%) and appropriate density (0.90±0.05 g/cm³).
- The system demonstrated excellent floating properties, with a lag time of 8.45 min and sustained flotation for over 12 hours.
- In vitro studies showed sustained cloxacillin release (56.72±0.85% in 8h) following the Korsmeyer-Peppas model with anomalous diffusion.
Conclusions:
- Liquid paraffin-entrapped alginate beads represent a promising gastroretentive drug delivery system for cloxacillin.
- The optimized formulation ensures prolonged drug release and extended gastric residence time, potentially improving therapeutic outcomes.
- The developed system offers a viable approach for enhancing the efficacy of antibiotics requiring sustained gastric presence.
