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Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles
Published on: August 28, 2015
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Silymarin loaded floating polymer(s) microspheres: characterization, in-vitro/in-vivo evaluation
Afaf A Ramadan1,2, Asmaa M Elbakry1,3, Hatem A Sarhan4
1Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy (Girls), Al-Azhar University, Cairo, Egypt.
Pharmaceutical Development and Technology
|July 14, 2020
Summary
Encapsulated floating microspheres were developed to improve silymarin delivery. These novel microspheres demonstrated enhanced bioavailability and prolonged release, offering a promising approach for effective liver disease management.
Area of Science:
- Pharmacology
- Materials Science
- Drug Delivery
Background:
- Silymarin exhibits a short half-life and intestinal degradation, necessitating frequent administration.
- Conventional silymarin formulations face challenges in achieving sustained therapeutic levels.
- Developing advanced drug delivery systems is crucial for optimizing silymarin's efficacy.
Purpose of the Study:
- To formulate and characterize silymarin-loaded floating microspheres using HPMC, EC, and their blends.
- To evaluate the in vitro and in vivo performance of the developed microspheres.
- To assess the potential of these microspheres for improved liver disease management.
Main Methods:
- Emulsion solvent evaporation technique was employed for microsphere preparation.
- Formulations were optimized based on drug:polymer ratio and emulsifier concentration.
- Characterization included SEM, drug entrapment efficiency, buoyancy, in vitro release, kinetics, stability, and in vivo bioequivalence studies.
Main Results:
- Formula F24 demonstrated high buoyancy (73.4%) and prolonged drug release (t90 = 190.7 days).
- In vivo studies showed a significantly higher Cmax (1021.3 ng/ml) and Tmax (6 h) for F24 compared to conventional silymarin.
- F24 exhibited a mean residence time (MRT) of 9.44 ± 0.03 hr and a relative bioavailability of 227%.
Conclusions:
- The developed silymarin-loaded floating microspheres offer a promising strategy for overcoming the limitations of conventional silymarin.
- These microspheres significantly enhance silymarin's bioavailability and provide sustained release, indicating potential for effective liver disease management.
- Further clinical investigations are warranted to confirm the therapeutic benefits in patients.
