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A novel pH-sensitive interferon-β (INF-β) oral delivery system for application in multiple sclerosis
Pierre P D Kondiah1, Lomas K Tomar, Charu Tyagi
1University of the Witwatersrand, Faculty of Health Sciences, Department of Pharmacy and Pharmacology, 7 York Road, Parktown, Johannesburg 2193, South Africa.
International Journal of Pharmaceutics
|September 6, 2013
Summary
pH-sensitive microparticles made from trimethyl-chitosan (TMC) and other polymers offer effective oral delivery of interferon-beta (INF-β). This novel formulation achieved higher plasma concentrations than subcutaneous injection.
Area of Science:
- Biomaterials Science
- Drug Delivery Systems
- Polymer Chemistry
Background:
- Oral delivery of protein therapeutics like interferon-beta (INF-β) is challenging due to degradation in the gastrointestinal tract.
- Trimethyl-chitosan (TMC) based microparticles offer potential for pH-sensitive drug release and enhanced mucoadhesion.
- Developing stable and effective oral formulations for biologics requires innovative material design and optimization.
Purpose of the Study:
- To develop and optimize pH-sensitive microparticles for oral delivery of interferon-beta (INF-β).
- To evaluate the efficacy of the optimized microparticulate system compared to subcutaneous injection in vivo.
- To investigate the potential of trimethyl-chitosan (TMC), poly(ethylene glycol)dimethacrylate (PEGDMA), and methacrylic acid (MAA) for oral protein delivery.
Main Methods:
- Free radical suspension polymerization was used to synthesize TMC-PEGDMA-MAA microparticles.
- A Box-Behnken experimental design optimized TMC concentration and crosslinker percentage.
- Characterization included morphological, porositometric, and mucoadhesive property assessments.
- In vitro release studies at different pH values and in vivo pharmacokinetic studies in rabbits were conducted.
Main Results:
- Optimized microparticles (0.5 g/100 mL TMC, 3% crosslinker) achieved 53.25% INF-β loading efficiency.
- In vitro studies showed significant INF-β release at intestinal pH (74%) but minimal release at gastric pH (3%).
- In vivo evaluation in rabbits demonstrated a sustained 24-hour release profile with higher INF-β plasma concentrations compared to subcutaneous injection.
Conclusions:
- The developed pH-sensitive microparticulate system based on TMC, PEGDMA, and MAA is a promising platform for oral interferon-beta delivery.
- The optimized formulation provides effective protection and controlled release of INF-β in the gastrointestinal tract.
- This approach offers a viable alternative to parenteral administration for protein therapeutics, enhancing patient compliance and therapeutic outcomes.
Keywords:
Box–Behnken experimental designCopolymeric microparticulate systemInsulinInterferon-β (INF-β)Oral delivery systempH-responsiveMore Related Videos
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