Percutaneous absorption of interferon-alpha by self-dissolving micropiles

Area of Science:

• Biomedical Engineering
• Pharmaceutical Sciences
• Drug Delivery Systems

Background:

• Interferon (IFN) is a crucial therapeutic protein with limited oral bioavailability.
• Developing effective delivery systems for IFN is essential for improving therapeutic outcomes.
• Self-dissolving micropiles (SDMPs) offer a promising approach for transdermal drug delivery.

Purpose of the Study:

• To evaluate the pharmaceutical utility of self-dissolving micropiles (SDMPs) loaded with interferon (IFN).
• To compare the efficacy of chondroitin sulfate-based and dextran-based SDMPs for IFN delivery.
• To assess the in vivo pharmacokinetic profile and bioavailability of IFN delivered via SDMPs.

Main Methods:

• Two types of IFN-loaded SDMPs were fabricated using chondroitin sulfate and dextran.
• Percutaneous administration of IFN-alpha2b SDMPs (5000 IU/kg) to rats.
• Serum IFN levels were monitored for 6 hours to determine pharmacokinetic parameters (Cmax, Tmax, AUC).
• In vitro drug release studies and assessment of SDMP stability and skin compatibility were performed.

Main Results:

• Chondroitin sulfate SDMPs achieved a higher Cmax (8.2 IU/ml) and faster Tmax (1.2 h) compared to dextran SDMPs (Cmax: 3.1 IU/ml, Tmax: 3.3 h).
• The bioavailability of IFN from chondroitin sulfate SDMPs was significantly higher (378.3%) than from dextran SDMPs (255.9%) and subcutaneous injection (320.9%).
• Chondroitin sulfate SDMPs exhibited a faster in vitro IFN release rate and demonstrated good stability and no skin irritation over 3 months.

Conclusions:

• Chondroitin sulfate-based SDMPs are a superior delivery system for interferon, enhancing its bioavailability and pharmacokinetic profile.
• These SDMPs offer a stable and safe alternative to conventional subcutaneous injection for IFN administration.
• The findings support the pharmaceutical potential of chondroitin sulfate SDMPs for transdermal delivery of therapeutic proteins like interferon.