High drug-loading and controlled-release hydroxyphenyl-polyacrylate adhesive for transdermal patch

Area of Science:

• Polymer chemistry
• Materials science
• Drug delivery systems

Background:

• Long-acting transdermal drug delivery systems (TDDS) require high drug-loading and controlled release.
• Improving drug-polymer miscibility is crucial for effective TDDS.

Purpose of the Study:

• To develop a novel pressure-sensitive adhesive (HP-PSA) for enhanced drug-loading and controlled release in TDDS.
• To investigate the mechanism of a doubly ionic H-bond interaction between drugs and HP-PSA.

Main Methods:

• Synthesis of hydroxyphenyl-modified pressure-sensitive adhesive (HP-PSA).
• Evaluation of drug-loading and release profiles using eight model drugs (R3N, R2NH, and no N types).
• Pharmacokinetic studies and assessment of safety and mechanical properties.

Main Results:

• HP-PSA demonstrated 1.5 to 7 times higher drug-loading compared to controls.
• Drug release rate was controlled to 1/5-1/2, with sustained plasma drug concentrations and no burst release.
• Pharmacokinetics showed over 2x AUC and 6x MRT, indicating long-acting potential.

Conclusions:

• The doubly ionic H-bond in HP-PSA significantly enhances drug-loading and controls drug release for TDDS.
• HP-PSA exhibits potential for developing safe and effective long-acting transdermal patches.
• The developed H-bond strategy offers inspiration for other drug delivery systems in non-polar environments.