Development of hot-melt pressure-sensitive adhesives for transdermal drug delivery

摘要

Styrene-isoprene-styrene (SIS) copolymer was epoxidized by in situ epoxidation to prepare a series of epoxidized SIS resins (ESIS). Their epoxidation degrees, phase structures, and compatibility with hydrocarbon resin were characterized with *H nuclear magnetic resonance spectroscopy, atomic force microscopy, and differential scanning calorimetry, respectively. These ESIS resins were melt-mixed with synthetic hydrocarbon resin, mineral oil, and antioxidants to fabricate a series of ESIS-based hot-melt pressure-sensitive adhesives (HMPSAs), which were used as carriers of transdermal drug delivery system. Their adhesive performances were measured, including holding power and 180° peel strength. Geniposide and oleanic acid were representatively chosen as hydrophilic and lipophilic drug, respectively. Their in vitro release behaviors in ESIS-based HMPSAs were investigated using a modified Franz-type horizontal diffusion cells. Although the introduction of epoxide groups could alter the compatibility and phase structures between SIS resins and additives, the adhesive performances were slightly affected, as SIS resins had lower epoxidation degree (<15%). It is even more important that the cumulative release rate of both hydrophilic and lipophilic drugs is markedly enhanced with the increase of epoxidation degree in these ESIS-based HMPSAs. Therefore, this kind of HMPSAs has a promising future as a carrier of transdermal drug delivery system as their SIS resins are appropriately epoxidized.