Proteolytic enzyme conjugated to SC-glucan as an enzymatic transdermal drug penetration enhancer.
The objective of this study was to investigate the effect of papain, a proteolytic enzyme, on the percutaneous absorption of drugs. To guarantee the enzyme stability during the skin penetration, papain was modified by the conjugation to SC-glucan. The enhancing activity of drug penetration was evaluated using antipyrine and indomethacin as hydrophilic and hydrophobic model drugs, respectively. The SC-glucan-papain conjugate was found to be very effective for facilitating the percutaneous absorption of antipyrine. Microscopic observations showed that the thickness of stratum corneum and viable epidermis was increased by the treatment of the SC-glucan-papain conjugate. Moreover, it induced phase separation, lacuna formation, and lamellar disruption within the stratum corneum interstices. These structural changes by the SC-glucan-papain conjugate are likely to be induced from hydrolysis of extensive crosslinking of corneocyte envelopes and intracellular proteins. However, the SC-glucan-papain conjugate showed no skin irritation according to the Draize test, which may be due to the difficulty of the SC-glucan-papain conjugate in penetrating into the skin.
Amore Pacific R&D Center, Yongin-si, Gyounggi-do, South Korea.
Y C
YC
Sim
Y S
YS
Nam
Y H
YH
Shin
E
E
Shin
S
S
Kim
I S
IS
Chang
J S
JS
Rhee
D000279:Administration, Cutaneous; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000493:pharmacokinetics; D000983:Antipyrine / Q000008:administration & dosage / Q000493:pharmacokinetics; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D004058:Diffusion; D005079:Excipients / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D005936:Glucans / Q000494:pharmacology* / Q000633:toxicity; D006168:Guinea Pigs; D007213:Indomethacin / Q000008:administration & dosage / Q000493:pharmacokinetics; D007509:Irritants / Q000633:toxicity; D008854:Microscopy, Electron; D010206:Papain / Q000494:pharmacology* / Q000633:toxicity; D011817:Rabbits; D051381:Rats; D012567:Schizophyllum / Q000737:chemistry*; D012867:Skin / Q000187:drug effects / Q000648:ultrastructure; D012869:Skin Absorption / Q000187:drug effects*; D013268:Stimulation, Chemical
D000894:Anti-Inflammatory Agents, Non-Steroidal; D005079:Excipients; D005936:Glucans; D007509:Irritants; D010206:Papain; D000983:Antipyrine; D007213:Indomethacin