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Dermal absorption of mucopolysaccharide polysulfate (heparinoid) in human and minipig
Tadao Kumokawa1, Kazumasa Hirata, Keiichi Sato
1Research Laboratories, Kyoto R&D Center, Maruho Co. Ltd., Kyoto, Japan. kumokawa_bml@mii.maruho.co.jp
Abstract:
Dermal absorption of mucopolysaccharide polysulfate (MPS, the active ingredient of Hirudoid") in human and minipig was investigated by using 14C-labeled MPS. Three types of human and minipig skin samples were used: intact, dried and tape-stripped. At 24 h after application of 14C-MPS to intact human skin on a Franz cell in vitro, the radioactivity was detected in 0.98, 1.34, and 0.08% of the applied dose in stratum corneum, epidermal-dermal skin, and receptor fluid, respectively. In dried human skin, the amount of radioactivity detected was similar to that in intact human skin. By contrast, in tape-stripped human skin, higher radioactivity was detected in epidermal-dermal skin and receptor fluid (2.85 and 0.33% of the applied dose, respectively) than in intact or dried skin. Minipig skin showed 1.5 to 4.5 times greater dermal absorption of 14C-MPS, as compared with human skin. In an in vivo study with minipig, radioactivity was detected at the dosing skin site after dermal administration of 14C-MPS. The stability of 14C-MPS in human skin after dermal application was evaluated by agarose gel electrophoresis and ion-exchange chromatography. It was suggested that 14C-MPS absorbed into human skin would be stable because the chromatogram behaviors of the radioactivity on the two types of method were not shifted. Microautoradiography of human and minipig skins after 14C-MPS dosing showed that radioactivity was widely distributed in the epidermis in the area near hair follicles. The present results clearly demonstrate that MPS is stable and that a small fraction of it is percutaneously absorbed by human and minipig skin.
Insights
Mucopolysaccharide polysulfate (MPS) is stable and minimally absorbed through human and minipig skin. Tape-stripping increased MPS absorption, while minipig skin showed higher dermal absorption than human skin.
Area of Science:
- Pharmacokinetics
- Dermatology
- Drug Delivery
Background:
- Mucopolysaccharide polysulfate (MPS) is the active ingredient in Hirudoid.
- Understanding dermal absorption is crucial for topical drug efficacy.
Purpose of the Study:
- To investigate the dermal absorption and stability of mucopolysaccharide polysulfate (MPS) in human and minipig skin.
- To compare absorption rates across different skin conditions and species.
Main Methods:
- In vitro studies using Franz cells with 14C-labeled MPS on intact, dried, and tape-stripped human and minipig skin.
- In vivo study in minipigs to assess dermal absorption.
- Stability assessment using agarose gel electrophoresis and ion-exchange chromatography.
- Microautoradiography to visualize radioactivity distribution.
Main Results:
- Dermal absorption of MPS was low in intact and dried human skin (0.98-1.34% of applied dose).
- Tape-stripping significantly increased MPS absorption in human skin (up to 2.85% in epidermal-dermal layers).
- Minipig skin exhibited 1.5 to 4.5 times greater MPS dermal absorption compared to human skin.
- MPS demonstrated stability within human skin post-application.
- Radioactivity was primarily localized in the epidermis near hair follicles.
Conclusions:
- Mucopolysaccharide polysulfate (MPS) is stable and undergoes limited percutaneous absorption in both human and minipig skin.
- Skin integrity and species significantly influence MPS dermal penetration.
- The findings support the topical application of MPS, with potential for enhanced delivery under compromised skin conditions.
