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Binding of prednisolone and its ester prodrugs in the skin
1Department of Biochemical Science and Engineering, College of Computer Science and Biosystems Engineering, Kyushu Institute of Technology, Fukuoka, Japan.
Purpose:
Skin binding of prednisolone and its esters was investigated in the hairless mouse skin in vitro.
Methods:
The distribution of the amount of drugs bound in the skin was determined by a skin slicing technique. The model drugs used were prednisolone (PN, M.W. 360) and its esters, senesyonate (PN-C5, M.W. 442), geranate (PN-C10, M.W. 510), farnesylate (PN-C15, M.W. 578), and geranylgeranate (PN-C20, M.W. 646).
Results:
The distribution of bound drug was nonhomogeneous in the skin; the concentration of PN-C10 and PN-C15 in the skin increased gradually with the distance from the skin surface. The parent drug, PN, however, was hardly bound in the viable skin.
Conclusions:
These findings suggest that the prodrugs of prednisolone may prolong the dermal retention of the parent drug and minimize to delivery into the systemic circulation of the prodrug and metabolite.