Transdermal drug delivery using an osmolyte and vasoactive agent

摘要

A formulation and method for delivery of bioactive substances when applied to, or within, the skin or other exterior region of a mammal. for example, a patient, includes a vasoactive agent; an osmolyte; and an active ingredient. The formulation is sufficiently hygroscopic so as to create a condition of hypertonicity when absorbed by the skin. When the formulation is applied to the skin, the vasoactive agent can be delivered to the dermis so as to contact the vasculature of a patient.

主权项

1. A formulation for topical delivery of an active ingredient to a mammal, said mammal having a body surface and the body surface having a topical application site comprising skin, the formulation comprising:
a vasodilator, an osmolyte, and an active ingredient, wherein: a) the vasodilator is selected from the group consisting of arginine, methyl nicotinate, naftidrofuryl oxalate, papaverine, tolazoline, and combinations of the foregoing, b) the osmolyte is a sugar; c) the vasodilator and the osmolyte are present in amounts effective to work together in a synergistic manner to enable penetration of the active ingredient into or through the skin; d) the vasodilator, the osmolyte, and the active ingredient are non-identical; and e) the formulation has an osmolarity that is greater than 350 milliOsmol/L.