Drugs with poor oral bioavailability usually are administered by hypodermic injection, which causes pain, poor patient compliance, the need for trained personnel, and risk of infectious disease transmission. Transdermal (TD) delivery provides an excellent alternative, but the barrier of skin’s outer stratum corneum (SC) prevents delivery of most drugs. Micrometer-scale microneedles (MNs) have been used to pierce animal and human cadaver skin and thereby enable TD delivery of small molecules, proteins, DNA, and vaccines for systemic action. Here, we present a clinical study of MN-enhanced delivery of a medication to humans. Naltrexone (NTX) is a potent mu-opioid receptor antagonist used to treat opiate and alcohol dependence. This hydrophilic and skin-impermeant molecule was delivered from a TD patch to healthy human subjects with and without pretreatment of the skin with MNs. Whereas delivery from a standard NTX TD patch over a 72-h period yielded undetectable drug plasma levels, pret
|Journal||Proc Natl Acad Sci U S A|
|State||Published - 2008|
Wermeling, D. P., Banks, S. L., Hudson, D. A., Gill, H., Gupta, J., Prausnitz, M. R., & Stinchcomb, A. L. (2008). Microneedles permit transdermal delivery of a skin-impermeant medication to humans. Proc Natl Acad Sci U S A, 2058-63.