Systemic exposure to immunomodulators after intravenous or subcutaneous administration carries an intrinsic risk related to impaired host defense against infection

Unlike mAb therapeutics, aptamer therapeutics can be formulated for topical administration and very limited systemic exposure

Published precedent demonstrates that dermatologic formulations of oligonucleotides penetrate stratum corneum to reach epidermis and dermis in intact normal human skin at pharmacologically relevant concentrations

  • Topical application of IL-23 inhibitor aptamer cream (Lenn et al. 2018)

  • Topical application of ICAM-1 antisense oliogonucleotide cream (Mehta et al. 2000)

Cy3-labeled aptamer (orange) into intact human abdominal skin after 0 (wash control), 6, and 24 hours post dosing.

Uptake of IL-23 aptamer into skin keratinocytes (dashed lines indicating the epidermal junction)

Lenn DJ et al Journal of Investigative Dermatology (2018) 138, 282e290; doi:10.1016/j.jid.2017.07.851


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