Compositions and methods for topical diagnostic and therapeutic transport

摘要

Compositions and methods are provided that are useful for the delivery, including transdermal delivery, of biologically active agents, such as non-protein non-nucleotide therapeutics and protein-based therapeutics excluding insulin, botulinum toxins, antibody fragments, and VEGF. The compositions and methods are particularly useful for topical delivery of antifungal agents and antigenic agents suitable for immunization. Alternately, the compositions can be prepared with components useful for targeting the delivery of the compositions as well as imaging components.

主权项

1. A method of administering a biologically active protein to a subject in need thereof, the method comprising
topically applying to the skin or epithelium of the subject a composition comprising a biologically active protein and a positively charged carrier in an effective amount for transdermal delivery of the biologically active protein, wherein the positively charged carrier comprises a polypeptide having attached thereto positively charged efficiency groups comprising (i) amino acid sequences selected from the group consisting of -(gly)n1-(arg)n2 (SEQ ID NO. 1), wherein the subscript n1 is an integer of from 0 to about 20, and the subscript n2 is independently an odd integer of from about 5 to about 25; (gly)p-RGRDDRRQRRR-(gly)q (SEQ ID NO. 2), (gly)p-YGRKKRRQRRR-(gly)q (SEQ ID NO. 3), and (gly)p-RKKRRQRRR-(gly)q (SEQ ID NO. 4), wherein the subscripts p and q are each independently an integer of from 0 to 20; or (ii) Antennapedia protein transduction domain (PTD) peptide, wherein the biologically active protein excludes insulin, vascular endothelial growth factor (VEGF), and antibody fragments; wherein the composition does not comprise a negatively charged backbone; and wherein the positively charged carrier and the biologically active protein non-covalently and directly associate.