Compositions and Methods for Topical and Diagnostic and Therapeutic Transport

Abstract

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. Alternatively, the composition can be prepared with components useful for targeting the delivery of the compositions as well as imaging components.

1 . A composition comprising
 a non-protein, non-nucleotide biologically active agent; and   a positively charged carrier, the carrier comprising a polypeptide or a polyalkyleneimine backbone having attached thereto one or more positively charged branching groups selected from the group consisting of:
 (gly) n1 -(arg) n2  (SEQ ID NO. 1), 
 (gly) p -RGRDDRRQRRR-(gly) q  (SEQ ID NO. 2), 
 (gly) p -YGRKKRRQRRR-(gly) q  (SEQ ID NO. 3), 
 (gly) p -RKKRRQRRR-(gly) q  (SEQ ID NO. 4), and 
 Antennapedia protein transduction domain (PTD) peptide; 
   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; and the subscripts p and q are each independently an integer of from 0 to 20, and   wherein the association between the carrier and the biologically active agent is direct and non-covalent and without a negatively charged backbone.   
     
     
         2 . (canceled) 
     
     
         3 . The composition according to  claim 1 , wherein the biologically active agent has a therapeutic activity. 
     
     
         4 - 7 . (canceled) 
     
     
         8 . The composition according to  claim 1 , wherein the composition is a controlled release composition. 
     
     
         9 . The composition according to  claim 3 , wherein the composition is a controlled release composition. 
     
     
         10 . The composition according to  claim 1 , wherein the biologically active agent is an antifungal agent. 
     
     
         11 . The composition according to  claim 1 , wherein the biologically active agent is an agent for treating or preventing symptoms of psoriasis. 
     
     
         12 - 13 . (canceled) 
     
     
         14 . The composition according to  claim 10 , wherein the composition is a controlled release composition. 
     
     
         15 . The composition according to  claim 10 , wherein the antifungal agent is selective from amphotericin B, fluconazole, flucytosine, itraconazole, ketoconazole, clotrimazole, econozole, griseofulvin, miconazole, nystatin, and ciclopirox. 
     
     
         16 - 17 . (canceled)