Skin Permeating and Cell Entering (SPACE) Peptides and Methods of Use Thereof

Abstract

The present disclosure provides peptides and peptide compositions, which facilitate the delivery of an active agent or an active agent carrier wherein the compositions are capable of penetrating the stratum corneum (SC) and/or the cellular membranes of viable cells.

1 .- 138 . (canceled) 
     
     
         139 . A composition comprising a peptide comprising the amino acid sequence HSALTKH (SEQ ID NO:2), KTGSHNQ (SEQ ID NO:3), MGPSSML (SEQ ID NO:4), TDPNQLQ (SEQ ID NO:5), STHFIDT (SEQ ID NO:6); the amino acid sequence of SEQ ID NO:2, SEQ ID NO:3, SEQ ID NO:4, SEQ ID NO:5, or SEQ ID NO:6, wherein one or more of the amino acids of SEQ ID NO:2, SEQ ID NO:3, SEQ ID NO:4, SEQ ID NO:5, or SEQ ID NO:6, respectively, is replaced with a conservative amino acid substitution; or the amino acid sequence of ACTGSTQHQCG (SEQ ID NO:13), wherein one or more of the amino acids of SEQ ID NO:13 is replaced with a conservative amino acid substitution, wherein the peptide is associated with or conjugated to an active agent or an active agent carrier comprising the active agent, and wherein the composition is capable of penetrating a stratum corneum (SC) layer when contacted therewith or penetrating a cell when contacted therewith. 
     
     
         140 . The composition of  claim 139 , wherein the peptide is associated with an active agent or an active agent carrier comprising the active agent, and wherein the association results from hydrophobic, electrostatic or van der Walls interactions. 
     
     
         141 . The composition of  claim 139 , wherein the peptide is a cyclic peptide comprising a Cys-Cys disulfide bond. 
     
     
         142 . The composition of  claim 139 , wherein the composition is capable of penetrating the cellular membrane of viable non-human animal cells or of penetrating the cellular membrane of viable human cells. 
     
     
         143 . The composition of  claim 139 , wherein the composition is capable of penetrating the cellular membrane of viable epidermal or dermal cells. 
     
     
         144 . The composition of  claim 139 , wherein the active agent comprises a macromolecule. 
     
     
         145 . The composition of  claim 144 , wherein the macromolecule comprises a protein. 
     
     
         146 . The composition of  claim 145 , wherein the protein comprises an antibody or a fragment thereof comprising at least one paratope. 
     
     
         147 . The composition of  claim 144 , wherein the macromolecule comprises a nucleic acid. 
     
     
         148 . The composition of  claim 147 , wherein the nucleic acid is RNA and the RNA is interfering RNA. 
     
     
         149 . The composition of  claim 148 , wherein the interfering RNA is shRNA, miRNA or siRNA. 
     
     
         150 . The composition of  claim 149 , wherein the interfering RNA is siRNA, and the siRNA is a mutation-specific siRNA. 
     
     
         151 . The composition of  claim 139 , wherein the active agent is a pharmaceutical compound. 
     
     
         152 . The composition of  claim 139 , wherein the active agent comprises a detectable agent. 
     
     
         153 . The composition of  claim 139 , wherein the active agent is a nanoparticle. 
     
     
         154 . The composition of  claim 139 , wherein the active agent is a low molecular weight compound. 
     
     
         155 . The composition of  claim 139 , wherein the peptide is conjugated to an active agent carrier comprising the active agent. 
     
     
         156 . The composition of  claim 155 , wherein the active agent carrier is a liposome, a nanoparticle, or a polymeric micelle. 
     
     
         157 . The composition of  claim 139 , wherein the peptide is from 6 to 30 amino acids in length. 
     
     
         158 . The composition of  claim 157 , wherein the peptide is from 6 to 20 amino acids in length.