Abstract：
:Indolicidin (IL) is an antimicrobial peptide (AMP), which has been utilized as a cell penetrating peptide (CPP) for drug delivery. However, the hemolysis restricts its clinical application. Therefore, we investigated the delivery efficiency and hemocompatibility of IL and its derivatives. The transportation of fluorophore to NIH/3T3 cells could be improved either by in accompany with these peptides or in the form of peptide-conjugates. The hydrophobicity scales of these peptides were calculated according to their residues, which were compared to their effects on hemolysis as well as cell uptake efficiency. The results suggested that the cell penetrability of IL and its derivatives was related to their hydrophobicity scales based on the octanol-interface scale (ΔGoct-if), whereas their hemolysis levels depended on the hydrophobicity scales based on interface (ΔGwif). Consequently, we designed two peptides, IL-R57F89 and SAP10, to validate the correlation. These two peptides had similar ΔGwif; however, the ΔGoct-if of SAP10 was much higher than that of IL-K7F89. Both IL-R57F89 and SAP10 demonstrated extremely low hemolysis. Compared to the limit cell uptake of SAP10, IL-R57F89 greatly promoted the delivery efficiency. These results were consistent to our prediction, suggesting that hydrophobicity scales should be a useful preliminary guidance for AMP-derived CPP design.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Tsai CW,Hu WW,Liu CI,Ruaan RC,Tsai BC,Jin SL,Chang Y,Chen WYdoi
10.1016/j.ijpharm.2015.08.037subject
Has Abstractpub_date
2015-10-15 00:00:00pages
498-505issue
1eissn
0378-5173issn
1873-3476pii
S0378-5173(15)30134-4journal_volume
494pub_type
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