ENCAPSULATION OF ANTENNAPEDIA (PENETRATIN) PEPTIDE IN A POLYMERIC PLATFORM FOR EFFECTIVE TREATMENT OF INTRACELLULAR BACTERIA

Document Type : Original Article

Authors

1 Department of Industrial and Physical Pharmacy, Purdue University, 575 Stadium Mall Drive, West Lafayette, IN 47907, USA /Department of Industrial Pharmacy, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt

2 Department of Industrial Pharmacy, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt

3 Department of Industrial and Physical Pharmacy, Purdue University, 575 Stadium Mall Drive, West Lafayette, IN 47907, USA / Weldon School of Biomedical Engineering, Purdue University, West Lafayette, IN 47907, USA

Abstract

Antimicrobial peptides (AMP) and cell-penetrating peptides (CPP) are two classes of peptides that share some structural and physicochemical similarities. Antennapedia or penetratin (ANT) is one of the most known CPPs, that was proven to have antimicrobial activity against certain strains of planktonic bacteria. ANT can enter the cells but has no activity against intracellular bacteria. This is attributable to the inability of the peptide to reach bacteria reside within cellular components as well as low delivery efficiency, due to loss of activity by proteolysis and poor specificity. The aim of this work is to develop a formulation that can effectively reach and attack intracellular bacteria. To achieve this goal, ANT was encapsulated in PLGA platform as nanoparticles with the size range of 500-1000 nm, which allows for selective uptake by macrophages where bacteria mostly reside. ANT was loaded with high loading efficiency (12.7%) inspite of high water solubility. ANT-nanoparticles (ANT-NP) had no cytotoxicity on J774a.1 macrophages and were readily taken up by macrophages as confirmed by fluorescence microscopy. Antibacterial activity of ANT-NP remains to be tested against different intracellular bacteria.