Decoration of Nanovesicles with pH (Low) Insertion Peptide (pHLIP) for Targeted Delivery

Abstract

Acidity at surface of cancer cells is a hallmark of tumor microenvironments, which does not depend on tumor perfusion, thus it may serve as a general biomarker for targeting tumor cells. We used the pH (low) insertion peptide (pHLIP) for decoration of liposomes and niosomes. pHLIP senses pH at the surface of cancer cells and inserts into the membrane of targeted cells, and brings nanomaterial to close proximity of cellular membrane. DMPC liposomes and Tween 20 or Span 20 niosomes with and without pHLIP in their coating were fully characterized in order to obtain fundamental understanding on nanocarrier features and facilitate the rational design of acidity sensitive nanovectors. The samples stability over time and in presence of serum was demonstrated. The size, ζ-potential, and morphology of nanovectors, as well as their ability to entrap a hydrophilic probe and modulate its release were investigated. pHLIP decorated vesicles could be useful to obtain a prolonged (modified) release of biological active substances for targeting tumors and other acidic diseased tissues.Electronic supplementary materialThe online version of this article (10.1186/s11671-018-2807-8) contains supplementary material, which is available to authorized users.

Hydrophilic Silver Nanoparticles Loaded into Niosomes: Physical–Chemical Characterization in View of Biological Applications

“…NioTw20/AgNPs and NioSp20/AgNPs, as well as empty niosomes, were diluted in fetal bovine or human serum to obtain a final serum concentration of 45% at 37 °C. The average size, polydispersity index, and ζ-potential were evaluated by means of DLS at different time points (15 min, 30 min, 60 min, and 180 min) [58].…”

“…Stability studies up to 90 days at different temperatures—room temperature (RT) and 4 °C—were carried out by DLS to asses the dimension and ζ-potential of empty niosomes and Nio-AgNPs [58].…”

“…The hydrophilic probe (calcein 10 −2 M) was added to the film during hydration, and the excess of calcein was purified by gel filtration chromatography, as already mentioned [58].…”

Mechanistic insights into the pH-dependent membrane peptide ATRAM

“…However, the total accumulation of nanoparticles to tumors often remains low 3 . To overcome this problem, peptides have been utilized to actively target the nanoparticles to tumor sites [4][5][6] . Not only do peptides improve the tumor targeting of nanoparticles, they also enhance stability 5,7 .…”

Current Trends in ATRA Delivery for Cancer Therapy

“…[83]. Liposomes are vesicular drug carriers composed by phospholipids, where both hydrophobic lipid chain and two hydrophilic head groups are structured to form a closed bilayer, surrounding an aqueous core [84]. This particular structure allows them to encapsulate both hydrophobic and hydrophilic drugs, protecting them from harsh bloodstream environment and enhance their targeting to the diseased tissues.…”