Abstract
(1) Background: Nanomedicine has recently emerged as a new area of research, particularly to fight cancer. In this field, we were interested in the vectorization of pepstatin A, a peptide which does not cross cell membranes, but which is a potent inhibitor of cathepsin D, an aspartic protease particularly overexpressed in breast cancer. (2) Methods: We studied two kinds of nanoparticles. For pepstatin A delivery, mesoporous silica nanoparticles with large pores (LPMSNs) and hollow organosilica nanoparticles (HOSNPs) obtained through the sol–gel procedure were used. The nanoparticles were loaded with pepstatin A, and then the nanoparticles were incubated with cancer cells. (3) Results: LPMSNs were monodisperse with 100 nm diameter. HOSNPs were more polydisperse with diameters below 100 nm. Good loading capacities were obtained for both types of nanoparticles. The nanoparticles were endocytosed in cancer cells, and HOSNPs led to the best results for cancer cell killing. (4) Conclusions: Mesoporous silica-based nanoparticles with large pores or cavities are promising for nanomedicine applications with peptides.
Highlights
Mesoporous silica nanoparticles (MSNs) hold great promise for biological applications, in the field of theranostics and drug delivery, and the field has been extensively reviewed [1,2,3,4,5,6,7,8,9,10,11,12,13,14,15]
We present the syntheses of Large-pore mesoporous silica nanoparticles (LPMSNs) functionalized with fluorescein isothiocyanate (FITC)
This latest high variation of zeta potential suggests that pepstatin was mainly adsorbed onto the LPMSNs decreased from −19.5 mV to −22.6 mV, whereas the zeta potential of hollow organosilica nanoparticles (HOSNPs) decreased from +32 mV to −13.2 mV
Summary
Mesoporous silica nanoparticles (MSNs) hold great promise for biological applications, in the field of theranostics and drug delivery, and the field has been extensively reviewed [1,2,3,4,5,6,7,8,9,10,11,12,13,14,15] These nanoparticles (NPs) exhibit adjustable diameters (10 to 200 nm) and pore size (2–15 nm), leading to wide ranges of encapsulated drugs and biomolecules. The whose adsorption and release can be monitored by UV-visible spectroscopy, unlike pepstatin The endocytosis of these NPs was monitored in MCF-7 breast cancer cells, and delivery of pepstatin A was successfully successfully demonstrated demonstrated in in MCF-7.
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