Data di Pubblicazione:
2022
Citazione:
Polymersomes as selective drug delivery carriers for innovative anti-TB agents / G. Cazzaniga, M. Mori, F. Meneghetti, L.R. Chiarelli, G. Stelitano, I.L. Batalha, G. Battaglia, S. Villa. ((Intervento presentato al convegno Merck Young Chemists' Symposium : November, 21st - 23rd tenutosi a Rimini nel 2022.
Abstract:
Despite the global efforts to develop innovative therapeutic approaches, tuberculosis (TB) remains one
of the leading causes of mortality from a single infectious agent, surpassed in 2020 only by COVID-19.
We focused our attention on two protein targets known to be essential for the survival of Mycobacterium
tuberculosis (Mtb) during the infection: salicylate synthase I (MbtI), an enzyme that catalyses the first
step in the biosynthesis of the iron-chelating siderophores, and Low-Molecular-Weight Phosphatase B
(MptpB), which interferes with the host immune response.
We have previously developed effective MbtI and MptpB inhibitors [1,2]. Now, we have encapsulated
these potential drugs in poly(2-(methacryloyloxy)ethyl phosphorylcholine)–poly(2-
(diisopropylamino)ethyl methacrylate) (PMPC-PDPA) polymersomes (POs). These carriers allowed us
to (i) solubilise the hydrophobic drugs, (ii) target infected phagocytes via phenotypic association to
scavenger receptors class B, (iii) efficiently deliver the cargo within the cell cytosol where most bacilli
harbour, and (iv) effectively kill intracellular pathogens
selectively. POs combine the advantages of long-term
stability with the potential to encapsulate a broad range of
compounds. The POs were fully characterised by Dynamic
Light Scattering (DLS), High-Pressure Liquid
Chromatography (HPLC), and Transmission electron
microscopy (TEM); their cytotoxicity was assessed against
a macrophage cell line (THP-1) and Primary Human Lung
Fibroblasts (HLF). Future work includes evaluating the
antimycobacterial activity of the drug-containing POs in Mtb infected primary cells [3].
Tipologia IRIS:
14 - Intervento a convegno non pubblicato
Elenco autori:
G. Cazzaniga, M. Mori, F. Meneghetti, L.R. Chiarelli, G. Stelitano, I.L. Batalha, G. Battaglia, S. Villa
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