Mucosa-penetrating liposomes for esophageal local drug delivery

Franzé, Silvia; Rama, Francesco; Scarpa, Edoardo; Violatto, Martina Bruna; Peqini, Kaliroi; Gennari, Chiara Grazia Milena; Anderluzzi, Giulia; Camastra, Rebecca; Salmaso, Anita; Moscatiello, Giulia; Pellegrino, Sara; Rizzello, Loris; Bigini, Paolo; Cilurzo, Francesco

doi:10.1016/j.ijpharm.2024.124413

International Journal of Pharmaceutics

2024

DOI: 10.1016/j.ijpharm.2024.124413

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Mucosa-penetrating liposomes for esophageal local drug delivery

Silvia Franzé,

Francesco Rama,

Edoardo Scarpa

et al.

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Synthesis of Amphiphilic Amino Poly-Amido-Saccharide and Poly(lactic) Acid Block Copolymers and Fabrication of Paclitaxel-Loaded Mucoadhesive Nanoparticles

Sabatelle,

Geller,

et al. 2024

Bioconjugate Chem.

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Drug delivery to the esophagus through systemic administration remains challenging, as minimal drug reaches the desired target. Local delivery offers the potential for improved efficacy while minimizing offtarget toxicities but necessitates bioadhesive properties for mucosal delivery. Herein, we describe the synthesis of two new mucoadhesive amphiphilic copolymers prepared by sequential ring-opening copolymerization or postpolymerization click conjugation. Both strategies yield block copolymers containing a hydrophilic amine-functionalized poly-amido-saccharide and either a hydrophobic alkyl derivatized poly-amido-saccharide or poly(lactic acid), respectively. The latter resulting copolymers readily self-assemble into spherical, ≈200 nm diameter, positively charged mucoadhesive nanoparticles. The NPs entrap ultrahigh levels of paclitaxel via encapsulation of free paclitaxel and paclitaxel conjugated to a biodegradable, biocompatible poly(1,2-glycerol carbonate). Paclitaxel-loaded NPs rapidly enter cells, release paclitaxel, are cytotoxic to esophageal OE33 and OE19 tumor cells in vitro, and, importantly, demonstrate improved mucoadhesion compared to conventional poly(ethylene glycol)poly(lactic acid) nanoparticles to ex vivo esophageal tissue.

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Synthesis of Amphiphilic Amino Poly-Amido-Saccharide and Poly(lactic) Acid Block Copolymers and Fabrication of Paclitaxel-Loaded Mucoadhesive Nanoparticles

Sabatelle,

Geller,

et al. 2024

Bioconjugate Chem.

View full text Add to dashboard Cite

show abstract

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Mucosa-penetrating liposomes for esophageal local drug delivery

Cited by 1 publication

References 31 publications

Synthesis of Amphiphilic Amino Poly-Amido-Saccharide and Poly(lactic) Acid Block Copolymers and Fabrication of Paclitaxel-Loaded Mucoadhesive Nanoparticles

Synthesis of Amphiphilic Amino Poly-Amido-Saccharide and Poly(lactic) Acid Block Copolymers and Fabrication of Paclitaxel-Loaded Mucoadhesive Nanoparticles

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