Publication

Tuning the Extent and Depth of Penetration of Flexible Liposomes in Human Skin

Franze, Silvia; Donadonit, Giulia; Podesta, Alessandro; Procacci, Patrizia; Orioli, Marica; Carini, Marina; Minghetti, Paola; Cilurzo, Francesco: Mol. Pharm. 14 (2017) 1998-2009 [DOI: 10.1021/acs.molpharmaceut.7b00099]

In this work we made an attempt to assess the effect of drug-induced changes of flexibility on the penetration of deformable vesicles into the human skin. Eight cationic liposomes with different degrees of flexibility were obtained by entrapping unfractionated heparin, enoxaparin, and nadroparin. The deformability was studied by a novel, facile, and reliable extrusion assay appositely developed and validated by means of quantitative nanoscale mechanical AFM measurements of vesicle elastic modulus (log(10)(YM)). The proposed extrusion assay, determining the forces involved in vesicles deformation, resulted very sensitive to evidence of minimal changes in bilayer rigidity (sigma) and vesicle deformation (K). The drug loading caused a reduction of liposome flexibility with respect to the reference plain liposomes and in accordance to the heparin type, drug to cationic lipid (DOTAP) ratio, and drug distribution within the vesicles. Interestingly, the a a

Affiliation: Cilurzo, F (Reprint Author), Univ Milan, Dept Pharmaceut Sci, Via G Colombo 71, I-20133 Milan, Italy. Franze, Silvia; Donadonit, Giulia; Orioli, Marica; Carini, Marina; Minghetti, Paola; Cilurzo, Francesco, Univ Milan, Dept Pharmaceut Sci, Via G Colombo 71, I-20133 Milan, Italy. Podesta, Alessandro, Univ Milan, Dept Phys, Via Celoria 16, I-20133 Milan, Italy. Podesta, Alessandro, Univ Milan, CIMaINa, Via Celoria 16, I-20133 Milan, Italy. Procacci, Patrizia, Univ Milan, Biomed Sci Hlth, Via G Colombo, I-20133 Milan, Italy.