Among polymeric polycations, Chitosan, derived by deacetylation of the naturally occurring polysaccharide chitin, has recently emerged as a suitable material for the preparation of non-viral gene and drug delivery vectors [1]. Chitosan offers many advantages, a high degree of biodegradability and biocompatibility, as well as mucoadhesive and permeability-enhancing properties, but also large availability and relatively low cost. Its properties can be tuned to a considerable extent by simply controlling the degree of deacetylation and polymerization, or the pH-dependent degree of ionization. Moreover, the broad possibility of chitosan structure modification into desired constructs makes it a versatile component for drug delivery system design. In this work, different two-components drug delivery systems formed by a chitosan shell enclosing an inner core, formed by a surfactant vesicle or by a polymeric nanoparticle, have been investigated and proposed as new targeting vectors for skeletal muscle, with potential applications as delivery systems for modulation of myogenic differentiation. Span and Tween non-ionic surfactant vesicles (Niosomes) [2] and polylactic-co-glycolic acid (PLGA) [3] nanoparticles have been coated with chitosan and lactosylated-chitosan at different particle/polymer concentration ratio and have been characterized in terms of their size, shape, charge and formulation stability by different experimental techniques. The stability of the systems in serum and the release kinetics of model drugs from selected formulations have been evaluated. Chitosan-coated delivery systems containing a fluorescent dye, have been added to C2C12 skeletal muscle cell lines to investigate cytotoxicity and uptake efficiency. Our results show that CS coating is able to switch ζ-potential of negative Niosomes or PLGA nanoparticles from negative to positive, without modifying particle size distribution and to modulate the transfection efficiency of chitosan-based delivery systems by changing formulation-related parameters without inducing cytotoxicity.
CHITOSAN-COATED DRUG DELIVERY VECTORS FOR SKELETAL MUSCLE TARGETING / Sennato, Simona; Chronopoulou, Laura; Rinaldi, Federica; Berardinelli, MARIA GRAZIA; Dominici, Fabio; Marianecci, Carlotta; Carafa, Maria; Musaro', Antonio; Palocci, Cleofe; Bordi, Federico. - STAMPA. - (2015), pp. 139-139. (Intervento presentato al convegno 8th European Symposium on Biopolymers tenutosi a Rome, Italy nel 15-18/09/2015).
CHITOSAN-COATED DRUG DELIVERY VECTORS FOR SKELETAL MUSCLE TARGETING
SENNATO, Simona;CHRONOPOULOU, LAURA;Rinaldi, Federica;BERARDINELLI, MARIA GRAZIA;MARIANECCI, CARLOTTA;CARAFA, Maria;MUSARO', Antonio;PALOCCI, Cleofe;BORDI, FEDERICO
2015
Abstract
Among polymeric polycations, Chitosan, derived by deacetylation of the naturally occurring polysaccharide chitin, has recently emerged as a suitable material for the preparation of non-viral gene and drug delivery vectors [1]. Chitosan offers many advantages, a high degree of biodegradability and biocompatibility, as well as mucoadhesive and permeability-enhancing properties, but also large availability and relatively low cost. Its properties can be tuned to a considerable extent by simply controlling the degree of deacetylation and polymerization, or the pH-dependent degree of ionization. Moreover, the broad possibility of chitosan structure modification into desired constructs makes it a versatile component for drug delivery system design. In this work, different two-components drug delivery systems formed by a chitosan shell enclosing an inner core, formed by a surfactant vesicle or by a polymeric nanoparticle, have been investigated and proposed as new targeting vectors for skeletal muscle, with potential applications as delivery systems for modulation of myogenic differentiation. Span and Tween non-ionic surfactant vesicles (Niosomes) [2] and polylactic-co-glycolic acid (PLGA) [3] nanoparticles have been coated with chitosan and lactosylated-chitosan at different particle/polymer concentration ratio and have been characterized in terms of their size, shape, charge and formulation stability by different experimental techniques. The stability of the systems in serum and the release kinetics of model drugs from selected formulations have been evaluated. Chitosan-coated delivery systems containing a fluorescent dye, have been added to C2C12 skeletal muscle cell lines to investigate cytotoxicity and uptake efficiency. Our results show that CS coating is able to switch ζ-potential of negative Niosomes or PLGA nanoparticles from negative to positive, without modifying particle size distribution and to modulate the transfection efficiency of chitosan-based delivery systems by changing formulation-related parameters without inducing cytotoxicity.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.