TY - JOUR
T1 - Systemic heparin delivery by the pulmonary route using chitosan and glycol chitosan nanoparticles
AU - Trapani, Adriana
AU - Di Gioia, Sante
AU - Ditaranto, Nicoletta
AU - Cioffi, Nicola
AU - Goycoolea, Francisco M.
AU - Carbone, Annalucia
AU - Garcia-Fuentes, Marcos
AU - Conese, Massimo
AU - Alonso, Maria Jose
PY - 2013/4/15
Y1 - 2013/4/15
N2 - The aim of this study was to evaluate the performance of chitosan (CS) and glycol chitosan (GCS) nanoparticles containing the surfactant Lipoid S100 for the systemic delivery of low molecular weight heparin (LMWH) upon pulmonary administration. These nanoparticles were prepared in acidic and neutral conditions using the ionotropic gelation technique. The size and zeta potential of the NPs were affected by the pH and also the type of polysaccharide (CS or GCS). The size (between 156 and 385 nm) was smaller and the zeta potential (from +11 mV to +30 mV) higher for CS nanoparticles prepared in acidic conditions. The encapsulation efficiency of LMWH varied between 100% and 43% for the nanoparticles obtained in acidic and neutral conditions, respectively. X-ray photoelectron spectroscopy studies indicated that the surfactant Lipoid S100 was localized on the nanoparticle's surface irrespective of the formulation conditions. In vivo studies showed that systems prepared in acidic conditions did not increase coagulation times when administered to mice by the pulmonary route. In contrast, Lipoid S100-LMWH GCS NPs prepared in neutral conditions showed a pharmacological efficacy. Overall, these results illustrate some promising features of CS-based nanocarriers for pulmonary delivery of LMWH.
AB - The aim of this study was to evaluate the performance of chitosan (CS) and glycol chitosan (GCS) nanoparticles containing the surfactant Lipoid S100 for the systemic delivery of low molecular weight heparin (LMWH) upon pulmonary administration. These nanoparticles were prepared in acidic and neutral conditions using the ionotropic gelation technique. The size and zeta potential of the NPs were affected by the pH and also the type of polysaccharide (CS or GCS). The size (between 156 and 385 nm) was smaller and the zeta potential (from +11 mV to +30 mV) higher for CS nanoparticles prepared in acidic conditions. The encapsulation efficiency of LMWH varied between 100% and 43% for the nanoparticles obtained in acidic and neutral conditions, respectively. X-ray photoelectron spectroscopy studies indicated that the surfactant Lipoid S100 was localized on the nanoparticle's surface irrespective of the formulation conditions. In vivo studies showed that systems prepared in acidic conditions did not increase coagulation times when administered to mice by the pulmonary route. In contrast, Lipoid S100-LMWH GCS NPs prepared in neutral conditions showed a pharmacological efficacy. Overall, these results illustrate some promising features of CS-based nanocarriers for pulmonary delivery of LMWH.
KW - Chitosan- and glycol chitosan-nanoparticles
KW - Lipoid
KW - Low molecular weight heparin
KW - Lung delivery
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U2 - 10.1016/j.ijpharm.2013.02.035
DO - 10.1016/j.ijpharm.2013.02.035
M3 - Article
C2 - 23454518
AN - SCOPUS:84875081201
VL - 447
SP - 115
EP - 123
JO - International Journal of Pharmaceutics
JF - International Journal of Pharmaceutics
SN - 0378-5173
IS - 1-2
ER -