title: Intracellular delivery of docetaxel using freeze-dried polysaccharide nanocapsules.
abstract: This article describes the development of a freeze-dried formulation of chitosan (CS) nanocapsules containing docetaxel (DCX) and the evaluation of its efficacy in the NCI-H460 cancer cell line. More specifically, two prototypes of nanocapsules differing in their coating, CS alone or in combination with poloxamer 188 were developed using the solvent displacement technique. These prototypes (150 nm and +45 mV) exhibited high encapsulation efficiencies of DCX (78%) and very similar release profiles. The nanocapsules made of solely CS could be freeze-dried and reconstituted without altering their particle size distribution. CS nanocapsules were tested for their ability to deliver intracellularly the anticancer drug DCX. The results showed that CS nanocapsules maintained the antiproliferative effect of the drug and that it was not affected by the freeze-drying process. Moreover, it was found that this cytostatic effect of DCX was related to its intracellular delivery in the cancer cells.
authors.affiliation: Department of Pharmaceutical Technology, University of Santiago de Compostela, Santiago de Compostela, Spain.
authors.forename: M V
authors.initials: MV
authors.lastname: Lozano
authors.forename: H
authors.initials: H
authors.lastname: Esteban
authors.forename: J
authors.initials: J
authors.lastname: Brea
authors.forename: M I
authors.initials: MI
authors.lastname: Loza
authors.forename: D
authors.initials: D
authors.lastname: Torres
authors.forename: M J
authors.initials: MJ
authors.lastname: Alonso
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D048271:Chitosan / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D000077143:Docetaxel; D016503:Drug Delivery Systems / Q000379:methods*; D005612:Freeze Drying; D006801:Humans; D053769:Nanocapsules / Q000737:chemistry*; D009369:Neoplasms / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D020442:Poloxamer / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D043823:Taxoids / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D053769:Nanocapsules; D043823:Taxoids; D020442:Poloxamer; D000077143:Docetaxel; D048271:Chitosan