title: Lyoprotected nanosphere formulations for paclitaxel controlled delivery.
abstract: The preparation and technological characterization of nanosphere formulations (NS) containing the anticancer drug paclitaxel (PTX) are reported. Poly(lactide) (PLA) and poly(lactide-co-glycolide) (PLGA) nanospheres (NS) were prepared by a solvent displacement method. They showed a mean particle size in the range 150-300 nm, with a high homogeneity (polydispersity index < 0.3). For long term stability, NS require additional procedures, such as freeze-drying. In this study, the effect on NS particle size and surface charge of different lyoprotectants (mono- and disaccharides, polyalcohols, and hydroxypropyl-beta-cyclodextrin) at various concentrations was tested by means of light scattering size analysis. The formulations freeze-dried with the addition of 10% glucose (w/v) showed interesting characteristics after freeze-drying. They were chosen for specific studies on drug encapsulation efficiency, in vitro drug release and biological activity on the human anaplastic thyroid carcinoma cell line 8305C. The PLGA NS, in particular, showed a cell growth inhibitory activity comparable to the free drug.
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Università degli Studi di Catania, v.le A. Doria, 6-I-95125 Catania, Italy.
authors.forename: T
authors.initials: T
authors.lastname: Musumeci
authors.forename: L
authors.initials: L
authors.lastname: Vicari
authors.forename: C A
authors.initials: CA
authors.lastname: Ventura
authors.forename: M
authors.initials: M
authors.lastname: Gulisano
authors.forename: R
authors.initials: R
authors.lastname: Pignatello
authors.forename: G
authors.initials: G
authors.lastname: Puglisi
mesh_terms: D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000737:chemistry; D045744:Cell Line, Tumor; D002626:Chemistry, Pharmaceutical / Q000379:methods; D003451:Cryoprotective Agents / Q000737:chemistry*; D003460:Crystallization / Q000379:methods; D003692:Delayed-Action Preparations / Q000737:chemistry*; D004058:Diffusion; D005612:Freeze Drying / Q000379:methods*; D006801:Humans; D008422:Materials Testing; D008657:Metabolic Clearance Rate; D043942:Nanotubes / Q000737:chemistry* / Q000648:ultrastructure; D017239:Paclitaxel / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics*; D010316:Particle Size; D013964:Thyroid Neoplasms / Q000378:metabolism*
chemical_list: D000970:Antineoplastic Agents; D003451:Cryoprotective Agents; D003692:Delayed-Action Preparations; D017239:Paclitaxel