title: Novel PLA microspheres with hydrophilic and bioadhesive surfaces for the controlled delivery of fenretinide.
abstract: Novel polylactide (PLA) microspheres endowed with hydrophilic and bioadhesive surfaces as injectable formulations for the controlled release of fenretinide were prepared, using a novel technique based on the co-precipitation of PLA with gelatin, at the interface of a liquid dispersion formed by the addition of N-methylpyrrolidone containing PLA and dextrin (DX), towards an aqueous solution of gelatin (G). The resulting PLA-G-DX microspheres were compared with others prepared by the same technique using polylactide-co-glycolide (PLGA), with or without DX, and with or without phosphatidylcholine. Of the different systems, the PLA-G-DX microspheres had the best morphological, dimensional and functional characteristics. They had the highest drug loading, and their drug release was the most efficient over time without any burst effect. Their in vitro anti-tumoural activity was strongly enhanced with respect to the pure fenretinide. This paralleled the increased drug concentration inside the cells due to their marked bioadhesion to the tumour cell membranes as indicated by scanning electron microscope images.
authors.affiliation: Department of Biomedical and NeuroMotor Sciences (DiBiNeM), Unit of Human Anatomy, University of Bologna , Via Irnerio 48, 40126 Bologna , Italy and.
authors.forename: Mirella
authors.initials: M
authors.lastname: Falconi
authors.forename: Stefano
authors.initials: S
authors.lastname: Focaroli
authors.forename: Gabriella
authors.initials: G
authors.lastname: Teti
authors.forename: Viviana
authors.initials: V
authors.lastname: Salvatore
authors.forename: Sandra
authors.initials: S
authors.lastname: Durante
authors.forename: Benedetta
authors.initials: B
authors.lastname: Nicolini
authors.forename: Isabella
authors.initials: I
authors.lastname: Orienti
mesh_terms: D000818:Animals; D023181:Antimicrobial Cationic Peptides / Q000737:chemistry / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology; D002417:Cattle; D045744:Cell Line, Tumor; D003692:Delayed-Action Preparations; D017313:Fenretinide / Q000737:chemistry / Q000494:pharmacology; D005780:Gelatin / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D064347:Microscopy, Electrochemical, Scanning; D008863:Microspheres; D009369:Neoplasms / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D010316:Particle Size; D010713:Phosphatidylcholines / Q000737:chemistry / Q000494:pharmacology; D011091:Polyesters / Q000737:chemistry / Q000494:pharmacology
chemical_list: D023181:Antimicrobial Cationic Peptides; D000970:Antineoplastic Agents; D003692:Delayed-Action Preparations; D010713:Phosphatidylcholines; D011091:Polyesters; C045866:peptide-Gly-Leu-amide; D017313:Fenretinide; C033616:poly(lactide); D005780:Gelatin