title: Pectin-coated chitosan microgels crosslinked on superhydrophobic surfaces for 5-fluorouracil encapsulation.
abstract: 5-Fluorouracil (5-FU)-loaded chitosan microgels for oral and topical chemotherapy were prepared applying a superhydrophobic surface-based encapsulation technology. Drug-loaded chitosan dispersions were cross-linked and then coated with drug-free chitosan or pectin layers at the solid-air interface in a highly efficient and environment-friendly way. The size of the microgels (with diameters of ca. 280 and 557 μm for the chitosan seeds and pectin-coated microgels respectively) was the lowest obtained until now using similar biomimetic methodologies. The microgels were characterized regarding 5-FU release profiles in vitro in aqueous media covering the pH range of the gastrointestinal tract, and cytotoxicity against two cancer cell lines sensitive to 5-FU. Owing to their control of 5-FU release in acidic medium, calcium pectinate-coated microgels can be considered as suitable for oral administration. Growth inhibition of cancer cells by 5-FU was greater when incorporated to chitosan microgels; these being potentially useful for treatment of skin and colorectal tumors.
authors.affiliation: Departamento de Farmacia y Tecnología Farmacéutica, Universidad de Santiago de Compostela, 15782 Santiago de Compostela, Spain.
authors.forename: Ana M
authors.initials: AM
authors.lastname: Puga
authors.forename: Ana Catarina
authors.initials: AC
authors.lastname: Lima
authors.forename: Joao F
authors.initials: JF
authors.lastname: Mano
authors.forename: Angel
authors.initials: A
authors.lastname: Concheiro
authors.forename: Carmen
authors.initials: C
authors.lastname: Alvarez-Lorenzo
mesh_terms: D000284:Administration, Oral; D002214:Capsules; D048271:Chitosan / Q000737:chemistry*; D004337:Drug Carriers / Q000737:chemistry*; D005472:Fluorouracil / Q000008:administration & dosage / Q000737:chemistry* / Q000494:pharmacology; D005782:Gels; D005976:Glutaral / Q000737:chemistry; D006367:HeLa Cells; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D010368:Pectins / Q000737:chemistry*; D013499:Surface Properties; D014867:Water / Q000737:chemistry
chemical_list: D002214:Capsules; D004337:Drug Carriers; D005782:Gels; D014867:Water; D010368:Pectins; D048271:Chitosan; D005976:Glutaral; D005472:Fluorouracil
keywords: Chitosan; Colorectal cancer; Pectin; Skin cancer; Superhydrophobic surfaces; pH-responsive release