title: Poly(D, L-lactide-co-glycolide)/montmorillonite nanoparticles for improved oral delivery of exemestane.
abstract: The aim of this study was to develop poly(D,L-lactide-co-glycolide)/montmorillonite (PLGA/MMT) nanoparticles formulations for improved oral delivery of exemestane. Exemestane-loaded PLGA nanoparticles and PLGA/MMT nanoparticles were prepared by a modified solvent extraction/evaporation technology with vitamin E succinated polyethylene glycol 1000 (TPGS) as emulsifier. The content of MMT was estimated by thermal gravimetric analysis. The drug encapsulation efficiency and in vitro drug release kinetics were measured by high-performance liquid chromatography. The size, size distribution, surface charge and morphology of the exemestane-loaded nanoparticles were characterized using a Zetasizer Nano ZS and field emission scanning electron microscopy. The physical status of exemestane in the nanoparticles was characterized by differential scanning calorimetry. In vitro cellular uptake of coumarin-6-loaded nanoparticles was investigated by confocal laser scanning microscope, demonstrating that the fluorescence nanoparticles were internalized by Caco-2 cells (as an in vitro gastrointestinal model). The results of in vitro cytotoxicity experiment on MCF-7 cells (as a model of breast cancer cells) showed the exemestane-loaded nanoparticles resulted in lower cell viability versus the pure exemestane solution. The cytotoxicity against MCF-7 cells for exemestane-loaded nanoparticles and pure exemestane solution was dependent on the drug concentration and incubation time. In conclusion, this study indicates the capability of PLGA nanoparticles and PLGA/MMT nanoparticles in enhancing the oral delivery of exemestane.
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University , Shenyang 110016, P R China.
authors.forename: Zhen
authors.initials: Z
authors.lastname: Li
authors.forename: Kexin
authors.initials: K
authors.lastname: Liu
authors.forename: Pengyuan
authors.initials: P
authors.lastname: Sun
authors.forename: Lin
authors.initials: L
authors.lastname: Mei
authors.forename: Tangna
authors.initials: T
authors.lastname: Hao
authors.forename: Yan
authors.initials: Y
authors.lastname: Tian
authors.forename: Zeyao
authors.initials: Z
authors.lastname: Tang
authors.forename: Lei
authors.initials: L
authors.lastname: Li
authors.forename: Dawei
authors.initials: D
authors.lastname: Chen
mesh_terms: D000730:Androstadienes / Q000008:administration & dosage* / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000494:pharmacology; D001546:Bentonite / Q000737:chemistry*; D001943:Breast Neoplasms / Q000188:drug therapy; D018938:Caco-2 Cells; D045744:Cell Line, Tumor; D004337:Drug Carriers / Q000737:chemistry*; D005260:Female; D006801:Humans; D019344:Lactic Acid / Q000737:chemistry*; D053758:Nanoparticles / Q000737:chemistry*; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer
chemical_list: D000730:Androstadienes; D000970:Antineoplastic Agents; D004337:Drug Carriers; D001546:Bentonite; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; C056516:exemestane