title: Nanoparticles of esterified polymalic acid for controlled anticancer drug release.
abstract: Esterification of microbial poly(malic acid) is performed with either ethanol or 1-butanol to obtain polymalate conjugates capable to form nanoparticles (100-350 nm). Degradation under physiological conditions takes place with release of malic acid and the corresponding alcohol as unique degradation products. The anticancer drugs Temozolomide and Doxorubicin are encapsulated in nanoparticles with efficiency of 17 and 37%, respectively. In vitro drug release assays show that Temozolomide is almost completely discharged in a few hours whereas Doxorubicin is steadily released along several days. Drug-loaded nano-particles show remarkable effectiveness against cancer cells. Partially ethylated poly(malic acid) nano-particles are those showing the highest cellular uptake.
authors.affiliation: Departament d'Enginyeria Química, Universitat Politècnica de Catalunya, ETSEIB, Diagonal 647, 08028, Barcelona, Spain.
authors.forename: Alberto
authors.initials: A
authors.lastname: Lanz-Landázuri
authors.forename: José
authors.initials: J
authors.lastname: Portilla-Arias
authors.forename: Antxon
authors.initials: A
authors.lastname: Martínez de Ilarduya
authors.forename: Montserrat
authors.initials: M
authors.lastname: García-Alvarez
authors.forename: Eggehard
authors.initials: E
authors.lastname: Holler
authors.forename: Julia
authors.initials: J
authors.lastname: Ljubimova
authors.forename: Sebastián
authors.initials: S
authors.lastname: Muñoz-Guerra
mesh_terms: D000903:Antibiotics, Antineoplastic / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D018906:Antineoplastic Agents, Alkylating / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D045744:Cell Line, Tumor; D003606:Dacarbazine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D003692:Delayed-Action Preparations / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D004317:Doxorubicin / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D008293:Malates / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D053769:Nanocapsules / Q000737:chemistry* / Q000648:ultrastructure; D011108:Polymers / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D000077204:Temozolomide
chemical_list: D000903:Antibiotics, Antineoplastic; D018906:Antineoplastic Agents, Alkylating; D003692:Delayed-Action Preparations; D008293:Malates; D053769:Nanocapsules; D011108:Polymers; C121060:poly(malic acid); D003606:Dacarbazine; D004317:Doxorubicin; D000077204:Temozolomide
keywords: biodegradable drug delivery systems; poly(malic acid); poly(malic acid) nanoparticles