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Nanoparticles of Esterified Polymalic Acid for Controlled Anticancer Drug Release
Author(s) -
LanzLandázuri Alberto,
PortillaArias José,
Martínez de Ilarduya Antxon,
GarcíaAlvarez Montserrat,
Holler Eggehard,
Ljubimova Julia,
MuñozGuerra Sebastián
Publication year - 2014
Publication title -
macromolecular bioscience
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.924
H-Index - 105
eISSN - 1616-5195
pISSN - 1616-5187
DOI - 10.1002/mabi.201400124
Subject(s) - chemistry , malic acid , doxorubicin , nanoparticle , drug , ethanol , in vitro , pharmacology , degradation (telecommunications) , drug carrier , drug delivery , nuclear chemistry , combinatorial chemistry , biophysics , biochemistry , nanotechnology , organic chemistry , materials science , chemotherapy , medicine , surgery , citric acid , telecommunications , computer science , biology
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.