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Novel Insights Into Appropriate Encapsulation Methods for Bioactive Compounds Into Polymers: A Study With Peptides and HDAC Inhibitors
Author(s) -
Hennig Dorle,
Schubert Stephanie,
Dargatz Harald,
Kostenis Evi,
Fahr Alfred,
Schubert Ulrich S.,
Heinzel Thorsten,
Imhof Diana
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.201300213
Subject(s) - plga , chemistry , nanoparticle , liposome , glycolic acid , peptide , polymer , combinatorial chemistry , biophysics , acetylation , in vitro , lactic acid , nanotechnology , biochemistry , organic chemistry , materials science , genetics , biology , bacteria , gene
The use of different nanoparticles (NPs) for successful encapsulation of bioactive substances is discussed. The inclusion efficiency into liposomes, acetalated dextran (Ac‐Dex), and variants of poly[(lactic acid)‐ co ‐(glycolic acid)] (PLGA) NPs is analyzed after chemical degradation. Efficient inclusion of SIRT1 inhibitor Ex527 in liposomes, Ac‐Dex‐ and PLGA‐NPs is observed for all procedures used. Activity of Ex527 is demonstrated by monitoring the acetylation status of SIRT1‐target p53. In contrast, small peptides are only incorporated into acid‐terminated PLGA‐NPs and marginally into Ac‐Dex‐NPs. The yield depends on peptide sequence and terminal modifications. Activity is exemplified for angiotensin II using the dynamic mass redistribution technology.