title: Novel insights into appropriate encapsulation methods for bioactive compounds into polymers: a study with peptides and HDAC inhibitors.
abstract: 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.
authors: Center for Molecular Biomedicine, Institute of Biochemistry and Biophysics, Department of Biochemistry, Friedrich Schiller University Jena, Hans-Knöll-Str. 2, D-07745, Jena, Germany.
authors: Dorle
authors: D
authors: Hennig
authors: Stephanie
authors: S
authors: Schubert
authors: Harald
authors: H
authors: Dargatz
authors: Evi
authors: E
authors: Kostenis
authors: Alfred
authors: A
authors: Fahr
authors: Ulrich S
authors: US
authors: Schubert
authors: Thorsten
authors: T
authors: Heinzel
authors: Diana
authors: D
authors: Imhof
mesh_terms: D000107:Acetylation; D000804:Angiotensin II / Q000737:chemistry / Q000494:pharmacology; D002227:Carbazoles / Q000737:chemistry* / Q000494:pharmacology; D003911:Dextrans / Q000737:chemistry; D004337:Drug Carriers / Q000737:chemistry; D057809:HEK293 Cells / Q000187:drug effects; D056572:Histone Deacetylase Inhibitors / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D006877:Hydroxamic Acids / Q000737:chemistry; D019344:Lactic Acid / Q000737:chemistry; D008081:Liposomes / Q000737:chemistry* / Q000494:pharmacology; D053758:Nanoparticles / Q000737:chemistry*; D010455:Peptides / Q000737:chemistry*; D011100:Polyglycolic Acid / Q000737:chemistry; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D056564:Sirtuin 1 / Q000037:antagonists & inhibitors; D014635:Valproic Acid / Q000737:chemistry
chemical_list: C550547:6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide; D002227:Carbazoles; D003911:Dextrans; D004337:Drug Carriers; D056572:Histone Deacetylase Inhibitors; D006877:Hydroxamic Acids; D008081:Liposomes; D010455:Peptides; D000804:Angiotensin II; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; C012589:trichostatin A; D014635:Valproic Acid; C447939:SIRT1 protein, human; D056564:Sirtuin 1
keywords: HDAC inhibitors; cellular uptake; liposomes; nanoparticles; peptide drugs