Novel Insights into Appropriate Encapsulation Methods for Bioactive Compounds into Polymers: A Study with Peptides and HDAC Inhibitors

Hennig, Dorle; Schubert, Stephanie; Dargatz, Harald; Kostenis, Evi; Fahr, Alfred; Schubert, Ulrich S.; Heinzel, Thorsten; Imhof, Diana

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.

Year:

2014

Type of Publication:

Article

Journal:

Macromolecular Bioscience

Volume:

14

Pages:

69 - 80