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