Gaining insights into specific drug formulation additives for solubilizing a 
potential Anti-Alzheimer disease drug B4A1

Lawatscheck, Carmen; Pickhardt, Marcus; Grafl, Anna; Linkert, Katharina; Polster, Frank; Mandelkow, Eckhard; Boerner, Hans G.

doi:10.1002/mabi.201700109

Item

ITEM ACTIONSEXPORT

Add to Basket

Please note that a newer version of this item is available:
https://pure.mpg.de/pubman/item/item_2601746_4

DetailsSummary

Released

Journal Article

Gaining insights into specific drug formulation additives for solubilizing a potential Anti-Alzheimer disease drug B4A1

MPS-Authors

Pickhardt, Marcus
external;
Neuronal Cytoskeleton and Alzheimer's Disease, Cooperations, Center of Advanced European Studies and Research (caesar), Max Planck Society;

Mandelkow, Eckhard
external;
Neuronal Cytoskeleton and Alzheimer's Disease, Cooperations, Center of Advanced European Studies and Research (caesar), Max Planck Society;

External Resource

https://onlinelibrary.wiley.com/doi/abs/10.1002/mabi.201700109
(Publisher version)

Fulltext (restricted access)

There are currently no full texts shared for your IP range.

Fulltext (public)

There are no public fulltexts stored in PuRe

Supplementary Material (public)

There is no public supplementary material available

Citation

Lawatscheck, C., Pickhardt, M., Grafl, A., Linkert, K., Polster, F., Mandelkow, E., et al. (2017). Gaining insights into specific drug formulation additives for solubilizing a potential Anti-Alzheimer disease drug B4A1. Macromolecular Bioscience, 17(10, S1): 1700109. doi:10.1002/mabi.201700109.

Cite as: https://hdl.handle.net/21.11116/0000-0001-78D8-5

Abstract

The pharmacological profiles of small molecule drugs are often challenged by their poor water solubility. Sequence-defined peptides attached to poly(ethylene glycol) (PEG) offer opportunities to overcome these difficulties by acting as drug-specific formulation additives. The peptide-PEG conjugates enable specific, noncovalent drug binding via tailored peptide/drug interactions as well as provide water solubility and drug shielding by well-solvated PEG-blocks. A systematic set of specific solubilizers for B4A1 as a potential anti-Alzheimer disease drug is synthesized and variations involve the length of the PEG-blocks as well as the sequences of the peptidic drug-binding domain. The solubilizer/B4A1 complexes are studied in order to understand contributions of both PEG and peptide segments on drug payload capacities, drug/carrier aggregate sizes, and influences on inhibition of the Tau-protein aggregation in an in vitro assay.