Specific Drug Formulation Additives: Revealing the Impact of Architecture and Block Length Ratio.

Abstract:

:Combining poly(ethylene glycol) (PEG) with sequence-defined peptides in PEG-peptide conjugates offers opportunities to realize next-generation drug formulation additives for overcoming undesired pharmacological profiles of difficult small molecule drugs. The tailored peptide segments provide sequence-specific, noncovalent drug binding, and the hydrophilic PEG block renders the complexes water soluble. On the basis of a peptide sequence known to bind the photosensitizer m-tetra(hydroxyphenyl)chlorin (m-THPC) for photodynamic cancer therapy, a set of different conjugate architectures is synthesized and studied. Variations in PEG block length and amplification of the peptidic binding domain of PEG-peptide conjugates are used to fine tune critical parameters for hosting m-THPC, such as drug payload capacities, aggregation sizes, and drug release and activation kinetics.

journal_name

Biomacromolecules

journal_title

Biomacromolecules

authors

Wieczorek S,Schwaar T,Senge MO,Börner HG

doi

10.1021/acs.biomac.5b00961

subject

Has Abstract

pub_date

2015-10-12 00:00:00

pages

3308-12

issue

10

eissn

1525-7797

issn

1526-4602

journal_volume

16

pub_type

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