Advancing Drug Formulation Additives toward Precision Additives with Release Mediating Peptide Interlayer

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• 作者：Sebastian Wieczorek ; André Dallmann ; Zdravko Kochovski ; Hans G. Börner
• 刊名：Journal of the American Chemical Society
• 出版年：2016
• 出版时间：August 3, 2016
• 年：2016
• 卷：138
• 期：30
• 页码：9349-9352
• 全文大小：249K
• 年卷期：0
• ISSN：1520-5126

文摘

Amphiphilic drug formulation additives based on palmitic acid-modified poly(ethylene glycol) (Pal-PEG) are combined with a tailored drug binding peptide that is positioned at the hydrophobic–hydrophilic interface. The peptide originates from combinatorial selection and enables precise modulation of the drug release profiles. While Pal provides a cost-effective reservoir for drug storage, the PEG realizes solubility and shielding. The precision additives reach high payloads close to 1:1, rendering a photosensitizer water-soluble and providing adjustable drug activation kinetics by fine-tuning the peptide interface layer.