A New Strategy for Intestinal Drug Delivery via pH-Responsive and Membrane-Active Nanogels

• Published in: ACS applied materials & interfaces Vol. 10; no. 43; pp. 36622 - 36627
• Main Authors: Wang, Shiqi, Ha, Youlim, Huang, Xiaozhen, Chin, Benjamin, Sim, Wen, Chen, Rongjun
• Format: Journal Article
• Language: English
• Published: United States American Chemical Society 31.10.2018
• Subjects: Administration, Oral; Cell Membrane - metabolism; Cross-Linking Reagents - chemistry; Doxorubicin - therapeutic use; Drug Carriers - chemistry; Epithelial Cells - metabolism; Gels; HeLa Cells; Humans; Hydrogen-Ion Concentration; Hydrophobic and Hydrophilic Interactions; Intestines - drug effects; Nanomedicine - methods; Nanoparticles - chemistry; Particle Size; Polyethylene Glycols - chemistry; Polyethyleneimine - chemistry; Polymers; membrane-active; pH-responsive; hydrophobic drug; oral delivery; nanogel
• ISSN: 1944-8244; 1944-8252
• DOI: 10.1021/acsami.8b15661

Oral administration of hydrophobic and poorly intestinal epithelium-permeable drugs is a significant challenge. Herein, we report a new strategy to overcome this problem by using novel, pH-responsive, and membrane-active nanogels as drug carriers. Prepared by simple physical cross-linking of amphiphilic pseudopeptidic polymers with pH-controlled membrane-activity, the size and hydrophobicity–hydrophilicity balance of the nanogels could be well-tuned. Furthermore, the amphiphilic nanogels could release hydrophobic payloads and destabilize cell membranes at duodenum and jejunum pH 5.0–6.0, which suggests their great potential for intestinal drug delivery.