Formulation and Quality – Biomolecular
2019 PharmSci 360
Biomacromolecules drugs (BMDs), such as nucleic acid or protein, exhibited great superior on the treatment of various diseases. However, the application of BMDs was largely limited by the undesired in vivo performance because it was very difficult for BMDs to breakthrough bio-barriers to reach target site. Therefore, there is an urgent need of safe and efficient carrier to improve the therapeutic efficacy of BMDs. Recent years, we ultilized the negatively charged domains of BMDs and prepared an ATP (adenosine triphosphate, abundant in tumor cells) fuelled charge reversal system for highly efficient BMDs delivery. In the blood circulation, the delivery system could effectively protect the BMDs from enzyme degradation and cover its’ bioactivities. Once the BMDs were successfully delivered to the tumor cells, the ATP would reversibly trigger the release and the activation of BMDs. The ATP fuelled assembly/disassembly strategy significantly improve the in vivo application of BMDs.