Citation: Jing Gao, Wei-qi Wang, Hai-jun Yu. Acid-activatable Polymeric Drug Delivery Systems for Cancer Therapy[J]. Acta Polymerica Sinica, ;2019, 50(11): 1156-1166. doi: 10.11777/j.issn1000-3304.2019.19133 shu

Acid-activatable Polymeric Drug Delivery Systems for Cancer Therapy

1.
State Key Laboratory of Drug Research & Center of Pharmaceutics, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203
2.
School of Pharmacy, Nantong University, Nantong 226001

Corresponding author: Hai-jun Yu, hjyu@simm.ac.cn
Received Date: 12 July 2019
Revised Date: 9 August 2019

The polymeric drug delivery systems (DDS) have showed promising potential for improving cancer therapy, which can lengthen the blood circulation and minimize the adverse effect of chemotherapeutics. Despite promising, the therapeutic performance of polymeric-based DDS is affected by a series of physiological barriers, including limited tumor accumulation, restricted tumor penetration, insufficient cellular uptake, and slow drug release inside the tumor cells. It has been well-investigated that there is an acidic microenvironment inside the solid tumors due to the abnormal glucose metabolism of tumor cells. Moreover, the subcellular organelles including endosome and lysosome display much lower acidic pH than that of cytosol. The extracellular and intracellular acidic microenvironments have thus been exploited as both a trigger and target for tumor-targeted drug delivery. In this review article, we summarized our recent advances in developing acid-responsive polymeric DDS by taking the advantage of the acidic microenvironment of tumor tissue and tumor cells. We particularly highlighted the acid-responsive chemical bonds and components employed for constructing the acid-activatable DDS. These acid-activatable nanovectors have been exploited for combating the physiological barriers by surface charge conversion, nanostructure dissociation, and ligand presentation. We also provided a perspective regarding of the challenges and opportunities about clinical translation of the stimuli-activatable DDS.
- Nanosized drug delivery system,
- Tumor acidic microenvironment,
- Polymeric nanoparticles,
- Physiological barriers
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