Synthesis of Acid-Labile Poly(Doxazolidine) as a Polyprodrug with an Ultra-High Drug Content for Self-Delivery of High-Performance Chemotherapeutics

Abstract

Drug self-delivery systems (DSDSs) have attracted intense attention due to their high drug content. However, their practical application still suffers from their premature drug leakage, slow drug release, and/or low antitumor efficacy of the released small molecular drugs. Here, acid-labile poly(Doxazolidine) (P(Doxaz)) is designed as a polyprodrug for the self-delivery of high antitumor chemotherapeutics (Doxazolidine (Doxaz)), with an ultrahigh Doxaz content of 92.45%. The P(Doxaz) nanoparticles could completely degrade into Doxaz within 10 h in the simulated tumor intracellular microenvironment, with a low drug leakage of 12.9% over 12 h in the normal physiological media. Owing to the ultrahigh drug content, fast acid-triggered degradation and drug release, and high antitumor efficacy of Doxaz, the proposed DSDS possesses an enhanced antiproliferation efficacy compared to the free DOX, demonstrating its potential in future tumor treatments.

Novel one-pot strategy for fabrication of a pH-Responsive bone-targeted drug self-frame delivery system for treatment of osteoporosis

“…Recently, drug self-frame delivery systems (DSFDS) have received increasing attention because they are constructed with the participation of free drug molecules without the need for additional nanocarriers [ 38 ]. DSFDS form particles with nanoscales by self-assembly between multiple active drugs, which achieve intracellular delivery independently without relying on nanocarriers [ [39] , [40] , [41] , [42] , [43] ]. In Hou's study, the authors successfully prepared a DSFDS for cancer treatment with a drug loading capacity of up to 87.1% by polymerization of HCCP and doxorubicin (DOX) [ 44 ].…”