Recent advances in prodrug-based nanoparticle therapeutics

Dynamic crosslinked polymeric nano-prodrugs for highly selective synergistic chemotherapy

“…3 B, less than 10% of cisplatin was released from PPD-NPs at pH 7.4 in 24 h, owing to constant particle sizes based on stable physicochemical properties under neutral conditions. PPD-NPs released about 20% of cisplatin at pH 6.8 in 24 h owing to the loose structure triggered by partial degradation of poly(ortho ester)s. In fact, cisplatin existed as the prodrug in dialysates at pH 6.8 and could not be released in the absence of GSH [32] . In contrast, above 80% of cisplatin was released from PPD-NPs in 24 h due to rapid disintegration at pH 5.0/GSH.…”

Stimulus-responsive self-assembled prodrugs in cancer therapy

“…More importantly, by properly encoding suitable linker chemistries, the resulting self-assembled prodrugs could be tailored for tumor-specific temporal/spatial controlled-release of drugs in response to chemical or biological stimuli present at the tumor sites. 54,55…”

pH-Sensitive Twin Liposomes Containing Quercetin and Laccase for Tumor Therapy

“…Cases of remodeling the form, shape, and physical properties of drug-delivery vehicles through biomimetic studies and using them for antitumor research are recently increasing. , Thus, the combination of novel drug-carrying vehicles and enzyme-catalyzed prodrug therapy can be highly attractive in terms of alleviating the side effects of drugs and enhancing the efficiency of antitumor treatment and converting nontoxic prodrugs into forms that are aggressive to tumor cells under specific conditions and specific environments. − In particular, the spatiotemporal-selective antitumor activity of prodrugs can be improved by incorporating functional nanovehicles. − In this study, we focused on twin nanoparticles and multicompartmental particles with functionalities for highly efficient prodrug therapy. − For example, when a prodrug is activated by a different bioactive catalyst, the individual encapsulation of the prodrug and bioactive catalyst in different compartments in a single particle and its delivery to a specific site (while maintaining the status of the nontoxic prodrug until reaching the target site) may enhance the therapeutic effect significantly more than encapsulating both the prodrug and bioactive catalyst in the same compartment. − Each substance can be simply mixed and administered to the body; , however, a multicompartmental drug carrier can be an efficient method for overcoming the complex in vivo environment, in which prodrugs and bioactive catalysts (released from adjacent drug storage compartments) can be combined to consequently enhance antitumor activity. Although there have been attempts to connect the two nanoparticles, − there has been no attempt to control the release behaviors of drugs loaded in each compartment. Therefore, these studies should further elucidate their effects in the future.…”