Polymer nanoparticles for the intravenous delivery of anticancer drugs: the checkpoints on the road from the synthesis to clinical translation

In this review article we discuss some of the key aspects concerning the development of a polymer-based nanoparticle formulation for intravenous drug delivery. Since numerous preparations fail before and during clinical trials, our aim is to emphasize the main issues that a nanocarrier has to face once injected into the body. These include biocompatibility and toxicity, drug loading and release, nanoparticle storage and stability, biodistribution, selectivity towards the target organs or tissues, internalization in cells and biodegradability. They represent the main checkpoints to define a polymer-based formulation as safe and effective. Indeed, this review is intended to provide guidelines to be followed in the early development of a new nanotherapeutic to hopefully increase the success rate of polymer-based formulations entering clinical trials. The corresponding requirements and characteristics are discussed in the context of some relevant case studies taken from the literature and mainly related to the delivery of lipophilic anticancer therapeutics. The checkpoints for polymer nanoformulations from synthesis to clinic application are proposed as guidelines to develop safe and effective therapeutics.