Advances in nano‐preparations for improving tetrandrine solubility and bioavailability

Abstract Tetrandrine (TET) is a natural bis‐benzylisoquinoline alkaloid isolated from Stephania species with a wide range of biological and pharmacologic activities; it mainly serves as an anti‐inflammatory agent or antitumor adjuvant in clinical applications. However, limitations such as prominent hydrophobicity, severe off‐target toxicity, and low absorption result in suboptimal therapeutic outcomes preventing its widespread adoption. Nanoparticles have proven to be efficient devices for targeted drug delivery since drug‐carrying nanoparticles can be passively transported to the tumor site by the enhanced permeability and retention (EPR) effects, thus securing a niche in cancer therapies. Great progress has been made in nanocarrier construction for TET delivery due to their outstanding advantages such as increased water‐solubility, improved biodistribution and blood circulation, reduced off‐target irritation, and combinational therapy. Herein, we systematically reviewed the latest advancements in TET‐loaded nanoparticles and their respective features with the expectation of providing perspective and guidelines for future research and potential applications of TET.