Tailored Beta‐Lapachone Nanomedicines for Cancer‐Specific Therapy

Abstract

Nanotechnology shows the power to improve efficacy and reduce the adverse effects of anticancer agents. As a quinone‐containing compound, beta‐lapachone (LAP) is widely employed for targeted anticancer therapy under hypoxia. The principal mechanism of LAP‐mediated cytotoxicity is believed due to the continuous generation of reactive oxygen species with the aid of NAD(P)H: quinone oxidoreductase 1 (NQO1). The cancer selectivity of LAP relies on the difference between NQO1 expression in tumors and that in healthy organs. Despite this, the clinical translation of LAP faces the problem of narrow therapeutic window that is challenging for dose regimen design. Herein, the multifaceted anticancer mechanism of LAP is briefly introduced, the advance of nanocarriers for LAP delivery is reviewed, and the combinational delivery approaches to enhance LAP potency in recent years are summarized. The mechanisms by which nanosystems boost LAP efficacy, including tumor targeting, cellular uptake enhancement, controlled cargo release, enhanced Fenton or Fenton‐like reaction, and multidrug synergism, are also presented. The problems of LAP anticancer nanomedicines and the prospective solutions are discussed. The current review may help to unlock the potential of cancer‐specific LAP therapy and speed up its clinical translation.

Advancing Precision: A Controllable Self-Synergistic Nanoplatform Initiating Pyroptosis-Based Immunogenic Cell Death Cascade for Targeted Tumor Therapy

“…β-Lapachone (Lap), a Food and Drug Administration (FDA)approved chemotherapeutic agent, has demonstrated promising therapeutic potential in the treatment of tumors. 21 After catalysis by the enzyme NAD(P)H:quinone oxidoreductase 1 (NQO1), Lap can selectively generate endogenous ROS in tumor cells that express high NQO1 levels, giving it excellent biosecurity. However, its efficiency in producing ROS is limited by the level of NQO1 expression.…”