Recent advances on small‐molecule nanomedicines for cancer treatment

Abstract

Nanomedicines have made important contributions in the development of cancer therapies due to their tumor selectivity, multifunctionality, and synergistic effect between the payloads. In addition to the required pharmaceutical ingredients, nanomedicines are generally composed of nonpharmaceutical excipients. These excipients generally form a large proportion of the nanomedicine, and they may have potential toxicity and greatly increase the cost for drug development. Small molecule nanomedicines (SMNs) minimize or abandon the excipients and are directly assembled from pharmaceutical ingredients, which can largely improve the drug delivery efficiency and biosafety while also relieving the financial burden of drug development. In this review, we summarize recently developed SMNs that are composed of a single drug, physical mixtures of multiple drugs, drug–drug covalent conjugates, dyes with drugs, photosensitizers with drugs, photosensitizers with peptides, and drugs with peptides. This review focuses on the SMN's applications in cancer treatments, their limitations, and the future development outlook of SMNs. We hope that our insights on SMNs may be helpful to the future of drug development and make nanomedicine more powerful in the battle with cancer. This article is categorized under: Therapeutic Approaches and Drug Discovery > Nanomedicine for Oncologic Disease

Molecular photoswitches in aqueous environments

“…In biomedical research and the pharmaceutical world, small molecule actuators are extensively applied to regulate biological processes. [543][544][545][546] In this way, a wide range of biomolecules, such as proteins, [547][548][549] DNA and RNA, 550 as well as oligosaccharides, [551][552][553] can be targeted. Small molecules are usually applied remotely and reach the actual target site by diffusion.…”

Nanoparticles of a New Small-Molecule P-Selectin Inhibitor Attenuate Thrombosis, Inflammation, and Tumor Growth in Two Animal Models

“…Small molecule nanomedicines are directly assembled from pharmaceutical molecules with or without minimum excipients, which can largely improve drug-delivery efficiency and biosafety. 48 TEM and SEM of THCMA ( Figure 4 ) show that THCMA self-assembled into nanorings about 100 nm in diameter. The Tyndall effect, ζ-potential, and particle-size tests ( Figure 5 ) also confirmed that THCMA functioned as a stable small-molecule nanomedicine at various concentrations in both a neutral environment (pH 7) and an acidic environment like gastric fluid (pH 2).…”

Ultrashort Peptide Self-Assembly: Front-Runners to Transport Drug and Gene Cargos

“…Nanomedicines directly assembled from pharmaceutical ingredients, termed as small molecule nanomedicines (SMNs), have the potential to improve the drug delivery efficiency, biosafety and largely reduce the research and development cost. Xue et al (2020) highlighted the recent advances in a section on drugs and photosensitizers with peptides and exhibited advantages of SMNs in the review article.…”