Abstract
Melittin (MEL) is a 26-amino acid polypeptide with a variety of pharmacological and toxicological effects, which include strong surface activity on cell lipid membranes, hemolytic activity, and potential anti-tumor properties. However, the clinical application of melittin is restricted due to its severe hemolytic activity. Different nanocarrier systems have been developed to achieve stable loading, side effects shielding, and tumor-targeted delivery, such as liposomes, cationic polymers, lipodisks, etc. In addition, MEL can be modified on nano drugs as a non-selective cytolytic peptide to enhance cellular uptake and endosomal/lysosomal escape. In this review, we discuss recent advances in MEL’s nano-delivery systems and MEL-modified nano drug carriers for cancer therapy.
Highlights
MEL selectively inhibits expression of matrix metalloproteinase-9 (MMP-9), which plays an important role in the migration of cancer cells [50,58,59] via down-regulating activator protein-1 (AP-1) and NF-κB expression
MEL and doxorubicin (DOX) were co-loaded to citric acid-functionalized Fe3 O4 magnetic nanoparticles (CA-MNPs). The release of both MEL and DOX was strongly enhanced at pH 4.5 and the nanoparticles were potentially applied in magnetically targeted cancer therapy
The co-loading of MEL and paclitaxel in lipodisks did not induce hemolysis, the lipodisks loaded with MEL alone exhibited hemolytic toxicity at high concentrations [94], which may imply that the safety of lipid disks loaded with MEL needs to be further improved
Summary
Publisher’s Note: MDPI stays neutral with regard to jurisdictional claims in published maps and institutional affiliations. MEL is a major component of honeybee (Apis mellifera) venom with various biological and pharmacological properties [1]. Its strong surface activity on lipid membranes, anti-microbial, anti-inflammatory, and anti-cancer properties has been widely studied and proved. The use and application of MEL in clinical experiments is hindered because of its intense toxic side effects. Multiple strategies have been adopted and optimized to develop a safe and stable MEL delivery system. This review focusses on the recent progress of MEL carriers and drug delivery systems with MEL as a functional molecule in cancer therapy. Measures to lower the side effects of MEL are discussed, along with the improvements and challenges relevant to each strategy
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