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Nanoarchitectonics of melittin-based polymersomes inducing lysosomal rupture for anticancer therapy.

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Title: Nanoarchitectonics of melittin-based polymersomes inducing lysosomal rupture for anticancer therapy.
Authors: Cho, Youngheun1 (AUTHOR), Moon, Jooho1 (AUTHOR), Han, Hyounkoo2 (AUTHOR), Park, Suhyeon2 (AUTHOR), Lim, Yeon-Su3 (AUTHOR), Lee, Hee-Young3 (AUTHOR), Jin, Kyeong Sik4 (AUTHOR), Kim, Junmin1 (AUTHOR), Nam, Soobin1 (AUTHOR), Park, Minwoo5 (AUTHOR), Kim, Hyeong Jun5 (AUTHOR), Kim, Hyuncheol1,6 (AUTHOR) hyuncheol@sogang.ac.kr
Source: Journal of Industrial & Engineering Chemistry. Mar2026, Vol. 155, p639-648. 10p.
Subjects: Polymersomes, Lysosomes, Melittin, Nanoparticles, Ligands (Biochemistry), Antineoplastic agents, Cell receptors, Drug delivery systems
Abstract: A schematic overview of HSA–coated PLLA–Cys–melittin polymersomes (PMH NPs). PMH NPs target tumors via SPARC receptors and the EPR effect, then release melittin in acidic, glutathione–rich lysosomes to induce rupture and cell death. [Display omitted] Melittin, a 26-amino-acid peptide derived from honeybee venom, exhibits potent anticancer activity but is limited by non-specific hemolysis and rapid in vivo clearance. To overcome these challenges, amphiphilic PLLA-Cys-melittin was synthesized by conjugating hydrophobic polylactic acid (PLLA) with hydrophilic melittin via a disulfide bond, forming self-assembling polymersomes in aqueous solutions. To enhance delivery efficiency and reduce hemolysis, the cationic polymersomes were coated with anionic human serum albumin (HSA), producing HSA-coated PLLA-Cys-melittin nanoparticles (PMH NPs). This HSA coating facilitates SPARC (Secreted Protein, Acidic and Rich in Cysteine)-mediated internalization into cancer cells, thereby ensuring targeted and safer delivery. Once internalized, the HSA layer dissociates under glutathione-rich conditions in lysosomes and the cytosol, releasing melittin and leading to cancer cell death. Cellular uptake studies revealed specific internalization and increased toxicity of PMH NPs in SPARC-positive cells, along with reduced hemolysis. In vivo experiments demonstrated a significant reduction in tumor volume in PMH NP-treated groups, without affecting body weight or causing major organ toxicity. Collectively, these findings suggest that PMH NPs offer a promising platform for the safe and effective delivery of melittin, providing a viable strategy for cancer therapy. [ABSTRACT FROM AUTHOR]
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Database: Engineering Source
Description
Abstract:A schematic overview of HSA–coated PLLA–Cys–melittin polymersomes (PMH NPs). PMH NPs target tumors via SPARC receptors and the EPR effect, then release melittin in acidic, glutathione–rich lysosomes to induce rupture and cell death. [Display omitted] Melittin, a 26-amino-acid peptide derived from honeybee venom, exhibits potent anticancer activity but is limited by non-specific hemolysis and rapid in vivo clearance. To overcome these challenges, amphiphilic PLLA-Cys-melittin was synthesized by conjugating hydrophobic polylactic acid (PLLA) with hydrophilic melittin via a disulfide bond, forming self-assembling polymersomes in aqueous solutions. To enhance delivery efficiency and reduce hemolysis, the cationic polymersomes were coated with anionic human serum albumin (HSA), producing HSA-coated PLLA-Cys-melittin nanoparticles (PMH NPs). This HSA coating facilitates SPARC (Secreted Protein, Acidic and Rich in Cysteine)-mediated internalization into cancer cells, thereby ensuring targeted and safer delivery. Once internalized, the HSA layer dissociates under glutathione-rich conditions in lysosomes and the cytosol, releasing melittin and leading to cancer cell death. Cellular uptake studies revealed specific internalization and increased toxicity of PMH NPs in SPARC-positive cells, along with reduced hemolysis. In vivo experiments demonstrated a significant reduction in tumor volume in PMH NP-treated groups, without affecting body weight or causing major organ toxicity. Collectively, these findings suggest that PMH NPs offer a promising platform for the safe and effective delivery of melittin, providing a viable strategy for cancer therapy. [ABSTRACT FROM AUTHOR]
ISSN:1226086X
DOI:10.1016/j.jiec.2025.08.012