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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]
Copyright of Journal of Industrial & Engineering Chemistry is the property of Elsevier B.V. and its content may not be copied or emailed to multiple sites without the copyright holder's express written permission. Additionally, content may not be used with any artificial intelligence tools or machine learning technologies. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)
Database: Engineering Source
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Header DbId: egs
DbLabel: Engineering Source
An: 191448295
AccessLevel: 6
PubType: Periodical
PubTypeId: serialPeriodical
PreciseRelevancyScore: 0
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  Label: Title
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  Data: Nanoarchitectonics of melittin-based polymersomes inducing lysosomal rupture for anticancer therapy.
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  Data: <searchLink fieldCode="AR" term="%22Cho%2C+Youngheun%22">Cho, Youngheun</searchLink><relatesTo>1</relatesTo> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Moon%2C+Jooho%22">Moon, Jooho</searchLink><relatesTo>1</relatesTo> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Han%2C+Hyounkoo%22">Han, Hyounkoo</searchLink><relatesTo>2</relatesTo> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Park%2C+Suhyeon%22">Park, Suhyeon</searchLink><relatesTo>2</relatesTo> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Lim%2C+Yeon-Su%22">Lim, Yeon-Su</searchLink><relatesTo>3</relatesTo> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Lee%2C+Hee-Young%22">Lee, Hee-Young</searchLink><relatesTo>3</relatesTo> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Jin%2C+Kyeong+Sik%22">Jin, Kyeong Sik</searchLink><relatesTo>4</relatesTo> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Kim%2C+Junmin%22">Kim, Junmin</searchLink><relatesTo>1</relatesTo> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Nam%2C+Soobin%22">Nam, Soobin</searchLink><relatesTo>1</relatesTo> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Park%2C+Minwoo%22">Park, Minwoo</searchLink><relatesTo>5</relatesTo> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Kim%2C+Hyeong+Jun%22">Kim, Hyeong Jun</searchLink><relatesTo>5</relatesTo> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Kim%2C+Hyuncheol%22">Kim, Hyuncheol</searchLink><relatesTo>1,6</relatesTo> (AUTHOR)<i> hyuncheol@sogang.ac.kr</i>
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  Data: <searchLink fieldCode="JN" term="%22Journal+of+Industrial+%26+Engineering+Chemistry%22">Journal of Industrial & Engineering Chemistry</searchLink>. Mar2026, Vol. 155, p639-648. 10p.
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  Data: <searchLink fieldCode="DE" term="%22Polymersomes%22">Polymersomes</searchLink><br /><searchLink fieldCode="DE" term="%22Lysosomes%22">Lysosomes</searchLink><br /><searchLink fieldCode="DE" term="%22Melittin%22">Melittin</searchLink><br /><searchLink fieldCode="DE" term="%22Nanoparticles%22">Nanoparticles</searchLink><br /><searchLink fieldCode="DE" term="%22Ligands+%28Biochemistry%29%22">Ligands (Biochemistry)</searchLink><br /><searchLink fieldCode="DE" term="%22Antineoplastic+agents%22">Antineoplastic agents</searchLink><br /><searchLink fieldCode="DE" term="%22Cell+receptors%22">Cell receptors</searchLink><br /><searchLink fieldCode="DE" term="%22Drug+delivery+systems%22">Drug delivery systems</searchLink>
– Name: Abstract
  Label: Abstract
  Group: Ab
  Data: 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]
– Name: AbstractSuppliedCopyright
  Label:
  Group: Ab
  Data: <i>Copyright of Journal of Industrial & Engineering Chemistry is the property of Elsevier B.V. and its content may not be copied or emailed to multiple sites without the copyright holder's express written permission. Additionally, content may not be used with any artificial intelligence tools or machine learning technologies. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract.</i> (Copyright applies to all Abstracts.)
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RecordInfo BibRecord:
  BibEntity:
    Identifiers:
      – Type: doi
        Value: 10.1016/j.jiec.2025.08.012
    Languages:
      – Code: eng
        Text: English
    PhysicalDescription:
      Pagination:
        PageCount: 10
        StartPage: 639
    Subjects:
      – SubjectFull: Polymersomes
        Type: general
      – SubjectFull: Lysosomes
        Type: general
      – SubjectFull: Melittin
        Type: general
      – SubjectFull: Nanoparticles
        Type: general
      – SubjectFull: Ligands (Biochemistry)
        Type: general
      – SubjectFull: Antineoplastic agents
        Type: general
      – SubjectFull: Cell receptors
        Type: general
      – SubjectFull: Drug delivery systems
        Type: general
    Titles:
      – TitleFull: Nanoarchitectonics of melittin-based polymersomes inducing lysosomal rupture for anticancer therapy.
        Type: main
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            NameFull: Cho, Youngheun
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            NameFull: Moon, Jooho
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            – D: 25
              M: 03
              Text: Mar2026
              Type: published
              Y: 2026
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