Skip to content
DraconiticResearch
Search Sources API
190,869 studies31 sourcesUpdated 42 min ago
Peer-reviewedCC BYActa naturae

A Targeted Liposomal Delivery System for Hydrophobic Antitumor Compounds Using the Example of a 1,2,3,4-Tetrahydroisoquinoline Derivative.

  • G M Proshkina1
  • O N Ashirov2
  • M N Zharkov3
  • A Al-Khadj Aioub3
  • V I Vinogradova2
  • D Zhu4
  • R Yan5
  • Sh S Azimova2
  • E I Shramova1
  • N A Pyataev3
  • S M Deyev1,3,6
6 affiliations
  1. 1Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, Moscow, 117997 Russia.
  2. 2Yunusov Institute of the Chemistry of Plant Substances, Academy of Sciences of the Republic of Uzbekistan, Tashkent, 100170 Uzbekistan.
  3. 3Ogarev National Research Mordovia State University, Saransk, 430005 Russia.
  4. 4Center of Advanced Pharmaceuticals and Biomaterials, China Pharmaceutical University, Nanjing, 211198 China.
  5. 5School of Science, China Pharmaceutical University, Nanjing, 211198 China.
  6. 6Moscow Engineering Physics Institute, National Research Nuclear University "MEPhI", Moscow, 115409 Russia.
Read full textPDFDOICite

Abstract

Cancer is the second leading cause of death worldwide, after cardiovascular disorders. One of the main constraints of anticancer agents is their limited water solubility, which complicates preclinical in vivo studies. In this work, we propose a versatile approach for stabilizing hydrophobic antitumor agents using liposomes based on natural phospholipids. The efficacy of the method is demonstrated for hydrophobic 1-tridecyl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline, a promising tetrahydroisoquinoline derivative with proven antitumor activity against lymphoid and epithelial cancer cells. We show that the liposomal formulation ensures drug stability in aqueous media. Modification of the liposome surface with a HER2-specific non-immunoglobulin module strongly improved targeting efficiency. The targeting index differed markedly between cells with low versus high HER2 expression levels (3.02 and 18.98, respectively), demonstrating that the targeted liposomal formulation exerts a substantially enhanced cytotoxicity against HER2-overexpressing cells. The proposed liposomal platform can also be utilized to deliver other hydrophobic anticancer drugs.

Related

  1. Safety and Antitumor Activity of the Usnic Acid Derivative OL9-116, a TDP1 Inhibitor, as an Adjunctive Therapy in Combination with Topotecan
    Tatyana E. Kornienko, Alexandra L. Zakharenko, Irina A. Chernyshova +12
    International Journal of Molecular SciencesPeer-reviewedCC BY 4.0Full textMolecular biology & gene regulationCrossrefEurope PMC
  2. Next-Generation Liposomal and Nanoparticle-Based Systems for Glioblastoma: Molecular Targeting Strategies to Overcome the Blood–Brain Barrier
    Joaquin Fiallo Arroyo, Bernardo Castellón, Jose E. Leon-Rojas
    International journal of molecular sciencesPeer-reviewedCC BYFull textGeneral biochemistryEurope PMC
  3. In situ CAR-M engineered by liposomal mRNA nanomedicine remodels fibrotic microenvironment for ameliorating liver fibrosis
    Hong Xiao, Xiaoxia Li, Kaimin Cai +5
    Science AdvancesPeer-reviewedCC BY-NCFull textMolecular biology & gene regulationCrossrefEurope PMC
  4. Waste-to-Nanomedicine: Scalable Production of Apple Pomace Nanovesicle-Enriched Fractions as Nanocarriers for Hydrophobic Bioactives at the Intestinal Epithelial Interface
    Edoardo Bertania, Angelo Modena, Elia Bari +13
    Sustainable Food TechnologyPeer-reviewedCC BYFull textMolecular biology & gene regulationHAL
  5. A tertiary network couples hydrophobic substitutions to terminal contacts in an IDP
    Lindsey M. Riggs, Ruchi Lohia, Grace Brannigan
    ChemRxivPreprintCC BYMolecular biology & gene regulationChemRxiv

Cite

BibTeXRIS
BibTeX
@article{proshkina2026targeted,
  title = {{A Targeted Liposomal Delivery System for Hydrophobic Antitumor Compounds Using the Example of a 1,2,3,4-Tetrahydroisoquinoline Derivative.}},
  author = {G M Proshkina and O N Ashirov and M N Zharkov and A Al-Khadj Aioub and V I Vinogradova and D Zhu and R Yan and Sh S Azimova and E I Shramova and N A Pyataev and S M Deyev},
  journal = {Acta naturae},
  year = {2026},
  month = jul,
  doi = {10.32607/actanaturae.28027},
  url = {https://europepmc.org/article/MED/42960371},
  note = {CC BY},
}
RIS
TY  - JOUR
TI  - A Targeted Liposomal Delivery System for Hydrophobic Antitumor Compounds Using the Example of a 1,2,3,4-Tetrahydroisoquinoline Derivative.
AU  - G M Proshkina
AU  - O N Ashirov
AU  - M N Zharkov
AU  - A Al-Khadj Aioub
AU  - V I Vinogradova
AU  - D Zhu
AU  - R Yan
AU  - Sh S Azimova
AU  - E I Shramova
AU  - N A Pyataev
AU  - S M Deyev
PY  - 2026
DA  - 2026/07/01
JO  - Acta naturae
DO  - 10.32607/actanaturae.28027
UR  - https://europepmc.org/article/MED/42960371
AB  - Cancer is the second leading cause of death worldwide, after cardiovascular disorders. One of the main constraints of anticancer agents is their limited water solubility, which complicates preclinical in vivo studies. In this work, we propose a versatile approach for stabilizing hydrophobic antitumor agents using liposomes based on natural phospholipids. The efficacy of the method is demonstrated for hydrophobic 1-tridecyl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline, a promising tetrahydroisoquinoline derivative with proven antitumor activity against lymphoid and epithelial cancer cells. We show that the liposomal formulation ensures drug stability in aqueous media. Modification of the liposome surface with a HER2-specific non-immunoglobulin module strongly improved targeting efficiency. The targeting index differed markedly between cells with low versus high HER2 expression levels (3.02 and 18.98, respectively), demonstrating that the targeted liposomal formulation exerts a substantially enhanced cytotoxicity against HER2-overexpressing cells. The proposed liposomal platform can also be utilized to deliver other hydrophobic anticancer drugs.
SN  - 2075-8251
ER  -