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<p>Nanomedicine has enormous potential in the diagnosis and treatment of malignant neoplasms. However, the clinical translation of various nanoparticles (NPs) as drug delivery systems (DDSs) for tumor therapy remains poor. The main bottleneck is the limited database on the correlation between the design of NPs with unique physicochemical features and their therapeutic efficiency. In this study, we aim to design and investigate structurally variant nanocarriers composed of polylactide (PLA), silicon dioxide (SiO<sub>2</sub>), calcium carbonate (CaCO<sub>3</sub>), and barium carbonate (BaCO<sub>3</sub>) to reveal the relationship between their physicochemical features and therapeutic effectiveness against melanoma in vitro and in vivo. Specifically, we (1) examined their morphology, size, and structural characteristics; (2) evaluated colloidal stability; (3) verified the drug-loading and release efficiency of a 2-aminothiophene scaffold (2AmT); (4) investigated cellular uptake and tumor spheroid penetration efficiency; (5) analyzed in vivo biodistribution; and (6) estimated therapeutic efficiency. The main characteristics of inorganic and organic NPs were collected and compared systematically. Considering the advantages and drawbacks of each NP type, the following tumor growth inhibition against melanoma was observed: CaCO<sub>3</sub> (87.9%–93.4% for 0.4 g/kg of 2AmT)&gt;SiO<sub>2</sub> (75.6%–93.2% for 0.4 g/kg of 2AmT)&gt;PLA (80.3%–88.2% for 0.4 g/kg of 2AmT)&gt;BaCO<sub>3</sub> (58.8%–83.7% for 0.4 g/kg of 2AmT). Thus, this study contributes to the development of fundamental nanomedicine and accelerates the clinical translation of nanocarriers for effective melanoma therapy.</p>

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Design and manufacturing of structurally variant nanocarriers for boosting localized chemotherapy against melanoma

  • 期刊论文

  • 发表日期：

    2026年5月18日

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  • Timofey E. Karpov,
  • Anna Rogova,
  • Yulia A. Tishchenko,
  • Irina A. Gorbunova,
  • Radmila R. Sergeeva,
  • Sofya V. Faizullina,
  • Thanh Son Cam,
  • Konstantin Chebyshev,
  • Anastasia S. Khapugina,
  • Eugenia J. Platonova,
  • Ivan N. Gaponenko,
  • Alena I. Shakirova,
  • Sergei A. Shipilovskikh,
  • Alexander S. Timin

摘要

Nanomedicine has enormous potential in the diagnosis and treatment of malignant neoplasms. However, the clinical translation of various nanoparticles (NPs) as drug delivery systems (DDSs) for tumor therapy remains poor. The main bottleneck is the limited database on the correlation between the design of NPs with unique physicochemical features and their therapeutic efficiency. In this study, we aim to design and investigate structurally variant nanocarriers composed of polylactide (PLA), silicon dioxide (SiO2), calcium carbonate (CaCO3), and barium carbonate (BaCO3) to reveal the relationship between their physicochemical features and therapeutic effectiveness against melanoma in vitro and in vivo. Specifically, we (1) examined their morphology, size, and structural characteristics; (2) evaluated colloidal stability; (3) verified the drug-loading and release efficiency of a 2-aminothiophene scaffold (2AmT); (4) investigated cellular uptake and tumor spheroid penetration efficiency; (5) analyzed in vivo biodistribution; and (6) estimated therapeutic efficiency. The main characteristics of inorganic and organic NPs were collected and compared systematically. Considering the advantages and drawbacks of each NP type, the following tumor growth inhibition against melanoma was observed: CaCO3 (87.9%–93.4% for 0.4 g/kg of 2AmT)>SiO2 (75.6%–93.2% for 0.4 g/kg of 2AmT)>PLA (80.3%–88.2% for 0.4 g/kg of 2AmT)>BaCO3 (58.8%–83.7% for 0.4 g/kg of 2AmT). Thus, this study contributes to the development of fundamental nanomedicine and accelerates the clinical translation of nanocarriers for effective melanoma therapy.