Scholarlink

<p>Melanoma is among the most aggressive forms of skin cancer, characterized by high metastatic potential and limited responsiveness to conventional chemotherapy. Paclitaxel (PTX) is an efficacious anticancer agent; however, its clinical utility in melanoma is restricted by poor aqueous solubility, non-specific biodistribution, and dose-limiting systemic toxicity. To overcome these limitations, this study aimed to develop and evaluate folate-targeted poly(lactic-co-glycolic acid) nanoparticles (FA-PTX-PLGA-NPs) as a targeted nanotherapeutic approach for melanoma treatment. Paclitaxel-loaded PLGA nanoparticles were synthesized through an emulsion–solvent evaporation process, followed by surface functionalization with folic acid to promote targeting by folate receptor. Nanosized particle formation with acceptable stability and drug encapsulation was confirmed by physicochemical characterization. The anticancer efficacy of FA-PTX-PLGA-NPs in B16 melanoma cells was assessed using cell viability and apoptosis assays compared with free paclitaxel and non-targeted PTX-PLGA nanoparticles. The findings indicated a distinct formulation-dependent therapeutic response. The most pronounced reduction in cell viability (25.94 ± 5.18%) was observed with FA-PTX-PLGA-NPs compared to free PTX (59.07 ± 5.98%) and PTX-PLGA nanoparticles (42.90 ± 4.10%). Consistently, apoptosis analysis revealed a significant increase in apoptotic cell populations following treatment with FA-PTX-PLGA-NPs (68.47 ± 6.53%) compared to free PTX and non-targeted nanoparticles (<i>p</i> &lt; 0.001). These observations suggest that the increased anticancer potency is primarily mediated through apoptosis, with a strong association to folate receptor–mediated cellular uptake. Finally, folate-targeted PLGA nanoparticles could markedly enhance the therapeutic properties of paclitaxel against melanoma by improving intracellular drug delivery and promoting apoptotic cell death. It is worth noting that such a targeted nanocarrier platform may present a promising platform for melanoma chemotherapy and needs to be further evaluated in vivo to show its translational potential. This study presents a novel folate-targeted PLGA nanoparticle system for enhanced delivery of paclitaxel in melanoma cells, demonstrating improved cytotoxic and apoptotic effects compared to non-targeted nanoparticles.</p>

错误：搜索内容不能为空，请输入英文关键词
错误：关键词超出字数限制，请精简
高级检索

Folate-targeted PLGA nanoparticles enhance paclitaxel-induced cytotoxicity and apoptosis in B16 melanoma cells

  • 期刊论文

  • 出版模式：

    开放获取

  • 发表日期：

    2026年5月7日

查看全文
  • Zena Hasan Sahib,
  • Entisar Al-Muhktar,
  • Fizel Alhimyari,
  • Entidhar Jasim Khamees

摘要

Melanoma is among the most aggressive forms of skin cancer, characterized by high metastatic potential and limited responsiveness to conventional chemotherapy. Paclitaxel (PTX) is an efficacious anticancer agent; however, its clinical utility in melanoma is restricted by poor aqueous solubility, non-specific biodistribution, and dose-limiting systemic toxicity. To overcome these limitations, this study aimed to develop and evaluate folate-targeted poly(lactic-co-glycolic acid) nanoparticles (FA-PTX-PLGA-NPs) as a targeted nanotherapeutic approach for melanoma treatment. Paclitaxel-loaded PLGA nanoparticles were synthesized through an emulsion–solvent evaporation process, followed by surface functionalization with folic acid to promote targeting by folate receptor. Nanosized particle formation with acceptable stability and drug encapsulation was confirmed by physicochemical characterization. The anticancer efficacy of FA-PTX-PLGA-NPs in B16 melanoma cells was assessed using cell viability and apoptosis assays compared with free paclitaxel and non-targeted PTX-PLGA nanoparticles. The findings indicated a distinct formulation-dependent therapeutic response. The most pronounced reduction in cell viability (25.94 ± 5.18%) was observed with FA-PTX-PLGA-NPs compared to free PTX (59.07 ± 5.98%) and PTX-PLGA nanoparticles (42.90 ± 4.10%). Consistently, apoptosis analysis revealed a significant increase in apoptotic cell populations following treatment with FA-PTX-PLGA-NPs (68.47 ± 6.53%) compared to free PTX and non-targeted nanoparticles (p < 0.001). These observations suggest that the increased anticancer potency is primarily mediated through apoptosis, with a strong association to folate receptor–mediated cellular uptake. Finally, folate-targeted PLGA nanoparticles could markedly enhance the therapeutic properties of paclitaxel against melanoma by improving intracellular drug delivery and promoting apoptotic cell death. It is worth noting that such a targeted nanocarrier platform may present a promising platform for melanoma chemotherapy and needs to be further evaluated in vivo to show its translational potential. This study presents a novel folate-targeted PLGA nanoparticle system for enhanced delivery of paclitaxel in melanoma cells, demonstrating improved cytotoxic and apoptotic effects compared to non-targeted nanoparticles.