Influence of polymer hydrophilicity/hydrophobicity and drug loading strategy (Free vs. polycaprolactone/chitosan nanoparticle-encapsulated) on tamoxifen-loaded polyvinyl alcohol and polycaprolactone nanofibers for breast cancer therapy

IF 5.2 3区医学 Q1 PHARMACOLOGY & PHARMACY

Journal of Drug Delivery Science and Technology Pub Date : 2026-03-01 Epub Date: 2026-01-29 DOI:10.1016/j.jddst.2026.108071

Samia Hammouda, Shimaa Husien, Noha El Salakawy, Wael Mamdouh

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Abstract

The development of effective localized drug delivery platforms is critical for enhancing tamoxifen (Tam) therapy in breast cancer (BC) treatment while minimizing systemic side effects. This study presents a comprehensive comparative evaluation of polyvinyl alcohol (PVA)- and polycaprolactone (PCL)-based nanofiber (NF) systems for Tam delivery, focusing on the impact of polymer hydrophilicity/hydrophobicity and Tam loading methos (Free Tam vs. Nanoparticle-encapsulated) on physicochemical characteristics and biological activities. Both NF systems successfully encapsulated Tam in amorphous form, with PCL-based NFs exhibiting larger fiber diameters (530–911 nm) compared to PVA-based NFs (160–270 nm), both of which mimic natural extracellular matrix components. Thermal analysis demonstrated superior drug stabilization by PCL-based NFs. In vitro release profiles revealed rapid release from PVA-based NFs (>90 % within 6 h), in contrast to controlled, biphasic release from PCL-based systems extending to 144 h in nanoparticle-encapsulated formulations under acidic conditions relevant to tumor microenvironments. Biologically, PVA-based NFs demonstrated 1.6-fold higher anticancer activity against MCF-7 cells (53 % vs. 32.7 % average cytotoxicity) due to faster drug availability but exhibited greater cytotoxicity to normal fibroblasts. Conversely, PCL-based NFs maintained 93 % biocompatibility with normal cells while providing enhanced antioxidant activity (39.3 %) and superior antibacterial performance, achieving inhibition zones up to 45 mm against Staphylococcus aureus. This comparative analysis highlights that PVA-based NFs are optimal for rapid therapeutic action, while PCL-based NFs provide sustained, controlled delivery suitable for long-term treatment with improved safety profiles. These findings emphasize the importance of polymer selection and nanoparticle incorporation in designing advanced drug delivery systems to improve breast cancer therapy outcomes.

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聚合物亲疏水性和载药策略（游离vs聚己内酯/壳聚糖纳米颗粒包封）对负载他莫昔芬的聚乙烯醇和聚己内酯纳米纤维用于乳腺癌治疗的影响

开发有效的局部给药平台对于加强他莫昔芬（Tam）在乳腺癌（BC）治疗中的治疗，同时最大限度地减少全身副作用至关重要。本研究对聚乙烯醇（PVA）和聚己内酯（PCL）纳米纤维（NF）系统进行了综合比较评价，重点研究了聚合物亲疏水性和Tam装载方式（自由Tam与纳米颗粒封装Tam）对物理化学特性和生物活性的影响。两种NF系统都成功地将Tam封装成无定形，与基于pvm的NF（160-270 nm）相比，基于pcl的NF具有更大的纤维直径（530-911 nm），两者都模拟了天然的细胞外基质成分。热分析表明pcl基NFs具有较好的药物稳定性。体外释放谱显示，pvm基NFs在6 h内快速释放（>90 %），相比之下，在与肿瘤微环境相关的酸性条件下，纳米颗粒封装配方中基于pcl的系统的可控双相释放可延长至144 h。生物学上，基于pva的NFs对MCF-7 细胞的抗癌活性高1.6倍（53. % vs. 32.7% %的平均细胞毒性），因为药物可用性更快，但对正常成纤维细胞表现出更大的细胞毒性。相反，基于pcl的NFs与正常细胞保持93 %的生物相容性，同时提供增强的抗氧化活性（39.3 %）和卓越的抗菌性能，对金黄色葡萄球菌的抑制区高达45 mm。这一对比分析强调，pva基NFs最适合快速治疗，而pcl基NFs提供持续、可控的长期治疗，安全性更高。这些发现强调了聚合物选择和纳米颗粒结合在设计先进的给药系统以改善乳腺癌治疗结果中的重要性。

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来源期刊

Journal of Drug Delivery Science and Technology 医学-药学

CiteScore

8.00

自引率

8.00%

发文量

879

审稿时长

94 days

期刊介绍： The Journal of Drug Delivery Science and Technology is an international journal devoted to drug delivery and pharmaceutical technology. The journal covers all innovative aspects of all pharmaceutical dosage forms and the most advanced research on controlled release, bioavailability and drug absorption, nanomedicines, gene delivery, tissue engineering, etc. Hot topics, related to manufacturing processes and quality control, are also welcomed.