Ahmad Ikhlaque, Khan Muhammad Farhan Ali, Rahdar Abbas, Hussain Saddam, Tareen Fahad Khan, Salim Muhammad Waqas, Ajalli Narges, Amirzada Muhammad Imran, Khan Ahmad
Department of Pharmacy, Faculty of Biological Sciences, Quaid-i-Azam University, Islamabad 45320, Pakistan.
Department of Physics, Faculty of Science, University of Zabol, Zabol 98613-35856, Iran.
Polymers (Basel). 2022 Jun 14;14(12):2403. doi: 10.3390/polym14122403.
Cancer is the most common cause of mortality worldwide. There is dire need of modern strategies-such as surface modification of nanocarriers-to combat this global illness. Incorporation of active targeting ligands has arisen as a novel platform for specific tumor targeting. The aim of the current study was to formulate PEG-protamine complex (PPC) of doxorubicin (DOX) for treatment of breast cancer (BC). DOX coupling with PEG can enhance cell-penetrating ability: combating resistance in MDA-MB 231 breast cancer cells. Ionic gelation method was adopted to fabricate a pH sensitive nanocomplex. The optimized nanoformulation was characterized for its particle diameter, zeta potential, surface morphology, entrapment efficiency, crystallinity, and molecular interaction. In vitro assay was executed to gauge the release potential of nanoformulation. The mean particle size, zeta potential, and polydispersity index (PDI) of the optimized nanoparticles were observed to be 212 nm, 15.2 mV, and 0.264, respectively. Crystallinity studies and Fourier transform infrared (FTIR) analysis revealed no molecular interaction and confirmed the amorphous nature of drug within nanoparticles. The in vitro release data indicate sustained drug release at pH 4.8, which is intracellular pH of breast cancer cells, as compared to the drug solution. PPC loaded with doxorubicin can be utilized as an alternative and effective approach for specific targeting of breast cancer.
癌症是全球最常见的死亡原因。迫切需要现代策略，如纳米载体的表面修饰，来对抗这种全球性疾病。引入活性靶向配体已成为一种新型的特异性肿瘤靶向平台。本研究的目的是制备用于治疗乳腺癌（BC）的阿霉素（DOX）聚乙二醇-鱼精蛋白复合物（PPC）。DOX与聚乙二醇偶联可增强细胞穿透能力，对抗MDA-MB 231乳腺癌细胞的耐药性。采用离子凝胶法制备了一种pH敏感纳米复合物。对优化后的纳米制剂进行了粒径、zeta电位、表面形态、包封率、结晶度和分子相互作用等表征。进行体外试验以评估纳米制剂的释放潜力。观察到优化后的纳米颗粒的平均粒径、zeta电位和多分散指数（PDI）分别为212nm、15.2mV和0.264。结晶度研究和傅里叶变换红外（FTIR）分析表明没有分子相互作用，并证实了纳米颗粒内药物的无定形性质。体外释放数据表明，与药物溶液相比，在乳腺癌细胞的细胞内pH值4.8时药物持续释放。负载阿霉素的PPC可作为乳腺癌特异性靶向的一种替代且有效的方法。
