Institute of Materials Science and Nanotechnology, National Nanotechnology Research Center (UNAM), Bilkent University, Ankara, 06800, Turkey.
Biomater Sci. 2016 Dec 20;5(1):67-76. doi: 10.1039/c6bm00656f.
Peptide amphiphiles (PAs) self-assemble into supramolecular nanofiber gels that provide a suitable environment for encapsulation of both hydrophobic and hydrophilic molecules. The PA gels have significant advantages for controlled delivery applications due to their high capacity to retain water, biocompatibility, and biodegradability. In this study, we demonstrate injectable supramolecular PA nanofiber gels for drug delivery applications. Doxorubicin (Dox), as a widely used chemotherapeutic drug for breast cancer treatment, was encapsulated within the PA gels prepared at different concentrations. Physical and chemical properties of the gels were characterized, and slow release of the Dox molecules through the supramolecular PA nanofiber gels was studied. In addition, the diffusion constants of the drug molecules within the PA nanofiber gels were estimated using fluorescence recovery after the photobleaching (FRAP) method. The PA nanofiber gels did not show any cytotoxicity and the encapsulation strategy enhanced the activity of drug molecules on cellular viability through prolonged release compared to direct administration under in vitro conditions. Moreover, the local in vivo injection of the Dox encapsulated PA nanofiber gels (Dox/PA) to the tumor site demonstrated the lowest tumor growth rate compared to the direct Dox injection and increased the apoptotic cells within the tumor tissue for local drug release through the PA nanofiber gels under in vivo conditions.
肽两亲物（PAs）自组装成超分子纳米纤维凝胶，为封装疏水性和亲水性分子提供了合适的环境。由于其高持水能力、生物相容性和可生物降解性，PA 凝胶在控制释放应用中具有显著优势。在这项研究中，我们展示了可注射的超分子 PA 纳米纤维凝胶在药物输送中的应用。阿霉素（Dox）作为一种广泛用于乳腺癌治疗的化疗药物，被包裹在不同浓度制备的 PA 凝胶中。对凝胶的物理化学性质进行了表征，并研究了 Dox 分子通过超分子 PA 纳米纤维凝胶的缓慢释放。此外，还使用荧光恢复后光漂白（FRAP）法估计了药物分子在 PA 纳米纤维凝胶中的扩散常数。PA 纳米纤维凝胶没有显示出任何细胞毒性，并且与直接给药相比，通过延长释放时间，封装策略增强了药物分子在细胞活力方面的活性，在体外条件下。此外，与直接 Dox 注射相比，将包裹 Dox 的 PA 纳米纤维凝胶（Dox/PA）局部注射到肿瘤部位，在体内条件下通过 PA 纳米纤维凝胶进行局部药物释放，肿瘤组织中凋亡细胞的数量增加，肿瘤生长速度最慢。
