Divanach Peter, Noti Antzela, Vouvopoulos Panagiotis, Athanasiou Thanasis, Kountourakis Nikos, Harmandaris Vagelis, Rissanou Anastassia N, Mitraki Anna
Department of Materials Science and Engineering, University of Crete, Voutes Campus, GR-70013 Heraklion, Greece.
Institute of Electronic Structure and Laser, Foundation for Research and Technology-Hellas (FORTH), Nikolaou Plastira 100, Vassilika Vouton, GR-70013 Heraklion, Greece.
Biomolecules. 2025 Jun 8;15(6):839. doi: 10.3390/biom15060839.
One major public health issue is cancer chemotherapy; despite constant progress in the area, administration of anticancer drugs to patients is often associated with serious side effects. It is therefore imperative to develop vehicles for encapsulation and controlled delivery of such drugs. Anticancer drugs include small peptide drugs, such as Bortezomib (BTZ). Self-assembling peptides have been recently reported as promising drug delivery agents. The research reported here proposes the encapsulation of BTZ into peptide hydrogels formed by the self-assembling FmocFF dipeptide as delivery vehicle. We selected FmocFF as an encapsulation vehicle based on our previous simulation study on the complexation propensity of Bortezomib (BTZ) with various peptide gelators. Herein we undertook additional computational studies that highlight the benefits of FmocFF as a potential effective nanocarrier for BTZ combined with experiments of encapsulation and evaluation of BTZ release. Based on these computational and experimental results, we propose the Fmoc-FF dipeptide hydrogel as a promising matrix for the controlled delivery of BTZ.
一个主要的公共卫生问题是癌症化疗；尽管该领域不断取得进展，但给患者使用抗癌药物往往会伴随严重的副作用。因此，开发用于封装和控制此类药物递送的载体势在必行。抗癌药物包括小肽药物，如硼替佐米（BTZ）。最近有报道称自组装肽是很有前景的药物递送剂。此处报道的研究提出将BTZ封装到由自组装的FmocFF二肽形成的肽水凝胶中作为递送载体。基于我们之前对硼替佐米（BTZ）与各种肽胶凝剂络合倾向的模拟研究，我们选择FmocFF作为封装载体。在此，我们进行了额外的计算研究，突出了FmocFF作为BTZ潜在有效纳米载体的优势，并结合了BTZ的封装实验和释放评估。基于这些计算和实验结果，我们提出Fmoc-FF二肽水凝胶是一种很有前景的用于BTZ控释的基质。
