Biofunctional Nanomaterials Group, School of Pharmacy, Queen's University Belfast, Medical Biology Centre, 97 Lisburn Road, Co Antrim, Belfast, Northern Ireland, BT9 7BL, UK.
Macromol Biosci. 2020 Jul;20(7):e2000115. doi: 10.1002/mabi.202000115. Epub 2020 Jun 2.
Peptide nanotubes are promising materials for a variety of biomedical applications with ultrashort (≤7 amino acids) forms providing particular promise for clinical translation. The manufacture of peptide nanotubes has, however, been associated with toxic organic solvents restricting clinical use. The purpose of this work is to formulate dipeptide nanotubes using mild techniques easily translated to industrial upscale and to characterize their physiochemical and biological properties. Phenylalanine-phenylalanine variants can be successfully formulated using distilled water as demonstrated here. Formulations are homogenous in shape (tubular), with apparent size (50-260 nm) and a zeta potential of up to +30 mV. L-(H N-FF-COOH), and D-enantiomers (H N-ff-COOH) demonstrate no toxicity against glioblastoma cells and are explored for ability to deliver a model hydrophilic molecule, sodium fluorescein, at pH 5.5 (tumor) and 7.4 (physiological). Peptide nanotubes loaded with >85% sodium fluorescein, demonstrate burst release characteristics, fitting the Weibull model of drug release. This research provides important data contributing to the pharmaceutical formulation of peptide nanotubes as drug delivery platforms for hydrophilic drugs.
肽纳米管是一种很有前途的生物医学材料，其中超短（≤7 个氨基酸）形式特别有希望用于临床转化。然而，肽纳米管的制造与有毒有机溶剂有关，限制了其临床应用。本工作的目的是使用温和的技术来制备二肽纳米管，这些技术易于转化为工业放大，并对其理化和生物学特性进行表征。如本文所示，苯丙氨酸-苯丙氨酸变体可以成功地用水合作用来制备。制剂在形状（管状）、表观尺寸（50-260nm）和zeta 电位高达+30mV 上是均匀的。L-（H N-FF-COOH）和 D-对映体（H N-ff-COOH）对神经胶质瘤细胞没有毒性，并探索了在 pH5.5（肿瘤）和 7.4（生理）下传递模型亲水分子，荧光素钠的能力。负载超过 85%荧光素钠的肽纳米管具有爆发释放特性，符合药物释放的 Weibull 模型。本研究提供了重要的数据，有助于将肽纳米管作为亲水性药物的药物传递平台进行药物制剂。
