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Pharmaceutical Formulation and Characterization of Dipeptide Nanotubes for Drug Delivery Applications.
Macromolecular Bioscience ( IF 4.4 ) Pub Date : 2020-06-02 , DOI: 10.1002/mabi.202000115
Simon L Porter 1 , Sophie M Coulter 1 , Sreekanth Pentlavalli 1 , Garry Laverty 1
Affiliation  

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‐(H2N‐FF‐COOH), and D‐enantiomers (H2N‐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.

中文翻译:

用于药物递送应用的二肽纳米管的药物配方和表征。

肽纳米管是用于多种生物医学应用的有前途的材料,具有超短(≤7个氨基酸)的形式,为临床翻译提供了特别的希望。然而,肽纳米管的制造已经与有毒的有机溶剂相关联,从而限制了临床用途。这项工作的目的是使用易于转化为工业规模的温和技术来配制二肽纳米管,并表征其理化和生物学特性。如此处所示,可以使用蒸馏水成功配制苯丙氨酸-苯丙氨酸变体。制剂的形状均一(管状),表观大小(50-260 nm),ζ电位高达+30 mV。L-(H 2 N-FF-COOH)和D-对映体(H 2N-ff-COOH)对胶质母细胞瘤细胞无毒性,并探索了在pH 5.5(肿瘤)和7.4(生理)下提供模型亲水分子荧光素钠的能力。载有> 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。这项研究提供了重要的数据,这些数据有助于肽纳米管的药物制剂作为亲水性药物的药物递送平台。
更新日期:2020-06-02
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