Peptide functionalized graphene oxide derivatives for drug and gene delivery

基于石墨烯的纳米材料已经扩大了其在生物医学上的应用，从生物传感器和成像到组织工程的支架，再到癌症治疗中的药物和基因传递。特别是，氧化石墨烯衍生物（GODs）是药物/基因传递领域深入研究的主要焦点，因为它们的氧官能使它们可溶于水生物介质。god可以通过共价键和非共价键与生物分子相互作用，这为靶向药物递送提供了更多机会。特异性靶向、有效的药物释放和细胞内运输是药物传递系统中最重要的要求。GOD交付性能还有待优化以满足所有这些要求。另一方面，多肽是一类重要的生物材料，提供独特的生物功能，如靶向、抗菌活性、细胞渗透和免疫治疗。在这里，我们提出探索肽功能化god在药物和基因传递中的可能性，根据它们的功能通用性和可调性。该团队由滑铁卢大学的研究人员和他们的行业合作伙伴Zerocor组成，他们将首先尝试了解肽和GOD之间的相互作用，以及不同肽和治疗药物之间在GOD结合方面的竞争。这部分的研究将为如何构建与不同类型肽功能化的基于god的药物载体提供信息。god -肽/药物复合物的物理化学性质将使用各种技术进行研究和表征，以揭示细胞摄取机制和细胞膜相互作用。该团队随后将研究选定数量的药物-肽- god复合物在肿瘤细胞靶向、溶酶体逃逸和触发药物/货物释放方面的功能。优化后的GOD/肽/药物复合物的配方将通过尺寸分布、组装形态、药物负载和功效来测试其在生理相关溶液中的稳定性。最终，基于god的多功能药物输送系统有望在未来的体内试验中获得。

Graphene-based nanomaterials have expanded their applications to biomedicine, ranging from biosensors andimaging to scaffolds for tissue engineering to drug and gene delivery in cancer treatment. In particular,graphene oxide derivatives (GODs) are the main focus of the intensive research in the field of drug/genedelivery, due to their oxygen functionalities that make them soluble in aqueous biological media. GODs caninteract with biological molecules through both covalent and non-covalent bonds that opens up moreopportunities in for targeted drug delivery. Specific targeting, efficient drug release and intracellular traffickingare the most important requirements in a drug delivery system. The GOD delivery performance has yet to beoptimized to meet all these requirements. On the other hand, peptides are an important class of biomaterialbuilding blocks, providing unique bio-functions such as targeting, antimicrobial activity, cell penetration, andimmunotherapy. Here, we propose to explore the possibility of peptide functionalized GODs in drug and genedelivery, in terms of their functional versatility and tunability. The team, consisting of University of Waterlooresearchers and their industry partner, Zerocor, will first try to understand the interaction between peptide andGOD, and the competition among different peptides and therapeutic drugs on GOD binding. This part of studywill provide information on how to construct GOD-based drug carriers that functionalize with different typesof peptides. The physicochemical properties of the GOD-peptide/drug complexes will be investigated andcharacterized using a variety of techniques, to reveal cellular uptake mechanisms and cell membraneinteractions. The team will subsequently study the functions of a selected number of drug-peptide-GODcomplexes, in terms of tumor cell targeting, lysosomal escape and triggered drug/cargo release. Optimizedformulations of GOD/peptide/drug complexes will be tested for their stability in physiologically relevantsolutions by means of size distribution, assembly morphology, drug loading and efficacy. Eventually, themultifunctional GOD-based drug delivery system is expected to be obtained for future in vivo tests.