Division of Molecular Pharmaceutics, and the Center for Nanotechnology in Drug Delivery, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, NC 27514, United States.
Int J Pharm. 2010 Nov 30;401(1-2):87-92. doi: 10.1016/j.ijpharm.2010.09.003. Epub 2010 Sep 15.
The present studies were aimed at investigating the engineering of NPs with protein-conjugated-surfactant at their surface. In order to increase the immunogenicity of a protein antigen, Brij 78 was functionalized by tresyl chloride and then further reacted with the primary amine of the model proteins ovalbumin (OVA) or horseradish peroxide (HRP). The reaction yielded Brij 78-OVA and Brij 78-HRP conjugates which were then used directly to form NP-OVA or NP-HRP using a one-step warm oil-in-water microemulsion precursor method with emulsifying wax as the oil phase, and Brij 78 and the Brij 78-OVA or Brij 78-HRP conjugate as surfactants. Similarly, Brij 700 was conjugated to HIV p24 antigen to yield Brij 700-p24 conjugate. The utility of these NPs for enhancing the immune responses to protein-based vaccines was evaluated in vivo using ovalbumin (OVA) as model protein and p24 as a relevant HIV antigen. In separate in vivo studies, female BALB/c mice were immunized by subcutaneous (s.c.) injection with NP-OVA and NP-p24 formulations along with several control formulations. These results suggested that with multiple antigens, covalent attachment of the antigen to the NP significantly enhanced antigen-specific immune responses. This facile covalent conjugation and incorporation method may be utilized to further incorporate other protein antigens, even multiple antigens, into an enhanced vaccine delivery system.
本研究旨在探索通过在纳米颗粒(NPs)表面偶联蛋白修饰剂来对其进行工程化处理。为了提高蛋白质抗原的免疫原性,先用三氯甲烷对 Brij 78 进行功能化修饰,然后使其与模型蛋白卵清蛋白(OVA)或辣根过氧化物酶(HRP)的伯胺进一步反应。反应生成 Brij 78-OVA 和 Brij 78-HRP 缀合物,然后直接使用一步法温油包水微乳液前体法,将乳化蜡作为油相,Brij 78 和 Brij 78-OVA 或 Brij 78-HRP 缀合物作为表面活性剂,形成 NP-OVA 或 NP-HRP。同样,将 Brij 700 与 HIV p24 抗原缀合,得到 Brij 700-p24 缀合物。使用该 NP 增强基于蛋白质的疫苗的免疫反应的实用性,通过以卵清蛋白(OVA)为模型蛋白和 p24 为相关 HIV 抗原进行体内研究。在单独的体内研究中,雌性 BALB/c 小鼠通过皮下(s.c.)注射 NP-OVA 和 NP-p24 制剂以及几种对照制剂进行免疫。这些结果表明,对于多种抗原,将抗原共价连接到 NP 上可显著增强抗原特异性免疫反应。这种简便的共价偶联和掺入方法可用于进一步将其他蛋白质抗原,甚至多种抗原,掺入增强的疫苗递送系统中。