Bobbala Sharan, Vincent Michael P, Scott Evan A
Department of Biomedical Engineering, Northwestern University, Evanston, Illinois, USA.
Nanoscale. 2021 Jul 8;13(26):11349-11359. doi: 10.1039/d1nr02188e.
Two major obstacles that limit the widespread usage of polymeric nanocarriers include the complexity of formulation methods and their stability during storage. To address both of these issues, here we present morphologically complex nanocarriers in a hydratable powder form, which bypasses the need for expensive, harsh, and/or time-consuming nanocarrier fabrication techniques. The powders are composed of carbohydrates and self-assembling polymer amphiphiles having a low glass transition temperature. Hydration requires less than one minute and only involves the addition of aqueous media (water or saline) to rapidly obtain self-assembled micelles, worm-like micelles (i.e. filomicelles), or polymersomes from poly(ethylene glycol)-b-poly(propylene sulfide) (PEG-b-PPS) polymers. The formulated powders are highly stable, achieving hydration into monodisperse nanocarriers following >6 months of storage. Diverse drug cargoes were efficiently encapsulated during hydration, including hydrophobic small molecules for micellar morphologies, as well as individual and concurrent loading of both hydrophobic and hydrophilic molecules for vesicular morphologies. Hydrated polymersomes are shown to load hydrophilic biological macromolecules, and encapsulated enzymes retain bioactivity. Furthermore, we demonstrate that inclusion of lipid-anchored ligands in powder form permits the surface-display of targeting ligands and enhances target cell uptake, thereby extending this technology to targeted drug delivery applications. Our powder-based formulation strategy was extendable to commercially available polymer amphiphiles, including PEG-b-polystyrene and PEG-b-polycaprolactone. The formulated nanotechnologies described herein are highly modular, require minimal preparation, and remain stable in ambient long-term storage (bypassing cold chain requirements), which will enable their use in medicine (human and veterinary), research, and commercial applications from cosmetics to agriculture.
限制聚合物纳米载体广泛应用的两个主要障碍包括制剂方法的复杂性及其在储存期间的稳定性。为了解决这两个问题,我们在此展示了一种水合粉末形式的形态复杂的纳米载体,它无需使用昂贵、苛刻和/或耗时的纳米载体制备技术。这些粉末由碳水化合物和具有低玻璃化转变温度的自组装聚合物两亲物组成。水合过程只需不到一分钟,仅需加入水性介质(水或盐水)即可快速从聚(乙二醇)-b-聚(硫化丙烯)(PEG-b-PPS)聚合物中获得自组装胶束、蠕虫状胶束(即丝状胶束)或聚合物囊泡。所制备的粉末具有高度稳定性,在储存超过6个月后仍能水合形成单分散纳米载体。在水合过程中能有效包封多种药物,包括用于胶束形态的疏水性小分子,以及用于囊泡形态的疏水性和亲水性分子的单独和同时负载。水合的聚合物囊泡显示能够负载亲水性生物大分子,并且包封的酶保留生物活性。此外,我们证明以粉末形式包含脂质锚定配体可实现靶向配体的表面展示并增强靶细胞摄取,从而将该技术扩展到靶向药物递送应用。我们基于粉末的制剂策略可扩展到市售的聚合物两亲物,包括PEG-b-聚苯乙烯和PEG-b-聚己内酯。本文所述的制备的纳米技术具有高度模块化,所需制备最少,并且在环境中长期储存时保持稳定(无需冷链要求),这将使其能够用于医学(人类和兽医)、研究以及从化妆品到农业的商业应用。