Smart Protein-Based Formulation of Dendritic Mesoporous Silica Nanoparticles: Toward Oral Delivery of Insulin
Smart Protein-Based Formulation of Dendritic Mesoporous Silica Nanoparticles: Toward Oral Delivery of Insulin
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DOI：
10.1002/chem.202000773
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发表时间：
2020-04-02
影响因子：
4.3
通讯作者：
Kleitz, Freddy
中科院分区：
文献类型：
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作者：
Juere, Estelle;Caillard, Romain;Kleitz, Freddy
口服胰岛素管理仍然是一个最重要的探索，几乎一个世纪的持续研究尝试都不足以满足。在临床前开发之前，口服胰岛素产品首先要在包封效率、抗蛋白水解能力、肠渗透能力等方面进行优化。使用树突状介孔二氧化硅纳米颗粒（dmsn）作为胰岛素宿主，并与基于蛋白质的赋形剂琥珀酰化β -乳球蛋白（BL）一起，ph响应片允许胰岛素在胃中早期释放/降解和介导胰岛素穿过肠细胞膜的渗透。在最初的基于胰岛素饥饿的体外细胞实验之后，直接细胞荧光可视化证明了dmsn如何确保胰岛素的肠细胞运输。
Oral insulin administration still represents a paramount quest that almost a century of continuous research attempts did not suffice to fulfill. Before pre-clinical development, oral insulin products have first to be optimized in terms of encapsulation efficiency, protection against proteolysis, and intestinal permeation ability. With the use of dendritic mesoporous silica nanoparticles (DMSNs) as an insulin host and together with a protein-based excipient, succinylated beta-lactoglobulin (BL), pH-responsive tablets permitted the shielding of insulin from early release/degradation in the stomach and mediated insulin permeation across the intestinal cellular membrane. Following an original in vitro cellular assay based on insulin starvation, direct cellular fluorescent visualization has evidenced how DMSNs could ensure the intestinal cellular transport of insulin.