We prepared nine residue peptide CKSTHPLSC (CKS9)-grafted starch stearate for the simultaneous realization of tyrosinase related protein-2 (Trp-2) shielding and microfold cell (M cell) targeting. The suited introduction of CKS9 and stearic acid endowed the prepared nanomicelles (200 ~ 250 nm) with the lower critical micelle concentration (0.0209 mg/mL) and affinity constant (2.10 ×10⁻⁷), robust encapsulation efficiency (61.59 ~ 72.23%) and loading capacity (49.43 ~ 55.71%), controllable release of Trp-2 peptide, excellent structure stability against the changes of physiological conditions, ultra-dilution and long-term storage. Approx.72% of the loaded cargos went through apical-to-basolateral transportation. The M cell targeting affinity of the designed micelles is 1.5 times stronger than that towards Caco-2 cells. All these performances can be ascribed to the special framework of the designed polymer, namely, the hydrophobic stearic acid side chains and stable M cell-targeting ligand with a higher proportion of hydrophilic domain, which ensured the formation of steady core-shell spherical nanomicelles and the full exposure of targeting ligand. These rationally designed micelles provide a promising potential for developing stable and effective drug delivery systems applicable for oral immunization.

我们制备了九个残基肽 CKSTHPLSC (CKS9) 接枝淀粉硬脂酸酯，用于同时实现酪氨酸酶相关蛋白 2 (Trp-2) 屏蔽和微折叠细胞 (M 细胞) 靶向。CKS9和硬脂酸的适当引入使制备的纳米胶束（200~250 nm）具有较低的临界胶束浓度（0.0209 mg/mL）和亲和常数（2.10 ×10 ^-7)、强大的包封率(61.59~72.23%)和负载能力(49.43~55.71%)、Trp-2肽的可控释放、对生理条件变化的优异结构稳定性、超稀释和长期储存。约 72% 的装载货物经过顶端到底侧的运输。设计的胶束对M细胞的靶向亲和力是对Caco-2细胞的1.5倍。所有这些性能都归因于所设计聚合物的特殊骨架，即疏水性硬脂酸侧链和具有较高亲水结构域比例的稳定的 M 细胞靶向配体，确保了稳定的核壳球形纳米胶束的形成和靶向配体的充分暴露。