通过使用DPPC脂质（L）和与精胺（SN）、生物素（BT）和叶酸（FA）共聚物进行共价连接的F127聚合物，得到了生物修饰的包膜脂质囊泡，从而形成了LF127-SN、LF127-BT和LF127-FA纳米平台。荧光敏化剂Hypericin（HY）通过薄膜法纳入纳米体系，并通过动态光散射、静电势、封装效率和透射电子显微镜进行表征。结果显示，所有纳米平台在至少5天的水分散体系中具有良好的稳定性。体外血清稳定性实验证明，HY负载的LF127-SN与BSA蛋白形成复合物的倾向较其类似物更低。LF127-SN是最稳定的HY配方，其次是LF127-BT和LF127-FA，通过关联常数（Kd）值进行确认：LF127、LF127 FA、LF127-BT和LF127-SN分别为600μmol L-1、1100μmol L-1、515μmol L-1和378μmol L-1。通过使用Caco-2、B16-F10、L-929和HaCat细胞进行细胞毒性试验，评估了HY的光动力学潜力。与其他纳米平台相比，HY负载的LF127-SN显示出显著增加的选择性。HY负载在LF127-BT和LF127-SN中显示出明显的摄取和生物分布，在静脉注射后2小时后。所有生物修饰的包膜脂质在应用后的72小时内显示出令人满意的代谢，没有在任何重要器官中发生显著积累或残留。这些结果表明，在这些纳米体系中负载HY可能是一种有前途的策略，即使使用细胞外涂层聚合物的少量粘合剂（0.02%w/v）。此外，这些结果表明，LF127-SN相对于其他评估的系统显示出明显的优势，对于未来的光动力学治疗和治疗诊断应用具有最突出的特点。版权所有©2023 Elsevier B.V. 保留所有权利。

Biomodified coated-lipid vesicles were obtained using the DPPC lipid (L) and F127 copolymer linked covalently with spermine (SN), biotin (BT), and folic acid (FA), resulting in LF127-SN, LF127-BT, and LF127-FA nanoplatforms. The photosensitizer hypericin (HY) was incorporated into the nanosystem by a thin-film method and characterized by dynamic light scattering, zeta potential, encapsulation efficiency, and transmission electronic microscopy. The results provided a good level of stability for all nanoplatforms for at least 5 days as an aqueous dispersion. The in vitro serum stability showed that the HY-loaded LF127-SN has a lower tendency to form complexes with BSA protein than with its analogs. LF127-SN was the most stable HY formulation, followed by LF127-BT and LF127-FA, confirmed by the association constant (Kd) values: 600 μmol L-1, 1100 μmol L-1, 515 μmol L-1, and 378 μmol L-1 for LF127, LF127 FA, LF127-BT, and LF127-SN, respectively. The photodynamic potential of HY was accessed by cytotoxicity assays using Caco-2, B16-F10, L-929, and HaCat cells. HY-loaded LF127-SN revealed a significant increase in the selectivity compared to other nanoplatforms. HY-loaded in LF127-BT and LF127-SN showed distinct uptake and biodistribution after 2 h of intravenous application. All biomodified coated-lipids showed satisfactory metabolism within 72 h after application, without significant accumulation or residue in any vital organ. These results suggest that incorporating HY-loaded in these nanosystems may be a promising strategy for future applications, even with a small amount of binders to the coating copolymer (0.02% w/v). Furthermore, these results indicate that the LF127-SN showed remarkable superiority compared to other evaluated systems, being the most distinct for future photodynamic therapy and theranostic applications.Copyright © 2023 Elsevier B.V. All rights reserved.