胶质瘤是恶性中枢神经系统肿瘤中最不典型的变种，由于患者生存率在过去几年间的微弱改善，对研究界构成了巨大的挑战。所提出的工作旨在开发诊断脑肿瘤的辅助工具，可以通过非侵入性鼻腔途径给予。由于中枢神经系统肿瘤中叶酸受体的过度表达比正常健康细胞高出500倍，因此我们旨在制作一种放射性标记的叶酸封装胶束传递系统以通过鼻腔途径给予。合成了叶酸共轭的双功能螯合剂，用99mTc标记并封装在胶束载体中。进一步评估了制备的微胶囊在大鼠的体内鼻毒性，并发现其安全可靠可用于鼻腔给药。研究发现，由于其纳米尺寸、黏附特性和增强的渗透性，与单独放射性叶酸共轭溶液相比，经鼻腔给药后，制备的微胶囊在小鼠体内的生物分布中有更高的大脑摄取量（4小时内约16%）。在更高级的动物中通过鼻腔给药后的单光子发射计算机断层显像显示出微胶囊的摄取量增加了。有理由相信前述的制剂不仅在发现脑肿瘤方面具有很大的诊断价值，而且在检测其他表达叶酸的癌症，如宫颈、乳腺和肺癌方面也是如此，因为该系统具有快速、非毒性、准确、非侵入性和简单等特点。©2023年，控制释放学会。

Glioma refers to the most atypical variant of the malignant central nervous system tumors posturing massive challenge to the research fraternity owing to the flimsy improvement in the patient survival rate over the past years. The aim of the proposed work was developing a diagnostic aid for brain tumors, which could be administered via the non-invasive intranasal route. Since overexpression of folate receptors in the central nervous system tumors is 500 times more than the normal healthy cells, we aimed at fabricating a radiolabeled folate encapsulated micellar delivery system to be given via the nasal route. Folate conjugated bifunctional chelating agent was synthesized, radiolabeled with 99mTc, and encapsulated in a micellar carrier. The fabricated micelles were further evaluated for in vivo nasal toxicity in rats and the same were found safe for intranasal administration. The fabricated micelles owing to their nano size, mucoadhesive nature, and enhanced permeation were observed to have a higher uptake into the brain (around 16% in 4 h) than as compared to the radiolabeled conjugated folate solution when studied for in vivo biodistribution in mice. Single-photon emission computerized tomography imaging performed in higher animals upon intranasal administration of the micellar formulation revealed enhanced uptake of the micelles into the animal brain. It is believed that the aforementioned formulation can be of a great diagnostic value in the detection of not only brain tumors but also other folate expressing cancers such as cervical, breast, and lungs as the system is fast, non-toxic, accurate, non-invasive, and simple.© 2023. Controlled Release Society.