Sulfo CY7 NHS ester在双靶向微球颗粒DPs中的的应用
瑞禧生物2025-08-20   作者:lkr   来源:
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文献:Orally Deliverable Dual-Targeted Pellets for the Synergistic Treatment of Ulcerative Colitis

文献链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8489837/

作者:Xiaomeng Tang, Meng Yang, Yongwei Gu,Liangdi Jiang, Yue Du, Jiyong Liu

相关产品:Sulfo CY7 NHS ester 水溶性七甲川花菁染料活性酯

原文摘要:Purpose: The effective treatment of ulcerative colitis (UC) poses substantial challenges, and the aetiopathogenesis of UC is closely related to infectious, immunological and environmental factors. Currently, there is a considerable need for the development of orally bioavailable dosage forms that enable the effective delivery of therapeutic drugs to local diseased lesions in the gastrointestinal tract.

Methods: Berberine (BBR) and Atractylodes macrocephala Koidz (AM) volatile oil, derived from the Chinese herbs Coptis chinensis Franch and Atractylodes macrocephala Koidz, have anti-inflammatory and immunomodulatory activities. In this study, we prepared colon-targeted pellets loaded with BBR and stomach-targeted pellets loaded with AM volatile oil for the synergistic treatment of UC. The Box–Behnken design and β- cyclodextrin inclusion technique were used to optimize the enteric coating formula and prepare volatile oil inclusion compounds.

Results: The two types of pellets were spherical and had satisfactory physical properties. The pharmacokinetic results showed that the AUC and MRT values of the dual-targeted (DPs) pellets were higher than those of the control pellets. In addition, in vivo animal imaging confirmed that the DPs could effectively deliver BBR to the colon. Moreover, compared with sulfasalazine and monotherapy, DPs exerted a more significant antiinflammatory effect by inhibiting the expression of inflammatory factors including IL-1β, IL-4, IL-6, TNF-α and MPO both in serum and tissues and enhancing immunity by decreasing the production of IgA and IgG.

Conclusion: The DPs play a synergistic anti-UC effect by exerting systemic and local anti

inflammatory and provide an effective oral targeted preparation for the treatment of UC.

 

Sulfo CY7 NHS ester是一种近红外荧光染料,通常为深绿色或绿色粉末状固体。因磺酸基团的存在,具有良好的水溶性,也易溶于甲醇、DMF等有机溶剂.它的最大吸收波长约750nm,最大发射波长约773nm,荧光量子产率较高,能提供强烈的荧光信号,其近红外特性适合深层组织和活体成像,可减少生物样本的自发荧光背景干扰,提高成像信噪比。NHS酯基团可与含有氨基的生物分子发生反应,形成稳定的酰胺键,从而实现对蛋白质、抗体、多肽等生物分子的荧光标记。该文献制备了含BBR的靶向颗粒和含AM挥发性油靶向颗粒。采用Box-Behnken设计和β-环糊精包合技术对涂层配方进行优化,制备了挥发性油包合物。过程如下:

GPs和EPs放大扫描电子显微镜照片 

图:GPs和EPs放大扫描电子显微镜照片

 

Sulfo CY7 NHS ester在DPs中的的应用:

首先制备了AM挥发性油/β-CD包合物。同时,液体化合物的凝固也为后续的胃包球的制备奠定了基础。用差示扫描量热法(DSC)和x射线粉末衍射(XRD)对所得产物进行分析,以确定包含是否成功。采用挤压-球化法制备了GPs和EPs岩芯。将HPMC加入到含有水溶性CY7 NHS ester的溶剂中,同时保持搅拌直至HPMC完全溶解形成均匀的溶液。将上述均匀的溶液通过特制的挤出机挤出,形成条状物,然后在滚圆设备中滚圆,真空干燥,得到球形的微丸芯。将®FS30D、®L 30D-55、GMS、TEC、Tween-80与纯化水混合制备包膜分散体。

生物体内荧光靶向微球的体内成像 

图:生物体内荧光靶向微球的体内成像

 

结论:Sulfo CY7 NHS ester参与制备的双靶向微球颗粒(DPs)为球形,具有良好的物理性能。双靶向(DPs)微球的AUC和MRT值均高于对照微球。此外,体内成像证实,DPs可以有效地将BBR传递到靶向部位。与柳氮磺胺吡啶相比,DPs通过抑制IL-1β、IL-4、IL-6、TNF-α和MPO在体内组织中的表达,并通过降低IgA和IgG的产生来发挥作用。