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首页> 外文期刊>RSC Advances >Targeted theranostic liposomes: rifampicin and ofloxacin loaded pegylated liposomes for theranostic application in mycobacterial infections
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Targeted theranostic liposomes: rifampicin and ofloxacin loaded pegylated liposomes for theranostic application in mycobacterial infections

机译：靶向治疗脂质体：利福平和氧氟沙星负载的聚乙二醇化脂质体，用于治疗分枝杆菌感染

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Theranostic liposomes are effective drug delivery systems for the management of infections. With added features of targeting and stealth, theranostic liposomes can be made more effective. We report the synthesis and validation of targeted stealth theranostic liposomes for the management of mycobacterial infections. The targeted drug delivery systems for infections are devised to improve the therapeutic window of encapsulated drugs by increasing their delivery to the target area and minimizing the drug-associated toxicity. FR+ targeted pegylated liposomal formulation was developed for in vivo imaging of mycobacterial infections. The encapsulated drugs for mitigation are rifampicin and ofloxacin. The prepared liposomes were characterized for physicochemical properties and stability. In vitro release properties, mycobacterial activity, in vivo blood-kinetics, bio-distribution, and bio-efficacy of the prepared lyophilized liposomes were assessed. The mean particle size of the liposomes was 160.6 nm with considerable colloidal stability observed up to 120 days. The results of in vitro investigations indicate good encapsulation efficiency of 66.89 (±10.9)% and 40.61 (±8.7)% for rifampicin and ofloxacin respectively with excellent anti-mycobacterial activity. The pharmacokinetics data corroborate a slow biphasic pattern with a much longer terminal half-life of 19.13 h. The tissue distribution studies revealed high blood pool activity even up to 24 h post injection (p.i.) with the maximum organ localization in the spleen, liver, and kidneys at one hour p.i. Further, in vivo scintigraphic studies in the murine model of TB infection showed higher uptake at infected lesions at two hours p.i. The blocking imaging experiments showed minimized uptake, which confirms specific targeting. Therapeutic efficacy studies further confirmed that liposomal delivery of the anti-TB drugs is efficacious in the murine model of infection. In conclusion, preliminary studies demonstrated that the formulated liposomes can be an effective theranostic agent against mycobacterial infections in the mouse model.
机译：Theranostic脂质体是用于管理感染的有效药物递送系统。随着靶向和隐身的增加的特征，可以更有效地进行治疗脂质体。我们报告了针对靶向隐身治疗脂质体的合成和验证治疗分枝杆菌感染。针对感染的靶向药物递送系统通过增加其向靶区域并最小化药物相关毒性来改善包封药物的治疗窗。 FR +靶向聚乙二醇化脂质体配方用于体内成像的分枝杆菌感染。用于缓解的包封的药物是利福平和氧氟沙星。制备的脂质体的特征在于物理化学性质和稳定性。评估体外释放性质，分枝杆菌活性，体内血液动力学，生物分布和制备的冻干脂质体的生物疗效。脂质体的平均粒度为160.6nm，胶体稳定性明显观察到120天。体外研究的结果分别表明利福平和氧氟沙星的良好封装效率为66.89（±10.9）％和40.61（±8.7）％，分别具有优异的抗分法活性。药代动力学数据证实了缓慢的双相模式，终端半衰期为19.13小时。组织分布研究揭示了高达24小时的高血液池活性（P.I.），脾脏，肝脏和肾脏的最大器官定位在1小时P.I.此外，在Tb感染的小鼠模型中，在TB感染的小鼠模型中的体内闪烁类别在P.I期间在感染病变中显示出更高的摄取。阻塞成像实验表明最小化的摄取，其确认了特定的靶向。治疗疗效研究进一步证实，抗结核药物的脂质体递送在感染的小鼠模型中是有效的。总之，初步研究表明，配制的脂质体可以是针对小鼠模型中的抗分枝杆菌感染的有效治疗剂。

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