Chinthapatla Rukesh, Stephens Jazz Q, Neumann-Rivera Isabel B, Henderson Nichol M, Nie Minhua, Haynes Hannah R, Pierce Joshua G, Meritet Danielle M, Brudno Yevgeny, Oh Annie
Joint Department of Biomedical Engineering, University of North Carolina at Chapel Hill, North Carolina State University, Raleigh, NC, USA.
Comparative Medicine Institute, North Carolina State University, Raleigh, NC, USA.
BMC Pharmacol Toxicol. 2024 Dec 5;25(1):92. doi: 10.1186/s40360-024-00819-6.
Local drug presentation made possible by drug-eluting depots provides benefits for a vast array of diseases, including cancer, microbial infection, and wound healing. Drug-eluting depots provide sustained drug release of therapeutics directly at disease sites with tunable kinetics, remove the need for drugs to access disease sites from circulation, and reduce the side effects associated with systemic therapy. Recently, we introduced an entirely novel approach to local drug presentation named Tissue-Reactive Anchoring Pharmaceuticals (TRAPs). TRAPs enables local drug presentation without any material carriers, capitalizing on innate tissue structures to anchor drugs at the site of administration.
In this report, we comprehensively evaluate the local and systemic toxicological profile of a paclitaxel version of TRAPs in mice by clinical observations, body weight monitoring, histopathological evaluations of injection sites and major organs, as well as blood and urine analyses.
We find that intradermal administration of TRAP-paclitaxel does not induce substantial toxic effects. Localized inflammatory responses were observed at the injection sites and secondary minimal, non-specific inflammation was observed in the liver. All other organs displayed unremarkable histological findings.
These findings support the potential of TRAP-paclitaxel as a promising candidate for localized cancer treatment, offering high-concentration drug delivery while mitigating scarring and adverse side effects.
药物洗脱贮库实现的局部药物递送为包括癌症、微生物感染和伤口愈合在内的多种疾病带来了益处。药物洗脱贮库能够在疾病部位直接实现治疗药物的持续释放,其动力学可调节,无需药物从循环系统进入疾病部位,并减少了与全身治疗相关的副作用。最近,我们引入了一种全新的局部药物递送方法,称为组织反应性锚定药物(TRAPs)。TRAPs能够在没有任何物质载体的情况下实现局部药物递送,利用固有组织结构将药物锚定在给药部位。
在本报告中,我们通过临床观察、体重监测、注射部位和主要器官的组织病理学评估以及血液和尿液分析,全面评估了小鼠中紫杉醇版TRAPs的局部和全身毒理学特征。
我们发现皮内注射TRAP-紫杉醇不会诱导实质性的毒性作用。在注射部位观察到局部炎症反应,在肝脏中观察到继发性轻微非特异性炎症。所有其他器官的组织学检查结果均无异常。
这些发现支持TRAP-紫杉醇作为局部癌症治疗的有前景候选药物的潜力,它能够提供高浓度药物递送,同时减轻瘢痕形成和不良副作用。