Biodistribution and anti-tumor efficacy of intratumorally injected necrosis-avid theranostic agent radioiodinated hypericin in rodent tumor models. (May 2015)

• Record Type: Journal Article
• Authors: Liu, Wei; Zhang, Dongjian; Feng, Yuanbo; Li, Yue; Huang, Dejian; Jiang, Cuihua; Gao, Meng; Peng, Fei; Wang, Xiaoning; Jing, Su; Jiang, Xiao; Ni, Yicheng; Zhang, Jian
• Is Part Of: Journal of drug targeting. Volume 23:Number 4(2015)
• Page Start: 371
• Page End: 379
• Publication Date: 2015-05
• Subjects: Drug delivery systems -- Periodicals; Drug Delivery Systems; Vehicles; Drug Administration Routes; Drug Evaluation; 615.7
• DOI: 10.3109/1061186X.2014.1000337
• Languages: English
• ISSNs: 1061-186X

Abstract

<abstract> <title>Abstract</title> <p>Hypericin has an excellent necrosis-specific targeting capacity; thus, we explored small-molecular tumor necrosis therapy (SMTNT) for inhibiting tumor growth in rodent tumor models. H22 and S180 tumor-bearing Kunming (KM) mice were intratumorally injected with ¹³¹I-monoiodohypericin (¹³¹I-MIH) to investigate the biodistribution of ¹³¹I-MIH as a function of time. Single-photon emission computed tomography (SPECT), autoradiography, fluorescence microscopy and hematoxylin and eosin (H&amp;E) staining were performed to determine the intra-tumoral distribution of ¹³¹I-MIH. A therapeutic evaluation study was also performed in the tumor-bearing KM mice using saline and a positive drug as controls. Gamma counting, SPECT images, autoradiography and fluorescence microscopy and H&amp;E staining results revealed intense retention of ¹³¹I-MIH in the necrotic tumor over 168 h and good <italic>in vivo</italic> stability of the agent. Therapy with a single dose of intra-tumoral administration of ¹³¹I-MIH caused significant tumor growth delay. A histopathological analysis of the tumors and normal organs further validated the therapeutic efficacy and limited systemic toxicity of ¹³¹I-MIH. The prolonged tumor retention and effective therapy indicated that ¹³¹I-MIH may be a promising intratumorally injected SMTNT agent.</p> </abstract>