Abstract | BACKGROUND: METHOD: Solubility of Hyp in serial solutions of already-approved hydroxypropyl-β- cyclodextrin (HP-β-CD) was evaluated by UVspectrophotometry and 50% HP-β-CD was chosen for further experiments. Two novel HP-β-CD-based formulations of 131I-Hyp were compared with previous DMSO-based formulation, with regards to necrosis-targetability and biodistribution, by magnetic resonance imaging, single-photon emission computed tomography (SPECT), gamma counting, autoradiography, fluorescence microscopy and histopathology. RESULTS: Hyp solubility was enhanced with increasing HP-β-CD concentrations. The radiochemical purity of 131I-Hyp was higher than 90% in all formulations. The necrosis-targetability of 131I-Hyp in the novel formulations was confirmed in vivo by SPECT and in vitro by autoradiography, fluorescence microscopy and histopathology. The plasma clearance of radioactivity was faster in the novel formulations. CONCLUSION:
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Authors | Yue Li, Shuncong Wang, Xiao Jiang, Xiaoxiong Wang, Xiang Zhou, Liangrong Wan, Haitao Zhao, Zhaoli Zhou, LingJie Gao, Gang Huang, Yicheng Ni, Xiaoyan He |
Journal | International journal of pharmaceutics
(Int J Pharm)
Vol. 599
Pg. 120393
(Apr 15 2021)
ISSN: 1873-3476 [Electronic] Netherlands |
PMID | 33639227
(Publication Type: Journal Article)
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Copyright | Copyright © 2021 Elsevier B.V. All rights reserved. |
Chemical References |
- Anthracenes
- Cyclodextrins
- Excipients
- 2-Hydroxypropyl-beta-cyclodextrin
- Perylene
- hypericin
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Topics |
- 2-Hydroxypropyl-beta-cyclodextrin
- Anthracenes
- Cyclodextrins
- Excipients
- Humans
- Neoplasms
- Perylene
(analogs & derivatives)
- Solubility
- Tissue Distribution
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