In vitro galactose-targeted study of RSPP050-loaded micelles against liver hepatocellular carcinoma
Issued Date
2022-01-01
Resource Type
ISSN
10837450
eISSN
10979867
Scopus ID
2-s2.0-85130624725
Pubmed ID
35388736
Journal Title
Pharmaceutical Development and Technology
Volume
27
Issue
4
Start Page
379
End Page
388
Rights Holder(s)
SCOPUS
Bibliographic Citation
Pharmaceutical Development and Technology Vol.27 No.4 (2022) , 379-388
Suggested Citation
Mazumder A., Dwivedi A., Assawapanumat W., Saeeng R., Sungkarat W., Nasongkla N. In vitro galactose-targeted study of RSPP050-loaded micelles against liver hepatocellular carcinoma. Pharmaceutical Development and Technology Vol.27 No.4 (2022) , 379-388. 388. doi:10.1080/10837450.2022.2063891 Retrieved from: https://repository.li.mahidol.ac.th/handle/20.500.14594/86896
Title
In vitro galactose-targeted study of RSPP050-loaded micelles against liver hepatocellular carcinoma
Author's Affiliation
Other Contributor(s)
Abstract
Andrographolide is a group of diterpenoid lactone isolated from Andrographis paniculata (Burm. F.) NEES. One of the analogues is 19-O-triphenylmethylandrographolide (RSPP050) which possesses anticancer activity. In seeking to capitalise on the last property, we have investigated the in vitro tumour targeting capabilities and MRI imaging for hepatocellular carcinoma. In this study, we have designed galactose-targeted and non-targeted micelles comprised of poly(ethylene glycol)-b-poly(lactide) that enveloped RSPP050 as an anticancer agent and superparamagnetic iron oxide (SPIO) as a contrast agent. The targeting abilities were endeavored by examining the cellular uptake with MTT assay, fluorescence microscopy, Prussian blue staining, and in vitro MRI. Targeted SPIO micelles as a T2* contrast agent decreased the relative T2* MRI intensity at 3 h. Results revealed that galactose micelles displayed 10.91 ± 0.19% drug loading content, −37.17 ± 0.63 mV zeta potential, and these micelles at the concentration of 0.5 µg/ml exhibited higher cytotoxicity than non-targeted micelles and free RSPP050 after incubation for 24 h. Fluorescence microscopy and Prussian blue staining at 3 h demonstrated significant cellular uptake by HepG2 cells. Thus, anticancer activity of RSPP050 could be improved using galactose as a targeting ligand and theranostic function was achieved using SPIO.