In Vitro Tracking of Sporozoites via Fluorescence Imaging and MRI Using Multifunctional Micelles.

Early detection could increase the treatment efficiency and prevent the recurrence of malaria disease. To track and detect malarial sporozoites, novel drug delivery systems have been explored for their ability to target these parasites specifically. This study investigates the potential of micelles to track Plasmodium vivax by targeting the Plasmodium vivax hexose transporter using glucose-based interactions. In vitro experiments were conducted using glucose/SPIO/Nile red (targeted) micelles and methoxy/SPIO/Nile red (nontargeted) micelles, revealing that the targeted micelles exhibited stronger fluorescence with the sporozoites and higher relative R2* values compared to the nontargeted micelles. These findings suggest that targeted micelles could be used for the specific detection of Plasmodium sporozoites using fluorescence imaging and MRI techniques, offering a promising approach for efficient malaria parasite detection.

In vitro galactose-targeted study of RSPP050-loaded micelles against liver hepatocellular carcinoma.

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.