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Engineered liposomes bearing camptothecin analogue for tumour targeting: in vitro and ex-vivo studies

Saraf, S and Jain, A and Tiwari, AK and Verma, AK and Jain, SK (2020) Engineered liposomes bearing camptothecin analogue for tumour targeting: in vitro and ex-vivo studies. In: Journal of Liposome Research .

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Official URL: https://doi.org/10.1080/08982104.2020.1801725


Topotecan (TPT) is a semi-synthetic, water-soluble derivative of camptothecin, which inhibits the action of topoisomerase I in the S-phase of the cell cycle leading to cell death. For the effective delivery of TPT to cancer cells, pH-sensitive sialic acid modified liposomes were developed. These liposomes were prepared by the thin-film hydration method using the active loading technique. Vesicle size, polydispersity index (PDI), zeta potential, and percentage entrapment efficiency were determined to be 167±3.78nm, 0.243, �8.39mV, and 79.88±1.67, respectively. The pH-sensitive sialic acid (SA) conjugated liposomes enhanced the drug release at acidic pH 4 (92.33±4.21) as compared to physiological pH 7.4 (63.11±4.51). A Sulforhodamine B (SRB) cytotoxicity assay was performed in Murine sarcoma S180 cell lines and the GI50 value of free TPT, Lipo, P-Lipo, SA-P-Lipo, and Adriamycin (ADR) were determined to be 10.07±0.15, 27.33±1.01, 28.76±0.87, 15.7±0.45, and 11.5±0.21µg/mL, respectively. Results obtained from the apoptosis study revealed that cell death by a combination of early apoptosis and apoptosis caused by SA-P-Lipo was �24 fold higher than the control. These results demonstrated that pH-sensitive sialic acid conjugated liposomes will be a potential formulation for improving the antitumor efficacy of TPT. However, further research is necessitated to expedite its applicability in clinical regimen in order to ascertain its safety and efficacy. © 2020 Informa UK Limited, trading as Taylor & Francis Group.

Item Type: Journal Article
Publication: Journal of Liposome Research
Publisher: Taylor and Francis Ltd
Additional Information: Copyright to this article belongs to Taylor and Francis Ltd
Department/Centre: Division of Mechanical Sciences > Materials Engineering (formerly Metallurgy)
Date Deposited: 30 Jul 2021 06:21
Last Modified: 30 Jul 2021 06:21
URI: http://eprints.iisc.ac.in/id/eprint/66391

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