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Engineered liposomes bearing camptothecin analogue for tumour targeting: in vitro and ex-vivo studies.
- Source :
- Journal of Liposome Research; December 2021, Vol. 31 Issue 4, p326-341, 16p
- Publication Year :
- 2021
-
Abstract
- 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 ± 3.78 nm, 0.243, −8.39 mV, 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 GI<subscript>50</subscript> 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 ± 0.21 µg/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. [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 08982104
- Volume :
- 31
- Issue :
- 4
- Database :
- Complementary Index
- Journal :
- Journal of Liposome Research
- Publication Type :
- Academic Journal
- Accession number :
- 152851097
- Full Text :
- https://doi.org/10.1080/08982104.2020.1801725