pH-Sensitive Liposomes for Enhanced Cellular Uptake and Cytotoxicity of Daunorubicin in Melanoma (B16-BL6) Cell Lines

• Published in: Pharmaceutics Vol. 14; no. 6; p. 1128
• Main Authors: Alrbyawi, Hamad, Poudel, Ishwor, Annaji, Manjusha, Boddu, Sai H S, Arnold, Robert D, Tiwari, Amit K, Babu, R Jayachandra
• Format: Journal Article
• Language: English
• Published: Switzerland MDPI AG 26.05.2022; MDPI
• Subjects: Cancer therapies; cardiolipin; Cardiotoxicity; Cell death; Chemical properties; Cholesterol; Cytotoxicity; Daunorubicin; Design and construction; Dosage and administration; Drug delivery systems; Drug therapy; Drugs; Hydration; Hydrogen-ion concentration; Lipids; Liposomes; Melanoma; Metastasis; pH-sensitive; Phase transitions; Physiological aspects; Tumors; Vehicles; United States; St Louis Missouri; United States > US; Germany; pH-sensitive; melanoma; liposomes; cardiolipin; daunorubicin
• ISSN: 1999-4923; 1999-4923
• DOI: 10.3390/pharmaceutics14061128

Daunorubicin (DNR) was delivered using a pH-sensitive liposomal system in B16-BL6 melanoma cell lines for enhanced cytotoxic effects. DNR was encapsulated within liposomes and CL as a component of the lipid bilayer. PEGylated pH-sensitive liposomes, containing CL, were prepared in the molar ratio of 40:30:5:17:8 for DOPE/cholesterol/DSPE-mPEG (2000)/CL/SA using the lipid film hydration method and loaded with DNR (drug: lipid ratio of 1:5). The CL liposomes exhibited high drug encapsulation efficiency (>90%), a small size (~94 nm), narrow size distribution (polydispersity index ~0.16), and a rapid release profile at acidic pH (within 1 h). Furthermore, the CL liposomes exhibited 12.5- and 2.5-fold higher cytotoxicity compared to DNR or liposomes similar to DaunoXome®. This study provides a basis for developing DNR pH-sensitive liposomes for melanoma treatment.