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

Hamad Alrbyawi; Ishwor Poudel; Manjusha Annaji; Sai H S Boddu; Robert D Arnold; Amit K Tiwari; R Jayachandra Babu

doi:10.3390/pharmaceutics14061128

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

Pharmaceutics. 2022 May 26;14(6):1128. doi: 10.3390/pharmaceutics14061128.

Authors

Hamad Alrbyawi^{1

2}, Ishwor Poudel¹, Manjusha Annaji¹, Sai H S Boddu^{3

4}, Robert D Arnold¹, Amit K Tiwari^{4

5}, R Jayachandra Babu¹

Affiliations

¹ Department of Drug Discovery and Development, Harrison School of Pharmacy, Auburn University, Auburn, AL 36849, USA.
² Pharmaceutics and Pharmaceutical Technology Department, College of Pharmacy, Taibah University, Medina 41477, Saudi Arabia.
³ Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, Ajman University, Ajman P.O. Box 346, United Arab Emirates.
⁴ Center of Medical and Bio-Allied Health Sciences Research, Ajman University, Ajman P.O. Box 346, United Arab Emirates.
⁵ Department of Pharmacology and Experimental Therapeutics, The University of Toledo, Toledo, OH 43614, USA.

Abstract

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.

Keywords: cardiolipin; daunorubicin; liposomes; melanoma; pH-sensitive.

Grants and funding

This research received no external funding.