Preparation and characterization of anticancer niosomal withaferin–A formulation for improved delivery to cancer cells: In vitro, in vivo, and in silico evaluation

• Published in: Journal of drug delivery science and technology 2020-10, Vol.59, p.101863, Article 101863
• Main Authors: Shah, Hamid Saeed, Usman, Faisal, Ashfaq–Khan, Muhammad, Khalil, Ruqaiya, Ul-Haq, Zaheer, Mushtaq, Aamir, Qaiser, Rabia, Iqbal, Jamshed
• Format: Article
• Language: English
• Subjects: Anticancer; Controlled release; Natural drug; Niosome; Withaferin–A
• ISSN: 1773-2247
• DOI: 10.1016/j.jddst.2020.101863

Novel synthetic variants of niosomes and their use as a carrier of anticancer drugs are promising in the field of oncology. In the present study, a non–ionic surfactant and cholesterol-based system were used in a predefined ratio to prepare niosome. Withaferin–A (WA), an active constituent of Withania somnifera, with strong anticancer properties was formulated in the nano vesicular system. The WA was stable inside the niosome as corroborated by DSC and FTIR analysis. The size of the niosome was 278 ± 5 nm with a tremendous loading efficiency of 87 ± 3%. Moreover, a smooth surface texture was spotted in SEM analysis. Anticancer activity of WA–niosome against HeLa cells was increased almost three times its pure form in SRB assay, which was further confirmed in flow cytometry and comet assays. Additionally, molecular modeling (in silico) had revealed that WA formed a stable assembly with niosome which offered persistent hydrophobic contacts (polar and apolar both) and helped in dragging delaying release attributes of the formulation. Finally, a significant in vivo antitumor effect of WA–niosome were observed as an archetype for cancer treatment and henceforth opened up more opportunities to maximize the potential of drugs that were obtained from natural sources. [Display omitted]