Folate-conjugated liposome as effective Drug delivery system for Quercetin

Abstract

Active ingredient (AI), particularly quercetin (Q), has been known as types of nature-derived chemotherapic agents in cancer treatment. However, the advantages of this agent concerning antineoplastic activity were restricted by its poor water solubility. Therefore, the encapsulation of AI in nano-mediated drug delivery is expected to create diverse effects and can sufficiently increase their therapeutic outcomes. The aim of this present study was to effectively prepare folate-conjugated liposome (L-F) that can enhance the delivery of Q. L-F containing Q (Q-L-F) was successfully prepared by thin film technique, using tween 80-ethylenediamine-acid folic as the surface-modified moiety. Physicochemical parameters, including morphology, particles size, zeta potential, drug encapsulation efficiency and release profiles were investigated. In addition, in vitro cytotoxicity of the prepared formulation was evaluated against NCI-H460 cell line. Results showed that the prepared Q-L-F had a mean size of about 166.8 nm with low polydispersity index (below 0.5) and high encapsulation efficiency (96.6%). The release profile showed a sustained release of Q up to 48 h. Moreover, Q-L-F liposomal system was proposed to have the enhanced toxicity effect toward cancerous cells with expressed folate receptors due to the targeting of folic acid conjugated. In support for this, cell proliferation using SRB assay on NCI-H460 cells demonstrated that Q-L-F exhibited higher cytotoxicity than quercetin loaded conventional liposome (Q-L). For the purpose of researching, the data could serve as proof for the potential of L-F as a sustained delivery system for Q in anti-cancer therapy.