Liposomal Nanoformulation as a Carrier for Curcumin and pEGCG—Study on Stability and Anticancer Potential

Abstract

Nanoformulations are regarded as a promising tool to enable the efficient delivery of active pharmaceutical ingredients to the target site. One of the best-known and most studied nanoformulations are liposomes—spherical phospholipid bilayered nanocarriers resembling cell membranes. In order to assess the possible effect of a mixture of polyphenols on both the stability of the formulation and its biological activity, two compounds were embedded in the liposomes—(i) curcumin (CUR), (ii) a peracetylated derivative of (−)-epigallocatechin 3-O-gallate (pEGCG), and (iii) a combination of the aforementioned. The stability of the formulations was assessed in two different temperature ranges (4–8 and 20 °C) by monitoring both the particle size and their concentration. It was found that after 28 days of the experiment, the liposomes remained largely unchanged in terms of the particle size distribution, with the greatest change from 130 to 146 nm. The potential decomposition of the carried substances was evaluated using HPLC. The combined CUR and pEGCG was sensitive to temperature conditions; however its stability was greatly increased when compared to the solutions of the individual compounds alone—up to 9.67% of the initial concentration of pEGCG in liposomes after 28 days storage compared to complete decomposition within hours for the non-encapsulated sample. The potential of the prepared formulations was assessed in vitro on prostate (LNCaP) and bladder cancer (5637) cell lines, as well as on a non-cancerous human lung fibroblast cell line (MRC-5), with the highest activity of IC50 equal 15.33 ± 2.03 µM for the mixture of compounds towards the 5637 cell line.

Natural Compounds in Liposomal Nanoformulations of Potential Clinical Application in Glioblastoma

“…Liposomes were prepared according to a literature procedure [ 36 ] from 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine (POPC) and 1,2-dioleoyl-3-trimethylammonium-propane (DOTAP) mixture (8:2), and either CUR, BDMC, ORI, or ACT or their combination with the following molar ratio of 0.1:8:2 (CUR/ORI/ACT/BDMC:POPC:DOTAP), 0.05:0.05:8:2 (CUR:ORI:POPC:DOTAP), and 0.05:0.05:8:2 (ACT:BDMC:POPC:DOTAP). The final concentrations were as follows: 36.8 µg/mL CUR, 130.8 µg/mL BDMC, 44.8 µg/mL ORI, 62.5 µg/mL ACT, 6 080.6 µg/mL POPC, 1 397.1 µg/mL DOTAP and mixtures of compounds, respectively, 18.4 + 22.4 µg/mL CUR + ORI and 15.4 + 31.2 µg/mL BDMC + ACT.…”

Nano-Based Drug Delivery of Polyphenolic Compounds for Cancer Treatment: Progress, Opportunities, and Challenges

“…Incorporating polyphenolic compounds into liposomes can also enhance their stability. Some researchers discovered that embedding the polyphenolic compounds curcumin or/and EGCG into liposomes can increase their stability in blood circulation [ 145 ]. Moreover, these nanoformulations also possessed good anti-cancer performances in prostate cancer cells and bladder cancer cells [ 145 ].…”

“…Some researchers discovered that embedding the polyphenolic compounds curcumin or/and EGCG into liposomes can increase their stability in blood circulation [ 145 ]. Moreover, these nanoformulations also possessed good anti-cancer performances in prostate cancer cells and bladder cancer cells [ 145 ]. Liposomes can also be applied for drug delivery in special physiological environments, such as the gastrointestinal environment.…”

Co‐administration of curcumin with other phytochemicals improves anticancer activity by regulating multiple molecular targets

“…In a recent study, liposome synthesized from 1‐palmitoyl‐2‐oleoyl‐sn glycero‐3‐phosphocholine was utilized to increase the stability of the phytochemicals, which resulted in further increasing the stability of curcumin in co‐embedded in the nano‐liposome than curcumin encapsulated alone. The finding showed that the studied nanoformulation could be attended to for in vivo tests and used instead of dimethyl sulfoxide solvent in the in vitro tests (Piwowarczyk et al, 2022). Thus, targeted therapy based on liposomes could be a favorable vehicle to increase the concentration of related phytochemicals by careful delivery into cancer cells.…”