Cancer is the second leading cause of death globally. Cancer resistance become a global crisis, as there is no magic treatment till now.
Medicinal plants have proven, historically, their value as a source of molecules with therapeutic potential, scientific and research interest is drawing its attention towards naturally-derived compounds in cancer therapy as they are considered to have less toxic side effects compared to current treatments such as chemotherapy, radiotherapy and chemically derived drugs.
Recent studies have shown that Capsaicin has profound anticancer effects in several types of human cancers, while Capsaicin's clinical use is handicapped due to its pharmacokinetics.
This study aim to optimized methods of isolation and purification of Capsaicin from Capsicum annuum growing in Jordan then enhances Capsaicin's pharmacokinetic properties by loaded in nanoliposomes model, then anticancer and anti-inflammatory activity test.
Methods of extraction have been optimized using different solvents polarity, qualitative and quantitative analysis of Capsaicin was made using thin-layer chromatography (TLC). High-Performance Liquid Chromatography (HPLC), Capsaicin identification was made by 1H and 13C NMR. Moreover, to optimized the pharmacokinetic properties of Capsaicin, it was loaded into nanocarriers (nano-Liposomes).
Nanoliposomes were prepared using a thin-film method. The nanoliposomes characteristics were investigated by observing morphology, analysis of particle size, zeta potential, and stability. Additionally, qualitative and quantitative analyses of encapsulation efficiency and drug loading were performed using HPLC at different lipid ratio/Capsaicin amounts.
In vitro anticancer activity of Capsicum annuum crude extract, Capsaicin and Capsaicin loaded nanoliposomes were assessed against MCF7, MDA-MB-231, K562, PANC1, and A375 cancers cell lines, where Cell viability (MTT) assay was used to determine IC50. Moreover, anti-inflammatory of Capsaicin loaded nanoliposomes against MDA-MB-231 cancer cells was investigated. The inflammatory cytokines were quantified using Cytometric Beads Array (CBA) Human Inflammatory Cytokines Kit (Biosciences, USA).
Our results showed that this study's extraction method of Capsaicin from Capsicum annuum was fast, simple, low cost, and reproducible. Moreover, our results showed the significant impact of solvents polarity on Capsaicin yield and purity of crude extract.
Capsaicin loaded nanoliposomes showed optimum characteristics of morphology, particle size, zeta potential, and stability. Furthermore, Capsaicin loaded nanoliposomes showed significant improvement in anticancer activity against, (MCF7, MDA-MB-231, K562, PANC1, and A375) cancers cell lines, and increase the selectivity of Capsaicin loaded nanoliposomes against cancer cells compared to Capsaicin.
Additionally, Anti-inflammatory activity of Capsaicin Loaded-nano liposomes showed a noticeable reduction in the production of IL-6 and IL-8 in comparison with untreated cell; this novel formula could reduce MDA-MB-231 tumor cell density and cell migration As there is a notable relationship between MDA-MB-231 tumor cell density and cell migration, and IL-6 and IL-8 production.
In conclusion, Capsaicin's isolation and purification from Capsicum annuum growing in Jordan optimized, the encapsulated Capsaicin in nanoliposomes showed significant improvement in pharmacokinetics properties and enhancement the anticancer activity and selectivity comparing with Capsaicin. This model could open a door for developing Capsaicin as the prevention and treatment of cancer.