Development and Characterization of a Phospholipid Complex for Effective Delivery of Capsaicin

Abstract

Cancer is the main causes of morbidity throughout the world [1][2] . Among the different cancers, breast cancer is the second most important cause of cancer death. Though significant progress has been made in breast cancer treatment, only a few patients benefit from breast cancer by adjuvant chemotherapy and most patients with metastatic cancer are resistant to chemotherapy [3] . In addition, chemotherapy causes acute and chronic toxicities that include sterility, congestive heart failure, osteoporosis and neuropathy [4] . Recently, many new avenues of cancer treatment have opened up but the costs of treatment have sky-rocketed too. Hence, screening of indigenously available plant and animal resources for anticarcinogenic potential is an important branch of anticancer research. Chili peppers are the regularly consumed naturally occurring spices worldwide [5][6] . Capsaicin, (8-methyl-N-vanillyl-6nonenamide, fig. 1a) is the main constituent of chili peppers with therapeutic activity [7] . The chemical formula of capsaicin is C 18 H 27 NO 3 and the molecular weight is 305.4 g/mol [8] . Capsaicin is a hydrophobic, colourless, pungent and volatile crystalline powder. It has a benzene ring and a polar amide group with a long hydrophobic carbon tail. Due to its water insolubility, alcohols and organic solvents are used to dissolve capsaicin.Capsaicin induces apoptosis in several cancer cell lines including liver cancer, prostate cancer, colon cancer, pancreatic cancer, and breast cancer without affecting normal cells [9] . In human breast cancer, epidermal growth factor-2 (HER-2) and human epidermal growth factor receptor are over expressed [10,11] . Capsaicin inhibited breast cancer cell growth in vitro by reducing the protein expression of human epidermal growth factor receptor and epidermal growth factor-2 [12] .

Inclusion of phenolic bioactives in high amylose corn starch for gastro-intestinal delivery

“…DSC curves obtained for pure CAP or CUR give acuminate single peaks at 66.63 ± 0.01°C and 174.56 ± 0.02°C with an enthalpy of Δ H = 73.85 ± 1.15 J/g and Δ H = 124.97 ± 0.69 J/g, respectively. This concurs with previous values reported in the literature ( 51 , 52 ) and suggest the additional peaks observed in HACS-CAP and HACS-CUR arise from some non-complexed CAP or CUR.…”

Enhanced oral bioavailability of capsaicin‐loaded microencapsulation complex via electrospray technology: Preparation, in vitro and in vivo evaluation

“…The reason for the enhanced oral bioavailability of capsaicin‐PVP electrosprayed complex may be ascribed to increased solubility of capsaicin in the gastrointestinal tract. The addition of phospholipids in the prescription could make it easy for the drug to penetrate the biological membrane (Mondal et al., 2019; Weng et al., 2019; Zhang et al., 2015). As a component of the lipid membrane, phospholipid has a high affinity for the cell membrane, which can promote absorption of the drug and also improve the bioavailability of capsaicin.…”

“…The reason for the enhanced oral bioavailability of capsaicin-PVP electrosprayed complex may be ascribed to increased solubility of capsaicin in the gastrointestinal tract. The addition of phospholipids in the prescription could make it easy for the drug to penetrate the biological membrane (Mondal et al, 2019;Weng et al, 2019;Zhang et al, 2015).…”

Improved Activity of Herbal Medicines through Nanotechnology

“…Kumar, et al (2021) conducted a study in which a taxifolin ethyl acetate fraction derived from Cedrus deodara bark extract was loaded into a phytosome delivery system, with aims to evaluate the antioxidant and anticancer activity of taxifolin [50]. Phytosomes can increase the lipophilicity of the active compound so that they enhance the absorption of the active substance and increase its ability to cross biological membranes [66]. Based on the research of Kumar, et al (2021), phytosomes showed high antioxidant activity with a lower IC50 value compared to the ethyl acetate and the standard.…”