Abstract
Background: Medicinal plants have proven their value as a source of molecules with therapeutic potential, and recent studies have shown that capsaicin has profound anticancer effects in several types of human cancers. However, its clinical use is handicapped due to its poor pharmacokinetics. This study aims to enhance capsaicin’s pharmacokinetic properties by loading the molecule into nanoliposomes model and testing its anticancer activity. Methods: Nanoliposomes were prepared using the thin-film method, and characteristics were examined followed by qualitative and quantitative analyses of encapsulation efficiency and drug loading using HPLC at different lipid/capsaicin ratios. Cell viability assay (MTT) was used to determine IC50. Results: Capsaicin-loaded nanoliposomes showed optimum characteristics of morphology, particle size, zeta potential, and stability. In vitro anticancer activity of capsaicin and capsaicin-loaded nanoliposomes were compared against MCF7, MDA-MB-231, K562, PANC1, and A375 cell lines. Capsaicin-loaded nanoliposomes showed significant improvement in anticancer activity against cancers cell lines studied (p < 0.001), with increased selectivity against cancer cells compared to capsaicin. Conclusion: The encapsulated capsaicin nanoliposomes produced an improvement in pharmacokinetics properties, enhancing the anticancer activity and selectivity compared with capsaicin. This model seems to offer a potential for developing capsaicin formulations for the prevention and treatment of cancer.
Highlights
Cancer is the second leading cause of mortality worldwide and cancer resistance has become a global crisis
CAP-loaded nanoliposomes were formulated by using different ratios of Lipids (DPPC: Cholesterol: DSPE/PEG2000), F1-85:10:5, F2-75:20:5, F3-65:30:5, respectively
Encapsulation and characterization studies of CAP-loaded nanoliposomes were dedicated to formulating an optimum nanoliposome carrier for CAP to evaluate the anticancer activity against a group of cancer cell lines (MCF7, MDA-MB-231, A375, K562, and PANC1)
Summary
Cancer is the second leading cause of mortality worldwide and cancer resistance has become a global crisis. Cancer represents a real crisis affecting the health of all humans It is a diverse disease at the tissue level, and this diversity presented a challenge in the specificity of diagnosis and efficacy of treatment against different types of cancer [1,2]. Capsaicin-loaded nanoliposomes showed significant improvement in anticancer activity against cancers cell lines studied (p < 0.001), with increased selectivity against cancer cells compared to capsaicin. Conclusion: The encapsulated capsaicin nanoliposomes produced an improvement in pharmacokinetics properties, enhancing the anticancer activity and selectivity compared with capsaicin. This model seems to offer a potential for developing capsaicin formulations for the prevention and treatment of cancer
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