Formulation Strategies for Enhancing Pharmaceutical and Nutraceutical Potential of Sesamol: A Natural Phenolic Bioactive

Abstract

Natural plants and their products continue to be the major source of phytoconstituents in food and therapeutics. Scientific studies have evidenced the benefits of sesame oil and its bioactives in various health conditions. Various bioactives present in it include sesamin, sasamolin, sesaminol, and sesamol; among these, sesamol represents a major constituent. This bioactive is responsible for preventing various diseases including cancer, hepatic disorders, cardiac ailments, and neurological diseases. In the last decade, the application of sesamol in the management of various disorders has attracted the increasing interest of the research community. Owing to its prominent pharmacological activities, such as antioxidant, antiinflammatory, antineoplastic, and antimicrobial, sesamol has been explored for the above-mentioned disorders. However, despite the above-mentioned therapeutic potential, its clinical utility is mainly hindered owing to low solubility, stability, bioavailability, and rapid clearance issues. In this regard, numerous strategies have been explored to surpass these restrictions with the formulation of novel carrier platforms. This review aims to describe the various reports and summarize the different pharmacological activities of sesamol. Furthermore, one part of this review is devoted to formulating strategies to improve sesamol’s challenges. To resolve the issues such as the stability, low bioavailability, and high systemic clearance of sesamol, novel carrier systems have been developed to open a new avenue to utilize this bioactive as an efficient first-line treatment for various diseases.

Sesamol Mitigates Chronic Iron Overload‐Induced Cognitive Impairment and Systemic Inflammation via IL‐6 and DMT1 Regulation

“…[ 37 ] Various carrier systems are currently being explored to improve the efficiency of sesamol delivery and application in vivo, such as lipid nanoparticles, emulsions, polymer nanoparticles, and gelatin nanoparticles. [ 47 ]…”

“…[34][35][36][43][44][45][46] Even though sesamol has alleviative potential for the above diseases, clinical trials are limited because of its low solubilization, stability, and bioavailability. [47] According to pharmacokinetic studies, sesamol is primarily absorbed from the gastrointestinal tract and is present in plasma as sesamol metabolites, including sulfate and glucuronide conjugates. [37,48] In the liver, the concentrations of sesamol metabolites are significantly higher than those of sesamol.…”

“…[37] Various carrier systems are currently being explored to improve the efficiency of sesamol delivery and application in vivo, such as lipid nanoparticles, emulsions, polymer nanoparticles, and gelatin nanoparticles. [47] Iron overload syndromes can be induced by hereditary hemochromatosis, multiple blood transfusions, secondary iron overload, and dietary iron overload. [49,50] In this study, the mice were given intraperitoneal injections of dextran iron (250 mg kg −1 b.w.)…”