Development of sesamin-loaded solid dispersion with α-glycosylated stevia for improving physicochemical and nutraceutical properties

Sato, Hideyuki; Aoki, Aiko; Tabata, Aiko; Kadota, Kazunori; Tozuka, Yuichi; Seto, Yoshiki; Onoue, Satomi

doi:10.1016/j.jff.2017.05.054

Cited by 13 publications

(7 citation statements)

References 27 publications

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“…The solubility and permeability of drugs are usually determined in accordance with the BCS specifications. The solubility of SSM in water is approximately 2.5 μg/mL [ 10 ]. A previous study reported that compounds with a poor water solubility (<100 μg/mL) are mostly classified as belonging to BCS class II [ 26 ].…”

Section: Resultsmentioning

confidence: 99%

“…Additionally, the results obtained after intravenous (IV) bolus administration indicated that the absolute bioavailability rates observed for SSM-SNEDDS and SSM suspension were 4.4% and 0.3%, respectively. A previous work has reported the application of α-glycosylated stevia as the excipient for preparing solid dispersion SSM by the spray-drying method [10]. The results indicated that this solid dispersion formulation provided a C max of 793 ng/mL, the time to maximum concentration (T max ) of 8 h, and a 30-fold improvement of the oral bioavailability of SSM when compared with that of the crystalline one.…”

Section: Pharmacokinetic Studymentioning

confidence: 95%

“…Nevertheless, this study only discussed the drug distribution and dose-dependent contents of sesame extract in serum and the brain and lacked pharmacokinetic data. Furthermore, it has been reported that solid dispersion can increase the solubility and bioavailability of SSM [10]. Although components existing in an amorphous state in solid dispersion can improve the solubility, such a formulation has the disadvantage of being unstable.…”

Section: Introductionmentioning

confidence: 99%

“…Although several studies have demonstrated the advantages of SSM, the poor solubility of SSM in water (2.5 μg/mL) has considerably limited the dissolution rates of its components and its release efficiency [ 10 ]. Moreover, the poor aqueous solubility of SSM has prevented a discussion of its class in the biopharmaceutics classification system (BCS).…”

Section: Introductionmentioning

confidence: 99%

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Self-Nanoemulsifying Drug Delivery Systems for Enhancing Solubility, Permeability, and Bioavailability of Sesamin

et al. 2020

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Sesamin (SSM) is a water-insoluble compound that is easily eliminated by liver metabolism. To improve the solubility and bioavailability of SSM, this study developed and characterized a self-nanoemulsifying drug delivery system (SNEDDS) for the oral delivery of SSM and conducted pharmacokinetic assessments. Oil and surfactant materials suitable for SNEDDS preparation were selected on the basis of their saturation solubility at 37 ± 0.5 °C. The mixing ratios of excipients were determined on the basis of their dispersibility, transmittance (%), droplet sizes, and polydispersity index. An SNEDDS (F10) formulation comprising glyceryl trioctanoate, polyoxyethylene castor oil, and Tween 20 at a ratio of 10:10:80 (w/w/w) was the optimal formulation. This formulation maintained over 90% of its contents in different storage environments for 12 weeks. After the self-emulsification of SNEDDS, the SSM dispersed droplet size was 66.4 ± 31.4 nm, intestinal permeability increased by more than three-fold, relative bioavailability increased by approximately 12.9-fold, and absolute bioavailability increased from 0.3% to 4.4%. Accordingly, the developed SNEDDS formulation can preserve SSM’s solubility, permeability, and bioavailability. Therefore, this SNEDDS formulation has great potential for the oral administration of SSM, which can enhance its pharmacological application value.

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Section: Resultsmentioning

confidence: 99%

Section: Pharmacokinetic Studymentioning

confidence: 95%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Self-Nanoemulsifying Drug Delivery Systems for Enhancing Solubility, Permeability, and Bioavailability of Sesamin

et al. 2020

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“…Examples of exploitation of drug delivery systems to enhance the solubility of sesamin were the formation of the micelle, solid dispersion, and nano-emulsion carrier delivery systems. The improvement in solubility, dissolution profiles, oral bioavailability, intestinal permeability of sesamin, and consequently pharmacological activities of sesamin were evident [ 70 , 71 , 72 ]. Interestingly, there is less study regarding the sesamolin’s physicochemical properties enhancement.…”

Section: Future Prospectsmentioning

confidence: 99%

An Insight into Sesamolin: Physicochemical Properties, Pharmacological Activities, and Future Research Prospects

Rosalina

Weerapreeyakul

2021

Molecules

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Sesame seeds are rich in lignan content and have been well-known for their health benefits. Unlike the other sesame lignan compounds (i.e., sesamin and sesamol), the study of the pharmacological activity of sesamolin has not been explored widely. This review, therefore, summarizes the information related to sesamolin’s pharmacological activities, and the mechanism of action. Moreover, the influence of its physicochemical properties on pharmacological activity is also discussed. Sesamolin possessed neuroprotective activity against hypoxia-induced reactive oxygen species (ROS) and oxidative stress in neuron cells by reducing the ROS and inhibiting apoptosis. In skin cancer, sesamolin exhibited antimelanogenesis by affecting the expression of the melanogenic enzymes. The anticancer activity of sesamolin based on antiproliferation and inhibition of migration was demonstrated in human colon cancer cells. In addition, treatment with sesamolin could stimulate immune cells to enhance the cytolytic activity to kill Burkitt’s lymphoma cells. However, the toxicity and safety of sesamolin have not been reported. And there is also less information on the experimental study in vivo. The limited aqueous solubility of sesamolin becomes the main problem, which affects its pharmacological activity in the in vitro experiment and clinical efficacy. Therefore, solubility enhancement is needed for further investigation and determination of its pharmacological activity profiles. Since there are fewer reports studying this issue, it could become a future prospective research opportunity.

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Nanomaterials in nutraceutical and phytonutrient industries

Amalraj¹,

Jude²,

Sukumaran³

et al. 2019

Industrial Applications of Nanomaterials

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Development of sesamin-loaded solid dispersion with α-glycosylated stevia for improving physicochemical and nutraceutical properties

Cited by 13 publications

References 27 publications

Self-Nanoemulsifying Drug Delivery Systems for Enhancing Solubility, Permeability, and Bioavailability of Sesamin

Self-Nanoemulsifying Drug Delivery Systems for Enhancing Solubility, Permeability, and Bioavailability of Sesamin

An Insight into Sesamolin: Physicochemical Properties, Pharmacological Activities, and Future Research Prospects

Nanomaterials in nutraceutical and phytonutrient industries

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