Solidified phospholipid-TPGS as an effective oral delivery system for improving the bioavailability of resveratrol

Liu, Cuiru; Tong, Peiyue; Yang, Rujie; You, Yingnan; Liu, Hongzhuo; Zhang, Tianhong

doi:10.1016/j.jddst.2019.02.025

Cited by 11 publications

(8 citation statements)

References 39 publications

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“…16 These two agents displayed inferior dissolution profiles to RES/GA-PC in the present study. The cumulative dissolution percentages of RES in the solidified phospholipid complex 12 and the solid dispersion 11 reached 85−100% in 0.1 mol/L HCl, which might be comparable to that in RES/GA-PC or even better. RES/GA-PC enhanced the cumulative dissolution percentage of GA from 19.8 to 80.3% with similar dissolution rates at equal times.…”

Section: ■ Results and Discussionmentioning

confidence: 82%

“…48 In good accordance with the dissolution study in vitro, the solubilization agents, the nanocrystal 13 and the nanoparticle, 16 enhanced the C max of RES by approximately 2.21-and 1.22fold, respectively, all less than 3.61 times achieved by RES/GA-PC in the present study. The C max was increased by 3.41-fold with solidified RES-PC prepared by Liu et al, 12 but only a 1.65-fold bioavailability improvement was observed. The same result was obtained in the RES-PC group in our study, in which the speed of absorption of RES increased significantly, but the bioavailability of RES did not.…”

Section: ■ Results and Discussionmentioning

confidence: 94%

“…Therefore, compared with crystalline drugs, amorphous drugs improve thermodynamic properties and hence the dissolution rate and extent. 12 Compared with RES/GA-PC, the RES nanocrystal showed 95% cumulative dissolution with Tween 80 (0.1%) in the dissolution medium, 13 and the nanoparticle showed 40% in pH 7.4. 16 These two agents displayed inferior dissolution profiles to RES/GA-PC in the present study.…”

Section: ■ Results and Discussionmentioning

confidence: 96%

“…RES-PC was obtained according to the procedure optimized by our lab. 12 For RES/GA-PC, the effect of the RES/GA-PL ratio, reaction solvent, refluxing temperature, and reflux time on the water solubility of RES and GA was investigated. Finally, equal molar ratios of RES/GA (molar ratio of 1:1.5) and PC were transferred into a 250 mL round bottom flask and dissolved in ethyl acetate.…”

Section: ■ Materials and Methodsmentioning

confidence: 99%

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Dual Strategy for Improving the Oral Bioavailability of Resveratrol: Enhancing Water Solubility and Inhibiting Glucuronidation

Zhang

et al. 2021

J. Agric. Food Chem.

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Resveratrol (RES) suffers from poor water solubility and extensive metabolism, which lead to low bioavailability. A phospholipid complex (PC) containing RES and a UDP-glucuronosyltransferase (UGT) inhibitor was prepared to address these two limiting factors, thereby improving RES bioavailability. First, 11 natural active ingredients metabolized by similar enzyme subtypes to RES were screened in a glucuronidation assay in liver microsomes. Then, glycyrrhetinic acid (GA), the strongest inhibitor, was prepared with RES in a PC. RES-PC was prepared as a control. As expected, the water solubility and the cumulative dissolution of RES were significantly enhanced by RES-PC and RES/GA-PC. Compared with the RES group, the AUC 0−10 of RES and resveratrol-3-glucuronide (R-3-G) in the RES/GA-PC group showed increases of 2.49-and 1.70-fold, respectively, with the proportion of RES absorption to total absorption increasing 1.45 times. These results demonstrated that RES/GA-PC could improve the bioavailability of RES by increasing its water solubility and inhibiting its glucuronidation.

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Section: ■ Results and Discussionmentioning

confidence: 82%

Section: ■ Results and Discussionmentioning

confidence: 94%

Section: ■ Results and Discussionmentioning

confidence: 96%

Section: ■ Materials and Methodsmentioning

confidence: 99%

See 2 more Smart Citations

Dual Strategy for Improving the Oral Bioavailability of Resveratrol: Enhancing Water Solubility and Inhibiting Glucuronidation

Zhang

et al. 2021

J. Agric. Food Chem.

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“…This can alter the duration of therapeutic activity and the bioavailability [ 100 ]. Stilbenoids can be delivered by different types of systems [ 101 ], namely, microspheres [ 102 ], microcapsules [ 103 ], self-emulsifying drug delivery system (SEDDS) [ 101 , 104 ], self-microemulsifying drug delivery system (SMEDDS) [ 105 , 106 , 107 ], nanosponges [ 108 ], nanoemulsions [ 109 , 110 ], self-nanoemulsifying drug delivery system (SNEDDS) [ 111 , 112 , 113 , 114 ], self-double-emulsifying drug delivery system (SDEDDS) [ 115 ], liposomes [ 116 , 117 ], nanoparticles [ 118 , 119 , 120 , 121 , 122 , 123 , 124 , 125 , 126 ], nanostructured lipid carriers [ 127 ], nanosuspensions [ 128 ], chitosan–gellan nanofiber [ 129 ], solidified phospholipid complex [ 130 ], spiral dextrin [ 131 ], and buccal cyclodextrin delivery system [ 132 ]. All delivery systems are extensively studied, but there is little clinical data.…”

Section: Enhancing the Bioavailability Of Stilbenoidsmentioning

confidence: 99%

Enhancing Bioavailability of Nutraceutically Used Resveratrol and Other Stilbenoids

2021

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Stilbenoids are interesting natural compounds with pleiotropic in vitro and in vivo activity. Their well-documented biological properties include anti-inflammatory effects, anticancer effects, effects on longevity, and many others. Therefore, they are nowadays commonly found in foods and dietary supplements, and used as a part of treatment strategy in various types of diseases. Bioactivity of stilbenoids strongly depends on different types of factors such as dosage, food composition, and synergistic effects with other plant secondary metabolites such as polyphenols or vitamins. In this review, we summarize the existing in vitro, in vivo, and clinical data from published studies addressing the optimization of bioavailability of stilbenoids. Stilbenoids face low bioavailability due to their chemical structure. This can be improved by the use of novel drug delivery systems or enhancers, which are discussed in this review. Current in vitro and in vivo evidence suggests that both approaches are very promising and increase the absorption of the original substance by several times. However, data from more clinical trials are required.

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Current Updated Review on Applications of Different Grades of Sylysia in Pharmaceutical Formulation Development

Patra,

Singha,

Sahu

et al. 2024

Biomedical Materials & Devices

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Solidified phospholipid-TPGS as an effective oral delivery system for improving the bioavailability of resveratrol

Cited by 11 publications

References 39 publications

Dual Strategy for Improving the Oral Bioavailability of Resveratrol: Enhancing Water Solubility and Inhibiting Glucuronidation

Dual Strategy for Improving the Oral Bioavailability of Resveratrol: Enhancing Water Solubility and Inhibiting Glucuronidation

Enhancing Bioavailability of Nutraceutically Used Resveratrol and Other Stilbenoids

Current Updated Review on Applications of Different Grades of Sylysia in Pharmaceutical Formulation Development

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