Involvement of metabolism-permeability in enhancing the oral bioavailability of curcumin in excipient-free solid dispersions co-formed with piperine

Wang, Ruoning; Han, Jiawei; Jiang, Ai; Huang, Rong; Fu, Tingming; Wang, Lingchong; Zheng, Qi; Wen, Li; Li, Junsong

doi:10.1016/j.ijpharm.2019.02.027

Cited by 89 publications

(64 citation statements)

References 43 publications

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“…Zhang et al [94] aimed to improve the oral absorption of baicalin, which has low solubility and poor permeability, by using a micellar formulation comprised of the carriers Pluronic P123 copolymer and sodium taurocholate. Sustained release profile of baicalin-loaded mixed micelles, in in vitro drug release experiment, held in several pH conditions, showed 14% drug released after 2 h in gastric conditions and 54% release within 48 h in intestinal conditions, compared to 34% and 79% release [105], nanoparticles [106][107][108][109][110], phytosome [111], nanoliposome [112], mixed micelles [113,114], SNEDDS [115,116], nanocarrier [117,118], nanoemulsion [119], nanosuspension [ Mixed micelles [129,130], nanoparticles [131,132], solid dispersion [133,134] , SNEDDS [135] , SMEDDS [136], lipid carrier [137], copolymeric micelles [138], exosomes [139] Naringenin DENV, HCV SNEDDS [140], solid dispersion [141], nanoparticles [142,143] , liposome [144], nanosuspension [145,146] In vitro uptake studies, carried out with a caco-2 cell line, determined the absorption of baicalin within the mixed micelles and verified their internalization ability. Baicalin-loaded ST-P123-MMs formulation achieved high oral bioavailability (Fig.…”

Section: Delivery Of Herbal Extracts and Phytochemicalsmentioning

confidence: 99%

Antiviral effect of phytochemicals from medicinal plants: Applications and drug delivery strategies

Ben‐Shabat

Yarmolinsky²,

Porat

et al. 2019

Drug Deliv. and Transl. Res.

270

184

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Viral infections affect three to five million patients annually. While commonly used antivirals often show limited efficacy and serious adverse effects, herbal extracts have been in use for medicinal purposes since ancient times and are known for their antiviral properties and more tolerable side effects. Thus, naturally based pharmacotherapy may be a proper alternative for treating viral diseases. With that in mind, various pharmaceutical formulations and delivery systems including micelles, nanoparticles, nanosuspensions, solid dispersions, microspheres and crystals, self-nanoemulsifying and self-microemulsifying drug delivery systems (SNEDDS and SMEDDS) have been developed and used for antiviral delivery of natural products. These diverse technologies offer effective and reliable delivery of medicinal phytochemicals. Given the challenges and possibilities of antiviral treatment, this review provides the verified data on the medicinal plants and related herbal substances with antiviral activity, as well as applied strategies for the delivery of these plant extracts and biologically active phytochemicals.

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Section: Delivery Of Herbal Extracts and Phytochemicalsmentioning

confidence: 99%

Antiviral effect of phytochemicals from medicinal plants: Applications and drug delivery strategies

Ben‐Shabat

Yarmolinsky²,

Porat

et al. 2019

Drug Deliv. and Transl. Res.

270

184

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“…The drug curcumin is categorized as a BCS Class IV drug and shows not only poor solubility and dissolution properties but also poor permeability. The idea of the formation of a CAMS consisting of a BCS Class IV drug, here curcumin, and a permeability enhancer as a co-former was shown to be promising [133]. In most cases, an enhanced bioavailability due to enhanced dissolution properties could be demonstrated in the studies including in vivo investigations.…”

Section: In Vitro and In Vivo Performance Of Camsmentioning

confidence: 99%

Co-Amorphous Drug Formulations in Numbers: Recent Advances in Co-Amorphous Drug Formulations with Focus on Co-Formability, Molar Ratio, Preparation Methods, Physical Stability, In Vitro and In Vivo Performance, and New Formulation Strategies

Grohganz

Hempel

2021

Pharmaceutics

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Co-amorphous drug delivery systems (CAMS) are characterized by the combination of two or more (initially crystalline) low molecular weight components that form a homogeneous single-phase amorphous system. Over the past decades, CAMS have been widely investigated as a promising approach to address the challenge of low water solubility of many active pharmaceutical ingredients. Most of the studies on CAMS were performed on a case-by-case basis, and only a few systematic studies are available. A quantitative analysis of the literature on CAMS under certain aspects highlights not only which aspects have been of great interest, but also which future developments are necessary to expand this research field. This review provides a comprehensive updated overview on the current published work on CAMS using a quantitative approach, focusing on three critical quality attributes of CAMS, i.e., co-formability, physical stability, and dissolution performance. Specifically, co-formability, molar ratio of drug and co-former, preparation methods, physical stability, and in vitro and in vivo performance were covered. For each aspect, a quantitative assessment on the current status was performed, allowing both recent advances and remaining research gaps to be identified. Furthermore, novel research aspects such as the design of ternary CAMS are discussed.

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“…Eight ingredients significantly increased the plasma concentration of theanine compared with that in the case of administration of theanine powder, not rate of absorption of theanine ( Fig 1A , Table 1 ). In these ingredients, we focused on piperine, which is known as an enhancer of the absorption of various components, in Piper longum [ 26 , 27 ]. Piperine is known to be a potent inhibitor of cytochrome P450, particularly CYP3A4 and CYP1A2 [ 28 ].…”

Section: Discussionmentioning

confidence: 99%

An imaging approach for determining the mechanism of enhancement of intestinal absorption of an L-theanine supplement

et al. 2021

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Background & objective Theanine (L-glutamylethylamide) contained in green tea is a functional food component that has been attracting attention due to its relaxation effect. It was shown that the ingredients added to the theanine formulations increased the absorption of theanine. If this mechanism can be elucidated, it would be possible to contribute to development of evidence-based formulations. In this study, we investigated the effect of ingredients in the formulations on the absorption of theanine in detail. Main methods After oral administration of a mixture of theanine and additional components to Wistar rats the plasma concentration was determined by an HPLC and the pharmacokinetic parameters were calculated. In addition, a new system for evaluating intestinal blood flow was developed since the involvement of intestinal blood flow was considered as a factor that increased absorption of theanine. Key findings Plasma concentration of theanine increased significantly in the combined use group with eight ingredients containing piperine as compared with theanine only group. Piperine would increase theanine absorption by increased blood flow, not an inhibition of metabolism. We succeeded to develop a visual and quantitative system to evaluate the effect of these ingredients directly including piperine on the intestinal blood flow using indocyanine green while maintaining physiological conditions. Significance Increased intestinal blood flow by these ingredients including piperine enhanced the absorption of theanine. Other mechanisms may also be considered as the mechanism by which theanine absorption is increased in addition to increased blood flow.

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Involvement of metabolism-permeability in enhancing the oral bioavailability of curcumin in excipient-free solid dispersions co-formed with piperine

Cited by 89 publications

References 43 publications

Antiviral effect of phytochemicals from medicinal plants: Applications and drug delivery strategies

Antiviral effect of phytochemicals from medicinal plants: Applications and drug delivery strategies

Co-Amorphous Drug Formulations in Numbers: Recent Advances in Co-Amorphous Drug Formulations with Focus on Co-Formability, Molar Ratio, Preparation Methods, Physical Stability, In Vitro and In Vivo Performance, and New Formulation Strategies

An imaging approach for determining the mechanism of enhancement of intestinal absorption of an L-theanine supplement

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