Improved Bioavailability of β-Carotene by Amorphous Solid Dispersion Technology in Rats

Otani, Shuichi; Miki, Shohei; Nakamura, Yuta; Ishimoto, Kenji; Ago, Yukio; Nakagawa, Shinsaku

doi:10.3177/jnsv.66.207

Cited by 11 publications

(15 citation statements)

References 15 publications

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“…The nanoparticles prepared with THF displayed a larger size because of the relatively higher viscosity and lower diffusion coefficients in water. The results suggest that the properties of PLGA nanoparticles would be affected by the organic phase, and the particle size was consistent with that in our study [ 38 ].…”

Section: Discussionsupporting

confidence: 92%

“…Although the crystal signal was not different between the nanoparticles and physical mixture groups, disappearance of the endothermic peaks of the nanoformulations was observed, suggesting that the BC had an amorphous state. The amorphous state may benefit the solubility of BC and further improve the oral absorption [ 38 ]. For the in vitro release study, dissolution methods applying non-sink conditions have become an increasingly important tool to evaluate the true performance of supersaturating formulations and drug delivery systems [ 44 ].…”

Section: Discussionmentioning

confidence: 99%

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Poly (Lactic-Co-Glycolic) Acid–Poly (Vinyl Pyrrolidone) Hybrid Nanoparticles to Improve the Efficiency of Oral Delivery of β-Carotene

Liu

Hsieh

2022

Pharmaceutics

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The aim of this study was to develop a nanoparticle formulation made of poly (vinyl pyrrolidone) (PVP) and poly (lactic-co-glycolic) acid (PLGA) for the oral delivery of β-carotene (BC). The hybrid nanoparticles were prepared by the interfacial deposition method, and the physicochemical properties of this formulation were characterized in terms of its morphology, particle size, size distribution, encapsulation efficiency, dissolution, intestinal permeability, and in vivo pharmacokinetics. Our results demonstrated that BC-loaded nanoformulation and PLGA nanoparticles (PNP) significantly enhanced a release 6.1 times higher than BC suspension. The fortification of PVP into PLGA nanoparticles, named PLGA–PVP hybrid nanoparticles (PPNP), significantly reduced the particle size, as well as led to an increase 1.9 times higher in the in vitro release of BC, compared with PNP. For the ex vivo intestinal permeability assessment, PNP and PPNP–K15 significantly enhanced the intestinal permeability by 2.7 and 6.5 times at the jejunum, and 2.3 and 4.5 times at the ileum, when compared with unformulated BC. According to the pharmacokinetic study, the optimized hybrid formulation significantly increased the peak plasma concentration (Cmax) and the area under the curve (AUC0-t), and the oral relative bioavailability showed a five-fold enhancement compared with that of the BC suspension. Our results indicate that the hybrid nanoparticulate delivery system is an efficient strategy for the oral delivery of BC.

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Section: Discussionsupporting

confidence: 92%

Section: Discussionmentioning

confidence: 99%

Poly (Lactic-Co-Glycolic) Acid–Poly (Vinyl Pyrrolidone) Hybrid Nanoparticles to Improve the Efficiency of Oral Delivery of β-Carotene

Liu

Hsieh

2022

Pharmaceutics

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“…In the present study, we prepared serum samples with the highest NRG concentration obtained after oral NRG SD administration and used it in the intravenous administration test. This experiment was feasible because our SD had high C max ( 18 ). The pharmacokinetic analysis indicated that the distribution volume of the unchanged NRG and NRG metabolites was equivalent to ∼20% of the body weight and that the elimination rate constant k e was high ( Table 2 ).…”

Section: Discussionmentioning

confidence: 99%

“…Our SDs are prepared by mixing food-grade polymers and emulsifiers with low-solubility food ingredients at high temperature. Previous studies showed that amorphization of a functional food ingredient with poor water solubility, such as β-carotene, dramatically improved its gastrointestinal absorption ( 15 , 17 , 18 ). The main advantage of this method is that it develops safe formulations, and all functional and base materials are food-grade substances.…”

Section: Introductionmentioning

confidence: 99%

Physicochemical and Biochemical Evaluation of Amorphous Solid Dispersion of Naringenin Prepared Using Hot-Melt Extrusion

et al. 2022

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Naringenin (NRG) is a plant-derived flavonoid. Due to its antioxidant, anti-inflammatory, and analgesic activities it is beneficial to human health and is often used as a functional food ingredient; however, it has poor water solubility and low in vivo bioavailability. Therefore, the efficacy of NRG can be improved by enhancing its water solubility to increase gastrointestinal absorption. Conventional methods for the formulation of NRG are very complex and use toxic organic solvents, making them impractical for the production of functional foods. The objective of this study was to develop a safe and effective NRG-based functional food material. Previously, we established a technology to prepare amorphous solid dispersions (SDs) from functional food ingredients with poor water solubility and used hot-melt extrusion technology that is comparatively simple and does not involve the use of organic solvents. In this study, we prepared NRG SD and evaluated them both physicochemically and biochemically. NRG SD had superior water solubility and gastrointestinal absorption relative to native NRG and showed higher analgesic efficacy in rats than crystalline NRG. NRG SD was administered to mice in a mixed diet for 28 days, and organ weights and hematological/clinical biochemical parameters were assessed. NRG SD did not demonstrate severe adverse effects. The results suggest that NRG SD is a safe and highly efficacious formulation that can be used as a functional food material in the future.

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“…The low solubility of β-carotene in rats was improved via an amorphous state induced by solid dispersion prepared by hot-melt technology with polyvinylpyrrolidone and sucrose fatty acid esters. The importance of this technology is associated with improvements in the solubility of β-carotene without organic solvents with potential use in pharmaceutical as well as food industry [ 226 ]. Similarly, β-carotene solid dispersion prepared by hot-melt technology, which were found to have an amorphous structure, improves its solubility in water [ 227 ].…”

Section: The Content and Bioavailability Of Carotenoidsmentioning

confidence: 99%

Carotenoids in Cancer Apoptosis—The Road from Bench to Bedside and Back

Koklesová

Líšková

Samec

et al. 2020

Cancers

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An incidence and mortality of cancer are rapidly growing worldwide, especially due to heterogeneous character of the disease that is associated with irreversible impairment of cellular homeostasis and function. Targeting apoptosis, one of cancer hallmarks, represents a potent cancer treatment strategy. Carotenoids are phytochemicals represented by carotenes, xanthophylls, and derived compounds such as apocarotenoids that demonstrate a broad spectrum of anti-cancer effects involving pro-apoptotic signaling through extrinsic and intrinsic pathways. As demonstrated in preclinical oncology research, the apoptotic modulation is performed at post-genomic levels. Further, carotenoids demonstrate additive/synergistic action in combination with conventional oncostatic agents. In addition, a sensitization of tumor cells to anti-cancer conventional treatment can be achieved by carotenoids. The disadvantage of anti-cancer application of carotenoids is associated with their low solubility and, therefore, poor bioavailability. However, this deficiency can be improved by using nanotechnological approaches, solid dispersions, microemulsions or biofortification that significantly increase the anti-cancer and pro-apoptotic efficacy of carotenoids. Only limited number of studies dealing with apoptotic potential of carotenoids has been published in clinical sphere. Pro-apoptotic effects of carotenoids should be beneficial for individuals at high risk of cancer development. The article considers the utility of carotenoids in the framework of 3P medicine.

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Improved Bioavailability of β-Carotene by Amorphous Solid Dispersion Technology in Rats

Cited by 11 publications

References 15 publications

Poly (Lactic-Co-Glycolic) Acid–Poly (Vinyl Pyrrolidone) Hybrid Nanoparticles to Improve the Efficiency of Oral Delivery of β-Carotene

Poly (Lactic-Co-Glycolic) Acid–Poly (Vinyl Pyrrolidone) Hybrid Nanoparticles to Improve the Efficiency of Oral Delivery of β-Carotene

Physicochemical and Biochemical Evaluation of Amorphous Solid Dispersion of Naringenin Prepared Using Hot-Melt Extrusion

Carotenoids in Cancer Apoptosis—The Road from Bench to Bedside and Back

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