Application of hot-melt extrusion in the complexation of naringenin with cyclodextrin using hydrophilic polymers

Granados, Pedro A.; Pinho, Ludmila A.G.; Barreto, Lívia Cristina Lira de Sá; Gelfuso, Guilherme M.; Cunha-Filho, Marcílio

doi:10.1016/j.apt.2021.11.032

Cited by 17 publications

(17 citation statements)

References 58 publications

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“…Therefore, the selection of an appropriate stabilizer is of great importance [ 23 ]. Chitosan, polyvinylpyrrolidone (PVP), and other commonly used stabilizers have been used in the preparation of naringenin nanosuspensions (NRG-NSps) [ 24 , 25 , 26 , 27 ]. However, these NRG-NSps show certain drawbacks, such as low stability and poor bioavailability.…”

Section: Introductionmentioning

confidence: 99%

Preparation of Naringenin Nanosuspension and Its Antitussive and Expectorant Effects

et al. 2022

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Naringenin (NRG) is a natural flavonoid compound abundantly present in citrus fruits and has the potential to treat respiratory disorders. However, the clinical therapeutic effect of NRG is limited by its low bioavailability due to poor solubility. To enhance the solubility, naringenin nanosuspensions (NRG-NSps) were prepared by applying tocopherol polyethylene glycol succinate (TPGS) as the nanocarrier via the media-milling method. The particle size, morphology, and drug-loading content of NRG-NSps were examined, and the stability was evaluated by detecting particle size changes in different physiological media. NRG-NSps exhibited a flaky appearance with a mean diameter of 216.9 nm, and the drug-loading content was 66.7%. NRG-NSps exhibited good storage stability and media stability. NRG-NSps presented a sustainable release profile, and the cumulative drug-release rate approached approximately 95% within 7 d. NRG-NSps improved the antitussive effect significantly compared with the original NRG, the cough frequency was decreased from 22 to 15 times, and the cough incubation period was prolonged from 85.3 to 121.6 s. Besides, NRG-NSps also enhanced expectorant effects significantly, and phenol red secretion was increased from 1.02 to 1.45 μg/mL. These results indicate that NRG-NSps could enhance the bioavailability of NRG significantly and possess a potential clinical application.

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Section: Introductionmentioning

confidence: 99%

Preparation of Naringenin Nanosuspension and Its Antitussive and Expectorant Effects

et al. 2022

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“…The NRG NPs (1.0 mL) and the NRG powder suspension (1.0 mL) were placed in dialysis bags (MWCO: 8000-14,000, Sigma-Aldrich); then the dialysis bags were put in release media at 37 • C: artificial gastric juice (initial 4 h), artificial intestinal fluid (4-8 h), and PBS solution (8-96 h). The release medium (1.0 mL) was sampled at set time points (0.25, 0.5, 0.75, 1,2,4,6,8,10,12,24,36,48,72, and 96 h), and the extracted volume was replenished with fresh medium. The sampled media were filtered through 0.22 µm membrane and analyzed via HPLC-UV.…”

Section: In Vitro Release Profilementioning

confidence: 99%

“…Many biosafe and biodegradable materials have been utilized as nanocarriers to prepare the nanodelivery system for NRG, in particular, chitosan [21,22], cyclodextrin [23,24], polylactic acid [25,26], polylactic acid/glycolic acid copolymer [27,28], polycaprolactone [29,30], poly(vinylpyrrolidone) [31], and tocopheryl polyethylene glycol succinate (TPGS) [32,33]. Among them, TPGS has been utilized broadly as a nanocarrier to encapsulate NRG, because of its excellent amphiphilic properties, entrapment efficacy, and biosafety [34,35].…”

Section: Introductionmentioning

confidence: 99%

Optimization of Naringenin Nanoparticles to Improve the Antitussive Effects on Post-Infectious Cough

Dong

Wang

et al. 2022

Molecules

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Naringenin (NRG) is a natural compound with several biological activities; however, its bioavailability is limited owing to poor aqueous solubility. In this study, NRG nanoparticles (NPs) were prepared using the wet media milling method. To obtain NRG NPs with a small particle size and high drug-loading content, the preparation conditions, including stirring time, temperature, stirring speed, and milling media amount, were optimized. The NRG (30 mg) and D-α-tocopherol polyethylene glycol succinate (10 mg) were wet-milled in deionized water (2 mL) with 10 g of zirconia beads via stirring at 50 °C for 2 h at a stirring speed of 300 rpm. As a result, the NRG NPs, with sheet-like morphology and a diameter of approximately 182.2 nm, were successfully prepared. The NRG NPs were stable in the gastrointestinal system and were released effectively after entering the blood circulation. In vivo experiments indicated that the NRG NPs have good antitussive effects. The cough inhibition rate after the administration of the NRG NPs was 66.7%, cough frequency was three times lower, and the potential period was 1.8 times longer than that in the blank model group. In addition, the enzyme biomarkers and histological analysis results revealed that the NRG NPs can effectively regulate the inflammatory and oxidative stress response. In conclusion, the NRG NPs exhibited good oral bioavailability and promoted antitussive and anti-inflammatory effects.

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“…Continuous extrusion processes are controlled by the hot melt extruder panel, and the extrudate could be pelletized, milled, mixed and 3D printed to dosage forms such as tablets, film, granules, capsules, and so on, which promotes the scalability of this technology. Several HME commercial products approved by the Food and Drug Administration (FDA), currently available in the market with different release targets, prove the potential and success of this technology [ 24 , 25 , 26 , 27 ].…”

Section: Introductionmentioning

confidence: 99%

Preparation of Solid Dispersion of Polygonum Cuspidatum Extract by Hot Melt Extrusion to Enhance Oral Bioavailability of Resveratrol

Gao

et al. 2023

Molecules

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The aim of this study was to improve the solubility, bioavailability, and stability of resveratrol (RES-SD) Solid Dispersion in Polygonum cuspidatum extract (PCE) by hot melt extrusion (HME). In addition, the role of the auxiliary substances in PCE was also studied. The solid dispersion of Polygonum cuspidatum extract was prepared by hot-melt extrusion. The optimum formula was selected by single factor design and orthogonal test. The optimum formula was barrel temperature 140 °C, screw rotation speed 40 rpm/min, and the ratio of Polygonum cuspidatum extract to HPMCAS was 1:2. The dissolution test showed that PCE-SD increased the dissolution of RES from 46.75 ± 0.47% to 130.06 ± 0.12%. The pharmacokinetics curve of rats showed that PCE-SD increased AUC0-t of RES from 111,471.22 ± 11.4% to 160,458.968 ± 15.7%, indicating an approximately 1.44-fold increase in absorption. In addition, the rotation speed of PCE-SD screw is less than that of RES-SD screw. The bioavailability of PCE-SD was slightly better than that of RES-SD. PCE-SD is more hygroscopic than RES-SD. PCE-SD increased the solubility and oral bioavailability of RES. The auxiliary substances in Polygonum cuspidatum extract have influence on its preparation technology, stability, and bioavailability.

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Application of hot-melt extrusion in the complexation of naringenin with cyclodextrin using hydrophilic polymers

Cited by 17 publications

References 58 publications

Preparation of Naringenin Nanosuspension and Its Antitussive and Expectorant Effects

Preparation of Naringenin Nanosuspension and Its Antitussive and Expectorant Effects

Optimization of Naringenin Nanoparticles to Improve the Antitussive Effects on Post-Infectious Cough

Preparation of Solid Dispersion of Polygonum Cuspidatum Extract by Hot Melt Extrusion to Enhance Oral Bioavailability of Resveratrol

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