Enhancement of oral bioavailability of magnolol by encapsulation in mixed micelles containing pluronic F127 and L61

Shen, Hongxue; Liu, Sheng; Ding, Pinggang; Wang, Lulu; Ju, Jianming; Guo-hui, Liang

doi:10.1111/jphp.12887

Cited by 18 publications

(8 citation statements)

References 43 publications

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“…These findings support that magnolol being a smaller molecule compared to ibuprofen, caffeine, doxorubicin, and alendronate can be easily incorporated into the Uio-66(Zr) framework. This work presents better drug loading capacity of magnolol into the MOF compared to unfunctionalized and functionalized mesoporous silica (5.5% and 12.5%, respectively) [14], binary micelle system (SOL-HS15: 4.12%, and SOL-TPGS:4.03%) [13], Pluronic micelle system (27.58%) [12], polyketal microparticles (Mag-PK3: 7.86% and Mag-PLGA: 6.16%) [56], and ultrafine fibrous mats (20-30%) [57] but lower than hydrogel nanoparticles (91.6%) [15].…”

Section: Figurementioning

confidence: 91%

“…Furthermore, the use of Uio-66(Zr) prolonged the duration of the drug in the blood as indicated by a longer Tmax, T 1/2 , and abs T 1/2 . The Tmax of mag@uio-66(Zr) (3.26 h) is longer compared to other related drug delivery system of magnolol using Pluronic F127-L61 (0.75 ± 0.158) [12], SOL-HS15 micellar system (0.708 ± 0.188) [13], and SOL-TPGS micellar system (0.750 ± 0.158) [13].…”

Section: Figurementioning

confidence: 94%

“…Pure Uio-66(Zr) and mag@Uio-66(Zr) were characterized and compared to assess magnolol impregnation by thermogravimetric analysis (TGA), powder X-ray diffraction (PXRD), and nitrogen sorption isothermal techniques. Our study reports Approaches to increase the bioavailability of magnolol include the use of micellar particles [12,13], mesoporous silica [14], nanoparticles [15,16], solid dispersions [17,18], and liposomes [19]. As part of our continuing efforts to increase the bioavailability of biologically active natural products with limited solubility in aqueous systems, a metal organic framework (MOF) was utilized in this study as drug delivery system for crystalline yellow magnolol (1).…”

Section: Introductionmentioning

confidence: 99%

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Enhanced Oral Bioavailability of the Pharmacologically Active Lignin Magnolol via Zr-Based Metal Organic Framework Impregnation

et al. 2020

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Bioavailability plays an important role in drug activity in the human body, as certain drug amounts should be present to elicit activity. However, low bioavailability of drugs leads to negligible use for human benefit. In this study, the diversely active neolignan, magnolol, was impregnated onto a Zr-based organometallic framework [Uio-66(Zr)] to increase its low bioavailability (4–5%) and to test its potential acute oral toxicity. Synthesis of Uio-66(Zr) was done through the solvothermal method while simple impregnation at different time points was used to incorporate magnolol. The loading capacity of Uio-66(Zr) at 36 h was found to be significantly higher at 72.16 ± 2.15% magnolol than in other incubation time. Based on the OECD 425 (limit test), toxicity was not observed at 2000 mg kg−1 dose of mag@Uio-66(Zr) in female Sprague Dawley rats. The area under the curve (AUC) at 0–720 min of mag@Uio-66(Zr) was significantly higher than the AUC of free magnolol. Moreover, relative bioavailability increased almost two-folds using Uio-66(Zr). Unconjugated magnolol was found in the liver, kidney, and brain of rats in all treatment groups. Collectively, Uio-66(Zr) provided a higher magnolol bioavailability when used as drug carrier. Thus, utilization of Uio-66(Zr) as drug carrier is of importance for maximal use for poorly soluble and lowly bioavailable drugs.

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Section: Figurementioning

confidence: 91%

Section: Figurementioning

confidence: 94%

Section: Introductionmentioning

confidence: 99%

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Enhanced Oral Bioavailability of the Pharmacologically Active Lignin Magnolol via Zr-Based Metal Organic Framework Impregnation

et al. 2020

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“…To study the effect of dilution on particle size stability, the MMs and MNs samples were diluted 10, 50, 100, and 200fold with water (Shen et al, 2018), and the particle sizes of the samples were measured using a Malvern zeta sizer as described above. All the experiments were performed in triplicate.…”

Section: Dilution Stabilitymentioning

confidence: 99%

Enhanced oral bioavailability of magnolol via mixed micelles and nanosuspensions based on Soluplus ^® -Poloxamer 188

Yong-chun

et al. 2020

Drug Delivery

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Magnolol, known to have extensive biological activities, is the major bioactive ingredient isolated from the root and stem bark of Magnolia officinalis. However, the clinical application of magnolol is limited by poor aqueous solubility and absorption. The aim of this study is to develop novel mixed micelles and nanosuspensions composed of two biocompatible copolymers, Soluplus V R and Poloxamer 188, and to improve the solubility and oral bioavailability of magnolol. The magnolol-loaded mixed micelles (MMs) and magnolol nanosuspensions (MNs) were prepared to use film hydration and antisolvent methods, respectively. The optimal MMs and MNs formulations were prepared to use magnolol, Soluplus V R , and Poloxamer 188 in ratios of 1:12:5 and 2:1:1, respectively. The average particle size of MMs was 111.8 ± 14.6, and MNs was 78.53 ± 5.4 nm. The entrapment and drug loading efficiency for MMs were 89.58 ± 2.54% and 5.46 ± 0.65%, correspondingly. The drug loading efficiency of MNs was 42.50 ± 1.57%. In the in vitro release study, MMs showed a slow drug release while that of MNs was fast. The results of the Caco-2 transcellular transport study indicated that both MMs and MNs increased the permeation of magnolol. MMs and MNs markedly promoted gastrointestinal drug absorption by 2.85 and 2.27-fold, respectively, as shown in the pharmacokinetics study. These results indicated that both MMs and MNs formulations prepared with Soluplus V R and Poloxamer 188 are promising drug delivery systems for improving the oral absorption of insoluble drugs in the gastrointestinal tract.

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“…Due to the low water solubility and quick metabolism, magnolol has a low bioavailability and limits its applications in clinical development. The mixed micelles containing pluronic F127 and L61 for delivering magnolol might be a well strategy for resolving its problem of poor solubility and bioavailability [31]. Similarly, solid dispersion of magnolol with polyvinylpyrrolidone K-30 (PVP) has been shown to increase water solubility of magnolol from 12 to 105 μ g/mL, when PVP concentration increases from 0 to 100 μ M. The pharmacokinetic parameters indicate that the AUC 0- t and C max of magnolol in solid dispersion with PVP are 80.1% and 44.7%.…”

Section: Metabolism and Pharmacokinetic Features Of Magnololmentioning

confidence: 99%

Insights on the Multifunctional Activities of Magnolol

Zhang

Chen

Huang

et al. 2019

BioMed Research International

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Over years, various biological constituents are isolated from Traditional Chinese Medicine and confirmed to show multifunctional activities. Magnolol, a hydroxylated biphenyl natural compound isolated from Magnolia officinalis, has been extensively documented and shows a range of biological activities. Many signaling pathways include, but are not limited to, NF-κB/MAPK, Nrf2/HO-1, and PI3K/Akt pathways, which are implicated in the biological functions mediated by magnolol. Thus, magnolol is considered as a promising therapeutic agent for clinic research. However, the low water solubility, the low bioavailability, and the rapid metabolism of magnolol dramatically limit its clinical application. In this review, we will comprehensively discuss the last five-year progress of the biological activities of magnolol, including anti-inflammatory, antimicroorganism, antioxidative, anticancer, neuroprotective, cardiovascular protection, metabolism regulation, and ion-mediating activity.

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Enhancement of oral bioavailability of magnolol by encapsulation in mixed micelles containing pluronic F127 and L61

Abstract: The mixed micelles containing pluronic F127 and L61 as drug delivery system provided a well strategy for resolving the poor solubility and bioavailability problems of MAG.

Cited by 18 publications

References 43 publications

Enhanced Oral Bioavailability of the Pharmacologically Active Lignin Magnolol via Zr-Based Metal Organic Framework Impregnation

Enhanced Oral Bioavailability of the Pharmacologically Active Lignin Magnolol via Zr-Based Metal Organic Framework Impregnation

Enhanced oral bioavailability of magnolol via mixed micelles and nanosuspensions based on Soluplus ^® -Poloxamer 188

Insights on the Multifunctional Activities of Magnolol

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Enhancement of oral bioavailability of magnolol by encapsulation in mixed micelles containing pluronic F127 and L61

Abstract: The mixed micelles containing pluronic F127 and L61 as drug delivery system provided a well strategy for resolving the poor solubility and bioavailability problems of MAG.

Cited by 18 publications

References 43 publications

Enhanced Oral Bioavailability of the Pharmacologically Active Lignin Magnolol via Zr-Based Metal Organic Framework Impregnation

Enhanced Oral Bioavailability of the Pharmacologically Active Lignin Magnolol via Zr-Based Metal Organic Framework Impregnation

Enhanced oral bioavailability of magnolol via mixed micelles and nanosuspensions based on Soluplus ® -Poloxamer 188

Insights on the Multifunctional Activities of Magnolol

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Enhanced oral bioavailability of magnolol via mixed micelles and nanosuspensions based on Soluplus ^® -Poloxamer 188