Formulation and &lt;I&gt;In Vitro&lt;/I&gt; Evaluation of Quercetin Loaded Polymeric Micelles Composed of Pluronic P123 and D-a-Tocopheryl Polyethylene Glycol Succinate

Zhao, Liyan; Shi, Yikang; Zou, Shaohua; Sun, Min; Lil, Lingbing; Zhail, Guangxi

doi:10.1166/jbn.2011.1298

Cited by 58 publications

(45 citation statements)

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“…Consistent with previous reports, 47,48 the particle size of drug-loaded micelles was around 20 nm in our study (Figure 2). Small particles could reduce the uptake and reorganization of the reticuloendothelial system and prolong the systemic circulation time in the blood.…”

supporting

confidence: 93%

“…49 In addition, it was found that 90% LTG in the stock solution was released within the first 2 hours, while only 46.3% of LTG was released from the P123 micelles during the same time period (Figure 3), indicating a sustained release behavior, which is similar to previous studies. 47,48 It should be noted that about 20% of LTG remained in micelles even after 24 hours, and further release was negligible thereafter (data not shown). This kind of release behavior may be attributed to the crystalline formation of the abundant loaded drugs as a separate phase inside the micellar core, subsequently leading to a slower or even retarded drug release.…”

mentioning

confidence: 92%

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Enhanced brain delivery of lamotrigine with Pluronic® P123-based nanocarrier

Liu¹,

Wang²,

Zhou³

et al. 2014

IJN

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Background P-glycoprotein (P-gp) mediated drug efflux across the blood–brain barrier (BBB) is an important mechanism underlying poor brain penetration of certain antiepileptic drugs (AEDs). Nanomaterials, as drug carriers, can overcome P-gp activity and improve the targeted delivery of AEDs. However, their applications in the delivery of AEDs have not been adequately investigated. The objective of this study was to develop a nano-scale delivery system to improve the solubility and brain penetration of the antiepileptic drug lamotrigine (LTG). Methods LTG-loaded Pluronic ® P123 (P123) polymeric micelles (P123/LTG) were prepared by thin-film hydration, and brain penetration capability of the nanocarrier was evaluated. Results The mean encapsulating efficiency for the optimized formulation was 98.07%; drug-loading was 5.63%, and particle size was 18.73 nm. The solubility of LTG in P123/LTG can increase to 2.17 mg/mL, making it available as a solution. The in vitro release of LTG from P123LTG presented a sustained-release property. Compared with free LTG, the LTG-incorporated micelles accumulated more in the brain at 0.5, 1, and 4 hours after intravenous administration in rats. Pretreatment with systemic verapamil increased the rapid brain penetration of free LTG but not P123/LTG. Incorporating another P-gp substrate (Rhodamine 123) into P123 micelles also showed higher efficiency in penetrating the BBB in vitro and in vivo. Conclusion These results indicated that P123 micelles have the potential to overcome the activity of P-gp expressed on the BBB and therefore show potential for the targeted delivery of AEDs. Future studies are necessary to further evaluate the appropriateness of the nanocarrier to enhance the efficacy of AEDs.

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confidence: 93%

mentioning

confidence: 92%

Enhanced brain delivery of lamotrigine with Pluronic® P123-based nanocarrier

Liu¹,

Wang²,

Zhou³

et al. 2014

IJN

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“…For comparison, the release of GA from dimethyl sulfoxide solution was conducted under the same conditions. 31 Cell culture multidrug-resistant NCI/ADR-RES cells were obtained from the National Cancer Institute (Bethesda, MD). Cells were cultured in RPMI 1640 media supplemented with 10% fetal bovine serum and 1% penicillin/streptomycin (all from Mediatech, Manassas, VA).…”

Section: In Vitro Drug Releasementioning

confidence: 99%

Poloxamer 407/TPGS mixed micelles for delivery of gambogic acid to breast and multidrug-resistant cancer

Saxena¹,

Hussain²

2012

IJN

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Background: Delivery of a high concentration of anticancer drugs specifically to cancer cells remains the biggest challenge for the treatment of multidrug-resistant cancer. Poloxamers and D-α-Tocopheryl polyethylene glycol 1000 succinate (TPGS) are known inhibitors of P-glycoprotein (P-gp). Mixed micelles prepared from Poloxamer 407 and TPGS may increase the therapeutic efficacy of the drug by delivering high concentrations inside the cells and inhibiting P-gp. Gambogic acid (GA) is a naturally derived novel anticancer agent, but poor solubility and toxic side effects limit its use. In this study, we have developed Poloxamer 407 and TPGS mixed micelle-encapsulating GA for the treatment of breast and multidrug-resistant cancer. Methods: GA-loaded Poloxamer 407/TPGS mixed micelles were prepared using a thin film hydration method, and their physicochemical properties were characterized. Cellular accumulation and cytotoxicity of the GA-loaded Poloxamer 407/TPGS mixed micelles were studied in breast cancer cells, MCF-7 cells, and multidrug-resistant NCI/ADR-RES cells. Results:The diameter of GA-loaded Poloxamer 407/TPGS mixed micelles was about 17.4 ± 0.5 nm and the zeta potential -13.57 mV. The entrapment efficiency of GA was 93.1% ± 0.5% and drug loading was about 9.38% ± 0.29%. Differential scanning calorimetry and X-ray powder diffraction studies confirmed that GA is encapsulated by the polymers. The in vitro release studies showed that mixed micelles sustained the release of GA for more than 4 days. Results from cellular uptake studies indicated that GA-loaded Poloxamer 407/TPGS mixed micelles had increased cellular uptake of GA in NCI/ADR-RES cells. Cytotoxicity of GA-loaded Poloxamer 407/TPGS mixed micelles was found to be 2.9 times higher in multidrug-resistant NCI/ADR-RES cells, and 1.6 times higher in MCF-7 cells, as compared with unencapsulated GA. Conclusion: This study suggests that Poloxamer 407/TPGS mixed micelles can be used as a delivery system for GA to treat breast and multidrug-resistant cancer.

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“…25 The Que-LMPM solution containing 2 mg Que or 2 mL free Que solution (1 mg/mL in propylene glycol) was put into a separate dialysis bag (MWCO 3,500, Cellu-Sep ® T1 [Orange Scientific, Seguin, TX, USA]; Seguin, TX, USA). The bag was placed in a conical flask immersed in 100 mL of dissolution medium at 37°C with 100 rpm shaking.…”

Section: In Vitro Release Studiesmentioning

confidence: 99%

“…Notably, doxorubicin-loaded MPMs composed of Pluronic L61 and F127 were successfully evaluated in a Phase II study in patients with advanced esophageal carcinoma. 24 Zhao et al 25 prepared MPMs using Pluronic P123 and d-alpha tocopheryl polyethylene glycol succinate (TPGS), and the solubility of Que dramatically increased to 5.56 mg/ mL (a 2,738-fold increase compared to free Que). Therefore, MPMs offer synergistic properties such as increased drug stability, loading efficiencies, and efficacy that are superior to those of traditional micelles using individual components.…”

Section: Introductionmentioning

confidence: 99%

Development and characterization of self-assembling lecithin-based mixed polymeric micelles containing quercetin in cancer treatment and an in vivo pharmacokinetic study

Chen¹,

Chen²,

Su³

et al. 2016

IJN

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Quercetin (Que) is known to have biological benefits including an anticancer effect, but low water solubility limits its clinical application. The aim of this study was to develop a lecithin-based mixed polymeric micelle (LMPM) delivery system to improve the solubility and bioavailability of Que. The optimal Que-LMPM, composed of Que, lecithin, Pluronic ® P123, and 1,2-distearoyl- sn -glycero-3-phosphoethanolamine- N -methoxy[poly(ethylene glycol)-2000] in a proportion of 3:1:17.5:2.5 (w/w), was prepared by a thin-film method. The average size, polydispersion index, encapsulating efficiency, and drug loading of Que-LMPM were 61.60±5.02 nm, 0.589±0.198, 96.87%±9.04%, and 12.18%±1.11%, respectively. The solubility of Que in the Que-LMPM system increased to 5.81 mg/mL, compared to that of free Que in water of 0.17–7.7 μg/mL. The Que-LMPM system presented a sustained-release property in vitro. The in vitro cytotoxicity assay showed that the 50% inhibitory concentration values toward MCF-7 breast cancer cells for free Que, blank LMPMs, and Que-LMPMs were >200, >200, and 110 μM, respectively, indicating the nontoxicity of the LMPM carrier, but the LMPM formulation enhanced the cytotoxicity of Que against MCF-7 cells. A cellular uptake assay also confirmed the intake of Que-LMPM by MCF-7 cells. An in vivo pharmacokinetic study demonstrated that Que-LMPMs had higher area under the concentration–time curve and a longer half-life, leading to better bioavailability compared to a free Que injection. Due to their nanosize, core–shell structure, and solubilization potential, LMPMs were successfully developed as a drug delivery system for Que to improve its solubility and bioavailability.

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Formulation and <I>In Vitro</I> Evaluation of Quercetin Loaded Polymeric Micelles Composed of Pluronic P123 and D-a-Tocopheryl Polyethylene Glycol Succinate

Cited by 58 publications

References 0 publications

Enhanced brain delivery of lamotrigine with Pluronic® P123-based nanocarrier

Enhanced brain delivery of lamotrigine with Pluronic® P123-based nanocarrier

Poloxamer 407/TPGS mixed micelles for delivery of gambogic acid to breast and multidrug-resistant cancer

Development and characterization of self-assembling lecithin-based mixed polymeric micelles containing quercetin in cancer treatment and an in vivo pharmacokinetic study

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Formulation and <I>In Vitro</I> Evaluation of Quercetin Loaded Polymeric Micelles Composed of Pluronic P123 and D-a-Tocopheryl Polyethylene Glycol Succinate

Cited by 58 publications

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Enhanced brain delivery of lamotrigine with Pluronic&reg; P123-based nanocarrier

Enhanced brain delivery of lamotrigine with Pluronic&reg; P123-based nanocarrier

Poloxamer 407/TPGS mixed micelles for delivery of gambogic acid to breast and multidrug-resistant cancer

Development and characterization of self-assembling lecithin-based mixed polymeric micelles containing quercetin in cancer treatment and an in vivo pharmacokinetic study

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Product

Resources

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Enhanced brain delivery of lamotrigine with Pluronic® P123-based nanocarrier

Enhanced brain delivery of lamotrigine with Pluronic® P123-based nanocarrier