Physical characterization and <i>in vitro</i> skin permeation of solid lipid nanoparticles for transdermal delivery of quercetin

Han, Saet Byeol; Kwon, Soon Sik; Jeong, Yoo Min; Yu, Eun Ryeong; Park, S. N.

doi:10.1111/ics.12160

Cited by 60 publications

(25 citation statements)

References 28 publications

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“…The number of studies about the encapsulation of quercetin in lipid microparticles (nano or micro) has been increasing in the last five years (Li et al, 2009;Dhawan et al, 2011;Weiss-Angeli et al, 2012;Pool et al, 2013;Aditya et al, 2014;Han et al, 2014), but most studies have not evaluated the stability of encapsulated quercetin over the storage period. Scalia & Mezzena (2009) evaluated the stability of encapsulated quercetin in lipid microparticles that were composed of tristearin as the solid core and phosphatidylcholine as the surfactant, which were produced using ultra-agitation (mean diameters of 15-45 μm), and they found that 85% of the flavonoid remained in the particles after 90 days of storage in the dark.…”

Section: Physico-chemical Characterization and Stability Along The Stmentioning

confidence: 99%

Effect of different stress conditions on the stability of quercetin-loaded lipid microparticles produced with babacu ( Orbignya speciosa ) oil: evaluation of their potential use in food applications

Cazado

Pinho

2016

Food Sci. Technol

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Lipid micro and nanoparticles have been extensively investigated as carriers for hydrophobic bioactives in food systems because they can simultaneously increase the dispersibility of these lipophilic substances and help improve their bioavailability. In this study, lipid microparticles of babacu oil and denatured whey protein isolate were produced, and their ability to protect quercetin against degradation was evaluated over 30 days of storage. Additionally, the lipid microparticles were subjected to the typical stress conditions of food processing (presence of sucrose, salt, and thermal stresses), and their physico-chemical stability was monitored. The data show that the babacu microparticles efficiently avoided the oxidation of quercetin because 85% of the initial amount of the flavonoid was preserved after 30 days. The particles were notably stable up to a temperature of 70 °C for 10 minutes at relatively high concentrations of salt and sucrose. The type of stirring (mechanical or magnetic) also strongly affected the stability of the dispersions.

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Section: Physico-chemical Characterization and Stability Along The Stmentioning

confidence: 99%

Effect of different stress conditions on the stability of quercetin-loaded lipid microparticles produced with babacu ( Orbignya speciosa ) oil: evaluation of their potential use in food applications

Cazado

Pinho

2016

Food Sci. Technol

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“…With these features, SLN formulations have the potential to improve the bioavailability and stability of drugs for topical therapy . Therefore, SLN have been intensively explored for drug delivery in the last decade and have been studied for different routes of administration; oral, ocular, nasal, topical, for both local, and systemic effect; however, only few works have been introducing their use for treatment of buccal mucosal diseases, in which Karavana et al introduced a new approach for the treatment of recurrent aphthous stomatitis using SLN‐containing cyclosporine, dispersed in a gel matrix.…”

Section: Introductionmentioning

confidence: 99%

Gelucire-Based Nanoparticles for Curcumin Targeting to Oral Mucosa: Preparation, Characterization, and Antimicrobial Activity Assessment

Hazzah

Farid

Nasra

et al. 2015

Journal of Pharmaceutical Sciences

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“…Next, the cells were washed three times with cold PBS and stained with 4 ,6-diamidino-2-phenylindole (DAPI). Later, the coverslips were visualized using a laser scanning confocal microscope (LSCM, Leica TCS SP8 X, Wetzlar, Germany) using appropriate excitation and emission wavelengths (405/450 nm for DAPI and 470/504 nm for Cou-6) [38,39]. In Vitro Cytotoxicity Analysis Cytotoxicity of the CAT3 suspension, OA-CAT3-SLN, and blank SLN against the C6 brain glioma cell line was measured by 3-(4,5-dimethylthiazol-2-yl)-2,5 diphenyltetrazolium bromide (MTT) assay.…”

Section: In Vitro Cellular Uptake Studymentioning

confidence: 99%

Improving the Oral Bioavailability of an Anti-Glioma Prodrug CAT3 Using Novel Solid Lipid Nanoparticles Containing Oleic Acid-CAT3 Conjugates

Wang

Lin

et al. 2020

Pharmaceutics

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13a-(S)-3-pivaloyloxyl-6,7-dimethoxyphenanthro(9,10-b)-indolizidine (CAT3) is a novel oral anti-glioma pro-drug with a potent anti-tumor effect against temozolomide-resistant glioma in vivo. However, poor lipid solubility has limited the encapsulation efficacy during formulation development. Moreover, although the active metabolite of CAT3, 13a(S)-3-hydroxyl-6,7-dimethoxyphenanthro(9,10-b)-indolizidine (PF403), can penetrate the blood-brain barrier and approach the brain tissue with a 1000-fold higher anti-glioma activity than CAT3 in vitro, its bioavailability and Cmax were considerably low in plasma, limiting the anti-tumor efficacy. In this study, a novel oleic acid-CAT3 conjugate (OA-CAT3) was synthesized at the first time to increase the lipid solubility of CAT3. The OA-CAT3 loaded solid lipid nanoparticles (OA-CAT3-SLN) were constructed using an ultrasonic technique to enhance the bioavailability and Cmax of PF403 in plasma. Our results demonstrated that CAT3 was amorphous in the lipid core of OA-CAT3-SLN and the in vitro release was well controlled. Furthermore, the encapsulation efficacy and the zeta potential increased to 80.65 ± 6.79% and −26.7 ± 0.46 mV, respectively, compared to the normal CAT3 loaded SLN. As indicated by the high-performance liquid chromatography-mass spectrometry (HPLC-MS/MS) quantitation, the monolayer cellular transepithelial transport rate of OA-CAT3-SLN improved by 2.42-fold relied on cholesterol compared to the CAT3 suspension. Hence, the in vitro cell viability of OA-CAT3-SLN in C6 glioma cells decreased to 29.77% ± 2.13% and 10.75% ± 3.12% at 48 and 72 h, respectively. Finally, compared to the CAT3 suspension, the in vivo pharmacokinetics in rats indicated that the plasma bioavailability and Cmax of PF403 as afforded by OA-CAT3-SLN increased by 1.7- and 5.5-fold, respectively. Overall, the results indicate that OA-CAT3-SLN could be an efficacious delivery system in the treatment of glioma.

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Physical characterization and in vitro skin permeation of solid lipid nanoparticles for transdermal delivery of quercetin

Abstract: The results suggest that QSLN-2, prepared with a surfactant content of 2%, could be used as useful skin delivery system for transdermal delivery of hydrophobic antioxidants such as quercetin.

Cited by 60 publications

References 28 publications

Effect of different stress conditions on the stability of quercetin-loaded lipid microparticles produced with babacu ( Orbignya speciosa ) oil: evaluation of their potential use in food applications

Effect of different stress conditions on the stability of quercetin-loaded lipid microparticles produced with babacu ( Orbignya speciosa ) oil: evaluation of their potential use in food applications

Gelucire-Based Nanoparticles for Curcumin Targeting to Oral Mucosa: Preparation, Characterization, and Antimicrobial Activity Assessment

Improving the Oral Bioavailability of an Anti-Glioma Prodrug CAT3 Using Novel Solid Lipid Nanoparticles Containing Oleic Acid-CAT3 Conjugates

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