Preparation, optimization, characterization and cytotoxicity in vitro of Baicalin-loaded mixed micelles

Zhang, Haiqun; Zhao, Lili; Chu, Lianjun; Han, Xu; Zhai, Guangxi

doi:10.1016/j.jcis.2014.07.045

Cited by 43 publications

(24 citation statements)

References 49 publications

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“…effectively avoid being metabolized by the liver or filtered out by the kidneys (De et al, 2008;Yu et al, 2010). Therefore, these SF-IS mixed micelles with particle sizes of 12.88 nm could effectively avoid rapid metabolism and elimination, and guarantee the stability and long circulation time (Zhang et al, 2014). In addition, HS15 and F127 can markedly reduce IS efflux and improve the concentration of the drug in cells which could enhance permeability and retention (ERP) effect and passive targeting ability ( Figure 7B).…”

Section: Discussionmentioning

confidence: 99%

“…This system has several advantages including enhancing drug solubility, ability to control drug release, avoiding reticuloendothelial system (RES) uptake, and tumor targeting ability (Wu & Guan, 2015). Based on the theory of synergistic effect, mixed micelles composed of two and more excipients exhibit preferable characteristics to micelles formed from a single material (Zhang et al, 2014). In our previous study (Li et al, 2012), a self-assembled mixture micelles (fatty acid-IS-bile salts) was prepared to improve oral absorption in order to strengthen the effect of warming kidney enhancing yang, but the effect was not significant (Jun et al, 2015).…”

Section: Introductionmentioning

confidence: 99%

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Preparation and evaluation of icariside II-loaded binary mixed micelles using Solutol HS15 and Pluronic F127 as carriers

et al. 2016

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An effective anti-cancer drug, icariside II (IS), has been used to treat a variety of cancers in vitro. However, its poor aqueous solubility and permeability lead to low oral bioavailability. The aim of this work was to use Solutol Õ HS15 and Pluronic F127 as surfactants to develop novel mixed micelles to enhance the oral bioavailability of IS by improving permeability and inhibiting efflux. The IS-loaded mixed micelles were prepared using the method of ethanol thin-film hydration. The physicochemical properties, dissolution property, oral bioavailability of the male SD rats, permeability and efflux of Caco-2 transport models, and gastrointestinal safety of the mixed micelles were evaluated. The optimized IS-loaded mixed micelles showed that at 4:1 ratio of Solutol Õ HS15 and Pluronic F127, the particle size was 12.88 nm with an acceptable polydispersity index of 0.172. Entrapment efficiency (94.6%) and drug loading (9.7%) contributed to the high solubility (11.7 mg/mL in water) of IS, which increased about 900-fold. The SF-IS mixed micelle release profile showed a better sustained release property than that of IS. In Caco-2 cell monolayer models, the efflux ratio dramatically decreased by 83.5%, and the relative bioavailability of the mixed micelles (AUC 0-1 ) compared with that of IS (AUC 0-1 ) was 317%, indicating potential for clinical application. In addition, a gastrointestinal safety assay also provided reliable clinical evidence for the safe use of this micelle.

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Preparation and evaluation of icariside II-loaded binary mixed micelles using Solutol HS15 and Pluronic F127 as carriers

et al. 2016

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“…Mixed micelles have synergistic properties such as increased drug stability and drug loading efficiency compared to that of the individual components (Potluri et al, 2006;Pooja et al, 2014;Zhang et al, 2014). To the best of our knowledge, no studies have shown the influence of mixed micelles for the delivery of baohuoside I.…”

Section: Introductionmentioning

confidence: 99%

Hyaluronic acid-modified didecyldimethylammonium bromide/ d-a-tocopheryl polyethylene glycol succinate mixed micelles for delivery of baohuoside I against non-small cell lung cancer: in vitro and in vivo evaluation

et al. 2017

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Baohuoside I is an effective but a poorly soluble antitumor drug. In this study, we prepared baohuoside I-loaded mixed micelles with didecyldimethylammonium bromide (DDAB) and D-atocopheryl polyethylene glycol succinate (TPGS) (DTBM) and active targeting mixed micelles (HDTBM) with hyaluronic acid (HA) as the targeting ligand on the surface of the mixed micelles. We performed a systematic comparative evaluation of the antiproliferative effect, cellular uptake, antitumor efficacy, and in vivo tumor targeting of these micelles using A549 cells. HDTBM showed improved cellular uptake and had a greater hypersensitizing effect on A549 cell lines than baohuoside I; half-maximal inhibitory concentration (IC 50 ) was 8.86 versus 20.42 mg/mL, respectively. Results of the antitumor efficacy study and the imaging study for in vivo targeting showed that the mixed-micelle formulation had higher antitumor efficacy and achieved effective and targeted drug delivery. Therefore, our results indicate that HA/baohuoside I-M may be used as a potential antitumor formulation.

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“…Baicalin (BA) is considered as the bioactive constituent in Radix Scutellariae and exhibits multiple biological activities, such as anti-cancer, anti-oxidant 3 , anti-inflammatory, hepato-protective 4 , anti-bacterial, immunosuppression and spasmolysis functions. In recent years, the strong effect on HIV of BA was found 5 .…”

Section: Introductionmentioning

confidence: 99%

Synthesis of surface nano-molecularly imprinted polymers for sensitive baicalin detection in biological samples

Wang

et al. 2015

RSC Adv.

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Surface molecularly imprinted polymers (MIP@SBA-15) imprinted on the surface of hybrid nanostructured organic/inorganic materials (SBA-15) were prepared for the selective extraction and detection of baicalin (BA) from biological samples. The surface morphologies and characteristics of the imprinted and non-imprinted polymers were characterized by Fourier transform infrared (FT-IR), scanning electron microscopy (SEM), transmission electron microscopy (TEM), thermo–gravimetric analysis (TGA) and nitrogen adsorption–desorption isotherms. The results indicated that the polymers were successfully grafted on the surface of SBA-15 and possessed a highly ordered mesoporous structure. In binding tests, MIP@SBA-15 reached saturated adsorption within 80 min and exhibited significant specific recognition toward BA with large adsorption capacity. Meanwhile, the prepared MIP@SBA-15 was used as a selective sorbent for solid-phase extraction of BA from biological samples. Recoveries of BA from the liver and spleen ranged from 90.6% to 90.9% with RSD < 3.7%. All these results reveal that this method is simple, rapid and sensitive for effectively extracting and detecting trace BA in biological samples.

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Preparation, optimization, characterization and cytotoxicity in vitro of Baicalin-loaded mixed micelles

Cited by 43 publications

References 49 publications

Preparation and evaluation of icariside II-loaded binary mixed micelles using Solutol HS15 and Pluronic F127 as carriers

Preparation and evaluation of icariside II-loaded binary mixed micelles using Solutol HS15 and Pluronic F127 as carriers

Hyaluronic acid-modified didecyldimethylammonium bromide/ d-a-tocopheryl polyethylene glycol succinate mixed micelles for delivery of baohuoside I against non-small cell lung cancer: in vitro and in vivo evaluation

Synthesis of surface nano-molecularly imprinted polymers for sensitive baicalin detection in biological samples

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