Enhanced oral bioavailability of docetaxel by lecithin nanoparticles: preparation, in vitro, and in vivo evaluation

Hu, Kaili; Cao, Shan; Hu, Fuqiang; Jiao, Feng

doi:10.2147/ijn.s32880

Cited by 86 publications

(38 citation statements)

References 31 publications

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“…Briefly, phosphate-buffer saline pH 7.4 (PBS), 50 ml containing 0.5% (w/v) sodium lauryl sulfate (SLS) (Hu et al, 2012) was taken as drug release media in a borosilicate glass beaker of 100 ml capacity. Accurately weighed (5 mg) formulation (lyophilized) and an equivalent amount of free-drug suspension; and Taxotere Õ ; were reconstituted with 1 mL drug release media and poured into a dialysis bag (molecular weight cut-off 12-14 kDa).…”

Section: Percentage Of Drug Loading and Loading Efficiency Percentagementioning

confidence: 99%

Successful delivery of docetaxel to rat brain using experimentally developed nanoliposome: a treatment strategy for brain tumor

et al. 2017

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Docetaxel (DTX) is found to be very effective against glioma cell in vitro. However, in vivo passage of DTX through BBB is extremely difficult due to the physicochemical and pharmacological characteristics of the drug. No existing formulation is successful in this aspect. Hence, in this study, effort was made to send DTX through blood-brain barrier (BBB) to brain to treat diseases such as solid tumor of brain (glioma) by developing DTX-loaded nanoliposomes. Primarily drug-excipients interaction was evaluated by FTIR spectroscopy. The DTX-loaded nanoliposomes (L-DTX) were prepared by lipid layer hydration technique and characterized physicochemically. In vitro cellular uptake in C6 glioma cells was investigated. FTIR data show that the selected drug and excipients were chemically compatible. The unilamellar vesicle size was less than 50 nm with smooth surface. Drug released slowly from L-DTX in vitro in a sustained manner. The pharmacokinetic data shows more extended action of DTX from L-DTX in experimental rats than the free-drug and Taxotere Õ . DTX from L-DTX enhanced 100% drug concentration in brain as compared with Taxotere Õ in 4 h. Thus, nanoliposomes as vehicle may be an encouraging strategy to treat glioma with DTX.

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Section: Percentage Of Drug Loading and Loading Efficiency Percentagementioning

confidence: 99%

Successful delivery of docetaxel to rat brain using experimentally developed nanoliposome: a treatment strategy for brain tumor

et al. 2017

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“…41 In addition, the increased oral bioavailability of BA in the form of BA-LP might be attributed to the combination of several effects. [42][43][44] First, the particle size of BA-LP played a key role in the nanoparticle absorption rate -in general, the decreased particle size may improve the …”

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confidence: 99%

Preparation, pharmacokinetics and biodistribution of baicalin-loaded liposomes

Wei

Guo

Zheng

et al. 2014

IJN

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Baicalin (BA) is a major constituent of Scutellaria baicalensis Georgi , a medicinal herb. Previous pharmacokinetic studies of BA showed its low oral bioavailability. The aim of the present study was to develop a novel BA-loaded liposome (BA-LP) to enhance oral bioavailability. BA-LP, composed of BA, Tween ® 80, Phospholipon ® 90H, and citric acid at weight ratio of 96/50/96/50, respectively, was prepared by the effervescent dispersion technique and characterized in terms of morphology, size, zeta potential, encapsulation efficiency, and the in vitro release. Pharmacokinetics and biodistribution studies were carried out in rats after oral administration of BA-LP and a carboxymethyl cellulose suspension containing BA (BA-CMC) as a control. BA-LP exhibited a spherical shape by transmission electron microscopy observation. BA-LP had a mean particle size of 373±15.5 nm, zeta potential of −20.1±0.22 mV, and encapsulation efficiency of 82.7%±0.59%. The BA-LP showed a sustained-release behavior, and the in vitro drug-release kinetic model fit well with the Weibull distribution equation: lnln (1/(1−Q)) =0.609 lnt −1.230 ( r =0.995). The oral bioavailability and the peak concentration of the BA-LP was threefold and 2.82-fold that of BA-CMC, respectively. The in vivo distribution results indicated that drug concentrations were significantly increased in the liver, kidney, and lung in the case of BA-LP, which were 5.59-fold, 2.33-fold, and 1.25-fold higher than those of BA-CMC, respectively. In conclusion, the study suggested that BA-LP might be a potential oral drug delivery system to improve bioavailability of BA.

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“…This result shows that the TSIIA in the SDs exhibited a faster absorption rate and higher bioavailability, which may be attributed to several characteristics, including that SDs with silica nanoparticles as carriers can strongly potentiate their dissolution and increase the contact area with the gastrointestinal tract, resulting in an accelerated absorption rate and improved bioavailability. 57,58 Time (hours) Figure 6 The mean plasma concentration-time curve of TSIIA in rats after oral administration of SDs, PMs, and TSIIA equivalent to 60 mg kg −1 of TSIIA (n = 6). Notes: The values are represented as the mean ± standard deviation (n = 6/group/ time point).…”

Section: Stability Testmentioning

confidence: 99%

Preparation, characterization, and in vivo evaluation of tanshinone IIA solid dispersions with silica nanoparticles

Jiang¹,

Zhang²,

Liu³

et al. 2013

IJN

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Abstract:We prepared solid dispersions (SDs) of tanshinone IIA (TSIIA) with silica nanoparticles, which function as dispersing carriers, using a spray-drying method and evaluated their in vitro dissolution and in vivo performance. The extent of TSIIA dissolution in the silica nanoparticles/TSIIA system (weight ratio, 5:1) was approximately 92% higher than that of the pure drug after 60 minutes. However, increasing the content of silica nanoparticles from 5:1 to 7:1 in this system did not significantly increase the rate or extent of TSIIA dissolution. The physicochemical properties of SDs were investigated using scanning electron microscopy, differential scanning calorimetry, X-ray powder diffraction, and Fourier transforms infrared spectroscopy. Studying the stability of the SDs of TSIIA revealed that the drug content of the formulation and dissolution behavior was unchanged under the applied storage conditions. In vivo tests showed that SDs of the silica nanoparticles/TSIIA had a significantly larger area under the concentration-time curve, which was 1.27 times more than that of TSIIA (P , 0.01). Additionally, the values of maximum plasma concentration and the time to reach maximum plasma concentration of the SDs were higher than those of TSIIA and the physical mixing system. Based on these results, we conclude that the silica nanoparticle based SDs achieved complete dissolution, increased absorption rate, maintained drug stability, and showed improved oral bioavailability compared to TSIIA alone.

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Enhanced oral bioavailability of docetaxel by lecithin nanoparticles: preparation, in vitro, and in vivo evaluation

Cited by 86 publications

References 31 publications

Successful delivery of docetaxel to rat brain using experimentally developed nanoliposome: a treatment strategy for brain tumor

Successful delivery of docetaxel to rat brain using experimentally developed nanoliposome: a treatment strategy for brain tumor

Preparation, pharmacokinetics and biodistribution of baicalin-loaded liposomes

Preparation, characterization, and in vivo evaluation of tanshinone IIA solid dispersions with silica nanoparticles

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