Linolenic acid-modified PEG-PCL micelles for curcumin delivery

Song, Zhen; Zhu, Wenqi; Liu, Na; Yang, Fan; Feng, Runliang

doi:10.1016/j.ijpharm.2014.05.059

Cited by 86 publications

(65 citation statements)

References 50 publications

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“…The characteristic high-intensity diffraction peaks of the original curcumin indicated it was in a highly crystalline form before the SEDS process. 32 However, the intensity of these characteristic diffraction peaks weakened after the SEDS process. Curcumin nanoparticles showed a lower value for the peak areas (indicative of crystallinity) than that of original curcumin (556.5 vs 828.3).…”

Section: Xrpd Analysismentioning

confidence: 99%

Formation of curcumin nanoparticles via solution-enhanced dispersion by supercritical CO2

Zhao¹,

Xie²,

Li³

et al. 2015

IJN

135

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In order to enhance the bioavailability of poorly water-soluble curcumin, solution-enhanced dispersion by supercritical carbon dioxide (CO 2 ) (SEDS) was employed to prepare curcumin nanoparticles for the first time. A 2 4 full factorial experiment was designed to determine optimal processing parameters and their influence on the size of the curcumin nanoparticles. Particle size was demonstrated to increase with increased temperature or flow rate of the solution, or with decreased precipitation pressure, under processing conditions with different parameters considered. The single effect of the concentration of the solution on particle size was not significant. Curcumin nanoparticles with a spherical shape and the smallest mean particle size of 325 nm were obtained when the following optimal processing conditions were adopted: P =20 MPa, T =35°C, flow rate of solution =0.5 mL·min −1 , concentration of solution =0.5%. Fourier transform infrared (FTIR) spectroscopy measurement revealed that the chemical composition of curcumin basically remained unchanged. Nevertheless, X-ray powder diffraction (XRPD) and thermal analysis indicated that the crystalline state of the original curcumin decreased after the SEDS process. The solubility and dissolution rate of the curcumin nanoparticles were found to be higher than that of the original curcumin powder (approximately 1.4 μg/mL vs 0.2 μg/mL in 180 minutes). This study revealed that supercritical CO 2 technologies had a great potential in fabricating nanoparticles and improving the bioavailability of poorly water-soluble drugs.

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Section: Xrpd Analysismentioning

confidence: 99%

Formation of curcumin nanoparticles via solution-enhanced dispersion by supercritical CO2

Zhao¹,

Xie²,

Li³

et al. 2015

IJN

135

View full text Add to dashboard Cite

show abstract

“…As well as oral formulations of CUR, many injection formulations of CUR for chemotherapy have been developed (Song et al, 2014;Yang et al, 2015;Yoon et al, 2015).…”

mentioning

confidence: 99%

Cholesterol-modified poly(lactide-co-glycolide) nanoparticles for tumor-targeted drug delivery

Lee

Park

et al. 2016

International Journal of Pharmaceutics

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“…This might be relative to the appropriate proportion of hydrophobic PEG and hydrophilic PCL. 33 The hydrophobic interaction would be in favor of increasing solubility of CK, but when the length of the hydrophobic PCL exceeds a limit, it would lead to decreasing the solubility of CK. Thus, CK-M was successfully prepared, and the small size of the micelles could enhance CK concentration in tumor tissue.…”

Section: Mixed Micelle Formulation and Characterizationmentioning

confidence: 99%

“…However, the viability (%) of both cell types with CK-M was lower than that with CK; this may be because of the slower release from CK-M which resulted in a lower number of cells. 33 Free CK could possibly pass through the cells quickly by a passive-diffusion mechanism, while CK-M is transported into cells through endocytosis and shows a delayed release in cells. In vitro release results also support the above results.…”

mentioning

confidence: 99%

Targeted delivery of ginsenoside compound K using TPGS/PEG-PCL mixed micelles for effective treatment of lung cancer

Yang

Zhang

Hou

et al. 2017

IJN

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Ginsenoside compound K (CK) is one of the effective ingredients in antitumor composition of ginsenoside. However, the poor water solubility and significant efflux have limited the widespread clinical use of CK. In this study, preparation of novel CK-loaded d -alpha-tocopheryl polyethylene glycol 1,000 succinate/poly(ethylene glycol)-poly(ε-caprolactone) mixed micelles (CK-M) is discussed to solve the above problems. Particle size, zeta potential, and morphology were characterized using dynamic light scattering and transmission electron microscopy. CK-M are spherical shaped with an average particle size of 53.07±1.31 nm with high drug loading of 11.19%±0.87% and entrapment efficiency of 94.60%±1.45%. Water solubility of CK was improved to 3.78±0.09 mg/mL, which was ~107.35 times higher than free CK. A549 and PC-9 cells were used to evaluate in vitro cytotoxicity and cellular uptake. IC 50 values of CK-M in A549 and PC-9 cells (24 h) were 25.43±2.18 and 18.35±1.90 μg/mL, respectively. Enhanced cellular uptake of CK-M was observed in both cells. Moreover, CK-M promoted tumor cell apoptosis, inhibited tumor cell invasion, metastasis, and efflux through regulation of Bax, Bcl-2, matrix metalloproteinase-2, Caspase-3, and P-glycoprotein. In vivo imaging indicated that CK-M has excellent tumor targeting effect within 24 h, and the relative tumor inhibition rate of CK-M was 52.04%±4.62% compared with control group ( P <0.01). Thus, CK-M could be an appropriate delivery agent for enhanced solubility and antitumor effect of CK.

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Linolenic acid-modified PEG-PCL micelles for curcumin delivery

Cited by 86 publications

References 50 publications

Formation of curcumin nanoparticles via solution-enhanced dispersion by supercritical CO2

Formation of curcumin nanoparticles via solution-enhanced dispersion by supercritical CO2

Cholesterol-modified poly(lactide-co-glycolide) nanoparticles for tumor-targeted drug delivery

Targeted delivery of ginsenoside compound K using TPGS/PEG-PCL mixed micelles for effective treatment of lung cancer

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