Non-ionic dendritic glycerol-based amphiphiles: Novel excipients for the solubilization of poorly water-soluble anticancer drug Sagopilone

2010 ◽  
Vol 40 (1) ◽  
pp. 48-55 ◽  
Author(s):  
Annett Richter ◽  
Achim Wiedekind ◽  
Michael Krause ◽  
Thomas Kissel ◽  
Rainer Haag ◽  
...  
2014 ◽  
Vol 32 (4) ◽  
pp. 1451-1461 ◽  
Author(s):  
Wenli Zhang ◽  
Guangji Wang ◽  
James R. Falconer ◽  
Bruce C. Baguley ◽  
John P. Shaw ◽  
...  

2017 ◽  
Vol 53 (70) ◽  
pp. 9749-9752 ◽  
Author(s):  
Liqing Shangguan ◽  
Qi Chen ◽  
Bingbing Shi ◽  
Feihe Huang

A water-soluble pillar[6]arene functions as a solubilizing agent to enhance the solubility and bioactivity of poorly water-soluble anticancer drug tamoxifen.


2020 ◽  
Vol 138 (7) ◽  
pp. 49858
Author(s):  
Ngoc Thuy Trang Le ◽  
Dinh Tien Dung Nguyen ◽  
Ngoc Hoi Nguyen ◽  
Cuu Khoa Nguyen ◽  
Dai Hai Nguyen

2012 ◽  
Vol 1416 ◽  
Author(s):  
Tatsiana G. Shutava ◽  
Kirill A. Arapov ◽  
Pravin P. Pattekari ◽  
Yuri M. Lvov ◽  
Tatyana S. Levchenko ◽  
...  

ABSTRACTA novel nanoparticulated form of the poorly water-soluble anticancer drug paclitaxel (PTX) suitable for intravenous administration has been developed using sonication-assisted layer-by-layer (LbL) assembly. The nanoparticles contain up to 70 wt.% of the drug and consist of 150-180 nm solid crystal paclitaxel cores coated with 20-30 nm thick shells of alternative layers of PEGylated poly-L-lysine and heparin. Dispersions of PTX nanoparticles are stable in different biological solvents at concentrations up to 5 mg/ml. Intravenous administration of the LbL-coated nano-crystalline PTX to mice via tail injection provided the preliminary confirmation of their safety and tolerability.


2011 ◽  
Vol 47 (18) ◽  
pp. 5235 ◽  
Author(s):  
Nanda Gopal Sahoo ◽  
Hongqian Bao ◽  
Yongzheng Pan ◽  
Mintu Pal ◽  
Mitali Kakran ◽  
...  

2012 ◽  
pp. 31-35
Author(s):  
Truong Dinh Thao Tran ◽  
Ha Lien Phuong Tran ◽  
Nghia Khanh Tran ◽  
Van Toi Vo

Purposes: Aims of this study are dissolution enhancement of a poorly water-soluble drug by nano-sized solid dispersion and investigation of machenism of drug release from the solid dispersion. A drug for osteoporosis treatment was used as the model drug in the study. Methods: melting method was used to prepare the solid dispersion. Drug dissolution rate was investigated at pH 1.2 and pH 6.8. Drug crystallinity was studied using differential scanning calorimetric and powder X-ray diffraction. In addition, droplet size and contact angle of drug were determined to elucidate mechanism of drug release. Results: Drug dissolution from the solid dispersion was significantly increased at pH 1.2 and pH 6.8 as compared to pure drug. Drug crystallinity was changed to partially amorphous. Also dissolution enhancement of drug was due to the improved wettability. The droplet size of drug was in the scale of nano-size when solid dispersion was dispersed in dissolution media. Conclusions: nano-sized solid dispersion in this research was a successful preparation to enhance bioavailability of a poorly water-soluble drug by mechanisms of crystal changes, particle size reduction and increase of wet property.


Author(s):  
Meka Lingam ◽  
Vobalaboina Venkateswarlu

The low aqueous solubility of celecoxib (CB) and thus its low bioavailability is a problem.    Thus, it is suggested to improve the solubility using cosolvency and solid dispersions techniques. Pure CB has solubility of 6.26±0.23µg/ml in water but increased solubility of CB was observed with increasing concentration of cosolvents like PEG 400, ethanol and propylene glycol. Highest solubility (791.06±15.57mg/ml) was observed with cosolvency technique containing the mixture of composition 10:80:10%v/v of water: PEG 400: ethanol. SDs with different polymers like PVP, PEG were prepared and subjected to physicochemical characterization using Fourier-transform infrared (FTIR) spectroscopy, X-ray diffractometry (XRD), differential scanning calorimetry (DSC), solubility and dissolution studies. These studies reveals that CB exists mainly in amorphous form in prepared solid dispersions of PVP, PEG4000 and PEG6000 further it can also be confirmed by solubility and dissolution rate studies. Solid dispersions of PV5 and PV9 have shown highest saturation solubility and dissolution rate


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