Nanosuspension formulations of poorly water-soluble compounds for intravenous administration in exploratory toxicity studies:in vitroandin vivoevaluation

2016 ◽  
Vol 36 (10) ◽  
pp. 1259-1267
Author(s):  
Hisako Fujimura ◽  
Takao Komasaka ◽  
Taizo Tomari ◽  
Yasunori Kitano ◽  
Kouji Takekawa
Keyword(s):  
Intravenous Administration ◽  
Water Soluble ◽  
Poorly Water Soluble

Stable Colloids of Paclitaxel Nanoparticles Coated with PEGylated Polyelectrolyte Shells

2012 ◽  
Vol 1416 ◽  
Author(s):  
Tatsiana G. Shutava ◽  
Kirill A. Arapov ◽  
Pravin P. Pattekari ◽  
Yuri M. Lvov ◽  
Tatyana S. Levchenko ◽  
...  
Keyword(s):  
Anticancer Drug ◽  
Intravenous Administration ◽  
Water Soluble ◽  
Layer By Layer ◽  
Lbl Assembly ◽  
Nano Crystalline ◽  
Solid Crystal ◽  
Poorly Water Soluble ◽  
Thick Shells

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.

NANO-SIZED SOLID DISPERSION OF A POORLY WATER-SOLUBLE DRUG

2012 ◽  
pp. 31-35
Author(s):  
Truong Dinh Thao Tran ◽  
Ha Lien Phuong Tran ◽  
Nghia Khanh Tran ◽  
Van Toi Vo
Keyword(s):  
Drug Release ◽  
Droplet Size ◽  
Solid Dispersion ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Dissolution Enhancement ◽  
Particle Size Reduction ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

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.

Enhancement of Solubility and Dissolution Rate of Poorly Water Soluble Drug using Cosolvency and Solid Dispersion Techniques

1970 ◽  
Vol 1 (4) ◽  
pp. 349-356
Author(s):  
Meka Lingam ◽  
Vobalaboina Venkateswarlu
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersions ◽  
Physicochemical Characterization ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Scanning Calorimetry ◽  
Peg 400 ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

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

scholarly journals Nanoformulation and Evaluation of Oral Berberine-Loaded Liposomes

Molecules ◽  
2021 ◽  
Vol 26 (9) ◽  
pp. 2591
Author(s):  
Thuan Thi Duong ◽  
Antti Isomäki ◽  
Urve Paaver ◽  
Ivo Laidmäe ◽  
Arvo Tõnisoo ◽  
...  
Keyword(s):  
Thin Film ◽  
Drug Release ◽  
Size Distribution ◽  
Water Soluble ◽  
Release Behavior ◽  
Uniform Size ◽  
Ethanol Injection ◽  
Drug Release Behavior ◽  
Poorly Water Soluble

Berberine (BBR) is a poorly water-soluble quaternary isoquinoline alkaloid of plant origin with potential uses in the drug therapy of hypercholesterolemia. To tackle the limitations associated with the oral therapeutic use of BBR (such as a first-pass metabolism and poor absorption), BBR-loaded liposomes were fabricated by ethanol-injection and thin-film hydration methods. The size and size distribution, polydispersity index (PDI), solid-state properties, entrapment efficiency (EE) and in vitro drug release of liposomes were investigated. The BBR-loaded liposomes prepared by ethanol-injection and thin-film hydration methods presented an average liposome size ranging from 50 nm to 244 nm and from 111 nm to 449 nm, respectively. The PDI values for the liposomes were less than 0.3, suggesting a narrow size distribution. The EE of liposomes ranged from 56% to 92%. Poorly water-soluble BBR was found to accumulate in the bi-layered phospholipid membrane of the liposomes prepared by the thin-film hydration method. The BBR-loaded liposomes generated by both nanofabrication methods presented extended drug release behavior in vitro. In conclusion, both ethanol-injection and thin-film hydration nanofabrication methods are feasible for generating BBR-loaded oral liposomes with a uniform size, high EE and modified drug release behavior in vitro.

scholarly journals Solubility enhancement of carvedilol using drug–drug cocrystallization with hydrochlorothiazide

2020 ◽  
Vol 6 (1) ◽  
Author(s):  
Shivarani Eesam ◽  
Jaswanth S. Bhandaru ◽  
Chandana Naliganti ◽  
Ravi Kumar Bobbala ◽  
Raghuram Rao Akkinepally
Keyword(s):  
Aqueous Solubility ◽  
Sem Analysis ◽  
Water Soluble ◽  
High Permeability ◽  
Poorly Water Soluble Drugs ◽  
Drug Discovery And Development ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Dissolution In Vitro

Abstract Background Increasing hydrophilicity of poorly water-soluble drugs is a major challenge in drug discovery and development. Cocrystallization is one of the techniques to enhance the hydrophilicity of such drugs. Carvedilol (CAR), a nonselective beta/alpha1 blocker, used in the treatment of mild to moderate congestive heart failure and hypertension, is classified under BCS class II with poor aqueous solubility and high permeability. Present work is an attempt to improve the solubility of CAR by preparing cocrystals using hydrochlorothiazide (HCT), a diuretic drug, as coformer. CAR-HCT (2:0.5) cocrystals were prepared by slurry conversion method and were characterized by DSC, PXRD, FTIR, Raman, and SEM analysis. The solubility, stability, and dissolution (in vitro) studies were conducted for the cocrystals. Results The formation of CAR-HCT cocrystals was confirmed based on melting point, DSC thermograms, PXRD data, FTIR and Raman spectra, and finally by SEM micrographs. The solubility of the prepared cocrystals was significantly enhanced (7.3 times), and the dissolution (in vitro) was improved by 2.7 times as compared to pure drug CAR. Further, these cocrystals were also found to be stable for 3 months (90 days). Conclusion It may be inferred that the drug–drug (CAR-HCT) cocrystallization enhances the solubility and dissolution rate of carvedilol significantly. Further, by combining HCT as coformer could well be beneficial pharmacologically too.

Formulation and Food Effects on the Oral Absorption of a Poorly Water Soluble, Highly Permeable Antiretroviral Agent

2002 ◽  
Vol 91 (6) ◽  
pp. 1390-1395 ◽  
Author(s):  
Bruce J. Aungst ◽  
Nhung H. Nguyen ◽  
Nancy J. Taylor ◽  
Dilbir S. Bindra
Keyword(s):  
Oral Absorption ◽  
Water Soluble ◽  
Food Effects ◽  
Poorly Water Soluble
Sign in / Sign up

Export Citation Format

Share Document