Preparation, optimization of intravenous ZL-004 nanosuspensions by the precipitation method, effect of particle size on in vivo pharmacokinetics and tissue distribution

2019 ◽  
Vol 50 ◽  
pp. 313-320 ◽  
Author(s):  
Chengyue Guo ◽  
Yanna Chen ◽  
Junzhe Zhu ◽  
Jiaxin Wang ◽  
Ying Xu ◽  
...  
Processes ◽  
2021 ◽  
Vol 9 (4) ◽  
pp. 574
Author(s):  
Nikhat Perween ◽  
Sultan Alshehri ◽  
T. S. Easwari ◽  
Vivek Verma ◽  
Md. Faiyazuddin ◽  
...  

Molecules with poor aqueous solubility are difficult to formulate using conventional approaches and are associated with many formulation delivery issues. To overcome these obstacles, nanosuspension technology can be one of the promising approaches. Hence, in this study, the feasibility of mefenamic acid (MA) oral nanosuspension was investigated for pediatric delivery by studying the role of excipients and optimizing the techniques. Nanosuspensions of MA were prepared by adopting an antisolvent precipitation method, followed by ultrasonication with varying concentrations of polymers, surfactants, and microfluidics. The prepared nanosuspensions were evaluated for particle size, morphology, and rheological measures. Hydroxypropyl methylcellulose (HPMC) with varying concentrations and different stabilizers including Tween® 80 and sodium dodecyl sulfate (SLS) were used to restrain the particle size growth of the developed nanosuspension. The optimized nanosuspension formula was stable for more than 3 weeks and showed a reduced particle size of 510 nm with a polydispersity index of 0.329. It was observed that the type and ratio of polymer stabilizers were responsive on the particle contour and dimension and stability. We have developed a biologically compatible oral nanoformulation for a first-in-class drug beautifully designed for pediatric delivery that will be progressed toward further in vivo enabling studies. Finally, the nanosuspension could be considered a promising carrier for pediatric delivery of MA through the oral route with enhanced biological impact.


2020 ◽  
Vol 25 (8) ◽  
pp. 971-988
Author(s):  
Sonia Gera ◽  
Venkatesh Pooladanda ◽  
Chandraiah Godugu ◽  
Veerabhadra Swamy Challa ◽  
Jitendra Wankar ◽  
...  

1997 ◽  
Vol 1997 ◽  
pp. 197-197
Author(s):  
R. Sanderson ◽  
S.J. Lister ◽  
A. Sargeant ◽  
M.S. Dhanoa

The objectives of this study were a) to examine the effect of particle size and silage dry matter (DM) content on the rate and pattern of fermentation of fresh silages in vitro as an aid to modelling the in vivo situation and b) to compare the rate and pattern of fermentation of fresh silage samples with those obtained for freeze-dried material.


Pharmaceutics ◽  
2019 ◽  
Vol 11 (11) ◽  
pp. 589 ◽  
Author(s):  
Chang-baek Lim ◽  
Sharif Md Abuzar ◽  
Pankaj Ranjan Karn ◽  
Wonkyung Cho ◽  
Hee Jun Park ◽  
...  

Here, we aimed to prepare and optimize liposomal amphotericin B (AmB) while using the supercritical fluid of carbon dioxide (SCF-CO2) method and investigate the characteristics and pharmacokinetics of the SCF-CO2-processed liposomal AmB. Liposomes containing phospholipids, ascorbic acid (vit C), and cholesterol were prepared by the SCF-CO2 method at an optimized pressure and temperature; conventional liposomes were also prepared using the thin film hydration method and then compared with the SCF-CO2-processed-liposomes. The optimized formulation was evaluated by in vitro hemolysis tests on rat erythrocytes and in vivo pharmacokinetics after intravenous administration to Sprague-Dawley rats and compared with a marketed AmB micellar formulation, Fungizone®, and a liposomal formulation, AmBisome®. The results of the characterization studies demonstrated that the SCF-CO2-processed-liposomes were spherical particles with an average particle size of 137 nm (after homogenization) and drug encapsulation efficiency (EE) was about 90%. After freeze-drying, mean particle size, EE, and zeta potential were not significantly changed. The stability study of the liposomes showed that liposomal AmB that was prepared by the SCF method was stable over time. In vivo pharmacokinetics revealed that the SCF-CO2-processed-liposomes were bioequivalent to AmBisome®; the hemolytic test depicted less hematotoxicity than Fungizone®. Therefore, this method could serve as a potential alternative for preparing liposomal AmB for industrial applications.


Author(s):  
VISHAL S REDDY ◽  
GOWDA DV ◽  
VISHAL GUPTA N

Objective: The present research is to formulate Glimepiride and Atorvastatin Calcium Nanoparticles for the type-2 diabetes mellitus for improvement of glucose tolerance associated with dyslipidemia formulated by liquid antisolvent precipitation technique. Method: Glimepiride nanoparticles and atorvastatin calcium nanoparticles were prepared by using a liquid antisolvent precipitation technique. Solvent to antisolvent ratio used was 3.5:6.5 and 2.5:7.5 and the drug concentration used was 40 mg/ml and 60mg/ml respectively. Result: The XRD was determined, the data of the optimized Glimepiride formulation revealed that the prepared nanosized Glimepiride powder was existed in crystalline form. The percent yield for the formulations of Glimepiride and atorvastatin calcium nanoparticles was found to be 72.8±1.8%, 75.3±2.2% respectively. In-vivo studies in albino wistar rats demonstrated that the Cmax and AUC0−24h of optimized Glimepiride and atorvastatin calcium  nanosized formulation was found to be 24451.14±2170.5 ng/ml, 162945.12±241.5 ng/ml and 1385.43±153.3 ng/ml,3636.57±65.2 ng/ml respectively. Dissolution study of optimized formulations shows that marked enhancement of dissolution rate. The stability studies of mixture of Glimepiride and atorvastatin calcium powder when stored at 4±3oC refrigerated temperature has shown no significant changes in physical appearance, drug content, particle size and PDI. Conversely the sample stored at room temperature has shown significant increase in particle size and PDI, with no significant changes in drug content and physical appearance. Conclusion: The Formulation of glimepiride and atorvastatin calcium drug nanoparticles shows increase in the surface-to-volume ratio of API, resulting in better drug solubility and hence increasing the bio-availability when compared to its pure form.


2019 ◽  
Vol 52 ◽  
pp. 778-783 ◽  
Author(s):  
Xiao-han Wang ◽  
Yuan Liu ◽  
Cheng-ying Shen ◽  
Bao-de Shen ◽  
Rui-na Zhong ◽  
...  

2009 ◽  
Vol 24 (5) ◽  
pp. 1756-1760 ◽  
Author(s):  
Xixian Luo ◽  
Wanghe Cao ◽  
Mingming Xing

Monodisperse spherical Y2O2S:Yb,Ho nanocrystals with particle size about 50 nm were prepared by a modified homogeneous precipitation method combined with low-temperature sulfurization process. The Y2O2S:Yb,Ho nanocrystals exhibit an intense green emission assigned to the Ho3+ ions 5F4, 5S2 → 4I15/2 transition under 980 nm infrared pump. The upconversion luminescence brightness of Y2O2S:Yb,Ho is 526 Cd/m2 under 4.63 W/cm2 pump density, indicating that the as-prepared Y2O2S:Yb,Ho nanocrystals can meet the requirement of in vivo imaging. The formation mechanism of monodisperse spherical oxysulfide nanoparticles is also discussed.


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