scholarly journals Production of Rosuvastatin Calcium Nanoparticles Using Gas Antisolvent Technique

Author(s):  
Mohammad Najafi ◽  
Nadia Esfandiari ◽  
Bizhan Honarvar ◽  
Zahra Arab Aboosadi

The activity of pharmaceutical substances crucially depends on the bioavailability of the substances. The bioavailability of drugs in body and their rate of dissolution in the biological fluids are increased if the particle size is decreased. In the present paper, the Gas Anti-Solvent (GAS) method was used to lower the size of rosuvastatin particles. The effects of temperature (313–338 K), pressure (105–180 bar) and initial solute concentration (20–60 mg/ml) were evaluated by Response Surface Methodology (RSM). The optimum initial solute concentration, temperature and pressure were found to be 20 mg/ml, 313 K and 180 bar, respectively which resulted in the minimum particle size. Furthermore, the particles were characterized by Differential Scanning Calorimetry (DSC), Dynamic Light Scattering (DLS), Fourier Transform Infrared (FTIR) spectroscopy, scanning electron microscopy (SEM), and X-Ray Diffraction (XRD). The analyses showed that the rosuvastatin particles (60.3 nm) precipitated by GAS process become significantly smaller than the initial particles (45.8 µm).

2021 ◽  
Vol 18 ◽  
Author(s):  
Sonia S. Pandey ◽  
Farhinbanu I. Shaikh ◽  
Arti R. Gupta ◽  
Rutvi J. Vaidya

Background: Despite significant biological effects, the clinical use of chrysin has been restricted because of its poor oral bioavailability. Objective: The purpose of the present research was to investigate the targeting potential of Mannose decorated chrysin (5,7- dihydroxyflavone) loaded solid lipid nanocarrier (MC-SLNs) for gastric cancer. Methods: The Chrysin loaded SLNs (C-SLNs) were developed optimized, characterized and further mannosylated. The C-SLNs were developed with high shear homogenizer, optimized with 32 full factorial designs and characterized by Fourier Transform Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), X-ray Diffraction (XRD) and Scanning Electron Microscope (SEM) and evaluated for particle size/polydispersity index, zeta-potential, entrapment efficiency, % release and haemolytic toxicity. The ex-vivo cytotoxicity study was performed on gastric cancer (ACG) and normal cell lines. Results: DSC and XRD data predict the chrysin encapsulation in lipid core and FTIR results confirm the mannosylation of C-SLNs. The optimized C-SLNs exhibited a narrow size distribution with a particle size of 285.65 nm. The % Entrapment Efficiency (%EE) and % controlled release were found to be 74.43% and 64.83%. Once C-SLNs were coated with mannose, profound change was observed in dependent variable - increase in the particle size of MC-SLNs (307.1 nm) was observed with 62.87% release and 70.8% entrapment efficiency. Further, the in vitro studies depicted MC- SLNs to be least hemolytic than pure chrysin and C-SLNs. MC-SLNs were most cytotoxic and were preferably taken up ACG tumor cells as evaluated against C-SLNs. Conclusion: These data suggested that the MC-SLNs demonstrated better biocompatibility and targeting efficiency to treat the gastric cancer.


Molecules ◽  
2022 ◽  
Vol 27 (2) ◽  
pp. 421
Author(s):  
Yao Yu ◽  
Yang Tian ◽  
Hui Zhang ◽  
Qingxian Jia ◽  
Xuejun Chen ◽  
...  

Meloxicam (MLX) is a non-steroidal anti-inflammatory drug used to treat rheumatoid arthritis and osteoarthritis. However, its poor water solubility limits the dissolution process and influences absorption. In order to solve this problem and improve its bioavailability, we prepared it in nanocrystals with three different particle sizes to improve solubility and compare the differences between various particle sizes. The nanocrystal particle sizes were studied through dynamic light scattering (DLS) and laser scattering (LS). Transmission electron microscopy (TEM) was used to characterize the morphology of nanocrystals. The sizes of meloxicam-nanocrystals-A (MLX-NCs-A), meloxicam-nanocrystals-B (MLX-NCs-B), and meloxicam-nanocrystals-C (MLX-NCs-C) were 3.262 ± 0.016 μm, 460.2 ± 9.5 nm, and 204.9 ± 2.8 nm, respectively. Molecular simulation was used to explore the distribution and interaction energy of MLX molecules and stabilizer molecules in water. The results of differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD) proved that the crystalline state did not change in the preparation process. Transport studies of the Caco-2 cell model indicated that the cumulative degree of transport would increase as the particle size decreased. Additionally, plasma concentration–time curves showed that the AUC0–∞ of MLX-NCs-C were 3.58- and 2.92-fold greater than those of MLX-NCs-A and MLX-NCs-B, respectively. These results indicate that preparing MLX in nanocrystals can effectively improve the bioavailability, and the particle size of nanocrystals is an important factor in transmission and absorption.


2015 ◽  
Vol 1112 ◽  
pp. 489-492
Author(s):  
Ali Mufid ◽  
M. Zainuri

This research aims to form particles of hematite (α-Fe2O3) with a basis of mineral iron ore Fe3O4 from Tanah Laut. Magnetite Fe3O4 was synthesized using co-precipitation method. Further characterization using X-ray fluorescence (XRF) to obtain the percentage of the elements, obtained an iron content of 98.51%. Then characterized using thermo-gravimetric analysis and differential scanning calorimetry (TGA-DSC) to determine the calcination temperature, that at a temperature of 445 °C mass decreased by 0.369% due to increase in temperature. Further Characterization of X-ray diffraction (XRD) to determine the phases formed at the calcination temperature variation of 400 °C, 445 °C, 500 °C and 600 °C with a holding time of 5 hours to form a single phase α-Fe2O3 hematite. Testing with a particle size analyzer (PSA) to determine the particle size distribution, where test results indicate that the α-Fe2O3 phase of each having a particle size of 269.7 nm, 332.2 nm, 357.9 nm, 412.2 nm. The best quantity is shown at a temperature of 500 °C to form the hematite phase. This result is used as the calcination procedure to obtain a source of Fe ions in the manufacture of Lithium Ferro Phosphate.


Coatings ◽  
2018 ◽  
Vol 8 (9) ◽  
pp. 305 ◽  
Author(s):  
Yan Zhang ◽  
Hui Zhang ◽  
Fang Wang ◽  
Li-Xia Wang

The ginger essential oil/β-cyclodextrin (GEO/β-CD) composite, ginger essential oil/β-cyclodextrin/chitosan (GEO/β-CD/CTS) particles and ginger essential oil/β-cyclodextrin/chitosan (GEO/β-CD/CTS) microsphere were prepared with the methods of inclusion, ionic gelation and spray drying. Their properties were studied by using scanning electron microscopy (SEM), differential scanning calorimetry (DSC), thermo-gravimetry analysis (TGA), Fourier transform infrared spectroscopy (FT-IR) and X-ray diffraction (XRD). The results showed that the particle size of GEO/β-CD composite was smaller than that of β-CD and GEO/β-CD/CTS particles were loose and porous, while the microsphere obtained by spray drying had certain cohesiveness and small particle size. Besides, results also indicated that β-CD/CTS could modify properties and improve the thermal stability of GEO, which would improve its application value in food and medical industries.


2006 ◽  
Vol 118 ◽  
pp. 651-654
Author(s):  
Young Soon Kwon ◽  
Pyuck Pa Choi ◽  
Ji Soon Kim ◽  
Dae Hwan Kwon ◽  
K.B. Gerasimov

The particle size effect on the peritectic melting of FeSn2 particles in FeSn-FeSn2 nanocomposites was studied using differential scanning calorimetry and X-ray diffraction. FeSn-10 wt.% FeSn2 compounds, mechanically milled for 30 min and slowly heated in a differential scanning calorimeter, showed incongruent melting at 680 K. Although FeSn2 grains grew from 10 to 40 nm upon heating before peritectic melting set in, the melting temperature was more than 100 K lower than the equilibrium value. A small latent heat during peritectic melting and a large amount of interfacial energy of FeSn-FeSn2 nanocomposites are held responsible for this large particle size effect. Grain growth is hardly possible in the case of rapid local heating during mechanical milling. Therefore, a decrease in the peritectic melting temperature is even expected to be substantially larger.


Author(s):  
Sejal Patel ◽  
Anita P Patel

In the interest of administration of dosage form oral route is most desirable and preferred method. Poor solubility and slow dissolution rate major challenges in upcoming and existing therapeutically active compound. Water insoluble drug indicate insufficient bioavailability as well dissolution resulting in fluctuating plasma level. Benidipine (BND) is Biopharmaceutical Classification System Class-II drug having low solubility and high permeability, antihypertensive drug has lower bioavailability. The purpose of the present study was to improve solubility as well dissolution profile of Benidipine HCL. BND nanosuspension was formulated using precipitation technique. Various polymers were evaluated  viz. HPMC E15, Tween 20, PVP K30 in preliminary trial to stabilized nanosuspension but PVP K30 was selected among them. The solubility of BND was carried out using different solvents like Ethanol, Acetonitrile; Acetone. Ethanol was used as a preferred solvent as BND shows high solubility in it.  The effect of different important process parameters e.g. selection of polymer concentration X1(10 mg), solvent concentration X2 (0.2 ml) were investigated by Central Composite factorial design to accomplish desired particle size and rate of dissolution. Stirring speed and time of stirring was kept constant as 1000 rpm and 2h respectively. To achieve optimized batch, 9 formulations (F1-F9) were prepared.  The optimized batch had 237 nm particle size Y1, and showed in-vitro dissolution Y2 98±0.72 % in 30 mins related to pure BND (58±0.25%) and zeta potential was -15.3. None of interaction between drug and polymer was confirmed by Differential scanning calorimetry (DSC) and FT-IR analysis. The obtained results showed that issues related particle size (nm) and rate of dissolution of BND has been solved when nanosuspension can be prepared by precipitation method by considering optimized parameter due to formation of nanosized particles


2021 ◽  
Vol 876 ◽  
pp. 7-12
Author(s):  
Petr Urban ◽  
Fátima Ternero Fernández ◽  
Rosa M. Aranda Louvier ◽  
Raquel Astacio López ◽  
Jesus Cintas Físico

The effect of milling time on the microstructure evolution and formation of amorphous phase of Ti60Si40 alloy produced by mechanical alloying (MA) has been investigated. Laser diffraction, Scanning Electron Microscopy (SEM), X-ray Diffraction (XRD), Transmission Electron Microscopy (TEM) and Differential Scanning Calorimetry (DSC) were employed to characterize the particle size, morphology and structure of mechanically alloyed Ti60Si40. When the milling time is increased to 20 h, the particle size decreases from 23.7 to 4.7 μm, the shape of the particles changes to spherical and the crystalline structure is transformed into an amorphous phase. The amorphous Ti60Si40 alloy is stable when heating up to 750oC. Above this temperature, the cold crystallization of the intermetallic compounds Ti5Si3 and/or Ti5Si4 begins.


2009 ◽  
Vol 67 ◽  
pp. 45-51
Author(s):  
Rohit Kumar Gupta ◽  
Vijaya Agarwala ◽  
Sunayan Thakur ◽  
Ramesh Chandra Agarwala ◽  
Bhanu Pant

High energy ball milling (HEBM) had been carried out to produce submicron size titanium aluminide intermetallics (TiAl) using elemental powders of Ti and Al alongwith Ni-P coated graphite. 1% graphite powders was added to stoichiometric composition of Ti48Al and ball milling was conducted for different milling time at varying rpm. The effect of milling time and rpm on particle size has been studied. The prepared samples have been characterized using X-ray diffraction, differential scanning calorimetry (DSC) and scaning elecron microscopy (SEM). Grain size as low as 500 nm could be achieved. Formation of Ti3Al, TiAl and carbon containing intermetallic compounds had been confirmed through X-ray diffraction. Milling time and rpm of mill is found to be important factors which control the final particle size.


2015 ◽  
Vol 51 (2) ◽  
pp. 449-459 ◽  
Author(s):  
Mayre Aparecida Borges da Costa ◽  
Ana Lucia Vazquez Villa ◽  
Rita de Cássia da Silva Ascenção Barros ◽  
Eduardo Ricci-Júnior ◽  
Elisabete Pereira dos Santos

<p>This paper reports the development, characterization and <italic>in vitro</italic>dissolution behavior of sulfasalazine suspensions for treatment of chronic intestinal inflammatory diseases. Three formulations were developed, from powdered sulfasalazine obtained from different suppliers. The sulfasalazine was characterized regarding concentration, Fourier Transform Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), X-Ray Diffraction (XRD), particle size distribution, polydispersion and solubility. The suspensions were developed and characterized regarding pH, viscosity, density, particle size, sedimentation volume, concentration and dissolution. The pH values were slightly acidic. The method of preparing the suspensions reduced the particle sizes and made the size distribution more homogeneous. The dissolution studies showed that the sulfasalazine suspensions had low solubility in acidic media, but dissolve quickly, reaching levels of 85%, in neutral media or media containing 0.5% of surfactants such as polysorbate 80. Besides this, the sulfasalazine suspensions were classified as having immediate dissolution because they reached dissolution levels near 100% in 20 minutes.</p>


2010 ◽  
Vol 148-149 ◽  
pp. 1575-1579
Author(s):  
Qing Zhang ◽  
Rui Yuan Niu ◽  
Min Wang ◽  
Bin Cui ◽  
Zhu Guo Chang

Li-Ti-O (abbreviated as LTO) nano-composites were synthesized via sol-gel process, and then doped BaTiO3 based X7R type ceramics. The LTO nano-composites and their ceramics were characterized by means of thermaogravimetric, Fourier-transform infrared, X-ray diffraction methods, transmission electron microscopy. We also characterized the dielectric properties of the LTO doped BaTiO3 based ceramics of X7R type. The results indicated that LTO nano-composites were nanometer scale powders. The pH value and calcining temperature had an influence on particle size of LTO sintering aids. At pH about 3 and with calcining at 600 °C, the nano-composites attained minimum particle size (about 10 nm). By adding 0.10 wt% of the LTO nano-composites, the temperature permittivity achieved about 4200 when sintered at 1240 °C for 4 h, and the dielectric properties met X7R standard.


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