Enhance the dissolution rate and oral bioavailability of pranlukast by preparing nanosuspensions with high-pressure homogenizing method

2012 ◽  
Vol 38 (11) ◽  
pp. 1381-1389 ◽  
Author(s):  
Lan Wang ◽  
Yanli Hao ◽  
Nan Liu ◽  
Mingshu Ma ◽  
Zhe Yin ◽  
...  
Keyword(s):  
High Pressure ◽  
Dissolution Rate ◽  
Oral Bioavailability

scholarly journals FORMULATION AND EVALUATION OF POLYMERIC NANOSUSPENSION OF NARINGENIN

2017 ◽  
Vol 9 (6) ◽  
pp. 60 ◽  
Author(s):  
R. Sumathi ◽  
S. Tamizharasi ◽  
T. Sivakumar
Keyword(s):  
Particle Size ◽  
High Pressure ◽  
Dissolution Rate ◽  
Oral Bioavailability ◽  
Safety Evaluation ◽  
Drug Formulation ◽  
High Pressure Homogenization ◽  
Erythrocyte Hemolysis ◽  
Poorly Soluble

Objective: The objective of this study was to formulate and evaluate the poorly soluble drug, naringenin (NAR) into nanosuspension to increase the solubility and enhance the dissolution rate and then improve its bioavailability.Methods: Nanosuspenion of naringenin (NARNS) was prepared using high-pressure homogenization method using Soya lecithin, Polaxamer-407, Polaxamer-188, Hydroxypropyl methyl cellulose (HPMC) and Tween-80. Ten formulations were prepared to show the effect of stabilizer and its ratio. D-α-Tocopheryl polyethene glycol succinate 1000 (TPGS) was added as a co-stabilizer. All these formulations were evaluated for their particle size, PDI, zeta potential, FT-IR study, drug content, saturation solubility studies, entrapment efficiency, in vitro permeability and in vitro drug release. The formulation was further evaluated for scanning electron microscope (SEM), differential scanning calorimetry (DSC) and Powder X-ray diffraction (P-XRD) and hemocompatibility assessment.Results: All the prepared formulations were in the nano size. The optimum concentration of the stabilizer was in the formulation was found 1:1.5:1 (drug: stabilizer: co-stabilizer ratio). Dramatic effect of the particle size reduction was found by the addition of the co-stabilizer (TPGS) in formulation N2 that has P. S 80.52±0.13 nm. The solubility and dissolution of NAR in the form of NARNS were significantly higher than those of pure NAR. SEM report shows that naringenin nanosuspension revealed a smooth texture. P-XRD crystallography diffraction and DSC studies indicated that the crystalline state of NAR was converted into amorphous nature. The safety evaluation showed that NARNS provided a lower rate of erythrocyte hemolysis. Conclusion: In this study, (NARNS) was successfully carried out by high-pressure homogenization technique and characterized. The physio-chemical characterization shown that crystalline naringenin was converted to a polymorphic form (DSC and P-XRD Study) which evidenced by enhanced dissolution rate in comparisons of the formulation with (NAR) pure drug. The NARNS has shown 7.5±0.4 fold increased relative bioavailability when compared to the NAR. The increased drug dissolution rate may have a significant impact in absorption which in turn the improved oral bioavailability of naringenin. Thus, this delivery system may prefer to improve the dissolution of poorly soluble drugs like NAR and thus enhanced oral bioavailability. The safety evaluation showed that nanoformulation (NF2) shows a lower rate of erythrocyte hemolysis. These findings suggest that the selected formulation may represent a promising new drug formulation for intravenous administration in the treatment of certain cancers.

scholarly journals Investigation of Nanosized Crystalline Form to Improve the Oral Bioavailability of Poorly Water Soluble Cilostazol

2011 ◽  
Vol 14 (2) ◽  
pp. 196 ◽  
Author(s):  
Xiaoqing Miao ◽  
Changshan Sun ◽  
Tongying Jiang ◽  
Li Zheng ◽  
Tianyi Wang ◽  
...  
Keyword(s):  
Particle Size ◽  
High Pressure ◽  
Dissolution Rate ◽  
Surface Area ◽  
Oral Bioavailability ◽  
Nitrogen Adsorption ◽  
High Pressure Homogenization ◽  
Crystalline Powder ◽  
X Ray ◽  
Spray Dried

Purpose: The aim of this study was to develop cilostazol (CLT) nanocrystals intended to improve its dissolution rate and enhance its bioavailability. Methods: In this study, CLT nanosuspension was prepared by the anti-solvent and high-pressure homogenization method. The effects of the production parameters, such as the stabilizer concentration, pressure and number of cycles, were investigated. Characterization of the product was performed by scanning electron microscopy (SEM), Nitrogen adsorption, differential scanning calorimetry (DSC), X-ray powder diffraction analysis (XRPD), X-ray Photoelectron Spectroscopy (XPS), particle size analysis and dissolution testing. Additionally, the comparison studies of oral bioavailability in beagle dogs of three type tables were performed. Results: The images of SEM showed a spherical smooth CLT powder, and Nitrogen adsorption test revealed spray dried powder were porous with high BET surface area compared with that of raw CLT. DSC and XRPD results demonstrated that the combination of preferred polymorph B and C of CLT were prepared successfully, the saturation solubility of the nanosized crystalline powder is about 5 fold greater than that of raw CLT, and the dissolution rate was enhanced 4 fold than that of raw CLT. The Cmax and AUC0–48h of CLT nanosized crystalline tablets were 2.1 fold and 1.9 fold, and 3.0 fold and 2.3 fold compared with those of the nanosized tablets and commercial tablets, respectively. Conclusion: The anti-solvent–high-pressure homogenization technique was employed successfully to produce cilostazol nanosuspensions. The bioavailability of CLT tablets prepared using spray dried nanosized crystalline powder after oral administration to dogs was markedly increased compared with that produced by nanosized tablets and commercial tablets, because of its greater dissolution rate owing to its transition of the crystalline state to form C and form B, reduced particle size and porous structure with increased surface area. This article is open to POST-PUBLICATION REVIEW. Registered readers (see “For Readers”) may comment by clicking on ABSTRACT on the issue’s contents page.

Pretreatment of Fir Powder and Its Dissolution in Ionic Liquid of 1-(2-Hydroxylethyl)-3-Ethylene Imidazolium Chloride

2011 ◽  
Vol 236-238 ◽  
pp. 87-90
Author(s):  
Li Ying Guo
Keyword(s):  
High Pressure ◽  
Ionic Liquid ◽  
Dissolution Rate ◽  
Mass Fraction ◽  
Wood Powder ◽  
Imidazolium Chloride ◽  
Chemical Structures ◽  
Good Solubility ◽  
Temperature And Pressure ◽  
Pressure Dissolution

Ionic liquid, 1-(2-hydroxylethyl)-3-ethylene imidazolium chloride ([HeVIM]Cl) was synthesized and its chemical structures was examined by FTIR and 1HNMR. Fir powder was extracted with a mixture of benzene/ethanol or activated with 25% (mass fraction) NaOH under normal temperature and pressure, microwave and high pressure. Dissolution of the pretreated wood powder in [HeVIM]Cl by microwave (90°C, 400w) was studied. The results showed that the ionic liquid [HeVIM]Cl exhibited a good solubility. Wood powder pretreated with 25% NaOH under high pressure had the lowest crystallinity (2.4%) and the highest dissolution rate (21.6%).

scholarly journals Oral Bioavailability Enhancement and Anti-Fatigue Assessment of the Andrographolide Loaded Solid Dispersion

2020 ◽  
Vol 21 (7) ◽  
pp. 2506 ◽  
Author(s):  
Ching-Chi Yen ◽  
Yu-Kai Liang ◽  
Chao-Pei Cheng ◽  
Mei-Chich Hsu ◽  
Yu-Tse Wu
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Oral Bioavailability ◽  
Water Solubility ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Amorphous State ◽  
Vehicle Group ◽  
Time To Exhaustion ◽  
Pharmacokinetic Studies

Andrographolide (AG), a major diterpene lactone isolated from Andrographis paniculata (Burm. f.) Nees (Acanthaceae), possesses a wide spectrum of biological activities. However, its poor water solubility and low bioavailability limit its clinical application. Therefore, this study aimed to develop a solid dispersion (SD) formulation to increase the aqueous solubility and dissolution rate of AG. Different drug-polymer ratios were used to prepare various SDs. The optimized formulation was characterized for differential scanning calorimetry, Fourier transform infrared spectroscopy, and powder X-ray diffraction. The analysis indicated that the optimized SD enhanced AG solubility and dissolution rates by changing AG crystallinity to an amorphous state. The dissolution behaviors of the optimum SD composed of an AG-polyvinylpyrrolidone K30-Kolliphor EL ratio of 1:7:1 (w/w/w) resulted in the highest accumulated dissolution (approximately 80%). Pharmacokinetic studies revealed that Cmax/dose and the AUC/dose increased by 3.7-fold and 3.0-fold, respectively, compared with AG suspension. Furthermore, pretreatment using the optimized AG-SD significantly increased the swimming time to exhaustion by 1.7-fold and decreased the plasma ammonia level by 71.5%, compared with the vehicle group. In conclusion, the optimized AG-SD formulation appeared to effectively improve its dissolution rate and oral bioavailability. Moreover, the optimized AG-SD provides a promising treatment against physical fatigue.

Potential of erlotinib cyclodextrin nanosponge complex to enhance solubility, dissolution rate, in vitro cytotoxicity and oral bioavailability

2016 ◽  
Vol 137 ◽  
pp. 339-349 ◽  
Author(s):  
Chander Parkash Dora ◽  
Francesco Trotta ◽  
Varun Kushwah ◽  
Naresh Devasari ◽  
Charan Singh ◽  
...  
Keyword(s):  
Dissolution Rate ◽  
Oral Bioavailability ◽  
In Vitro Cytotoxicity

scholarly journals Pure Trans-Resveratrol Nanoparticles Prepared by a Supercritical Antisolvent Process Using Alcohol and Dichloromethane Mixtures: Effect of Particle Size on Dissolution and Bioavailability in Rats

Antioxidants ◽  
2020 ◽  
Vol 9 (4) ◽  
pp. 342 ◽  
Author(s):  
Eun-Sol Ha ◽  
Heejun Park ◽  
Seon-Kwang Lee ◽  
Woo-Yong Sim ◽  
Ji-Su Jeong ◽  
...  
Keyword(s):  
Particle Size ◽  
Dissolution Rate ◽  
Oral Bioavailability ◽  
In Vitro Dissolution ◽  
Absolute Bioavailability ◽  
Simulated Gastric Fluid ◽  
Mean Particle Size ◽  
Supercritical Antisolvent ◽  
Effect Of Particle Size

The aim of this study was to prepare pure trans-resveratrol nanoparticles without additives (surfactants, polymers, and sugars) using a supercritical antisolvent (SAS) process with alcohol (methanol or ethanol) and dichloromethane mixtures. In addition, in order to investigate the effect of particle size on the dissolution and oral bioavailability of the trans-resveratrol, two microparticles with different sizes (1.94 μm and 18.75 μm) were prepared using two different milling processes, and compared to trans-resveratrol nanoparticles prepared by the SAS process. The solid-state properties of pure trans-resveratrol particles were characterized. By increasing the percentage of dichloromethane in the solvent mixtures, the mean particle size of trans-resveratrol was decreased, whereas its specific surface area was increased. The particle size could thus be controlled by solvent composition. Trans-resveratrol nanoparticle with a mean particle size of 0.17 μm was prepared by the SAS process using the ethanol/dichloromethane mixture at a ratio of 25/75 (w/w). The in vitro dissolution rate of trans-resveratrol in fasted state-simulated gastric fluid was significantly improved by the reduction of particle size, resulting in enhanced oral bioavailability in rats. The absolute bioavailability of trans-resveratrol nanoparticles was 25.2%. The maximum plasma concentration values were well correlated with the in vitro dissolution rate. These findings clearly indicate that the oral bioavailability of trans-resveratrol can be enhanced by preparing pure trans-resveratrol nanoparticles without additives (surfactants, polymers, and sugars) by the SAS process. These pure trans-resveratrol nanoparticles can be applied as an active ingredient for the development of health supplements, pharmaceutical products, and cosmetic products.

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