Application of Central Composite Design in Optimization of Valsartan Nanosuspension to Enhance its Solubility and Stability

Vuppalapati, Lavakumar; Cherukuri, Sowmya; Neeli, Vijaykumar; Yeragamreddy, Padmanabha Reddy; Kesavan, Bhaskar Reddy

doi:10.2174/1567201812666150724094358

Cited by 14 publications

(9 citation statements)

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“…The optimal predictive values were particle size of 106.9 nm and PDI of 0.12. The actual values for optimal formulation were particle size of 110.7 ± 11.2 nm and PDI of 0.141 ± 0.054, which was consistent with the predicted values and favourable for enhancing saturated solubility and dissolution rate of poorly soluble drugs [16].…”

Section: Formulation Optimization Of Lutein Nanosuspensionsupporting

confidence: 81%

Improved oral bioavailability for lutein by nanocrystal technology: formulation development,in vitroandin vivoevaluation

Chang

Cao

et al. 2017

Artificial Cells, Nanomedicine, and Biotechnology

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Lutein is a kind of natural carotenoids possessing many pharmacological effects. The application of lutein was limited mainly due to its low oral bioavailability caused by poor aqueous solubility. Nanocrystal formulation of lutein was developed to improve the oral bioavailability in this study. The nanosuspension was prepared by the anti-solvent precipitation-ultrasonication method and optimized by Box-Behnken design, followed by freeze-drying to obtain lutein nanocrystals. The nanocrystals were characterized on their physical properties, in vitro dissolution and in vivo absorption performance. Lutein nanocrystals showed as tiny spheres with an average particle size of 110.7 nm. The result of diffractograms indicated that the percent crystallinity of lutein was 89.4% in coarse powder and then declined in nanocrystal formulation. The saturated solubility of lutein in water increased from 7.3 μg/ml for coarse powder up to 215.7 μg/ml for lutein nanocrystals. The dissolution rate of lutein nanocrystals was significantly higher than that of coarse powder or the physical mixture. The C and AUC of lutein nanocrystals after oral administration in rats was 3.24 and 2.28 times higher than those of lutein suspension, respectively. These results indicated that the nanocrystal formulation could significantly enhance the dissolution and absorption of lutein and might be a promising approach for improving its oral bioavailability.

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Section: Formulation Optimization Of Lutein Nanosuspensionsupporting

confidence: 81%

Improved oral bioavailability for lutein by nanocrystal technology: formulation development,in vitroandin vivoevaluation

Chang

Cao

et al. 2017

Artificial Cells, Nanomedicine, and Biotechnology

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“…Results suggested no significant change in EE content of liquid EENS and lyophilized EENS when stored at different storage conditions indicating that both the liquid and lyophilized NS are chemically stable at these storage conditions. Noteworthy, for physical stability of liquid EENS, lyophilization and storage at refrigerated conditions are recommended [45] .…”

Section: Fig 5: Cytotoxicity Of Eens and Eeaqd Cytotoxicity Of Ethinmentioning

confidence: 99%

Lyophilized Ethinylestradiol Nanosuspension: Fabrication, Characterization and Evaluation of in vitro Anticancer and Pharmacokinetic Study

Powar¹,

Hajare²

2020

ijps

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The present investigation was aimed to fabricate lyophilized nanosuspension of poorly soluble ethinylestradiol in order to enhance oral bioavailability and stability. The top-down high-pressure homogenization technique was used to formulate the desired dosage form. The formulations were characterized and optimized for compatibility, crystallographic investigation, surface topography, drug release, in vitro apoptosis and cytotoxicity and in vivo pharmacokinetic investigations. The mean particle size and zeta potential of the optimized lyophilized ethinylestradiol nanosuspension were 220±0.37 nm and -19.3±6.73 mV, respectively. The surface topographical studies showed needle-shaped particles from bar shape upon nanonization by high-pressure homogenization technique. Differential scanning calorimetry and X-ray powder diffraction studies confirmed the crystalline nature of ethynylestradiol after nanonization. The dissolution rate of ethinylestradiol nanosuspension was improved as compared to ethinylestradiol powder. In vitro cytotoxicity of ethinylestradiol nanosuspension on MCF-7 cell line showed more than 80 % inhibition of viability of cells relative to that produced by ethinylestradiol aqueous dispersion. Noteworthy, apoptotic cells treated with ethinylestradiol nanosuspension showed shrinkage, followed by fragmentation and cell death. Significantly, ethinylestradiol nanosuspension enhanced C max and AUC 0-t by 1.5-fold and 1.7-fold compared to that of the aqueous solution. The relative bioavailability of ethinylestradiol was enhanced 2-fold and high concentrations were found to be distributed to liver, spleen and stomach. Thus lyophilized nanosuspension could be a better approach to enhance solubility, oral bioavailability and stability of ethinylestradiol in pharmaceutical formulations.

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“…4 For an electrostatic stability nanosuspension should have zeta potential a minimum of ±30mVs.For combined electrostatic and steric stabilization a minimum of ±20mV is required. The zeta potential of nanosuspension was measured using Malvern Zetasizer ZS200 at 25 ± 0.5ºC.…”

Section: Zeta Potentialmentioning

confidence: 99%

“…3 This type of drugs has always been a challenging problem to pharmaceutical scientists in formulating suitable dosage forms. 4 Solubility may be stated in units of concentration, molality, mole fraction, mole ratio, and other units. 5 Meropenem is a broad-spectrum carbapenem antibiotic 6 and classified as BCS class IV drug 7 means having low solubility and low permeability.…”

Section: Introductionmentioning

confidence: 99%

Solubility and Dissolution Enhancement of Meropenem by Nano Suspension Approach

chirumamilla¹,

Padasala²,

Aravally³

et al. 2017

JYP

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Objective: To prepare and evaluate the suitable nanosuspensions of Meropenem (BCS-IV drug) to increase its solubility and dissolution. Methodology: The meropenem nanosuspensions were prepared by emulsification solvent evaporation technique by applying ultrasonic energy through probe sonicator, where the organic phase of drug solution in methanol was emulsified in aqueous phase containing hydroxy propyl methyl cellulose as solubilizer and sodium lauryl sulphate as stabilizer. The prepared nanosuspensions were characterised for particle size, zeta potential, surface morphology by SEM, drug excipient compatibility by FTIR and DSC and conducted in-vitro drug release studies. Results: Results showed that the prepared nanosuspensions were having particle size range from 1 to 1000nm and the zeta potential from -10 to -20 mVs. Scanning electron microscopic pictures revealed that the obtained nanosuspension particles were spherical in shape with surface smoothness and in-vitro drug release studies notified that the prepared nanosuspensions showed increase in solubility and dissolution of meropenem when compared with the pure form. Conclusion: The nanosuspensions of meropenem could be successfully prepared and can be concluded that the nanosuspension formulation is a promising approach to increase the solubility and dissolution of BCS-IV drugs like meropenem.

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Application of Central Composite Design in Optimization of Valsartan Nanosuspension to Enhance its Solubility and Stability

Cited by 14 publications

References 0 publications

Improved oral bioavailability for lutein by nanocrystal technology: formulation development,in vitroandin vivoevaluation

Improved oral bioavailability for lutein by nanocrystal technology: formulation development,in vitroandin vivoevaluation

Lyophilized Ethinylestradiol Nanosuspension: Fabrication, Characterization and Evaluation of in vitro Anticancer and Pharmacokinetic Study

Solubility and Dissolution Enhancement of Meropenem by Nano Suspension Approach

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