Dissolution Enhancement of Gendarusin A by Poloxamer 188 Addition in Justicia gendarussa Burm. f Ethanolic Extract Granule Matrix

2021 ◽

Vol 69 (2) ◽

Author(s):

Sohansinh S. Vaghela ◽

Samkit M. Shah ◽

Sanjesh G. Rathi ◽

Shrenik K. Shah

Keyword(s):

Solid Dispersion ◽

Aqueous Solubility ◽

Dissolution Enhancement ◽

Phase Solubility ◽

Fusion Method ◽

Poloxamer 188 ◽

X Ray ◽

Solubility Study ◽

Phase Solubility Study

Flurbiprofen solid dispersion Adsorbate (SDA) has been prepared using PEG 4000 and Poloxamer 188 as carrier and Neusilin as adsorbent material. The SDA of Flurbiprofen was prepared by using Fusion method in various drugs to carrier ratios. The phase solubility study concludes that both polymers have ability to improve the aqueous solubility of flurbiprofen. Pure API Flurbiprofen and final formulation samples of SDA are characterized by FTIR, DSC and X-ray diffraction spectroscopy. X-ray powder diffraction and DSC study indicated that the drug was present in amorphous form. FTIR study revealed that the characteristic peaks in spectra of pure Flurbiprofen are also present in spectra of SDA’s. Drug found compatible with the excipients. The highest improvement in solubility and in-vitro drug release were observed in solid dispersion prepared with Poloxamer 188 (F14) by fusion method. The increased dissolution rate of drug from solid dispersion adsorbates may be due to surface tension lowering effect of polymer to the medium and increased wettability and dispersibility of drug. Hence, F14 Solid dispersion adsorbates with the Poloxamer carrier in 1:2 ratio considered as most satisfactory among all solid dispersion adsorbates.

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Evaluation of Dissolution Enhancement of Aprepitant Drug in Ternary Pharmaceutical Solid Dispersions with Soluplus® and Poloxamer 188 Prepared by Melt Mixing

Sci ◽

10.3390/sci1020048 ◽

2019 ◽

Vol 1 (2) ◽

pp. 48

Author(s):

Stavroula Nanaki ◽

Rodanthi Maria Eleftheriou ◽

Panagiotis Barmpalexis ◽

Margaritis Kostoglou ◽

Evangelos Karavas ◽

...

Keyword(s):

Solid Dispersions ◽

Polarized Light ◽

Dissolution Enhancement ◽

Release Mechanism ◽

Mechanism Analysis ◽

Scanning Calorimetry ◽

Melt Mixing ◽

Element Analysis ◽

Poloxamer 188 ◽

Enhanced Dissolution

In the present study Aprepitant (APT) ternary solid dispersions (SDs) were developed and evaluated for the first time. Specifically, ternary SDs of APT with Poloxamer 188 and Soluplus® (SOL) were prepared via melt mixing and compared to binary APT/Poloxamer 188 and APT/SOL SDs. Initially, combined thermo-gravimetric and hot-stage polarized light microscopy studies indicated that all tested compounds were thermally stable up to 280 °C, while Poloxamer 188 acted as a plasticizer to SOL by significantly reducing the temperature required to fully solubilize the API during SD preparation. Differential scanning calorimetry combined with wide angle X-ray diffraction studies showed that crystalline API was dispersed in both binary and ternary SDs, while Fourier transformation-infrared spectroscopy studies revealed no molecular interactions among the components. Scanning electron microscopy combined with EDAX element analysis showed that the API was dispersed in nano-scale within the polymer matrices, while increasing APT content led to increasing API nano-crystals within the SDs. Finally, dissolution studies showed that the prepared formulations enhanced dissolution of Aprepitant and its mechanism analysis was further studied. A mathematical model was also investigated to evaluate the drug release mechanism.

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The Promising Role of Chitosan–Poloxamer 188 Nanocrystals in Improving Diosmin Dissolution and Therapeutic Efficacy against Ferrous Sulfate-Induced Hepatic Injury in Rats

Pharmaceutics ◽

10.3390/pharmaceutics13122087 ◽

2021 ◽

Vol 13 (12) ◽

pp. 2087

Author(s):

Neamet S. Lotfy ◽

Thanaa M. Borg ◽

Elham A. Mohamed

Keyword(s):

Water Solubility ◽

Chemical Interaction ◽

High Surface ◽

High Surface Area ◽

Dissolution Enhancement ◽

Hepatic Tissue ◽

Poloxamer 188 ◽

Ft Ir ◽

Electrostatic And Steric Stabilization ◽

Oxide Synthase

Diosmin (DSN) exhibits poor water solubility and low bioavailability. Although nanocrystals (NCs) are successful for improving drug solubility, they may undergo crystal growth. Therefore, DSN NCs were prepared, employing sonoprecipitation utilizing different stabilizers. The optimum stabilizer was combined with chitosan (CS) as an electrostatic stabilizer. NCs based on 0.15% w/v poloxamer 188 (PLX188) as a steric stabilizer and 0.04% w/v CS were selected because they showed the smallest diameter (368.93 ± 0.47 nm) and the highest ζ-potential (+40.43 ± 0.15 mV). Mannitol (1% w/v) hindered NC enlargement on lyophilization. FT-IR negated the chemical interaction of NC components. DSC and XRD were performed to verify the crystalline state. DSN dissolution enhancement was attributed to the nanometric rod-shaped NCs, the high surface area, and the improved wettability. CS insolubility and its diffusion layer may explain controlled DSN release from CS-PLX188 NCs. CS-PLX188 NCs were more stable than PLX188 NCs, suggesting the significance of the combined electrostatic and steric stabilization strategies. The superiority of CS-PLX188 NCs was indicated by the significantly regulated biomarkers, pathological alterations, and inducible nitric oxide synthase (iNOS) expression of the hepatic tissue compared to DSN suspension and PLX188 NCs. Permeation, mucoadhesion, and cellular uptake enhancement by CS may explain this superiority.

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Evaluation of Dissolution Enhancement of Aprepitant Drug in Ternary Pharmaceutical Solid Dispersions with Soluplus® and Poloxamer 188 Prepared by Melt Mixing

Sci ◽

10.3390/sci1010011.v1 ◽

2019 ◽

Vol 1 (1) ◽

pp. 11 ◽

Cited By ~ 1

Author(s):

Stavroula Nanaki ◽

Rodanthi Maria Eleftheriou ◽

Panagiotis Barmpalexis ◽

Margaritis Kostoglou ◽

Evangelos Karavas ◽

...

Keyword(s):

Solid Dispersions ◽

Polarized Light ◽

Dissolution Enhancement ◽

Release Mechanism ◽

Mechanism Analysis ◽

Scanning Calorimetry ◽

Melt Mixing ◽

Element Analysis ◽

Poloxamer 188 ◽

Enhanced Dissolution

In the present study Aprepitant (APT) ternary solid dispersions (SDs) were developed and evaluated for the first time. Specifically, ternary SDs of APT with Poloxamer 188 and Soluplus® (SOL) were prepared via melt mixing and compared to binary APT/Poloxamer 188 and APT/SOL SDs. Initially, combined thermo-gravimetric and hot-stage polarized light microscopy studies indicated that all tested compounds were thermally stable up to 280 °C, while Poloxamer 188 acted as a plasticizer to SOL by significantly reducing the temperature required to fully solubilize the API during SD preparation. Differential scanning calorimetry combined with wide angle X-ray diffraction studies showed that crystalline API was dispersed in both binary and ternary SDs, while Fourier transformation-infrared spectroscopy studies revealed no molecular interactions among the components. Scanning electron microscopy combined with EDAX element analysis showed that the API was dispersed in nano-scale within the polymer matrices, while increasing APT content led to increasing API nano-crystals within the SDs. Finally, dissolution studies showed that the prepared formulations enhanced dissolution of Aprepitant and its mechanism analysis was further studied. A mathematical model was also investigated to evaluate the drug release mechanism.

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