Microwave Processed Solid Dispersions for Enhanced Dissolution of Gemfibrozil using non-Ordered Mesoporous Silica

Talib Hussain, Laura J. Waters, Gareth M.B. Parkes, Yasser Shahzad

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7 Citations (Scopus)

Abstract

This study describes the application of three non-ordered mesoporous silicas (Syloid AL-1, Syloid 72 and Syloid 244) in improving the dissolution rate of a poorly aqueous soluble drug, namely gemfibrozil. For this purpose, solid dispersions were formulated using a robust and controlled microwave heating method. Prepared formulations were subjected to solid state characterisation and dissolution behaviour. Differential scanning calorimetry (DSC) and X-ray diffraction (XRD) results confirmed that microwave heating method incorporated gemfibrozil in an amorphous form in Syloid 72 and Syloid 244. This was attributed to a large pore volume and diameter compared with Syloid AL-1 which has a small pore volume. Presence of more crystalline drug in the case of Syloid AL-1 based formulations was attributed to larger surface area where drug was adsorbed in layers as confirmed by the scanning electron microscopy. DSC and XRD results also confirmed stability of formulations when stored for 3 months under stressed conditions (40 °C and 75% RH). FT-IR results show lack of interaction between silica and the drug in all cases. It was also noted that all three silica types improved the dissolution behaviour of gemfibrozil when compared with dissolution properties of pure drug. The surface properties of Syloid 72 were found optimum as it enhanced the rate of dissolution of gemfibrozil from microwave processed formulation far better than physically mixed formulations and those prepared with Syloid AL-1 and Syloid 244
Original languageEnglish
Pages (from-to)428-435
Number of pages8
JournalColloids and Surfaces A: Physicochemical and Engineering Aspects
Volume520
Early online date4 Feb 2017
DOIs
Publication statusPublished - 5 May 2017

Fingerprint

Gemfibrozil
Ephrin-A5
Dispersions
Silicon Dioxide
dissolving
Dissolution
drugs
Silica
Microwaves
silicon dioxide
formulations
microwaves
Microwave heating
Pharmaceutical Preparations
Differential scanning calorimetry
heat measurement
porosity
X ray diffraction
heating
scanning

Cite this

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title = "Microwave Processed Solid Dispersions for Enhanced Dissolution of Gemfibrozil using non-Ordered Mesoporous Silica",
abstract = "This study describes the application of three non-ordered mesoporous silicas (Syloid AL-1, Syloid 72 and Syloid 244) in improving the dissolution rate of a poorly aqueous soluble drug, namely gemfibrozil. For this purpose, solid dispersions were formulated using a robust and controlled microwave heating method. Prepared formulations were subjected to solid state characterisation and dissolution behaviour. Differential scanning calorimetry (DSC) and X-ray diffraction (XRD) results confirmed that microwave heating method incorporated gemfibrozil in an amorphous form in Syloid 72 and Syloid 244. This was attributed to a large pore volume and diameter compared with Syloid AL-1 which has a small pore volume. Presence of more crystalline drug in the case of Syloid AL-1 based formulations was attributed to larger surface area where drug was adsorbed in layers as confirmed by the scanning electron microscopy. DSC and XRD results also confirmed stability of formulations when stored for 3 months under stressed conditions (40 °C and 75{\%} RH). FT-IR results show lack of interaction between silica and the drug in all cases. It was also noted that all three silica types improved the dissolution behaviour of gemfibrozil when compared with dissolution properties of pure drug. The surface properties of Syloid 72 were found optimum as it enhanced the rate of dissolution of gemfibrozil from microwave processed formulation far better than physically mixed formulations and those prepared with Syloid AL-1 and Syloid 244",
keywords = "Amorphous, Dissolution enhancement, Gemfibrozil, Microwave heating, Silica, Solid dispersion",
author = "Talib Hussain and Waters, {Laura J.} and Parkes, {Gareth M.B.} and Yasser Shahzad",
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T1 - Microwave Processed Solid Dispersions for Enhanced Dissolution of Gemfibrozil using non-Ordered Mesoporous Silica

AU - Hussain, Talib

AU - Waters, Laura J.

AU - Parkes, Gareth M.B.

AU - Shahzad, Yasser

N1 - Not OA compliant - no AAM on ePrints.

PY - 2017/5/5

Y1 - 2017/5/5

N2 - This study describes the application of three non-ordered mesoporous silicas (Syloid AL-1, Syloid 72 and Syloid 244) in improving the dissolution rate of a poorly aqueous soluble drug, namely gemfibrozil. For this purpose, solid dispersions were formulated using a robust and controlled microwave heating method. Prepared formulations were subjected to solid state characterisation and dissolution behaviour. Differential scanning calorimetry (DSC) and X-ray diffraction (XRD) results confirmed that microwave heating method incorporated gemfibrozil in an amorphous form in Syloid 72 and Syloid 244. This was attributed to a large pore volume and diameter compared with Syloid AL-1 which has a small pore volume. Presence of more crystalline drug in the case of Syloid AL-1 based formulations was attributed to larger surface area where drug was adsorbed in layers as confirmed by the scanning electron microscopy. DSC and XRD results also confirmed stability of formulations when stored for 3 months under stressed conditions (40 °C and 75% RH). FT-IR results show lack of interaction between silica and the drug in all cases. It was also noted that all three silica types improved the dissolution behaviour of gemfibrozil when compared with dissolution properties of pure drug. The surface properties of Syloid 72 were found optimum as it enhanced the rate of dissolution of gemfibrozil from microwave processed formulation far better than physically mixed formulations and those prepared with Syloid AL-1 and Syloid 244

AB - This study describes the application of three non-ordered mesoporous silicas (Syloid AL-1, Syloid 72 and Syloid 244) in improving the dissolution rate of a poorly aqueous soluble drug, namely gemfibrozil. For this purpose, solid dispersions were formulated using a robust and controlled microwave heating method. Prepared formulations were subjected to solid state characterisation and dissolution behaviour. Differential scanning calorimetry (DSC) and X-ray diffraction (XRD) results confirmed that microwave heating method incorporated gemfibrozil in an amorphous form in Syloid 72 and Syloid 244. This was attributed to a large pore volume and diameter compared with Syloid AL-1 which has a small pore volume. Presence of more crystalline drug in the case of Syloid AL-1 based formulations was attributed to larger surface area where drug was adsorbed in layers as confirmed by the scanning electron microscopy. DSC and XRD results also confirmed stability of formulations when stored for 3 months under stressed conditions (40 °C and 75% RH). FT-IR results show lack of interaction between silica and the drug in all cases. It was also noted that all three silica types improved the dissolution behaviour of gemfibrozil when compared with dissolution properties of pure drug. The surface properties of Syloid 72 were found optimum as it enhanced the rate of dissolution of gemfibrozil from microwave processed formulation far better than physically mixed formulations and those prepared with Syloid AL-1 and Syloid 244

KW - Amorphous

KW - Dissolution enhancement

KW - Gemfibrozil

KW - Microwave heating

KW - Silica

KW - Solid dispersion

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VL - 520

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JO - Colloids and Surfaces A: Physicochemical and Engineering Aspects

JF - Colloids and Surfaces A: Physicochemical and Engineering Aspects

SN - 0927-7757

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