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Curcumin (CUR) is highly lipophilic drug that shows degradation at alkaline pH which restricts it... more Curcumin (CUR) is highly lipophilic drug that shows degradation at alkaline pH which restricts its oral bioavailability. The aim of the present study was to enhance the oral bioavailability of CUR by increasing its solubility and dissolution rate. Solid dispersions (SDs) of CUR in aqueous and organic solvent using Eudragit EPO (EuD) were prepared by spray drying and rota evaporation technique. The solubility of plain CUR in acidic pH 1.2 is only 0.02% whereas SDs containing EuD have solubilities of 40.29% and 18.78% by spray drying and rota evaporation technique respectively. Physical characterization by SEM, IR, DSC, and XRD studies, revealed the changes in solid state during the formation of dispersion and justified the decreased crystallinity of CUR SDs. Dissolution studies showed that pH values influenced the release profile lower the pH values higher the release speed (pH 1.2). CUR in pH 1.2 showed negligible release even after 120 min (2e5%) whereas, SDs showed 20e45% drug release after 60 min. Further, insilico docking study was carried out followed by molecular dynamic simulations to understand the molecular level binding interactions between drug and polymer. The insilico studies demonstrates the role of van der Waals interactions in binding of CUR to EuD.
A novel directly compressible (DC) co-processed excipient with improved functionality and masking... more A novel directly compressible (DC) co-processed excipient with improved functionality and masking the undesirable properties of individual excipients was developed without any chemical modification by using simple laboratory technique. For the development of co-processed excipient, release retarding polymers such as Polyethylene oxide (Polyox® WSR 301) and hydroxyl propyl methyl cellulose (Methocel® K4M) were used. Co-processed excipient was prepared in polymers weight ratio of 1:9 to 9:1 by roller compaction technique. Co-processed excipient prepared from polymers ratio of 7:3 and 8:2 showed good physico-chemical properties. The developed DC grade co-processed excipient was characterized for DSC, FTIR, SEM, XRD which confirms the absence of any chemical changes during co-processing. Highly water soluble Metoprolol succinate and poorly water soluble anhydrous Theophylline was used as model drugs for Invitro release study. Formulations prepared using co-processed excipient showed sus...
Curcumin (CUR) is highly lipophilic drug that shows degradation at alkaline pH which restricts it... more Curcumin (CUR) is highly lipophilic drug that shows degradation at alkaline pH which restricts its oral bioavailability. The aim of the present study was to enhance the oral bioavailability of CUR by increasing its solubility and dissolution rate. Solid dispersions (SDs) of CUR in aqueous and organic solvent using Eudragit EPO (EuD) were prepared by spray drying and rota evaporation technique. The solubility of plain CUR in acidic pH 1.2 is only 0.02% whereas SDs containing EuD have solubilities of 40.29% and 18.78% by spray drying and rota evaporation technique respectively. Physical characterization by SEM, IR, DSC, and XRD studies, revealed the changes in solid state during the formation of dispersion and justified the decreased crystallinity of CUR SDs. Dissolution studies showed that pH values influenced the release profile lower the pH values higher the release speed (pH 1.2). CUR in pH 1.2 showed negligible release even after 120 min (2e5%) whereas, SDs showed 20e45% drug release after 60 min. Further, insilico docking study was carried out followed by molecular dynamic simulations to understand the molecular level binding interactions between drug and polymer. The insilico studies demonstrates the role of van der Waals interactions in binding of CUR to EuD.
A novel directly compressible (DC) co-processed excipient with improved functionality and masking... more A novel directly compressible (DC) co-processed excipient with improved functionality and masking the undesirable properties of individual excipients was developed without any chemical modification by using simple laboratory technique. For the development of co-processed excipient, release retarding polymers such as Polyethylene oxide (Polyox® WSR 301) and hydroxyl propyl methyl cellulose (Methocel® K4M) were used. Co-processed excipient was prepared in polymers weight ratio of 1:9 to 9:1 by roller compaction technique. Co-processed excipient prepared from polymers ratio of 7:3 and 8:2 showed good physico-chemical properties. The developed DC grade co-processed excipient was characterized for DSC, FTIR, SEM, XRD which confirms the absence of any chemical changes during co-processing. Highly water soluble Metoprolol succinate and poorly water soluble anhydrous Theophylline was used as model drugs for Invitro release study. Formulations prepared using co-processed excipient showed sus...
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bioavailability. The aim of the present study was to enhance the oral bioavailability of CUR by increasing
its solubility and dissolution rate. Solid dispersions (SDs) of CUR in aqueous and organic solvent using
Eudragit EPO (EuD) were prepared by spray drying and rota evaporation technique. The solubility of plain
CUR in acidic pH 1.2 is only 0.02% whereas SDs containing EuD have solubilities of 40.29% and 18.78% by
spray drying and rota evaporation technique respectively. Physical characterization by SEM, IR, DSC, and
XRD studies, revealed the changes in solid state during the formation of dispersion and justified the
decreased crystallinity of CUR SDs. Dissolution studies showed that pH values influenced the release
profile lower the pH values higher the release speed (pH 1.2). CUR in pH 1.2 showed negligible release
even after 120 min (2e5%) whereas, SDs showed 20e45% drug release after 60 min. Further, insilico
docking study was carried out followed by molecular dynamic simulations to understand the molecular
level binding interactions between drug and polymer. The insilico studies demonstrates the role of van
der Waals interactions in binding of CUR to EuD.
bioavailability. The aim of the present study was to enhance the oral bioavailability of CUR by increasing
its solubility and dissolution rate. Solid dispersions (SDs) of CUR in aqueous and organic solvent using
Eudragit EPO (EuD) were prepared by spray drying and rota evaporation technique. The solubility of plain
CUR in acidic pH 1.2 is only 0.02% whereas SDs containing EuD have solubilities of 40.29% and 18.78% by
spray drying and rota evaporation technique respectively. Physical characterization by SEM, IR, DSC, and
XRD studies, revealed the changes in solid state during the formation of dispersion and justified the
decreased crystallinity of CUR SDs. Dissolution studies showed that pH values influenced the release
profile lower the pH values higher the release speed (pH 1.2). CUR in pH 1.2 showed negligible release
even after 120 min (2e5%) whereas, SDs showed 20e45% drug release after 60 min. Further, insilico
docking study was carried out followed by molecular dynamic simulations to understand the molecular
level binding interactions between drug and polymer. The insilico studies demonstrates the role of van
der Waals interactions in binding of CUR to EuD.