Improving the Solubility and Bioavailability of Dihydroartemisinin by Solid Dispersions and Inclusion Complexes
Dihydroartemisinin (DHA) is a poorly water-soluble drug that displays low bioavailability after oral administration. Attempts have been made to improve the solubility of DHA. Yet, no information is available concerning improved bioavailability. This study aimed to improve the water solubility of DHA...
| Main Authors: | , , , |
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| Format: | Journal Article |
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Pharmaceutical Society of Korea
2011
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| Online Access: | http://hdl.handle.net/20.500.11937/43367 |
| _version_ | 1848756671888752640 |
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| author | Ansari, M. Batty, Kevin Iqbal, Ijaz Sunderland, Vivian |
| author_facet | Ansari, M. Batty, Kevin Iqbal, Ijaz Sunderland, Vivian |
| author_sort | Ansari, M. |
| building | Curtin Institutional Repository |
| collection | Online Access |
| description | Dihydroartemisinin (DHA) is a poorly water-soluble drug that displays low bioavailability after oral administration. Attempts have been made to improve the solubility of DHA. Yet, no information is available concerning improved bioavailability. This study aimed to improve the water solubility of DHA by two systems: solid dispersions with polyvinylpyrrolidone (PVPK30, PVPK25, PVPK15) and inclusion complexes with hydroxypropyl-β-cyclodextrin (HPβCD), as well as improving the bioavailability of both systems. The phase transition of DHA with hydrophilic polymers was evaluated by X-ray diffraction (XRD) and differential scanning calorimetery (DSC). DHA became amorphous in DHA-HPβCD complexes and showed more amorphous behavior in XRD analyses with rise in molecular weight of PVP. Melting onset temperature of DHA decreased, while DSC thermograms revealed the peak area and enhanced enthalpy change (DH) in solid dispersions as well as inclusion complexes. DHA solubility was enhanced 84-fold in DHA-HPβCD complexes and 50-times in DHA-PVPK30. The improved solubility using the four polymers was in the following order: HPβCD > PVPK30 > PVPK25 > PVPK15. Values of area under curve (AUC) and half life (t(1/2)) of DHA-PVPK30 were highest followed by DHA-HPβCD, DHA-PVPK15 and DHA-PVPK25. V(d)/f of DHA-PVPK30 was 7-fold. DHA-HPβCD, DHA-PVPK15 and DHA-PVPK25 showed significantly different pharmacokinetic parameters compared with DHA solutions. The 95% confidence interval was meaningful in AUC and t(1/2). Pharmacokinetic parameters revealed that all four-test preparations were significantly more bioavailable than DHA alone. |
| first_indexed | 2025-11-14T09:15:55Z |
| format | Journal Article |
| id | curtin-20.500.11937-43367 |
| institution | Curtin University Malaysia |
| institution_category | Local University |
| last_indexed | 2025-11-14T09:15:55Z |
| publishDate | 2011 |
| publisher | Pharmaceutical Society of Korea |
| recordtype | eprints |
| repository_type | Digital Repository |
| spelling | curtin-20.500.11937-433672017-09-13T16:00:44Z Improving the Solubility and Bioavailability of Dihydroartemisinin by Solid Dispersions and Inclusion Complexes Ansari, M. Batty, Kevin Iqbal, Ijaz Sunderland, Vivian Dihydroartemisinin (DHA) is a poorly water-soluble drug that displays low bioavailability after oral administration. Attempts have been made to improve the solubility of DHA. Yet, no information is available concerning improved bioavailability. This study aimed to improve the water solubility of DHA by two systems: solid dispersions with polyvinylpyrrolidone (PVPK30, PVPK25, PVPK15) and inclusion complexes with hydroxypropyl-β-cyclodextrin (HPβCD), as well as improving the bioavailability of both systems. The phase transition of DHA with hydrophilic polymers was evaluated by X-ray diffraction (XRD) and differential scanning calorimetery (DSC). DHA became amorphous in DHA-HPβCD complexes and showed more amorphous behavior in XRD analyses with rise in molecular weight of PVP. Melting onset temperature of DHA decreased, while DSC thermograms revealed the peak area and enhanced enthalpy change (DH) in solid dispersions as well as inclusion complexes. DHA solubility was enhanced 84-fold in DHA-HPβCD complexes and 50-times in DHA-PVPK30. The improved solubility using the four polymers was in the following order: HPβCD > PVPK30 > PVPK25 > PVPK15. Values of area under curve (AUC) and half life (t(1/2)) of DHA-PVPK30 were highest followed by DHA-HPβCD, DHA-PVPK15 and DHA-PVPK25. V(d)/f of DHA-PVPK30 was 7-fold. DHA-HPβCD, DHA-PVPK15 and DHA-PVPK25 showed significantly different pharmacokinetic parameters compared with DHA solutions. The 95% confidence interval was meaningful in AUC and t(1/2). Pharmacokinetic parameters revealed that all four-test preparations were significantly more bioavailable than DHA alone. 2011 Journal Article http://hdl.handle.net/20.500.11937/43367 10.1007/s12272-011-0509-1 Pharmaceutical Society of Korea restricted |
| spellingShingle | Ansari, M. Batty, Kevin Iqbal, Ijaz Sunderland, Vivian Improving the Solubility and Bioavailability of Dihydroartemisinin by Solid Dispersions and Inclusion Complexes |
| title | Improving the Solubility and Bioavailability of Dihydroartemisinin by Solid Dispersions and Inclusion Complexes |
| title_full | Improving the Solubility and Bioavailability of Dihydroartemisinin by Solid Dispersions and Inclusion Complexes |
| title_fullStr | Improving the Solubility and Bioavailability of Dihydroartemisinin by Solid Dispersions and Inclusion Complexes |
| title_full_unstemmed | Improving the Solubility and Bioavailability of Dihydroartemisinin by Solid Dispersions and Inclusion Complexes |
| title_short | Improving the Solubility and Bioavailability of Dihydroartemisinin by Solid Dispersions and Inclusion Complexes |
| title_sort | improving the solubility and bioavailability of dihydroartemisinin by solid dispersions and inclusion complexes |
| url | http://hdl.handle.net/20.500.11937/43367 |