PENGEMBANGAN NANOSPONGE ATORVASTATIN KALSIUM BASIS ?-SIKLODEKSTRIN
Atorvastatin calcium (AC) is a BCS (biopharmaceutical classification system) class II drug which belongs to statin drug group (first line in dyslipidemia treatment). AC has poor aqueous solubility (0,8 mg/mL at 37 °C), high permeability at physiological pH of intestine (6–6,5), and low bioavailab...
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id-itb.:441172019-10-02T07:30:36ZPENGEMBANGAN NANOSPONGE ATORVASTATIN KALSIUM BASIS ?-SIKLODEKSTRIN Vania Boru Tobing, Ayu Indonesia Final Project Atorvastatin calcium, ?-cyclodextrin, nanosponges, solubility enhancement. INSTITUT TEKNOLOGI BANDUNG https://digilib.itb.ac.id/gdl/view/44117 Atorvastatin calcium (AC) is a BCS (biopharmaceutical classification system) class II drug which belongs to statin drug group (first line in dyslipidemia treatment). AC has poor aqueous solubility (0,8 mg/mL at 37 °C), high permeability at physiological pH of intestine (6–6,5), and low bioavailability (around 12%). The aim of this study was to develop ?-cyclodextrin based nanosponges as an effort to increase the solubility of AC. Blank nanosponges (NS) were obtained by reacting ?-cyclodextrin (CD) with carbonyldiimidazole (CDI) as cross-linker in different molar ratios (1:4 and 1:6) in dimethylformamide (DMF). The optimum formula was obtained based on the highest drug entrapment efficiency. The optimum formula was CD:CDI at molar ratio 1:4 and NS:AC at weight ratio 1:4 (AC-NS4 1:4). AC loaded NS were evaluated and characterized. AC loaded NS was obtained with particle size of 448.7 ± 7.7 nm, polydispersity index of 0.331 ± 0.029, and zeta potential of -12.81 mV. Chemical interactions analysis using FTIR and surface morphological analysis using SEM were performed on the AC loaded NS. Characterization using FTIR and SEM showed physical interaction between AC and NS. Based on the solubility test, nanosponges can increase the solubility of calcium atorvastatin significantly (p<0.05) in comparison to ?-cyclodextrin inclusion complex and HP-?-cyclodextrin (hydroxypropyl-?-siklodekstrin) inclusion complex. text |
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Atorvastatin calcium (AC) is a BCS (biopharmaceutical classification system) class II drug which
belongs to statin drug group (first line in dyslipidemia treatment). AC has poor aqueous solubility
(0,8 mg/mL at 37 °C), high permeability at physiological pH of intestine (6–6,5), and low
bioavailability (around 12%). The aim of this study was to develop ?-cyclodextrin based
nanosponges as an effort to increase the solubility of AC. Blank nanosponges (NS) were obtained
by reacting ?-cyclodextrin (CD) with carbonyldiimidazole (CDI) as cross-linker in different molar
ratios (1:4 and 1:6) in dimethylformamide (DMF). The optimum formula was obtained based on the
highest drug entrapment efficiency. The optimum formula was CD:CDI at molar ratio 1:4 and NS:AC
at weight ratio 1:4 (AC-NS4 1:4). AC loaded NS were evaluated and characterized. AC loaded NS was
obtained with particle size of 448.7 ± 7.7 nm, polydispersity index of 0.331 ± 0.029, and zeta
potential of -12.81 mV. Chemical interactions analysis using FTIR and surface morphological analysis
using SEM were performed on the AC loaded NS. Characterization using FTIR and SEM showed
physical interaction between AC and NS. Based on the solubility test, nanosponges can increase the
solubility of calcium atorvastatin significantly (p<0.05) in comparison to ?-cyclodextrin inclusion
complex and HP-?-cyclodextrin (hydroxypropyl-?-siklodekstrin) inclusion complex.
|
format |
Final Project |
author |
Vania Boru Tobing, Ayu |
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Vania Boru Tobing, Ayu PENGEMBANGAN NANOSPONGE ATORVASTATIN KALSIUM BASIS ?-SIKLODEKSTRIN |
author_facet |
Vania Boru Tobing, Ayu |
author_sort |
Vania Boru Tobing, Ayu |
title |
PENGEMBANGAN NANOSPONGE ATORVASTATIN KALSIUM BASIS ?-SIKLODEKSTRIN |
title_short |
PENGEMBANGAN NANOSPONGE ATORVASTATIN KALSIUM BASIS ?-SIKLODEKSTRIN |
title_full |
PENGEMBANGAN NANOSPONGE ATORVASTATIN KALSIUM BASIS ?-SIKLODEKSTRIN |
title_fullStr |
PENGEMBANGAN NANOSPONGE ATORVASTATIN KALSIUM BASIS ?-SIKLODEKSTRIN |
title_full_unstemmed |
PENGEMBANGAN NANOSPONGE ATORVASTATIN KALSIUM BASIS ?-SIKLODEKSTRIN |
title_sort |
pengembangan nanosponge atorvastatin kalsium basis ?-siklodekstrin |
url |
https://digilib.itb.ac.id/gdl/view/44117 |
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1822926776051957760 |