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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Bibliographic Details
Main Author: Vania Boru Tobing, Ayu
Format: Final Project
Language:Indonesia
Online Access:https://digilib.itb.ac.id/gdl/view/44117
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Institution: Institut Teknologi Bandung
Language: Indonesia
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Summary: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.