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Formulation and characterization of the atenolol-ßcyclodextrin-poloxamer 188 ternary inclusion complex with solvent evaporation method
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| Author:
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KARINA CITRA RANI, AGNES NUNIEK WINANTARI, MUHAMMAD HABIBUR ROHMAN, STEPHANIE
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| Abstract:
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Purpose: The aim of this study was to develop a ternary inclusion complex of atenolol-ß-cyclodextrinpoloxamer
188
to
enhance
the
dissolution
of
atenolol.
Methodology:The
ternary inclusion complex of atenolol-ß-cyclodextrin-poloxamer 188 in this study was
developed into three different ratios (1:1:0.00075; 1:1:0.00015; 1:1:0.00225). The solvent evaporation method
was employed to produce these inclusion complexes. The inclusion complexes were characterized using FT-IR,
DSC, XRD and SEM. The obtained inclusion complexes were also evaluated to determine the drug content
and dissolution parameters.
Results: The results of FT-IR analysis exhibited interaction of atenolol, ß-cyclodextrin, and poloxamer 188
through hydrogen bonding in the inclusion complex. Results of DSC and XRD study suggested the conversion
of atenolol from a crystalline form to amorphous form. SEM analysis of inclusion complexes revealed that
atenolol was entrapped in the ß-cyclodextrin cavities and poloxamer 188 attached on the surface of ßcyclodextrin.The
dissolution
profile
of
these
inclusion
complexes
showed
enhancement
of
atenolol
dissolution
compare
to pure atenolol. The inclusion complex using 1:1:0,00015 ratio performed the highest dissolution
efficiency among three ratios. Therewere a 1.2 fold increases in dissolution efficiency of inclusion complexes
compared to the pure drug.
Applications/Originality/Value: In ternary inclusion complex, ß-cyclodextrin served as a versatile carrier to
entrap the drug inside their cavity via hydrogen bound interaction. The addition of poloxamer 188 is also
required to enhance aqueous solubility and fasten the rate of dissolution of atenolol. There was no study to
develop a ternary inclusion complex of atenolol using ß-cyclodextrin and poloxamer 188.
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| Keyword:
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atenolol; ß-cyclodextrin; ternary inclusion complex; solvent evaporation
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| EOI:
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| DOI:
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| Download:
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