UNSUCCESSFUL DELIVERY OF TETRANDRINE FROM COLON-TARGETED DOSAGE FORMS COMPRISING ALGINATE/HYDROXYPROPYL METHYLCELLULOSE AND ALGINATEâ€“CHITOSAN BEADS
Objective: The objective of this study was to optimize the formulations of antifibrotic tetrandrine beads using alginate and various concentrations of
hydroxypropyl methylcellulose (HPMC) and chitosan.
Methods: Beads were formulated with six (F1â€“F6) concentrations of polymer and were then characterized using scanning electron microscopy,
differential scanning calorimetry, and X-ray diffraction; these beads were used for measurements of moisture contents, swelling, and in vitro drug
Results: Beads with the highest concentrations of HPMC and chitosan produced the highest entrapment efficiencies of 49.83% and 50.71%,
respectively. Moreover, drug release under stomach conditions (HCl pH 1.2 medium) was restricted to 75.01%, 61.01%, 51.86%, 74.84%, 66.00%,
and 41.63% with increasing HPMC and chitosan concentrations (F1â€“F6, respectively).
Conclusion: Beads of all formulations showed inadequate retention of tetrandrine under pH conditions of the upper gastrointestinal tract and would
likely be unsuccessful as colon-targeted dosage forms.
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