Abstract
Objective: The fundamental objective of this research investigation was to develop intravaginal diazepam (DZ)-loaded alginate beads for the management of acute pelvic floor dysfunction (PFD) pain with minimal sedative effect.Methods: DZ loaded beads were prepared by an ionotropic gelation method using SA (sodium alginate) alone, or in combination with either poloxamer 407 (PL), pectin (PC), or xanthan gum (XG) at different ratios in the presence of different concentrations of calcium chloride as a cross-linking agent. The successfully developed beads were evaluated for the particle size, pH, yield percentage, entrapment efficiency, in vitro bioadhesion, swelling percentage, and in vitro drug release. The stability, ex vivo drug permeation, and sedative action of the optimized beads formulations were studied.Results: The particle size of the formulated beads was from 395±3.3 to 515±2.8 μm, yield percentage was from 68.2±1.7 to 87.5±2.1, entrapment efficiency was from 65.6±1.6 to 87.5±2.1. pH ranged from 6.1±0.2 to 6.8±0.6, bioadhesion strength was from 71.5±1.3 to 87.6±3.1, and swelling percentage was in the range from 53.4±3.1 to 85.2±3.7. Approximately 92.4–72.6% of the loaded dose was released from the prepared beads. The optimized beads showed a good stability under the selected storage conditions. About 74.8%, 71.1%, 68.6%, and 63.4% of the loaded dose permeated through the rabbit vaginal mucosa from F7, F9, F3, and F11, respectively. The formulated beads decreased the sedative action associated with orally or parenterally administered DZ.Conclusion: The developed beads were considered a promising candidate to formulate DZ into a new dosage form for the treatment of PFD with a minimum central nervous system sedation.
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