Formulation and in-vitro evaluation of Propranolol Hcl mucoadhesive vaginal beads for contraceptive purposes.

Document Type : Original Article

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Department of Pharmaceutics, Faculty of Pharmacy, Zagazig University

Abstract

Purpose: Based on the clinical findings on the efficacy of propranolol Hcl as a potent spermicide, the present study was designed to develop new sustained-release intravaginal propranolol-HCl-loaded alginate beads for contraceptive purposes. Method: Mucoadhesive vaginal beads were developed using an ionotropic gelation method with different ratios of the mucoadhesive polymer (Na alginate) to the cross-linking agent (calcium chloride). The prepared beads were examined and evaluated for their particle size, pH, entrapment efficiency % and their yield percentage, in-vitro bioadhesion, percentage of swelling and tested for stability.

Results: The prepared formulations revealed micro-sized beads with yield percentage exceeding 90%, entrapment efficiency was much influenced by the drug: polymer ratio as well as CaCl2 concentration, pH ranged from 4.8±0.1 to 5.6±0.1 which was acidic enough to cause inhibition of sperm motility and cause spermicidal action, and satisfactory swelling percentage with optimum bioadhesive strength for good intravaginal application. The in vitro release of the drug proceeded over 8 hours with different release percentage according to the incorporated polymer and crosslinking agent. The critical impacts of increasing polymer concentration on increasing the EE% and mucoadhesion were emphasized. The developed beads showed acceptable stability results under the studied storage conditions.

Conclusion: Propranolol HCl-loaded alginate beads were suitable for vaginal application and suggested a promising formulation for spermicidal contraceptive purposes.

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