الفهرس 
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Abstract
Fluconazole (FlZ) and Voriconazole (VOZ) are triazole antifungals used
for treatment of vaginal candidiasis, but they have several disadvantages
when they are used orally as hepatic and renal problems. The objective of
this study was to formulate and evaluate different mucoadhesive vaginal
dosage forms of antifungal drugs.
The present study was divided into three parts as the following:
Part (I)
Formulation and Evaluation of Fluconazole Mucoadhesive Vaginal
Dosage Forms.
Chapter One
Formulation and in-vitro evaluation of Fluconazole mucoadhesive
vaginal gel.
1. In this chapter, different mucoadhesive gel formulations were prepared
using different polymers as Na CMC, HPMC 4000, Xanthan Gum (XG),
Na alginate and Carbopol 974 (Cbp 974). Different concentrations of
penetration enhancers (PEs) such as Tween 80 (T80) and Cetrimide (Ct)
were added to selected formulae.
2. The effect of certain variables on viscosity, spreadability diameter,
mucoadhesive strength and release of FlZ from the gel formulations were
studied and the following results were obtained:
a. Increasing the polymers concentration led to a significant increase
(p<0.05) in the gel viscosity and mucoadhesive strength, while the
spreadability diameter and the % released of FlZ were decreased.b. Addition of PEs led to a significant decrease (p<0.05) in the gel viscosity
and had no significant effect on the mucoadhesive force, but resulted in a
significant increase in the spreadability diameter and the % released of FlZ.
Chapter Two
Formulation and in-vitro evaluation of Fluconazole mucoadhesive
vaginal alginate beads.
1. In this chapter, FlZ alginate beads were prepared by ionotropic gelation
method using Calcium chloride and Aluminum chloride as cross linking
agents.
2. The effect of certain variables as Na alginate concentration, crosslinking
agent concentration and crosslinking agent type on entrapment efficiency
(EE), yield percentage, swelling index, bead size, mucoadhesive strength
and the % released of FlZ were studied and the following results were
obtained:
a. Increasing FlZ: Na alginate ratio from 1:1 to 1:3 at constant crosslinking
agent concentration led to a significant increase (p<0.05) in the EE, yield
percentage, swelling index, mucoadhesive strength and decrease in the %
released of FlZ.
b. The highest EE and yield percentage were obtained in alginate beads
prepared using Aluminum chloride as crosslinking agent.
c. Increasing Calcium chloride concentration from 2% to 6% resulted in a
significant increase (p<0.05) in the EE, but increasing Aluminum chloride
concentration above 2% did not enhance the entrapment efficiency.
d. Increasing crosslinking agent concentrations from 2% to 6% resulted in a
significant decrease (p<0.05) in the swelling index and size of beads.e. Increasing Na alginate concentration led to a significant decrease in the %
released of FlZ, also alginate beads which were prepared using Aluminum
chloride showed more sustained release than Calcium chloride alginate
beads.
Chapter Three
Formulation and in-vitro evaluation of Fluconazole mucoadhesive
vaginal films.
1. In this chapter, mucoadhesive vaginal films of FlZ were prepared by
solvent evaporation technique. Methocel k4000, Na CMC, Na alginate,
Pectin and combinations with HPMC E6 were used as polymers. 2%
Glycerol, 3% polyethylene glycol 400(PEG) and 1% Propylene glycol (PG)
were used as plasticizers.
2. Evaluation of thickness, weight variation, tensile strength, % elongation,
mucoadhesive strength and % released of FlZ were studied and the results
revealed that:
a. Increasing the polymers concentration resulted in a significant increase
(p<0.05) in the film thickness, weight, tensile strength, mucoadhesive
strength, but % elongation was decreased.
b. Increasing the polymers concentration resulted in a significant decrease in
the % released of FlZ.
Part (II)
Formulation and Evaluation of Voriconazole Mucoadhesive Vaginal
Dosage Forms.
The aim of this part was to formulate and evaluate different
mucoadhesive dosage forms of VOZ for vaginal application.