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Obj. 2 (obj. 1 - FYI)
Discuss drug delivery through Vagina.
Avoid 1st-pass metabolism
Rich vascularization
Relatively low enzymatic activity
Non-invasive, controlled transmucosal deliver for both local & systemic effects
Obj. 2 (cont.)
Discuss drug delivery through Vagina.
What are the vaginal features that affects retention of formulation, its absorption and drug release.
pH
Enzyme activity
Microflora
Obj. 2 (cont.)
Discuss drug delivery through Vagina.
What vaginal physiology affects the rate and extent of drug absorption after intravaginal administration?
Age
Stage in menstrual cycle
Formulation factors (penetration enhancer, viscosity, adhesives, etc.)
Obj. 3
Enlist 4 therapeutics application of vaginal drug delivery.
Contraceptives (effective route for hormone delivery)
AIDS/HIV
STDs
Vaginal infections
Obj. 4
List 3 advantages and 3 disadvantages of Vaginal drug delivery.
What are the 3 Advantages of vaginal drug delivery?
Advantages
Avoid hepatic 1st-pass metabolism
Minimal systemic effects
Local targeting of drugs to the reproductive organs
Obj. 4
List 3 advantages and 3 disadvantages of Vaginal drug delivery.
What are the 3 Disadvantages of vaginal drug delivery?
Disadvantages
Patient incompliance
Local irritation
Variable drug absorption → menstrual cycle, menopause, & pregnancy
Obj. 5
Discuss 2 mechanisms for vaginal drug absorption.
Transcellular (membrane) → lipophilic drug
Paracellular (tight junctions) → Hydrophilic drug
Obj. 6
Describe 3 factors affecting vaginal formulations.
Physiological
pH acidic (pH 3.5 - 4.5)
Enzymes
Micro-flora
Cyclic changes
Hormone level
Physiochemical (API)
Molecular size & weight
Partition coefficient (lipophilicity)
Ionization
Chemical nature
Formulation
Viscosity
Penetration enhancers
Bio-adhesive/mucoadhesive properties
Obj. 7
Describe 3 formulation factors affecting vaginal formulations.
Penetration Enhancers (promote absorption & penetration of drug through vaginal mucosa)
Mucoadhesive agents
Bio-adhesive formulation (Polymers - agents delivering API for extended period @ predictable rate)
Obj. 9 + 10 (obj. 8 - FYI)
Identify systemic & local drug delivery through vaginal route.
Local
Vaginal Suppositories
Vaginal Douches (vaginal irrigation), sprays, solutions
Vaginal gels, creams
Vaginal films, patches, rings
Systemic
Tablets
Capsules
Injectables
Implants