VAGINAL DRUG DELIVERY SYSTEMS .pptx

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1. DRUG DELIVERY SYSTEMS VAGINAL

2. 1 KEY ELEMENTS Introduction Anatomy Of Vagina Physiology Of Vagina Factors Affecting Vaginal Absorption Of Drug Properties Of Ideal Vaginal Drug Vaginal Drug Delivery Dosage Forms Vaginal Implants Advantages Of Vaginal Drug Therapy Disadvantages Of Vaginal Drug Therapy Quizzes

3. Introduction 2 In recent years, there is a number of technological advancements in drug delivery due to ongoing issues with patient tolerance of side effects as well as adherence, persistence, and compliance with traditional methods of drug administration. Vaginal drug delivery indicates the administration of medications within the vaginal cavity to produce local or, less frequently, systemic pharmacological effects. The vaginal route remains largely underexplored despite its potential as a non- invasive route.

4. 3 Introdution The vaginal route has been traditionally exploited for the management of local genital conditions such as infections, vaginitis, and labour inducing or prevention purposes. Variety of pharmacologically active substances, including antibacterials, antifungals , antiprotozoals , antivirals, labour inducers, spermicidal agents, and sexual hormones, have been formulated in vaginal dosage forms.

5. The vagina is a muscular canal lined with nerves and mucus membranes connecting the uterus and cervix to the outside of the body, allowing for menstruation, intercourse, and childbirth. Anatomy of vagina can vary, and factors such as age, hormonal changes, and childbirth can impact the structure and function of the vagina. The presence of a dense network of blood vessels in the vagina makes it an excellent route for delivery of both systemic and local therapy. 4 Anatomy Of Vagina

6. 5 Anatomy Of Vagina

7. Vagina receives blood from various arteries, including branches of the internal iliac artery. Blood Supply Nerve endings in the vagina contribute to sexual arousal. Nerve Innervation Length : from 8 to 12 cm. Surface area : from 65 to 105 cm2 . Size Mucosa : The innermost layer is lined with mucous membrane, which keep the vagina moist. This layer also contains rugae (folds) that allow for stretching. Muscularis : The middle layer is composed of smooth muscle fibers that provide the ability for the vagina to contract and expand. Adventitia : The outermost layer connects the vagina to surrounding structures. Structure E xtends from the cervix of the uterus to the external opening, known as the vaginal orifice. Location Vagina 6 Anatomy Of Vagina

8. Physiology Of Vagina 7 VAGINA The healthy female genital tract is acidic (pH 3.5-4.5). The pH is maintained within that range by bacterial conversion of glycogen from exfoliated epithelial cells to lactic acid . pH: The vaginal discharge is a mixture of multiple secretions that collect in the vagina from peritoneal, follicular tubal, uterine, Bartholin's and Skene's glands. Secretions: Low specific activity of different amino peptidases in vagina. Human genital tract has lower enzymatic activity leading to less degradation of protein. Enzymatic Activity:

9. 8 Factors Affecting Vaginal Absorption Of Drug Physical & Chemical Properties Of The Drug: The molecular size, lipophilicity, and ionization state of a drug can impact its ability to penetrate the vaginal mucosa. Small, lipophilic, and non-ionized drugs generally have better absorption. pH Of The Vaginal Environment: The pH of the vagina is slightly acidic, typically ranging from 3.5 to 4.5. The ionization state of drugs can be influenced by the pH of the surrounding environment, impacting their absorption. Menstrual Cycle & Hormonal Influence: The menstrual cycle, regulated by hormonal changes, influences the physiology of the vagina. During the menstrual cycle, the thickness and elasticity of the vaginal walls can vary. Increased estrogen levels contribute to greater blood flow, lubrication, and thickening of the vaginal lining.

10. 9 Factors Affecting Vaginal Absorption Of Drug Inflammatory Conditions : Inflammatory conditions or infections in the vaginal area may alter the permeability of the vaginal mucosa and impact drug absorption. The Microbial Balance: The disruption in microbial balance influences the pH of vagina which can influence drug absorption. Vaginal Fluid Volume & Viscosity: The vaginal fluids volume & viscosity can influence the absorption of drug. This effect vary by the nature of drug and the dosage form.

11. Properties Of Ideal Vaginal Drug 10 Have no adverse effect on coitus. Suitable for application several hours before intercourse. Odorless & colorless. Cause no local irritation. Amenable to use with or without an applicator Not associated with leakage, messiness, or feeling of vaginal fullness.

12. Applications Of Vaginal Drug Delivery Therapy 11 Antiseptic Contraception Hormone replacement therapy. Antiviral Antibacterial Antifungal Personal hygiene Overactive bladder (OAB) syndrome treatment Spermicide Labor inducing Odor elimination

13. 12 Vaginal Drug Delivery Dosage Forms

14. 13 Vaginal Drug Delivery Dosage Forms Examples In Market Main Excipients Dosage Form Crinone ® (Progesterone E.P. 8% ). Gelling agent Humectant Preservative Gel Dalacin ® (Clindamycin 2%) Oily/Aqueous base Emulsifying agent Preservative Cream Betadine ® (Povidone-Iodine 10%) Solubilizer Antioxidant Preservative Solution

15. 14 Vaginal Drug Delivery Dosage Forms Examples In Market Main Excipients Dosage Form Canesten ® (Clotrimazole 500mg) Disintegrant Glidant Anti-adherent Tablet NeoSampoon ® ( Menfegol 60mg) Disintegrant Glidant Foaming agent Foaming Tablet Dicoflor elle med ® (L. Rhamnosus GR-1. + L. Reuteri RC-14.) Disintegrant Glidant Anti-adherent Capsule

16. 15 Vaginal Drug Delivery Dosage Forms Examples In Market Main Excipients Dosage Form VCF ® (Nonoxyl-9) Film former Plasticizer Humectant Adhesive Film Mycoheal ® (Miconazole Nitrate 400mg) Oily/Emulsifying/Aqueous base Antioxidant Preservative Suppository pH-D ® (Boric acid) Propellant Emulsifying agent Foam

17. Vaginal Implants 16 Vaginal Rings Vaginal rings are flexible, circular devices that are inserted into the vagina. They release hormones to prevent pregnancy. The user typically wears the ring for three weeks and then removes it for a week to allow for menstruation. Intra-Uterine Devices IUDs are T-shaped devices inserted into the uterus through the cervix. While they are placed in the uterus, their strings extend into the upper part of the vagina. IUDs are used for long-term contraception. There have hormonal or non-hormonal options.

18. Advantages Of Vaginal Drug Therapy 17 Allow local & systemic effect Avoidance of first pass metabolism & enzymatic degradation in GIT, so high bioavailability & low side effects Permeability to large molecular weight drugs, (ex. peptides & proteins) Rich vascularized area, so rapid action Non-invasive Self insertion and removal, so achieves Patient compliance and convenience

19. Disadvantages Of Vaginal Drug Therapy 18 Gender specific nature, this route is for females only Adverse influence on coitus in sexually active individual, (N.B. Semen pH is slightly alkaline that can affect drug stability) Cultural sensitivity Perceived interference with personal hygiene Physiological factors, such as vaginal pH and the presence of vaginal flora, can impact drug stability and efficacy M enstrual cycle-ass o ciated vaginal changes Local irritation Leakage of drug from vagina

20. Quizzes 19 Choose the correct answer: 1- Ideal vaginal drug therapy should be: A- Neutral. B- Strong Alkaline. C- Slightly Alkaline. D- Slightly Acidic. 2- Contraceptives can be applied through vaginal route in: A- Adhesive Films. B- Vaginal Rings. C- IUDs. D- All of the above. True or False: 1- Vaginal route suitable for high molecular weight drugs. 2- Ideal vaginal drug therapy should be only used with applicator. 3- Oxybutynin as a treatment for OAB syndrome can be formulated in vaginal gel.