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Transmucosal permeability

Definition

  • The ability of substances to pass across mucous membranes (e.g., oral, nasal, intestinal), which act as barriers yet allow drug passage for systemic or local effects.

Anatomy of Buccal Mucosa:

  • Epidermal Layer: Non-keratinized stratified squamous epithelium allowing for better drug permeability.

  • Rich Blood Supply: Facilitates quick systemic absorption of the drug.

  • Minimal Enzymatic Activity: Reduces the likelihood of drug degradation.

Classification of Transmucosal Drug Delivery

  1. Oral: Sublingual (under tongue) or buccal (cheek pouch).

  2. Nasal: Drug delivered via nasal mucosa.

  3. Pulmonary: Drug delivered to lungs via inhalation.

  4. Rectal: Drug administered into rectum.

  5. Vaginal: Drug administered into the vaginal cavity.

  6. Ocular: Drug applied to the eye.

  7. Otic: Drug delivered to the ear.

Factors Influencing Transmucosal Permeability

  1. Substance Nature: Lipophilic and small molecules permeate more easily.

  2. Mucosal Thickness: Thicker membranes reduce permeability.

  3. Surface Area: Larger areas (e.g., intestines) allow more absorption.

  4. Blood Flow: Higher flow can aid faster absorption.

  5. Tight Junctions: Regulate passage across cells.

  6. pH and Charge: pH affects drug ionization, impacting permeability.

  7. Enzymatic Barriers: Enzymes may break down drugs, reducing absorption.

Advantages of Enhanced Transmucosal Permeability

  • Rapid Action: Quick systemic entry.

  • Avoids First-Pass Metabolism: Prevents liver degradation.

  • Alternative to Injection: Less invasive delivery.

Strategies to Improve Permeability

  1. Penetration Enhancers: Temporarily loosen tight junctions.

  2. Nanocarriers: Liposomes and nanoparticles improve absorption.

  3. Prodrug Approach: Modifies drugs to enhance permeability, converting back to active forms inside the body.


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