MUCOSAL DRUG DELIVERY SYSTEM Pradip Sontakke

MUCOSAL DRUG DELIVERY SYSTEM

1. MUCOSAL DRUG DELIVERY SYSTEM Presented By: Mr. Pradip F. Sontakke Assistant Professor Dept. of Pharmaceutics SHREE SAMBHAJI COLLEGE OF PHARMACY KHADKUT , NANDED.

2. Table of Content

3. Introduction What is Bioadhesion / Mucoadhesion ? The term bioadhesion implies attachment of a drug carrier system to a specified biological location. The biological surface can be epithelial tissue or it can be the mucus coat on the surface of a tissue. The adhesive attachment of the drug carrier system to a mucous coat/ layer, the phenomenon is referred to as mucoadhesion. A bioadhesive polymer is a synthetic or natural polymer which binds to biological substrates such as mucosal membranes. Such polymers are sometimes referred to as biological ‘glues’ because they are incorporated into drugs to enable the drugs to bind to their target tissues.

4. Mucoadhesive delivery system interact with the mucus layer covering the mucosal epithelial surface, & mucin molecules & increase the residence time of the dosage form at the site of the absorption. Mucoadhesive drug delivery system is a part of controlled delivery system. Combining the mucoadhesive with the enzyme inhibitory and enhances penetration and also improves patient compliance. Introduction

5. ADVANTAGES Enhanced Drug Retention : Mucoadhesive systems can adhere to the mucosal surface, allowing for prolonged drug contact and retention at the site of action. This ensures a sustained release of the drug, reducing the need for frequent dosing. Localized Delivery : By delivering drugs directly to the site of action, mucoadhesive systems can target specific tissues or regions. This targeted approach reduces systemic exposure, minimizing potential side effects and improving therapeutic outcomes. Improved Bioavailability : Mucoadhesive systems can enhance the absorption of poorly water-soluble drugs by increasing their residence time at the absorption site. This can lead to improved bioavailability and therapeutic efficacy. Protection and Healing : Mucoadhesive systems can be used to protect damaged or inflamed mucosal surfaces and promote healing by forming a protective barrier that prevents further irritation and promotes tissue regeneration.

6. 5.Reduced First-Pass Metabolism : By avoiding the gastrointestinal tract and bypassing the hepatic first-pass metabolism, mucoadhesive systems can improve the bioavailability of drugs that are susceptible to extensive metabolism in the liver. 6.Non-Invasive Route : Mucoadhesive drug delivery is often non-invasive, reducing the need for injections and minimizing patient discomfort. This makes them more patient-friendly and convenient. 7.Patient Compliance : The sustained release provided by mucoadhesive systems can lead to improved patient compliance, as patients may need to take medications less frequently compared to conventional dosage forms. 8.Treatment of Localized Conditions : Mucoadhesive systems are particularly useful for treating localized conditions, such as oral ulcers, periodontal diseases, and vaginal infections, where targeted drug delivery is crucial. ADVANTAGES

7. If MDDS are adhere too tightly it exert too much force to remove the formulation after use, otherwise the mucosa could be injured. Medications administered orally do not enter the blood stream. Lack of standardized techniques often lead to unclear results. Costly drug delivery system Some patient suffers unpleasant feeling. Prolongation of residence time. Ulcer causing drugs may precipitate ulcerogenic effect due to increase in residence time. DISADVANTAGES

8. TRANSMUCOSAL PERMEABILITY   Transmucosal permeability refers to the transport of material such as drugs across the oral mucosa. • Transmucosal permeability is a unique approach that aims at delivering the drug systemically through the oral mucosa. • As an alternative to enteral delivery of drugs, this route of drug delivery is less invasive • It doesn't require much technical equipment. • The main consideration with transmucosal delivery is that the absorption via this route is variable. Thus , making it unsuitable for delivering low potent drugs .

9. • Drugs traverse through the oral mucosa by different methods of absorption. Some of the commonly adopted routes are: Passive diffusion - refers to the non - ionic diffusion of drugs from the high concentration to the lower concentration and is the major absorption process. Facilitated diffusion - This is similar to passive diffusion but differs because it uses integral transmembrane proteins to facilitate the transport . Active transport - This transport requires energy for the drug's movement across the oral mucosa. The hydrolysis of ATP often provides the energy. Pinocytosis - In this type of transport, the entire drug molecule is engulfed into the cell as a small vesicle. This process also requires energy in the form of ATP. TRANSMUCOSAL PERMEABILITY Methods of Drug Absorption

10. The following factors must be considered, To ensure that the transmucosal route can successfully deliver a drug. Factors affecting Transmucosal permeability are: Lipophilicity of the drug - The permeability is higher for agents or drugs that are highly lipid. soluble. Salivary secretion - Higher the salivary secretion, the higher the drug's chances of being flushed out. This can lead to incomplete absorption of the drug. The saliva's pH - Absorption is favored when the pH is around 6. Binding to the oral mucosa - Proper binding of the drug carrier to the oral mucosa is essential. It helps permeates the drug across the mucosa to the systemic circulation. Oral epithelium thickness - The permeation rate of the drug from the drug carrier is dependent on the thickness of the oral epithelium. The thicker this layer, the longer the residence time of the drug.

11. FORMULATION CONSIDERATIONS OF THE BUCCAL DELIVERY SYSTEMS Buccal delivery systems refer to the administration of the drugs via the buccal mucosa. The buccal mucosa is the mucosa that lines the inner cheek. Formulations targeting this region are placed in the mouth between the upper gums and the cheek. This mucosa is highly vascularized and is relatively easy to access. The absorption of drugs in this region mainly occurs by passive diffusion into the lipoidal membrane. The various buccal formulations currently available in the market are buccal tablets, buccal patches/films, and buccal gels/ointments.

12. The main factors that must be considered before formulating these buccal delivery systems are : Size of the formulation  – Formulations with a size of 1 to 3 cm and a daily dose of 25 mg or less is preferred. The drug’s molecular weight  – Drugs with high molecular weight cannot readily permeate through the buccal mucosa. Hence low molecular weight drugs are often preferred. To facilitate the delivery of the former, penetration enhancers are used.  Nature of the drug  – Highly lipophilic drugs that can passively diffuse through the buccal mucosa is used while formulating buccal drug delivery systems . The pH of the formulation  – The pH of the carrier used in the system alters the drug’s absorption. Lowering the carrier pH increases some drugs’ absorption, while the opposite is true for other drugs.   

13. Physicochemical characteristics of the drug –  The drug should be odorless and not have an unpleasant taste. Due to the saliva’s washing effect and the mechanical stress, the drugs in these formulations are quickly removed from the oral cavity. Thus, to ensure an optimum therapeutic effect, the formulation must contain an optimum mucoadhesive agent. This helps maintain an intimate and prolonged contact of the formulation with the absorption site for at least 4 to 6 hours.  Excipients used for the formulation of buccal drug delivery Mucoadhesive polymers  – These synthetic or natural polymers interact with the mucosa’s epithelial surface to adhere to the mucosal layer. The commonly used polymers in buccal dry or partially hydrated dosage forms are polyacrylic acid, polyvinyl alcohol, sodium carboxymethyl cellulose, and sodium alginate. Penetration enhancers  – These substances increase the buccal mucosal membrane permeation rate. It also aids the delivery of drugs that have high molecular weight and are easily inactivated. E.g., Sodium laurate , sodium taurocholate , oleic acid, and chitosan , among others. Enzyme inhibitors  – are added to prevent the degradation of the drugs, especially peptides, or by the mucosal enzymes. These inhibitors also improve the drugs’ buccal absorption: Eg . Aprotinin , bestatin , puromycin , and bile salts.

14. THANK YOU SHRI SAMBHAJI COLLEG OF PHARMACY SHAMAL EDUCATIONAL CAMPUS, DEGAON ROAD, KHADKUT, NANDED 8788884756 [email protected]