MUCOADHESIVE DRUGDELIVERY SYSTEMPresented by:Sonam M.Gandhi1st M.PharmDept. of Industrial Pharmacy
INTRODUCTION Novel drug delivery systems (NDDS) are the system where the man searches for new methods of entry of drugs in to the body in order to show its activity in the body . The new drug delivery systems that have been developed and developing are the mucoadhesive drug delivery systems , drug patches, transdermal patches etc.
DEFINITION Mucoadhesive drug delivery system may be defined as a drug delivery system which utilize property of bioadhesion of certain water soluble polymers which become adhesive on hydration and hence can be used for targeting a drug to a particular region of the body for extended periods of time.
TYPES OF MUCOADHESIVE DRUG DELIVERY SYSTEM ORAL BUCCAL MUCOADHESIVE RECTALVAGINAL OCULAR NASAL
MECHANISM OF MUCOADHESIVE COMPOSITION OF MUCOUS Water > 95% Glycoprotein of high molecular weight Mineral salts – 1% Free salts – 0.5-1%
FACTORS AFFECTING MUCOADHESIVE 1. Polymer related factors i) Molecular weight : ii)Concentration of active polymer iii)Flexibility of polymer chains 2.Environment related factors : i)pH of polymer - substrate interface ii) Applied strength iii) Initial contact time iv)Swelling 3. Physiological factors: i)Disease state
ADVANTAGES First pass elimination associated with oral administration , so increase the bioavaibility and therapeutic activity. Both lipophilic and hydrophilic drug can be permeated. These dosage forms are readily localized in the region applied to improve and enhance the bioavailability of drugs Mucoadhesive dosage forms also prolong the residence time of the dosage form at the site of application and absorption to permit once or twice a day dosing.
DISADVANTAGES Oral ingestions results in more exposure of a drug to the GI tract. One of the side effects of many antibiotics is the destruction of normal GI flora resulting in diarrhea and overgrowth with dangerous organisms such as C. difficile. The absorption of mucoadhesive drugs is adversely affected by the presence of food. Tetracyclines, in particular, complicates the administration of this class of antibiotics via the oral route.
MUCOADHESIVE DOSAGE FORMSMucoadhesive Buccal Films: Mucoadhesive buccal films are most commonly prepared by the solvent casting technique in which various substrates including mercury, Teflon, glass and aluminium are used for film formation. Among these substrates, mercury was found to give best results. Mucoadhesive microspheres: Mucoadhesive microspheres have advantages of efficient absorption and enhanced bioavailability of drugs, a much more intimate contact with the mucus layer, and specific targeting of drugs to the absorption site.Mucoadhesive microparticles: Mucoadhesive microparticles is an improved drug delivery system which are believed to bind to the mucus layer coating the stomach and other regions of the GIT. These mucoadhesive microparticles bind to the mucus layer leading either to slow release into the GIT or direct delivery to the gastrointestinal mucosa.
Mucoadhesive microcapsules:Mucoadhesive microcapsules are a type of controlled-release dosage form.They offer numerous benefits including reducing stress resulting fromrestraint, handling, and dosing and avoiding expensive or difficult drugadministration procedures. They can be used for vaginal administration totreat vaginal infections and to increase patient convenience.Mucoadhesive tablets:Mucoadhesive tablets have been developed to increase the retention of drug inGIT and/or to keep a sustained release of drug towards the medium fromwhere it is constantly removed. Thus, treatment of many diseases is done.Mucoadhesive patches:These mucoadhesive formulations offer many advantages in comparison totraditional treatments and can be proposed as a new therapeutic tool againstdental and buccal diseases and disturbances.
EVALUATION TEST 1)Weight variation 2)Friability 3)Hardness 4)Content uniformity 5) Drug release study of Mucoadhesive tablets 6) Swelling index 7)Water sorption studies 8)Mucoadhesive strength
AIM AND OBJECTIVE DRUG CATEGORY CLASS HALF-LIFE The objective of the study mainly is to Diltiazem Anti-anginal, Calcium 3-4.5 develop, characterize channel hours Anti- and evaluate arrythmiatic blocking agent mucoadhesive Atenolol Anti- B- 6-7 hours dosage forms Hypertensive, adrenergic employing various Anti-anginal blocking agent mucoadhesive Nifedipine Anti- Calcium 2-5 hours polymers for Hypertensive, channel prolonged absorption. Anti-anginal blocking agent The mentioned Captopril Anti- Acetylcholin 2-5 hours Hypertensive e inhibitor drugs are most Anti angial commonly used in the preparation of mucoadhesive drug delivery systems.
Buccal drug delivery system Drug delivery according to membranes of oral cavity:A. Sublingual delivery: The membrane of tongue and the floor of the mouth. Administration of drug via sublingual mucosa to systemic circulation.B. Buccal delivery: The lining of cheek. Administration of drug via buccal mucosa to the systemic circulation. Local delivery : For the treatment of condition of the oral cavity. Eg. Apthous ulcer, fungal condition
ADVANTAGES1. Bypasses the hepatic first pass metabolism and greater bioavailability.2. Delivery device can be made unidirectional: only oral mucosal absorption.3. Buccal mucosa is less prone to damage or irritation than oral mucosa.4. Extent of perfusion is more , therefore quick and effective.5. Nausea and vomiting are greatly avoided. Since the formulation is light: •Less transport cost •Economy of raw material •cheap
DISADVANTAGES1. Relatively smaller area of absorption2. The thickness of delivery system should be limited to a few millimeter in order to avoid inconveniences for patient.3. Part of drug may be dissolve in saliva and may be swallowed.4. Drugs which irritate oral mucosa or have bitter taste cause allergic reaction , discoloration teeth cannot be formulated.5. If formulation contains antimicrobial agents, affect the natural microbial flora of mouth.