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MUCOADHESIVE DRUG
DELIVERY SYSTEM



Presented by:

Sonam M.
Gandhi
1st M.Pharm
Dept. 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            RECTAL
VAGINAL




                                 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. Tetracycline's, in
    particular, complicates the administration of this
    class of antibiotics via the oral route.
MUCOADHESIVE DOSAGE FORMS
Mucoadhesive 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 from
restraint, handling, and dosing and avoiding expensive or difficult drug
administration procedures. They can be used for vaginal administration to
treat vaginal infections and to increase patient convenience.


Mucoadhesive tablets:
Mucoadhesive tablets have been developed to increase the retention of drug in
GIT and/or to keep a sustained release of drug towards the medium from
where it is constantly removed. Thus, treatment of many diseases is done.

Mucoadhesive patches:
These mucoadhesive formulations offer many advantages in comparison to
traditional treatments and can be proposed as a new therapeutic tool against
dental 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
ADVANTAGES
1.   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
DISADVANTAGES
1.   Relatively smaller area of absorption
2.   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.
MUCUS




 EPITHELIUM




   BASAL LAMINA



CONNECTIVE TISSUE
REFERNCES
 1) Advanced in controlled and novel
    drug delivery, By N.K.Jain
 2) www.ualberta.ca/~csps/images
 3) www.drugdeliverytech.com
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Mucoadhesive drug delivery system copy

  • 1. MUCOADHESIVE DRUG DELIVERY SYSTEM Presented by: Sonam M. Gandhi 1st M.Pharm Dept. of Industrial Pharmacy
  • 2. 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.
  • 3. 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.
  • 4. TYPES OF MUCOADHESIVE DRUG DELIVERY SYSTEM ORAL BUCCAL MUCOADHESIVE RECTAL VAGINAL OCULAR NASAL
  • 5. MECHANISM OF MUCOADHESIVE COMPOSITION OF MUCOUS  Water > 95%  Glycoprotein of high molecular weight  Mineral salts – 1%  Free salts – 0.5-1%
  • 6. 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
  • 7. 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.
  • 8. 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. Tetracycline's, in particular, complicates the administration of this class of antibiotics via the oral route.
  • 9. MUCOADHESIVE DOSAGE FORMS Mucoadhesive 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.
  • 10. Mucoadhesive microcapsules: Mucoadhesive microcapsules are a type of controlled-release dosage form. They offer numerous benefits including reducing stress resulting from restraint, handling, and dosing and avoiding expensive or difficult drug administration procedures. They can be used for vaginal administration to treat vaginal infections and to increase patient convenience. Mucoadhesive tablets: Mucoadhesive tablets have been developed to increase the retention of drug in GIT and/or to keep a sustained release of drug towards the medium from where it is constantly removed. Thus, treatment of many diseases is done. Mucoadhesive patches: These mucoadhesive formulations offer many advantages in comparison to traditional treatments and can be proposed as a new therapeutic tool against dental and buccal diseases and disturbances.
  • 11. 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
  • 12. 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.
  • 13. 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
  • 14. ADVANTAGES 1. 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
  • 15. DISADVANTAGES 1. Relatively smaller area of absorption 2. 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.
  • 16. MUCUS EPITHELIUM BASAL LAMINA CONNECTIVE TISSUE
  • 17. REFERNCES 1) Advanced in controlled and novel drug delivery, By N.K.Jain 2) www.ualberta.ca/~csps/images 3) www.drugdeliverytech.com