1. A
Seminar
On
MUCOADHESIVE DRUD
DELIVERY SYSTEM
Presented By
SONAM M.GANDHI
Department of Industrial Pharmacy
2. INTRODUCTION
DEFINITION:
• It 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.
ADVANTAGES:
• First pass elimination associated with oral
administration , so increase the bioavaibility and
therapeutic activity.
• Both lipophilic and hydrophilic drug can be permeated.
3. TYPES OF MUCOADHESIVE DRUG DELIVERY SYSTEM
ORAL
BUCCAL
VAGINAL MUCOADHESIVE RECTAL
NASAL OCULAR
4. 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
cheeck.
Administration of drug via buccal mucosa
to the systemic circulation.
C. Local delivery:for the treatment of condition of the oral
cavity. Eg. Apthous ulcer, fungal condition
5. ADVANTAGES OF BUCCAL DELIVERY
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.
6. Used in case of unconscious and less co-operative patients.
7. It offers a passive system, which does not require activation and the
therapeutic serum concentration can be achieved rapidly.
•less packing cost
•Less transport cost
8. Since the formulation is light:
•Economy of raw material
•cheap
6. 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.
6. The patient cannot eat or drink or speak.
7. Only those drugs which are absorbed by passive diffusion can be
administered by this route.
8. Drugs which are unstable at buccal pH cannot be administered by
this route.
7. STRUCTURE OF ORAL MUCOSA
Oral cavity containing
The floor of mouth
Buccal mucous
The inner side of lips
The mucous membranes have a total area of 100 cm2
Blood supply to the oral tissue is delivered principally via
the external carotid artery.
The thickness of the epithelium varies considerably
between sites, the mucosa measures 500-800 μm
9. TRANSMUCOSAL PERMEATION
• MECHANISM: Two route involve in drug permeation across epithelial
membrane.
1) Paracellular route 2) Transcellular route
1) Paracellular route:
For hydrophilic compound.
• This compound is difficult to penetrate into the lipopholic cell
membrane
• Intercellular space is preferred route for drug transport
• Drug movement in this route (JH) can be written as:
JH = DH ε CD where ε fraction of surface area of paracellular route
hH DH diffusion coefficient
hH pathlength of paracellular route
CD is the donar side drug concentration
10. 2) Transcellular route:
For lipophilic compound
Drug molecule move across both lipophilic cell membrane and
hydrophilic cytoplasm as well as intercellular space.
The permeability of lipophilic compound across the epithelial cell
membrane is typically high.
Drug flux in transcellular route (JL) can be expressed as:
JL= (1- ε ) DH KP CD
hL
where KP is the partition coefficient between lipophilic and
hydrophilic region,
h L is pathlength of transcellular route.
11. MECHANISM AND KINETIC OF TRANSMUCOSAL PERMEATION
• Determine by using progesterone as the modal lipophilic molecule and
Mannitol as model hydrophilic molecule was studied using mucosal
membrane rabbit
• Both lipophilic and hydrophilic drug are capable of permeating through all
mucosal membranes at zero order kinetic.
• Nasal mucosa showing a significantly higher rate of permiation and a shorter
lag time than that rectal and vaginal mucosae.
The duration of lag time was noted to increase in the order :
Nasal < Rectal < vaginal mucosa
Mucosal membrane Thickness (µm)
Oral mucosa
• Buccal 594
• sublingual 111
Nasal mucosa 53.5
Rectal mucos 175.3
Vaginal mucosa 165.1
12. PERMIATION ENHANCER
Bioavibility
Permeation enhancer are added to increase Absorption rate
Membrane permiation
Enhancer efficasy depends on:
Physicochemical properties of the drug
Administration site
Nature of the vehicle
Enzymatic activity
Lipid composition
Cellular morphology
Potential protein interaction
Membrane thickness
Enhancer use alone or in combination
13. LIST OF MEMBRANE PERMIATION ENHANCER:
a) Bile salt and other steroidal detergent:
Sodium glycocholate
Sodium taurocholate
Saponins
sodium taurodihydrofusidate
Sodium glycodihydrofusidate
c) Other enhancers
b) Surfactants:
Azone
1. Nonnionics: Salicylates
Polysorbat 80 sulfoxides
Sucrose ester
2. Cationic:
Diethyltrimethyl ammonium bromide
3. Anionic
Sodiume lauryl sulphat