BUCCAL DRUG DELIVERY SYSTEM, BY DR. UMESH KUMAR SHARMA AND SHYMA MS

1. BUCCAL
DRUG
DELIVERY
SYSTEM
1
By :
Dr. Umesh Kumar Sharma and Shyma M S
Department of Pharmaceutics,
Mar Dioscorus College of Pharmacy,
Alathara, Sreekariyam,
Thiruvananthapuram, Kerala, India
Buccal Drug Delivery System: By- Dr. Umesh Kumar Sharma and Shyma M S

2. INTRODUCTION
• Delivery of drug through buccal mucosa of oral cavity
is called BDDS.
• One of the novel drug delivery system.
• It localises the delivery of drugs to the tissues of the
oral cavity for the treatment of bacterial & fungal
infections as well as periodontal diseases.
• Buccal mucosa lines the inner region of cheeks.
• The product is placed between upper gingiva (gum) &
cheek it delivers the drug to systemic circulation.
2Buccal Drug Delivery System: By- Dr. Umesh Kumar Sharma and Shyma M S

3. 3Buccal Drug Delivery System: By- Dr. Umesh Kumar Sharma and Shyma M S

4. ADVANTAGES
1. Ease of administration & termination.
2. Extinction of therapy in emergency can be
facilitated.
3. Drug release for prolonged period of time.
4. Useful for unconscious and trauma patient’s.
5. High bioavailability.
6. Drugs that are unstable in acidic environment of
stomach can be administered by buccal delivery.
7. Drug absorption by the passive diffusion.
8. Flexibility in physical state, shape, size and surface.
9. Maximized absorption rate due to close contact with
the absorbing membrane.
10. Rapid onset of action.
4Buccal Drug Delivery System: By- Dr. Umesh Kumar Sharma and Shyma M S

5. 11. Avoid first pass metabolism.
12. Fast cellular recovery.
13. In comparison to TDDS mucosal surface do not
have the major barrier layer stratum corneum.
14. Avoid acid/enzyme metabolism.
15. Large surface area with respect to sub- lingual
mucosa.
16. Permeation is faster with respect to skin & TDDS .
DISADVANTAGES
1. Drugs unstable at buccal pH (6.5-7) .
2. Drugs with bitter taste / unpleasant taste / an
obnoxious odor or irritate the mucosa cannot be
administered by this route.
5Buccal Drug Delivery System: By- Dr. Umesh Kumar Sharma and Shyma M S

6. 3. Small dose can only be administered.
4. Drugs absorbed by passive diffusion can only be
administered by this route.
5. Eating and drinking difficulty.
6. Not for children.
7. Less surface area than skin (0.01 sq m vs 100 sq m
for GIT.
8. Salivation & swallowing.
9. Taste of the drug.
10. Less permeable than the small intestine.
11. Movement affect mucoadhesive cell.
12. Salivary erosion & it may enter GIT& choke
esophagus.
6Buccal Drug Delivery System: By- Dr. Umesh Kumar Sharma and Shyma M S

7. PRINCIPLE OF MUCO-ADHESION
• The adhesion of polymer is restricted to the lining of
mucosal surface it is known as muco-adhesion.
• Muco- adhesive controlled release device can improve
the effectiveness of drug by-
* maintaining drug con: between effective & toxic level.
* inhibit dilution of drug in the body fluids.
* allow targeting &localization of drug in the specific site.
• MDDS facilitate the intimate contact with drug &
absorption surface and improve therapeutic
performance.
7Buccal Drug Delivery System: By- Dr. Umesh Kumar Sharma and Shyma M S

8. MECHANISM OF MUCO ADHESION
Divided in to 2 steps:
Contact stage
Consolidation stage
1) Contact stage
• Contact between the muco adhesive & mucus
membrane, with the spreading & swelling of the
formulation.
• Initiating its deep contact with mucus membrane
2) Consolidation stage
• Muco adhesive materials are activated by the presence
of moisture.
• Moisture plasticizes the system.
8Buccal Drug Delivery System: By- Dr. Umesh Kumar Sharma and Shyma M S

9. • It allow the muco adhesive system break free & link up
with weak wander walls & hydrogen bonds.
• This stage explaining by using two theories-
Diffusion theory and Hydration theory
9Buccal Drug Delivery System: By- Dr. Umesh Kumar Sharma and Shyma M S

10. THEORIES OF MUCO ADHESION
Wetting theory
• It apply liquid system
• Measure the affinity to the
surface in order to spread over it.
• Measure the affinity by using
contact angle.
• Low contact angle high affinity.
Diffusion theory
• Describe the inter penetration of the polymer & mucin
chain.
10Buccal Drug Delivery System: By- Dr. Umesh Kumar Sharma and Shyma M S

11. 11
• Sufficient depth to produce a semi permanent adhesive
bond (0.2-0.5) range
• Adhesion force increases the
degree of polymer chain
penetration increases.
• Penetration rate depend on Muco adhesive chain
flexibility, nature, mobility, contact time.
Buccal Drug Delivery System: By- Dr. Umesh Kumar Sharma and Shyma M S

12. Electronic theory
• Describe the adhesion occur by means electron
transfer between the mucus & mucoadhesive system.
• Double layer of electrical charges occur the interface.
12
Fracture theory
• Mechanical measurement of
muco adhesion.
• Determine the force
required to separate 2
surfaces after the adhesion.
• It only focus separation.
• Not focus penetration /
diffusion
Buccal Drug Delivery System: By- Dr. Umesh Kumar Sharma and Shyma M S

13. 13
Adsorption theory-
• Result various surface interaction (10& 20).
• 10-chemisorption (ionic, covalent, metallic bond).
• 20-vanderwalls force, hydrophobic interaction, H-bond.
• It require energy to break bond
Buccal Drug Delivery System: By- Dr. Umesh Kumar Sharma and Shyma M S

14. BASIC COMPONENTS OF BDDS
• Drug substance
• Bio-adhesive polymer
• Backing membrane
• Permeation enhancers
14Buccal Drug Delivery System: By- Dr. Umesh Kumar Sharma and Shyma M S

15. FACTORS AFFECTING MUCOADHESION
a) Polymer related factors
 Molecular weight
 Concentration of active polymer
 Flexibility of polymer chain
 Special confirmation
b) Environment related factors
 PH
 Strength
 Initial contact time
 Selection of the model substrate surface
15Buccal Drug Delivery System: By- Dr. Umesh Kumar Sharma and Shyma M S

16. Method of formulation
The buccal drug formulation should contain
Muco adhesive agent: maintain an intimate & prolonged
contact of the formulation with the absorption site.
Penetration enhancers: improve the drug permeation
across mucosa & epithelial layers.
Enzyme inhibitor: protect the dugs from mucosal enzyme
degradation
Solubility modifiers: enhance poorly soluble drugs
solubility.
16Buccal Drug Delivery System: By- Dr. Umesh Kumar Sharma and Shyma M S

17. NOVEL BUCCAL DOSAGE FORMS
 Buccal adhesive patches
 Semisolids (ointments, gels)
 Tablets
 Films
 Powders
17Buccal Drug Delivery System: By- Dr. Umesh Kumar Sharma and Shyma M S

18. Patches & films
• Laminates consisting of an
impermeable backing layer, a drug
containing reservoir layer, a bio
adhesive surface for muco adhesion.
• Backing layer control the direction of
drug release, prevent drug loss, prevent
deformation.
Eg. : Salbutamol buccal film.
Tablets
• Small ,flat, oval shape
• They soften, adher into the mucosa &
retain the position until dissolution /
Release complete.
Eg.: Metaprolol.
18Buccal Drug Delivery System: By- Dr. Umesh Kumar Sharma and Shyma M S

19. Ointment & gels-
• It consist of finely ground pectin ,gelatine &sodium
carboxy methyl cellulose.
• Dispersed in poly ethylene & mineral oil gel base.
• Which can maintain at its site of application for 15-
1550minutes.
Eg. : Chitosan glutamate buccal hydro gel.
Powder
• HPC & beclo methasone in powder form sprayed into
the mucosa of rat.
• It retain the solution long time in the buccal region.
19Buccal Drug Delivery System: By- Dr. Umesh Kumar Sharma and Shyma M S

20. 20
EVALUATION OF BUCCAL DRUG DELIVERY SYSTEM
Surface pH – Buccal films are kept on the surface of agar
plate for 2 hr. so that it can swell. The surface pH of the film
is than checked using pH paper.
Swelling Index : Weigh the patch individually (W1) Place the
individual patches on agar plate and incubate at 37 C and
examine the change at regular intervals for 3hr. After 3 hr.
take the patch and weigh (W2) and calculate the swelling
index using below mentioned formula-
W2 – W1
SI = X 100
W1
Buccal Drug Delivery System: By- Dr. Umesh Kumar Sharma and Shyma M S

21. Thickness measurements : Thickness of each film
measured at five different locations, using electronic
digital micrometre.
Thermal analysis: This study done y using differential
scanning calorimeter.
Morphological characterisation :This study done by
using electron microscope.
Folding endurance : Determined by folding one patch
at the time with out breaking.
21Buccal Drug Delivery System: By- Dr. Umesh Kumar Sharma and Shyma M S

22. Permeation study:
• Permeation studies should be done using Franz
Diffusion cell using animal buccal mucosal membrane.
The receptor compartment is filled with phosphate
buffer pH 6.8.
• and the hydrodynamics in the receptor compartment is
maintained by stirring with a magnetic bead at 50 rpm.
• Samples are withdrawn at predetermined time
intervals and analyzed for drug content.
22Buccal Drug Delivery System: By- Dr. Umesh Kumar Sharma and Shyma M S

23. 23
By :
Dr. Umesh Kumar Sharma and Shyma M S
Department of Pharmaceutics,
Mar Dioscorus College of Pharmacy,
Alathara, Sreekariyam,
Thiruvananthapuram, Kerala, India