This document provides an overview of buccal drug delivery systems. It discusses the concepts, advantages, and disadvantages of buccal drug delivery. Key points include that the buccal mucosa is an ideal site for localized and systemic drug delivery. Advantages include avoidance of first-pass metabolism and selective delivery of peptides/proteins. The document reviews the anatomy and permeability of the oral mucosa, factors affecting transmucosal permeability, and ideal drug candidates. It also discusses mimosa membrane, permeability enhancers, and the mechanisms of mucoadhesion and drug absorption for buccal delivery systems.
Approaches Of Gastro-Retentive Drug Delivery System or GRDDSAkshayPatane
Approaches Of Gastro-Retentive Drug Delivery System
Includes:
Floating and Non-Floating drug delivery system with their subtypes
Like Non-effervescent system, Effervescent system, Raft forming system,
High Density system, Expandable system, Muco-adhesive system,
Super porous hydrogel system and Magnetic Systems, etc.
Description about a type of activation modulated drug delivery system, which a type of control drug delivery system.
Also, give a detailed description about each subclassification.
CrDDS is one which delivers the drug at a predetermined rate, for locally or systematically, for a prolong period of time.
Mucoadhesive drug 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.
Since the early 1980,the concept of Mucoadhesion has gained considerable interest in pharmaceutical technology.
combine mucoadhesive with enzyme inhibitory & penetration enhancer properties & improve the patient complaince.
MDDS have been devloped for buccal ,nasal,rectal &vaginal routes for both systemic & local effects.
Hydrophilic high mol. wt. such as peptides that cannot be administered & poor absorption ,then MDDS is best choice.
Mucoadhesiveinner layers called mucosa inner epithelial cell lining is covered with viscoelasticfluid
Composed of water and mucin.
Thickness varies from 40 μm to 300 μm
General composition of mucus
Water…………………………………..95%
Glycoproteinsand lipids……………..0.5-5%
Mineral salts……………………………1%
Free proteins…………………………..0.5-1%
The mechanism responsible in the formation of mucoadhesive bond
Step 1 : Wetting and swelling of the polymer(contact stage)
Step 2 : Interpenetration between the polymer chains and the mucosal membrane
Step 3 : Formation of bonds between the entangled chains (both known as consolidation stage)
Electronic theory
Wetting theory
Adsorption theory
Diffusion theory
Fracture theory
Advantages over other controlled oral controlled release systems by virtue of prolongation of residence of drug in GIT.
Targeting & localization of the dosage form at a specific site
-Painless administration.
-Low enzymatic activity & avoid of first pass metabolism
If MDDS are adhere too tightlgy because it is undesirable to exert too much force to remove the formulation after use,otherwise the mucosa could be injured.
-Some patient suffers unpleasent feeling.
-Unfortunately ,the lack of standardized techniques often leads to unclear results.
-costly drug delivery system
Transdermal Drug Delivery System (TDDS) is the one of the novel technology to deliver the molecules through the skin for long period of time.
Transdermal Drug Delivery System (TDDS) are defined as self contained, discrete dosage forms which are also known as “patches” 2, 3 when patches are applied to the intact skin, deliver the drug through the skin at a controlled rate to the systemic circulation
This presentation includes introduction, physiology of GIT, factors affecting GRDDS, Advantages and disadvantages, approaches to GRDDS and their mechanism, some of the marketed products using GRDDS mechanism.
Approaches Of Gastro-Retentive Drug Delivery System or GRDDSAkshayPatane
Approaches Of Gastro-Retentive Drug Delivery System
Includes:
Floating and Non-Floating drug delivery system with their subtypes
Like Non-effervescent system, Effervescent system, Raft forming system,
High Density system, Expandable system, Muco-adhesive system,
Super porous hydrogel system and Magnetic Systems, etc.
Description about a type of activation modulated drug delivery system, which a type of control drug delivery system.
Also, give a detailed description about each subclassification.
CrDDS is one which delivers the drug at a predetermined rate, for locally or systematically, for a prolong period of time.
Mucoadhesive drug 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.
Since the early 1980,the concept of Mucoadhesion has gained considerable interest in pharmaceutical technology.
combine mucoadhesive with enzyme inhibitory & penetration enhancer properties & improve the patient complaince.
MDDS have been devloped for buccal ,nasal,rectal &vaginal routes for both systemic & local effects.
Hydrophilic high mol. wt. such as peptides that cannot be administered & poor absorption ,then MDDS is best choice.
Mucoadhesiveinner layers called mucosa inner epithelial cell lining is covered with viscoelasticfluid
Composed of water and mucin.
Thickness varies from 40 μm to 300 μm
General composition of mucus
Water…………………………………..95%
Glycoproteinsand lipids……………..0.5-5%
Mineral salts……………………………1%
Free proteins…………………………..0.5-1%
The mechanism responsible in the formation of mucoadhesive bond
Step 1 : Wetting and swelling of the polymer(contact stage)
Step 2 : Interpenetration between the polymer chains and the mucosal membrane
Step 3 : Formation of bonds between the entangled chains (both known as consolidation stage)
Electronic theory
Wetting theory
Adsorption theory
Diffusion theory
Fracture theory
Advantages over other controlled oral controlled release systems by virtue of prolongation of residence of drug in GIT.
Targeting & localization of the dosage form at a specific site
-Painless administration.
-Low enzymatic activity & avoid of first pass metabolism
If MDDS are adhere too tightlgy because it is undesirable to exert too much force to remove the formulation after use,otherwise the mucosa could be injured.
-Some patient suffers unpleasent feeling.
-Unfortunately ,the lack of standardized techniques often leads to unclear results.
-costly drug delivery system
Transdermal Drug Delivery System (TDDS) is the one of the novel technology to deliver the molecules through the skin for long period of time.
Transdermal Drug Delivery System (TDDS) are defined as self contained, discrete dosage forms which are also known as “patches” 2, 3 when patches are applied to the intact skin, deliver the drug through the skin at a controlled rate to the systemic circulation
This presentation includes introduction, physiology of GIT, factors affecting GRDDS, Advantages and disadvantages, approaches to GRDDS and their mechanism, some of the marketed products using GRDDS mechanism.
UNIT V
Mucoadhesive Delivery Systems:
Mechanism of bioadhesion, mucoadhesive materials, formulation and evaluation of Buccal and Nasal drug delivery systems.
Buccal drug delivery system is part of mucoadhesive drug delivery system and their principal and formulation ,mechanisam of adhesion to mucosa ,use of polymers in BDDS and permiability enhancers and evaluation parameters of buccal tablets and patchs
Avoid first pass effect,
Basic knowledge related to BUCCAL i.e The oral cavity is an attractive site for drug delivery due to ease of administration and avoidance of possible drug degradation in the gastrointestinal tract and first-pass metabolism.
There are four potential regions for drug delivery in the oral cavity, namely buccal, sublingual, palatal, and gingival.
Buccal drug delivery specifically refers to the delivery of drugs within/through the buccal mucosa to affect local/systemic pharmacological actions.
Delivery of drug through buccal mucosa of oral cavity is called BDDS. The buccal mucosa lines the inner cheek
It is placed between the upper gingivae and cheek.
Different Variable and Recent Development in Noval Buccal Drug Delivery Systemijtsrd
The buccal region of the oral cavity is an attractive target for administration of the drug of choice, particularly in overcoming deficiencies associated with the latter mode of administration. Problems such as high first pass metabolism and drug degradation in the gastrointestinal environment can be circumvented by administering the drug via the buccal route. Moreover, rapid onset of action can be achieved relative to the oral route and the formulation can be removed if therapy is required to be discontinued. It is also possible to administer drugs to patients who unconscious and less co operative. To prevent accidental swallowing of drugs adhesive mucosal dosage forms were suggested for oral delivery, which included adhesive tablets, adhesive gels, adhesive patches and many other dosage forms with various combinations of polymers, absorption enhancers. Natural polymers have recently gained importance in pharmaceutical field. Mucoadhesive polymers are used to improve drug delivery by enhancing the dosage form's contact time and residence time with the mucous membranes. Mucoadhesion may be defined as the process where polymers attach to biological substrate or a synthetic or natural macromolecule, to mucus or an epithelial surface. When the biological substrate is attached to a mucosal layer then this phenomenon is known as mucoadhesion. The substrate possessing bioadhesive polymer can help in drug delivery for a prolonged period of time at a specific delivery site. The studies of Mucoadhesive polymers provide a good approach of mucoadhesion and some factors which have the ability to affect the mucoadhesive properties of a polymer. Both natural and synthetic polymers are used for the preparation of mucoadhesive buccal patches. In addition to this, studies have been conducted on the development of controlled or slow release delivery systems for systemic and local therapy of diseases in the oral cavity. Deepak Chandra Sharma | Pranshu Tangri | Sunil Jawla | Ravinesh Mishra "Different Variable and Recent Development in Noval Buccal Drug Delivery System" Published in International Journal of Trend in Scientific Research and Development (ijtsrd), ISSN: 2456-6470, Volume-3 | Issue-5 , August 2019, URL: https://www.ijtsrd.com/papers/ijtsrd18934.pdfPaper URL: https://www.ijtsrd.com/pharmacy/novel-drug-delivery-sys/18934/different-variable-and-recent-development-in-noval-buccal-drug-delivery-system/deepak-chandra-sharma
Development And Evaluation Of Buccal Drug Delivery System For Anti-Anginal Dr...ASHISHKUMARTUDU1
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1. Buccal Drug Delivery System PRESENTED BY DANISH KURIEN M.PHARM FIRST YEAR DEPT. OF PHARMACEUTICS KLE UNIVERSITY’S COLLEGE OF PHARMACY BELGAUM 10/28/2010 1
3. Introduction The Buccal mucosa lines the inner cheek Placed between the upper gingivae and cheek Treat local and systemic conditions An ideal dosage regimen in the drug therapy of any disease. 3
5. Mucoadhesion can also be explained on the basis of molecular interactions composed of attractive (Vander Waal’s, Hydrogen bonding) and repulsive (Electrostatic, steric)forces. Biological membrane- the membrane of internal tract e.g.-GIT, buccal cavity, eye, nose ,vagina ,rectum are covered with a thick gel like structure know as mucin All polymer bind to mucin 5
6. 6 Impermeable membrane (1) Drug polymer layer (2) Mucoadhesive polymer layer (3) (1) (2) Mucous membrane saliva action Results in swelling (1) (2) (3) Mechanism of Absorption from a MucoadhesiveBuccal Drug Delivery System Drug release Attachment Internal jugular vein Bypasses first pass metabolism Systemic circulation Drug Release
7. Mechanism of bioadhesion The bioadhesion mainly depends upon nature of bioadhesive polymer . First stage involves an intimate contact between a bioadhesive & a membrane. Second stage involves penetration of the bioadhesive into tissue. Drug released. Bypasses first pass metabolism Enters systemic circulation. 7
8. Advantages 1.Termination of therapy is possible 2. Permits localization of drug to the oral cavity for extended period of time. 3. Ease of administration 4.Avoids first pass metabolism. 5.Reduction in dose can be achieved 6.Selective use of therapeutic agents like peptides, proteins and ionized species can be achieved. 8
9. 9 7. Drugs which are unstable in acidic environment of stomach or destroyed by the alkaline environment of intestine can be given by this route 8. Administration of drugs with poor bioavailablity 9. It follows passive diffusion. 10. Dissolution of drug is easy unlike in case of rectal and transdermal route.
10. 10 11.Administration of Drugs with short half life. 12. Prolongation of contact time with mucosa. 13.Flexibility in shifting the position of the drug in buccal cavity.
11. Disadvantages 11 1. Over hydration 2. Eating and drinking may become restricted 3. By mistake tablet can be swallowed 4. Saliva takes some drug into git 5.Only drug with small dose requirement can be administered. 6.Drug which irritate mucosa or have a bitter or unpleasant taste or an obnoxious odour cannot be administered by this route 7. Drugs which are unstable at buccal pH cannot be administered by this route. 8. Only those drugs which are absorbed by passive diffusion can be administered by this route
15. Structure of mucous membrane 14 a. Fibrous covering. b. Divided fibers of longitudinal muscular coat c. Transverse muscular fibers d. Submucous or areolar layer. e. Muscularis mucosae f. Mucous membrane, with vessels and part of a lymphoid nodule g. Stratified epithelial lining
20. Transport of Material Across the Oral Mucosa (Transmucosal Permeability) Drugs may cross a cell membrane by Passive diffusion, Facilitated diffusion, Active transport Pinocytosis Factors To Be Considered In The Transmucosal Permeability Liphophilicity of drug Salivary secretion pH of saliva : Around 6 favour absorption Binding to oral mucosa Oral epithelium thickness 18
21. Routes of Drug Transport 19 CELL MEMBRANE Two routes of drug transport :- Paracellular Transcellular Paracellular Route :- Primary route for hydrophilic drugs Intercellular spaces is the preferred route Transcellular Route :- Route for lipophillic compounds Lipophillic drugs passes through lipid rich plasma membranes of the epithelial cells. TRANSCELLULAR PARACELLULAR
22. Ideal Candidates for Buccal Drug Delivery System Molecular size Molecular weight. Drug nature. BuccalpH. Taste Drug should be odourless. Drugs following passive diffusion be used. 10/28/2010 Department Of Pharmaceutics 20
24. The Fluid Mosaic Model is used to describe the interactions of lipids and proteins in biological membranes. Fluid mosaic model is two dimensional model, which depicts a biological membrane composed of a fluid state lipid bilayer embedded with globular integral proteins. The integral membrane protein may also exist as sub-unit aggregates, which span through entire thickness of the lipid bilayer to form a continuous water-filled channels.
25. Permeability Enhancers Definition : Substances added to pharmaceutical formulation in order to increase the membrane permeation rate or absorption rate of coadministered drug. E.g. :By using di- and tri-hydroxy bile salts, the permeability of buccal mucosa to fluorescein isothiocynate (FITC) increased by 100-200 fold compared to FITC alone. Applications -Bioavailability of drugs – 5% - 40% Limitations -Potential membrane damage. 10/28/2010 Department Of Pharmaceutics 23
27. DESIGN OF BUCCAL DOSAGE FORM Matrix type: The Buccal patch designed in a matrix configuration contains drug, adhesive, and additives mixed together Bi-directional patches release drug in both the mucosa and the mouth Drug + Mucoadhesive Matrix …………………………………………………………………. ………………………………………………………………….
28. Contd… Reserviour type: The buccal patch designed in a reservoir system contains a cavity for the drug and additives separate from the adhesive Impermeable backing is applied to control the direction of drug delivery; to reduce patch deformation and disintegration while in the mouth; and to prevent drug loss Backing Layer MucoadhesiveMatrix+Drug ~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~
34. may not be as accurate as from tablets, patches, or films
35.
36. REFERENCES Y.W. Chein , Novel Drug Delivery Systems, 2 nd edition, revised and expanded , Marcel Dekker , Inc. New York , 1992(pg. no. 195 – 224) N.K. Jain , Controlled and Novel drug delivery , CBS Publishers & Distributors, New Delhi, First edition 1997 (reprint in 2001) S.P. Vyas and R.K.Khar, Controlled Drug Delivery, CBS Publishers & Distributors, New Delhi, First edition 1997.pg no. 259- 260