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Development of novel mucoadhesive delivery systems are being undertaken so as to understand the
various mechanism of mucoadhesion and improved permeation of active agents. Peel, shear and
tensile forces can be determined depending on the direction in which the mucoadhesive material is
detached from the biological surface. You can download the paper by clicking the button above. The
mucoadhesive ability of a dosage form is dependent upon a variety of factors, including the nature of
the mucosal tissue and the physicochemical properties of the polymeric formulation. Confocal
microscopy and multi- photon excitation microscopy of human skin in vivo. The Cys-rich sub-
domains are responsible for forming the large oligomers of mucin through disulfide bonds. Plenum
Press, New York, 1995. 49. Denk W. Two-photon excitation in functional biological imaging. J.
Biomed. Optics 1996;1: 296-304. 50. Denk WJ, Strickler JP and Webb WW. Environment-related
factors include pH, initial contact time, swelling and physiological variations. The main advantage of
these systems includes avoiding first pass metabolism of the drugs and hence availability of high
drug concentration at target site. Unless determined otherwise during the investigation, all authors
are deemed to be individually and collectively responsible for the content of a plagiarizing paper.
Larger molecular weight polymers will not hydrate readily to free the binding groups to interact with
a substrate, while lower molecular weight polymers will form weak gels and readily dissolve. Fair
and just food systems enabling local midstream businesses. Polymers are the backbone of a
pharmaceutical drug delivery system as they control the release of the drug from the device. The
release of metoprolol succinate from coated pellets was decreased with increased coating load of
polymer. This process leads to the mixture of formulation and mucus and can thus increase contact
time with the mucous membrane. The substrate possessing bioadhesive property can help in devising
a delivery system capable of delivering a bioactive agent for a prolonged period of time at a specific
delivery site. Mucoadhesive Drug Delivery Systems. Drug Dev Ind Pharm.23(5), 1997,489-515. 41.
Wong CF, Yuen KH, Peh KK. CONCLUSION Mucoadhesive drug delivery system shows
promising future in enhancing the bioavailability and specific needs by utilizing the physiochemical
characters of both the dosage form and the mucosal lining. Novel Mucoadhesion Tests for Polymers
and Polymer-Coated Particles to Design Optimal Mucoadhesive Drug Delivery Systems. Adv. Drug
Del. Rev.;57(11), 2005,1583- 94. 36. Hagerstrom H, Edsman K, Stromme M. The site provides an
opportunity to deliver pharmacologically active agents systemically by avoiding hepatic first-pass
metabolism in addition to the local treatment of the oral lesions. The various sites where
mucoadhesive polymers have played an important role include buccal cavity, nasal cavity, rectal
lumen, vaginal lumen and gastrointestinal tract. Unleashing the Power of AI Tools for Enhancing
Research, International FDP on. In rare cases for which it is extremely difficult to find a second
Reviewers to review the manuscript, or when the one Reviewer’s report has thoroughly convinced
the Editor, decisions at this stage to accept, reject or ask the author for a revision are made on the
basis of only one Reviewer’s report. The editor may confer with other editors or reviewers in making
this decision. They must not be shown to or discussed with others except as authorized by the editor.
Current use of mucoadhesive polymers to increase contact time for a wide variety of drugs and
routes of administration has shown dramatic improvement in both specific therapies and more
general patient compliance. Mucoadhesive polymers that adhere to the mucin-epithelial surface can
be conveniently divided into three broad classes: Polymers that become sticky when placed in water
and owe their mucoadhesion to stickiness. Advantages over other controlled oral controlled release
systems by virtue of prolongation of residence of drug in GIT. But opting out of some of these
cookies may affect your browsing experience. Recently, lectin was used to estimate the ability of a
polymer to mask the surface glycoconjugates and to determine the inhibition of surface-lectin
binding of a biotinylated lectin from Canavalia ensiformis (sword bean).
Mucoadhesion while considering drug delivery is having several merits, because of the ideal
physiochemical characters of the mucosal membrane. In this later case, porcine stomach, intestinal
and buccal mucus were tested, and also jejunum from rabbits. Polymers are used to provide muco-
adhesion of the dosage form, enhancing drug release pattern, solubility and dissolution of
inadequately soluble drugs. As one example to illustrate the improved bioadhesive properties of
thiolated polymers, Bernkop-Schnurch et al. The vaginal and the rectal lumen have also been
explored for the delivery of the active agents both systemically and locally. Upload Read for free
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Scribd. This force, sm, is frequently calculated in tests of resistance to rupture by the ratio of the
maximal detachment force, Fm, and the total surface area, A0, involved in the adhesive interaction.
Out of these, the cookies that are categorized as necessary are stored on your browser as they are
essential for the working of basic functionalities of the website. Bioadhesive Drug Delivery
Systems: Fundamentals, Novel Approaches, and Development. This review article aims to provide
an overview of the various aspects of mucoadhesion, mucoadhesive materials, factors affecting
mucoadhesion, evaluating methods, and finally various mucoadhesive drug delivery systems (buccal,
nasal, ocular, gastro, vaginal, and rectal). Since lectins are found in many species in the plant
kingdom (e.g. tomato, wheat germ, mistletoe), they are not likely to be toxic. A set of conjugated
apertures, one for illumination and one for detection of light function as spatial filters. They must
not be shown to or discussed with others except as authorized by the editor. In case of polymer
attached to the mucin layer of a mucosal tissue, the term mucoadhesion is used. When the biological
substrate is a mucosal layer then the phenomena is known as mucoadhesion. The inhibition of the
major proteolytic enzymes by these polymers is remarkable and represents yet another possible
approach for the delivery of therapeutic compounds, particularly protein and peptide drugs, through
the buccal mucosa. The second is the diffusion of polymer chains in the mucus layer. The difference
in concentration gradient draws the water into the formulation until the osmotic balance is reached.
Cookie Settings Accept All Reject All Privacy Policy Manage consent. The fact that the source
plants can be consumed raw, e.g. tomato fruit, would seem to suggest the safety of lectins. The
present review focuses in detail about various types of mucoadhesive drug delivery systems, polymer
characteristics and theories available to demonstrate mucoadhesion concept. With few exceptions,
however, mucoadhesive drug delivery systems have so far not reached their full potential in oral drug
delivery, because the adhesion of drug delivery systems in the GI tract is in most cases insufficient to
provide a prolonged residence time of delivery systems in the stomach or small intestine 6-8. Real
time video frame can be captured with a low light video camera which in turn can be connected to a
video recorder. That is why the drug delivery system should deliver drug at a state dictated by the
needs of the body over a specified period of treatment. Another example is the clinical application of
mistletoe lectin (Viscum album) for antitumor therapy in rabbits and cancer patients. The substrate
possessing bioadhesive property can help in devising a delivery system capable of delivering a
bioactive agent for a prolonged period of time at a specific delivery site. For linear polymers,
mucoadhesion increases with molecular weight, but the same relationship does not hold for non-
linear polymers. These represent potential sites for attachment of any mucoadhesive system and
hence, the mucoadhesive drug delivery system may include the following33: Gastrointestinal
delivery system, Nasal delivery system, Ocular delivery system, Buccal delivery system, Vaginal
delivery System, Rectal delivery system. The site provides an opportunity to deliver
pharmacologically active agents systemically by avoiding hepatic first-pass metabolism in addition to
the local treatment of the oral lesions. The main prospect of writing this review article is to present
comprehensive information related to mucoadhesion and mucoadhesive drug delivery systems. The
article has highlighted all the aspects of mucoadhesive drug delivery systems which will be helpful
for researches and academics.
The Editor’s decision will be sent to the author with recommendations made by the Reviewers,
which usually includes verbatim comments by the Reviewers. This review article aims to provide an
overview of the various aspects of mucoadhesion, mucoadhesive materials, factors affecting
mucoadhesion, evaluating methods, and finally various mucoadhesive drug delivery systems (buccal,
nasal, ocular, gastro, vaginal, and rectal). Mechanism of mucoadhesion is backed up by ionic bond,
covalent bond, Vander Waal bond and hydrogen bond. Once the material has been accepted for
publication, authors are asked to sign a copyright form verifying that they have the right to publish
the material and that they grant permission to the journal to publish their work online. An in vitro
investigation of mucosa adhesive materials for use in controlled drug delivery. The second is the
diffusion of polymer chains in the mucus layer. However, newer polymers are capable of forming
covalent bonds with the mucus and the underlying cell layers, and hence, exhibit improved chemical
interactions. For example, a partially hydrated polymer can be adsorbed by the substrate because of
the attraction by the surface water24. Semisolid Systems Containing Propolis for the Treatment of
Periodontal Disease: In Vitro Release Kinetics, Syringeability, Rheological, Textural and
Mucoadhesive Properties. When the biological substrate is a mucosal layer then the phenomena is
known as mucoadhesion. Due to the continuous formation of tears and blinking of eye lids there is a
rapid removal of the Page 3. Confocal microscopy and multi- photon excitation microscopy of
human skin in vivo. Although lectins are also found in bacteria, those from the plant kingdom still
remain the largest group of this class. Figure 4: Dehydration theory of mucoadhesion explaining
demonstrating water movement from the mucous region to mucoadhesive dosage form. The main
advantage of this drug delivery system is that it prolongs the residence time of the dosage form at
the site of application. Present and future applications of biomaterials in controlled drug delivery
systems, Biomaterials. 2(4), 1981,201- 14. 31. Park K, Robinson JR. Correlation of Two Bioadhesion
Assays: The Everted Sac Technique and the Cahn Microbalance. J. Control. Rel.61(2), 1999,113-22.
35. Takeuchi H, Thongborisute J, Matsui Y, Sugihara H, Yamamoto HH, Kamashima Y. Out of these,
the cookies that are categorized as necessary are stored on your browser as they are essential for the
working of basic functionalities of the website. Hassan and Gallo reported the rheological method
for mucoadhesion evaluation. We also use third-party cookies that help us analyze and understand
how you use this website. There are many advantages of mucoadhesive buccal drug delivery system
that made this a novel drug delivery system for the local as well as systemic delivery of various
drugs. The ability of bacteria to adhere to a specific target is rooted from particular cell-surface
components or appendages, known as fimbriae that facilitate adhesion to other cells or inanimate
surfaces. Mucoadhesive dosage forms may be designed to enable prolonged retention at the site of
application, providing a controlled rate of drug release for improved therapeutic outcome. Intrinsic
factors of the polymer are related to its molecular weight, concentration and chain flexibility. In vitro
And ex Vivo Intestinal Tissue Models to Measure Mucoadhesion of Poly (Methacrylate) and N-
Trimethylated Chitosan Polymers. Pharm. Res. 2005;22(1): 38-49. 44. Masters BR. Selected Papers
on Confocal Microscopy, SPIE Press, Bellingham, WA, 1996. 45. Barry Masters R, Peter TC. The
important work of Denk, Strickler and Webb which was published in Science in 1990 launched a
new revolution in nonlinear optical microscopy. Bioadhesion can be defined as the process by which
a natural or a synthetic polymer can adhere to a biological substrate. To browse Academia.edu and
the wider internet faster and more securely, please take a few seconds to upgrade your browser. This
parameter has been extensively used as a good indicator of the mucoadhesive properties of a material
and is calculated by the integration of the force vs.
You also have the option to opt-out of these cookies. J Pharm Pharmaceut Sci.1(1) 1998,15-30. 15.
Semalty M, Semalty A, Kumar G. Real time video frame can be captured with a low light video
camera which in turn can be connected to a video recorder. Additionally, an undesirable adhesion in
the esophagus can occur. Application of dosage forms to mucosal surfaces may be of benefit to drug
molecules not amenable to the oral route, such as those that undergo acid degradation or extensive
first-pass metabolism. The sublingual mucosa is relatively more permeable than the buccal mucosa
(due to the presence of large number of smooth muscle and immobile mucosa), hence formulations
for sublingual delivery are designed to release the active agent quickly while mucoadhesive
formulation is of importance for the delivery of active agents to the buccal mucosa where the active
agent has to be released in a controlled manner. However, highly pigmented cells and tissues could
be subjected to photo-induced thermal damage. Unfortunately, TL suffers from cross-reactivity with
mucus glycoprotein, leading to nonspecific binding. Those that meet the editorial policies and a
minimum quality level are normally passed on to at least 2 experts for review. Development of novel
mucoadhesive delivery systems are being undertaken so as to understand the various mechanism of
mucoadhesion and improved permeation of active agents. Here a tungsten or lazer illuminates and
detects the scattered or fluorescent light respectively within the vesicles. Manuscripts rejected at this
stage are insufficiently original, have serious scientific flaws, have poor grammar or English
language, or are outside the aims and scope of the journal. The mucin glycoproteins are the most
important structure-forming component of the mucus gel, resulting in its characteristic gel- like,
cohesive and adhesive properties. Since the early 1980,the concept of Mucoadhesion has gained
considerable interest in pharmaceutical technology. In order for diffusion to occur, it is important that
the components involved have good mutual solubility, that is, both the bio adhesive and the mucus
have similar chemical structures. These are extracellular, long thread like pro-tein polymers of bacteria
that play a major role in many diseases. Each step can be facilitated by the nature of the dosage form
and how it is administered. An in vitro investigation of mucosa adhesive materials for use in
controlled drug delivery. An overview of the last decade’s discoveries on mucoadhesion and
applications of mucoadhesive hydrogels as drug carriers is given. When the biological substrate is a
mucosal layer then the phenomena is known as mucoadhesion. The pH can influence the formation
of ionizable groups in polymers as well as the formation of charges on the mucus surface. To browse
Academia.edu and the wider internet faster and more securely, please take a few seconds to upgrade
your browser. Plenum Press, New York, 1995. 49. Denk W. Two-photon excitation in functional
biological imaging. J. Biomed. Optics 1996;1: 296-304. 50. Denk WJ, Strickler JP and Webb WW.
The general properties of these polymers for purpose of sustained release of chemicals are marginal in
being able to accommodate a wide range of physicochemical drug properties. Revised manuscripts
might be returned to the initial Reviewers who may then request another revision of a manuscript.
For example, hydrogen bonds are the prevalent interfacial forces in polymers containing carboxyl
groups. The present review focuses in detail about various types of mucoadhesive drug delivery
systems, polymer characteristics and theories available to demonstrate mucoadhesion concept. You
can download the paper by clicking the button above. The mechanisms governing mucoadhesion are
also determined by the intrinsic properties of the formulation and by the environment in which it is
applied. Lee, Park, Robinson, 2000 had described that it is unlikely that the mucoadhesion process is
the same for all cases and therefore it cannot be described by a single theory.
This force measured is related to the wettability of the mucin on the polymer surface and
corresponds to the adhesive force between the mucoadhesive polymer and the mucin glycoprotein.
You can download the paper by clicking the button above. Present review work is aimed to explore
the aspects of mucoadhesives, development and evaluation techniques of mucoadhesive
microcarriers that will aid in designing an efficient extended release oral mucoadhesive microcarrier
system. When the biological substrate is a mucosal layer then the phenomena is known as
mucoadhesion. However, the dehydration theory is not applicable for solid formulations or highly
hydrated forms. Factors Affecting Mucoadhesion Several factors have been identified as affecting
the strength of the solid mucoadhesive joint. Rate controlled drug delivery by using rate-
preprogrammed drug delivery sy. The mucoadhesive ability of a dosage form is dependent upon a
variety of factors, including the nature of the mucosal tissue and the physicochemical properties of
the polymeric formulation. The main advantage of these systems includes avoiding first pass
metabolism of the drugs and hence availability of high drug concentration at target site. While
considering a formulation development of mucoadhesive drug delivery dosage form, several
physiological factors also has to be considered at the site of action. The controlled release dosage
form should be tailored so that variations in the components can lead to predictable alterations in the
drug release profiles. Mucoadhesive drug delivery system is a part of controlled delivery system. It is
believed that the adhesion force increases with the degree of penetration of the polymer chains. So,
oral extended release drug delivery system becomes a very promising approach for those drugs that
are given orally but having the shorter half-life and high dosing frequency. Mucoadhesive drug
delivery systems are presently being explored because of their potential advantages including
increased residence time of the drug at the site of application, relatively rapid uptake of the drug into
the systemic circulation, and enhanced bioavailability of the therapeutic agents. These cookies ensure
basic functionalities and security features of the website, anonymously. Mucoadhesive drug delivery
system prolong the residence time of the dosage form at the site of application or absorption and
facilitate an intimate contact of the dosage form with the underline absorption surface and thus
contribute to improved and better therapeutic performance of the drug. Several synthetic and natural
polymers are identified as suitable candidates for mucoadhesive formulation. This potentially results
in an expansion of the spaces between the cells. In this later case, porcine stomach, intestinal and
buccal mucus were tested, and also jejunum from rabbits. The current section of the review will give
an overview of the above-mentioned delivery sites. Studies have shown that the mucoadhesive
properties of polymers containing ionisable groups are affected by the pH of the surrounding media.
The National Collaborating Centre for Methods and Tools Fair and just food systems enabling local
midstream businesses. Using this technique, it is possible to perform a previous evaluation of the
material’s adhesive capacity, evidencing mucoadhesion properties38-41. 3. Imaging methods by
AFM, CFSLM, MPEM Optical microscopes offer insufficient resolution for studying effects at a
molecular level. Download Free PDF View PDF See Full PDF Download PDF Loading Preview
Sorry, preview is currently unavailable. Conclusion: Mucoadhesive drug delivery systems were found
to be the best alternative approaches. Bioinvasive drug delivery systems have been developed based
on this bacterial mechanism, where bacteria could be used as a vehicle to introduce drug compounds
into host cells by means of multiple h1 chain integrin cell receptors, which are a member of the cell
adhesion molecule (CAM) family. Some adhesive systems deliver the drug towards the mucosa only
with an impermeable product surface exposed to the oral cavity which prevents the drug release into
oral cavity. It enlarges more than 109-fold, which enables visualization of isolated atoms and offers a
tridimensional image of the surface. This idealized objective points to the two aspects most important
to drug delivery, namely, spatial placement relates to targeting a drug to a specific organ or tissue
while temporal delivery refers to the control of rate of drug delivery to the target tissue. These are
extracellular, long thread like pro-tein polymers of bacteria that play a major role in many diseases.