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Drawing delivery system of the attention of oral medicine mucoadhesive

1. Introduction

Considerable attention focused in recent years in the delivery across the oral mucosa of drugs that have a high-pass metabolism first (ie mainly metabolized by the liver during the first pass by there and did not penetrate the blood) or degrade in the gastrointestinal tract. transmucosal delivery has also been considered for the treatment of local oral conditions anesthetic1.

Oral administration is the administration desired drug through the oral mucosa of the oral cavity. Contrary to administration of oral medications, which presents an environment opposed to drugs, especially proteins and polypeptides, due to acid hydrolysis and the extensive first pass metabolism, mucosal oral tissues provides an environment much smoother absorption2 drugs. Other routes such as nasal drug ocular, pulmonary, rectal and vaginal, have provided excellent opportunities for the provision of a variety of compounds. However, the mucosa of the oral cavity offers advantages distinct.

mucoadhesive controlled release devices can improve the effectiveness of a drug by maintaining the drug concentration between effective and toxic levels, inhibiting the dilution of the drug in bodily fluids, and allows the selection and location of drug in a given country .3

2. Advantages of Oral Drug Delivery Systems

Benefits of oral administration are known in commerce or in the medical literature. The first known advantage is speed of action. Drugs administered into the blood immediately vestibular after passing the oral mucosa rather than having to be swallowed, and then having to go through the gastrointestinal tract before being absorbed. This rapid action is one of the reasons by which a product commercially available and experimental pain relief were administered orally. The first of these products contain nitroglyerin, and is available as an oral tablet that adheres to the mucosa, which is sold under the brand Nitrogard. Product contains the second non-steroidal anti-inflammatory analgesic diclofenac has been used in experimental pill that adheres to the mucosa mouth. The second advantage of knowing the route is to allow oral administration of drugs that normally can not be given orally. Other unique benefits of oral drugs that exploit these advantages are described below and other drugs that could be administered vestibular exploit the advantages of above two Route4 oral.

Regarding the first advantage, speed of action, refers several classes of drugs have improved efficacy when administered orally. A class of drugs for which the speed action is important and could be placed in general tablet, buccal tablet buccal and inventiveness, in particular, are analgesics, including aspirin, ibuprofen, fenoprofen, sulindac, salsalate, diflunisal, mecleofenamate, naproxen, nabumetone, tolmetin, diclofenac, oxaprozin, indomethacin, ketoprofen, choline salicylate, piroxicam, mefenamic acid, etodolac and ketorolac.

Regarding the second advantage of oral administration, the ability to administer medications that can not be ingested because of the destruction of the drug, there are several medications that can be in this category. Testosterone may be placed in a compressed mouth, and then be administered orally to prevent the destruction through the first-pass metabolism passage. Normally, the metabolism and requires the administration of testosterone by injection or skin patch is used in large scrotum. However, the scrotal patch has a potential drawback of the scrotal skin and causes an increase in the amount of a metabolite of testosterone, dihydrotestosterone 5-alpha that can potentially stimulate prostate hypertrophy.5

Similarly, many drugs affect the liver metabolism of other drugs. This greatly affects would be mitigated by the administration of these drugs in oral form. A class of drugs in this category are drugs that inhibit enzymes metabolised in the liver resulting in increased concentrations of other drugs. Another class of drugs increases the metabolizing enzymes in the liver resulting in decreased concentrations of other drugs. By administering both classes of agents with a tablet mouth would be less effect on the concentration of other drugs, thus avoiding toxic substances, and levels of sub-therapeutic drugs. Drugs in the class of inhibitors of the liver that can be administered via an oral tablet include allopurinol, ketoconazole. Drugs class of inducers of liver enzymes that can be managed by a compressed cabamazepine include oral, phenytoin, glutethimide, primidone, rifampicin and barbiturates such as phenobarbital, pentobarbital, secobarbital,

The third These advantages of oral administration is involved much less exposure and the gastrointestinal tract of the drug compared to oral ingestion. One side effect of many antibiotics is the destruction of the normal gastrointestinal flora resulting in diarrhea and excessive growth of harmful organisms such as C. difficult. Antibiotics to be included in an oral tablet, which have increased security due to the reduction of toxic effects on the intestinal flora, including cephlosporins as cephalexin, cefadroxil, cefaclor, cefamandone, cefuroxime, cefprozil, cefixime, cefpodoxime and loracarbef also penicillins such as penicillin G, penicillin V, cloxacillin, dicloxacillin

The fourth of these advantages of oral administration is that it allows drug to be administered that would otherwise interfere with the absorption of other medications. In particular, iron supplements may be administered by a tablet mouth to prevent many adverse effects on the absorption of other medications such as thyroid hormone.

The fifth of the benefits of oral administration is that it increases the possibility of the drug whose absorption is affected by the presence of food. Tetracyclines, in particular, could be administered orally, avoiding the effects of food in the administration tetracycline, which otherwise complicate the administration of this class of oral antibiotics.

The sixth of these benefits administration orally is that it allows blood lipids such as cholesterol be lowered and modified so as not possible with the ingestion of drugs. The lipids can be incorporated into a buccal tablet. Lipids absorbed by the bypass hepatic metabolism and oral mucosa may interact directly with lipoprotein lipid levels and influencing endogenous blood. Recently, a significant reduction of cholesterol has been demonstrated by implementation of lecithin skin.6

Compared to oral, nasal and rectal medicines, the oral route has advantages such an effective blood supply and relatively low enzymatic activity. In addition, the oral mucosa is easily accessible and acceptable to patients, but allows the patient to interrupt drug administration by simply removing the drug delivery system. On the other hand, the oral route is characterized by certain inherent limitations (characteristics of the mucosal barrier, small area available for absorption the drug, the short residence time of the formulation caused by physiologic referral mechanisms) that must be taken into account in the design of the administration drug orally systems.7

3.3. Factors influencing the mucoadhesive buccal cavity

mucoadhesive characteristics are a factor in both the bioadhesive polymer and the environment in which the polymer resides. A variety of factors that influence the properties of polymers muco-adhesive, such as molecular weight, flexibility, the ability of hydrogen bonding, crosslinking density, charge, concentration and hydration (Swelling) of a polymer, which are briefly discussed below.

3.3.1. polymer-related factors

3.3.1.1. Molecular Weight

In general, it has been shown that the strength of a bioadhesive polymer increases with molecular weight greater than 100,000 August. For example, the direct correlation between the degree of bioadhesive polymer polyoxyethylene and their molecular weight of about of 200000-7000000 was demonstrated by Tiwari et al. 9

3.3.1.2. Flexibility

Bioadhesion begins with the release of polymer chains in the interfacial region. Therefore, it is important that the polymer chains containing a high degree of flexibility to achieve the entanglement desired with the mucus. A recent publication has demonstrated the use of polyethylene glycol linked ()-poly (acrylic acid) hydrogels and their copolymers 10 mucoadhesive properties improved. The interpenetration of the chain has increased has been attributed to the flexibility increased structural polymers in the incorporation of polyethylene glycol (). In general, mobility and flexibility of polymers can be related to its viscosity and diffusion coefficients, thus increasing the flexibility of a polymer leads to a broader network of 11 mucus.

3.3.1.3. The ability of hydrogen bond

Hydrogen bonding is another important factor in a mucoadhesive polymer. Robinson Park and found that mucoadhesive occur, must have wished polymer functional groups capable of forming hydrogen bridges 12. They also confirmed the flexibility of polymers is important for improving the potential of hydrogen bonds. Polymers such as poly (vinyl alcohol), hydroxylated methacrylate, and poly (methacrylic acid) and all copolymers are polymers with good capacity of 13 hydrogen bonds.

3.3.1.4. Density crosslinking

The average size of pores, the average molecular weight of crosslinked polymers and the crosslinking density of the three main parameters structural and attached to a network 11 of polymer. Therefore, it seems reasonable that with increasing density of crosslinking, the diffusion water in the polymer network occurs at a lower rate, which in turn causes inflammation of the polymer and a decrease in the rate of insufficient interpenetration between polymer and mucin 11. Flory 14 reported the general property of polymers, in which the degree of swelling at equilibrium inversely proportional to the degree of crosslinking of a polymer.

3.3.1.5. Load

Some generalizations on the charge bioadhesive polymers have been made previously, when non-ionic polymers seems to suffer a lower level of adherence compared anionic polymers. Peppas and Buri have shown that strong anionic charge in the polymer is one of the characteristics required for mucoadhesive 13. It was shown that certain cationic polymers may demonstrate superior mucoadhesive properties, especially in a neutral or slightly alkali half 15. In addition, some cationic polymers of high molecular weight chitosan as it has been shown to possess good properties adhesive.

3.3.1.6. Concentration

The importance of this factor lies in the development of a strong bond with the mucus, and can be explained by the length of the polymer chain available for penetration into the mucus layer. When the polymer concentration is very low, the number of polymer chains entering per unit volume of mucus is low, and the interaction between the polymer and the mucus is unstable 13. In Generally, the more concentrated polymer would result in a length of chain more widespread and better adhesion. However, for each polymer, exists a critical concentration above which the polymer produced a "Troubled" by the state to a spiral structure significantly. By Therefore, accessibility of the solvent in the polymer decreases, and the penetration of the polymer chain is significantly reduced. Therefore, higher concentrations of polymers does not necessarily improve and, in some cases, have reduced muco-adhesive properties. One studies that address this factor has been shown that high concentrations of flexible polymer films based on polyvinylpyrrolidone or poly (alcohol vinyl) polymer film-not further increase the mucoadhesive properties of polymer 16. Instead, the desired intensity decreased mucoadhesive 16.

3.3.1.7. On hydration (swelling)

Hydration is necessary for a mucoadhesive polymer expansion and create a true "mesh macromolecular" 11 of a sufficient size, and also to encourage mobility within the polymer chains to improve the process of interpenetration between the polymer and mucin. Polymer swelling allows mechanical entanglement exposing the hydrogen bonds bioadhesive sites and / or electrostatic interaction between the polymer and the mucous membranes of the network 11. However, some criticism of the hydration of the polymer mucoadhesive exists when the swelling and the optimum bioadhesion 13.

3.3.2. Environmental factors

The mucoadhesive a polymer depends not only on its molecular properties, but also environmental factors with the polymer. Saliva as a means of solution, affects the polymer behavior. According to the flow of saliva and method for determining the pH of the medium was estimated at between 6.5 and 7.5 17. The residence time dosage forms is limited by the time the turnover of mucin, which were estimated to range between 47 and 270 minutes in rats and 12-24 h at 18 Rights 19.

Movement of oral tissues by eating, drinking and talking, is another concern to take into consideration when designing a dosage form of the oral cavity. The movements within the oral cavity continue even during sleep, and can potentially lead to detachment of the form dosage. Therefore, an optimal time for administration of the dosage form is necessary to avoid many of these factors Obstruction 20.

4. delivery systems for oral drugs

bioadhesive polymers have been widely used in drug delivery systems to ensure retention oral dosage form. bioadhesive polymers are defined as polymers that can adhere to a biological substrate. The term mucoadhesive applies when the substrate is mucosal tissue 21. Different types of polymers have been studied for their potential use as mucoadhesive. This including synthetic polymers, cyanoacrylate monomer _ 22 23 polyacrylic acid, hydroxy propyl methylcellulose, 24 and 25as polymethyl derivatives, and, of course, polymers such as chitosan, hyaluronic acid, 26 and 27. Other synthetic polymers such as polyurethanes, epoxy resins, polystyrene, cement and natural products have also been studied extensively 28. In general, the formulations for to be administered orally should not cause irritation and should be small enough to be flexible enough to be accepted by the patient. These requirements can be met through the use of hydrogels. Hydrogels are hydrophilic matrices are able to swell when placed in an environment aqueous. Generally, hydrogels are closely linked so it will not dissolve in the medium and absorb only water. When Drugs are loaded into these hydrogels, the water is absorbed by the chain relaxation occurs and the polymer matrix drug molecules are released by spaces or channels within the hydrogel network. In a broader sense of the term hydrogel matrices also soluble in water are capable of swell in aqueous media, which include natural gums and cellulose derivatives.

Over the last decades, pharmaceutical, scientists "In the world are trying to explore roads and transmucosal patch as an alternative to injections. Among the various transmucosal sites available, the mucosa the oral cavity is the most convenient and easy access to the site of delivery of therapeutic agents for local and systemic delivery forms dosage of retention, as it spread smooth muscle is relatively immobile, abundant vascularization, rapid recovery time after exposure stress and the total absence of Langerhans cells. Direct access to the general circulation by avoiding internal jugular drug metabolism leading pass metabolism, leading high bioavailability. Moreover, these dosage forms are self-manageable, less expensive and have more respect for the patient. Development dosage form with the optimal pharmacokinetics is a promising area for further research, because it is extremely important and intellectually challenging29.

5. Oral dosage forms mucoadhesive

mucoadhesive oral dosage forms can be classified into three types according to their geometry. Type I is a single layer device with multi-drug output. This type of dosage form suffers from a significant loss of drugs due to ingestion. In device type II, an impermeable backing layer is superimposed over the layer of bioadhesive drug loaded, creating a double-layer and prevent the loss of the drug from the surface top of the dosage form in the oral cavity. Type III is a unidirectional discharge device from which the loss drug is minimal, since the drug is released only on the side adjacent to the oral mucosa. This can be achieved by a coating each side of the dosage form, except what is in contact with the oral mucosa.

oral dosage forms can also be classified as a "reservoir" or "matrix" type. In the type of deposit, an amount too much medication in the reservoir is surrounded by a polymer membrane, which controls the rate of release of drugs. In matrix-type systems, the drug is uniformly dispersed in the polymer matrix and release the drug is controlled by diffusion through the polymer network.

In addition, the mucoadhesive tablet was generally less well tolerated and has caused cases of gastro-intestinal adverse events related to drugs than those observed during the administration of ketoconazole systemic. The authors suggest that this particular dosage form is the first and only choice for topical treatment once per day for this disease 30.

5.1 Oral tablets

Tablets have been explored over the dosage form for oral administration of drugs to date. tablets wounds are small, flat and oval, with a diameter of 5-8 mm 31. Contrary to conventional tablets, buccal mucoadhesive tablets can drink and talk without significant discomfort. Feather, adhere to the mucosa, and remain in office until the dissolution and / or completion of a release. These tablets available are applied at different sites of the oral cavity, including the palate, cheek lining, and between the lip and gum. successive tablets may apply on alternative sides of the mouth. The major drawback of bioadhesive buccal tablets is their lack of physical flexibility, leading to patient compliance for use throughout the term and repeated poor.

Patch 5.2 Oral

The patches are layered consisting of an impermeable layer and the support of a reservoir layer containing drug, which releases the drug in a controlled manner and a bioadhesive surface attachment of the mucosa. Oral examination systems are similar to those used in the transdermal. There are two methods used to prepare adhesive stamps are casting solvent and milling directly. In the process of casting solvent, intermediate sheet is perforated patches were prepared by pouring the solution of the drug and polymer (s) on a sheet of backing layer and allowing the solvent (s) evaporate. In the method of direct treatment, the formulation components are mixed uniformly and compressed to the thickness desired, and patches predetermined size and shape are cut or punched. An impermeable backing layer can also be applied to control the direction of intelligent drug delivery, avoid loss of drugs, and minimize the distortion and disintegration the unit during the period of implementation.

5.3 Oral films

The films are the dosage form more recently developed for oral administration. dental films may be preferable adhesive tablets in terms of flexibility and comfort. In addition, to avoid time relatively short stay of gels in the oral mucosa, which are easy to wash and removed by saliva. In addition, in the case of local delivery of oral diseases, films also help protect the wound surface, helping to reduce pain and treat disease more effectively. An ideal film should be flexible, elastic and soft, but strong enough to withstand breakage due to stress mouth movements. It must also possess good bioadhesive strength to hold the mouth the desired duration of action. Swelling of the film, if it occurs, should not be too long to avoid discomfort.

5.4 gels and ointments Oral

dosage forms of semi-solid, such as gels and ointments, have the advantage of easy dispersion throughout the oral mucosa. However, the dose of medication semi-solid dosage forms may not be as accurate as tablets, patches, or films. retention of gels in the application site has been overcome by the use of bioadhesive formulations. Some bioadhesive polymers, for example, poloxamer 407 32 methylcellulose, sodium carboxy-33, carbomer, hyaluronic acid, xanthan gum, undergo a phase change liquid to semi-solid. This change in viscosity increases, leading to prolonged release and controlled drugs. However, these polymers have been studied for this purpose mainly in ocular drug administration.

Conclusion

The oral mucosa offers several advantages for the controlled release of drugs. The mucosa is well supplied with both vascular and lymphatic drainage, the first-pass metabolism in the liver and presystemic elimination in the gastrointestinal tract is avoided. The area is well suited for restraint and seems to be acceptable to patients. With the formulation and design of the dosage form, the permeability and the environment local mucosa can be controlled and manipulated to accommodate drug permeation. administration of oral medications is a promising area for the administration systemic drug molecule oral drugs and ineffective as an attractive alternative non-invasive delivery of peptide and can be powerful protein. However, the need for oral penetration safe and effective absorption enhancers is essential for a successful future in the field of administration of oral medications. An approach how rational drug design requires an understanding extensive physicochemical and biopharmaceutical properties of drugs and excipients. Advances in methods of calculation and will be useful for experimental shorten the processing time of the design development for clinical use.
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About the Author

Hitesh R. Patel*, Dr. M.M. Patel.
* Dept. of Pharmaceutics and pharmaceutical technology
S.K.Patel College of Pharm. Edu. And Research,
Ganpat Vidyanagar, Kherva-382711, Gujarat, India.



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