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Dr. Vijaya Khader Former Dean, Acharya N G Ranga Agricultural University Dr Paper No. 1 : Novel Drug Delivery Systems I Module No 7 : Factors affecting mucoadhesion and evaluation techniques Development Team Prof. Farhan J Ahmad Principal Investigator Jamia Hamdard, New Delhi Dr. Vijaya Khader Former Dean, Acharya N G Ranga Agricultural University Dr. Zeenat Iqbal Paper Coordinator Jamia Hamdard, New Delhi Content Writer Dr. Zeenat Iqbal Jamia Hamdard, New Delhi ProfDr. KamlaA K Tiwarey Pathak ContentContent Reviewer PunjabiRajv academy University, of pharmacy, Patiala Mathura Prof. Dharmendra.C.Saxena Dr. Vijaya Khader SLIET, Longowal Dr. MC Varadaraj 1 Pharmaceutical Novel Drug Delivery Systems I sciences Factors affecting mucoadhesion and evaluation techniques Description of Module Subject Name Pharmaceutical Sciences Paper Name Novel Drug Delivery Systems I Module Name/Title Factors affecting mucoadhesion and evaluation techniques Module Id Pre-requisites Objectives Keywords Factors affecting mucoadhesion Polymer related factors 1) Hydrophilicity: Bioadhesive polymers having hydrophilic functional groups, such as carboxyl and hydroxyl interact with the mucosal surface via hydrogen bonding. On contact with the 2 Pharmaceutical Novel Drug Delivery Systems I sciences Factors affecting mucoadhesion and evaluation techniques aqueous media, the polymer swells, resulting in exposure of potential anchor sites. Further, the swollen polymers have got the maximum distance between their chains which leads to greater level of flexibility and penetration of the polymer in the mucosa. 2) Molecular weight: The mucoadhesive ability of the polymer depends on its molecular weight. The bioadhesive force of the polymer increases up to 100,000 with the molecular weight. However, no further enhancement is observed beyond this value. 3) Cross linking and swelling: the density of cross linking density of the polymer is inversely related to its swelling. Low density leads to high degree of swelling and thus larger surface area and better mucoadhesion. It also leads to increased hydration rate and increased flexibility. However increased hydration and swelling may lead to slippery surface of the polymer which may result in its rapid removal from the biological substrate decreasing the retention time. The mucoadhesion can further be increased by including adhesion promoters such as polymers grafted onto the preformed network and free polymer chains. 4) Spatial Conformation: spatial conformation of the polymers determines its adhesive strength. Non-Linear polymers or polymers with helical structure may shield many active groups responsible for adhesion. E.g. dextran despite having a higher molecular weight of 19,500,500 have an adhesive strength similar to PEG with a much lower molecular weight of 200,000. This is because of the helical confirmation of dextran as compared to the linear PEG. 5) Concentration of active polymer: it has been found that the concentration of polymer influences bioadhesion. Beyond an optimum concentration of the polymer, a significant reduction in the bioadhesive capacity is observed. In concentrated solution, the coiled molecules become solvent deprived and the availability of chains to interpenetrate with the mucosal surface becomes less. 3 Pharmaceutical Novel Drug Delivery Systems I sciences Factors affecting mucoadhesion and evaluation techniques This result is mainly applicable to liquid mucoadhesive formulations. However for solid dosage forms such as tablets, higher polymer concentration, results in stronger mucoadhesion. 6) Hydrogen bonding capacity: hydrogen bonding capacity of the polymer is an important factor that determines bioadhesion. The polymers must have functional groups that are able to form hydrogen bond for bioadhesion. Environment related factors 1) pH: The pH at the interface of bioadhesive and the biological surface affects bioadhesion especially in case of bioadhesives with ionizable groups. Several bioadhesives are polyanions possessing carboxylic acid functional groups which are used in drug delivery. If the pH of the microenvironment is more than the pK of the polymer, it will be largely ionized and if the pH is below the pK of the polymer, it will be largely unionized. The maximum bioadhesive strength of poly (acrylic acid) polymers (pK=4-5) is observed around pH 4–5 and decreases gradually when it is above the pH of 6. There are numerous investigations which have shown that the carboxyl groups which are protonated rather than the ionized react with mucin molecules by forming hydrogen bonds with it. 2) Applied strength: For applying a mucoadhesive system, a definite strength is required. Higher shear force may lead to increased interaction and higher bioadhesive strength it affects the interaction of the adhesive with the mucous and hence determines the depth of penetration of the polymeric chains. Also greater the contact time between the mucoadhesive and the mucosal surface greater the swelling and interpenetration of polymer chains. 4 Pharmaceutical Novel Drug Delivery Systems I sciences Factors affecting mucoadhesion and evaluation techniques 3) Moistening: Moistening or wetting is required to allow the mucoadhesive polymer to spread over the mucosal surface and create a macromolecular network of sufficient size for the interpenetration of the polymer and mucin molecules and to increase the mobility of the polymer chains. 4) Presence of metal ions: ionic strength of the surrounding environment affects mucoadhesive bond. Interaction with charged groups of polymers and or mucus can shields the number of interaction sites required for adhesion and tightness of mucoadhesive bonding. However some polymers like gellan are reliant on the presence of divalent cations for in situ gelation. Physiological factors Mucin turnover Physiological conditions such as rate of mucus turnover as in disease state or in the presence of food affects mucoadhesion. Mucosal turn over limits the residence time of the mucoadhesive system resulting in detachment and excretion of mucoadhesive. Thus the contact time of the mucoadhesive with the mucosal surface depends on the turnover rate. In some tissues like oral and vaginal the mucous turnover rate is low as compared to intestines which has a high mucous turnover rate limiting the contact time of the adhesive polymer to not more than a few hours. In addition mucous turnover results in increased amount of soluble mucin molecules which interacts with the mucoadhesives before interacting with the mucosal layer. Disease state The properties of the mucus get changed in various disease conditions such as gastric ulcers, common cold, cystic fibrosis, ulcerative colitis, bacterial and fungal infections of reproductive tract and during inflammatory conditions of the eye. Thus mucoadhesives need to be evaluated used in such conditions. 5 Pharmaceutical Novel Drug Delivery Systems I sciences Factors affecting mucoadhesion and evaluation techniques Rate of renewal of mucoadhesive cells Rate of renewal of mucoadhesive cells varies for different types of mucosal surface and limits the residence time of the bioadhesive on the substrate. Mucosal viscosity Mucosal layer viscosity varies throughout the body, and also in disease states. Low mucus viscosity results in a weak interaction with the mucoadhesive polymer resulting in detachment and poor retention, whereas, a highly viscous mucus layer, such as those thickened due to white blood cell DNA, dead cells and inflammatory mediators restricts the interpenetration and increases the diffusion pathway through which the active agent must pass Tissue movement The movement of tissue in case of liquid and food uptake, speaking, peristalsis affects the retention of mucoadhesive system especially in case of gastroretentive systems. Techniques for the determination of mucoadhesion: The evaluation of bioadhesive properties is a fundamental tool in the development of novel bioadhesive drug delivery systems. The instrumental techniques used for the determination of mucoadhesion are in vitro methods for direct or indirect assessment of mucoadhesion of the system under study and involve the use of various techniques such as texture analysis, AFM (Atomic force microscopy), wetting measurements, rheological measurements and zeta potential measurements. The in vitro/ Ex vivo tests are important in the development of slow (controlled/ sustained) release mucoadhesive systems because they involve studies of mechanical and physical stability, interaction between formulation and mucous 6 Pharmaceutical Novel Drug Delivery Systems I sciences Factors affecting mucoadhesion and evaluation techniques membrane and strength of the bioadhesive bond. The majority of techniques for testing mucoadhesion are in vitro; however some in vivo methods have also been entailed. Since there are no standard apparatus available for bioadhesive strength testing, however a few test methods have been employed: Application of force: The commonly used technique of bioadhesive testing for the determination of force of separation is the application of force perpendicularly to the incised tissue/ adhesive interface, during which a state of tensile stress is established. But during the shear stress, the direction of the force is reoriented so that it acts along the joint interfaces. In both tensile strength and shear stress modes, an equal pressure is distributed across the contact area. Peel test: The aim of a peel test is to determine the adhesive strength of the material or the strength or force of the adhesive bond between two materials. 7 Pharmaceutical
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