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International Journal of Pharmacy & Life Sciences Review Article Nagpal et al., 7(5): May, 2016:5080-5088] CODEN (USA): IJPLCP ISSN: 0976-7126 INTERNATIONAL JOURNAL OF PHARMACY & LIFE SCIENCES (Int. J. of Pharm. Life Sci.) Evaluation Parameters of Mucoadhesive Drug Delivery System Garima Saini1, Jaideep Bajaj2, Ravi Dhawan2, Sandeep Rahar3, Manisha Arora3 and Navneet Nagpal1* 1, Department of Pharmaceutics, Khalsa College of Pharmacy, Amritsar, (Punjab) - India 2, Department of Pharmacology, Khalsa College of Pharmacy, Amritsar, (Punjab) - India 3, Department of Pharmaceutical Chemistry, Khalsa College of Pharmacy, Amritsar, (Punjab) - India Abstract 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 / or better therapeutic performance of the drug. Mucoadhesive drug delivery systems are available in the form of tablets, films, patches, and gels for oral,buccal, nasal, ocular, vaginal, rectal and topical routes for both systemic and local effects. This paper lays main emphasis on evaluation parameters of mucoadhesive drug delivery system. This review article presents the theories of mucoadhesion, factors affecting mucoadhesion and techniques for in-vitro and in-vivo evaluation of mucoadhesive dosage forms. Key-Words: Mucoadhesion, polymers, evaluation parameters Introduction The termmucoadhesion (bioadhesion)is used to The epithelia may be either single layered (e.g. the describe adhesion interactions between polymers and stomach, small and large intestine and bronchi) or mucus or mucosal surfaces (Suresh et al., multilayered/stratified (e.g. in the oesophagus, vagina 2013).Mucoadhesive dosage forms may be designed to and cornea) (Boddupalliet al., 2015). The enable prolonged retention at the site of application, mucoadhesive drug delivery system may include the providing a controlled rate of drug release for following systems. improved therapeutic outcome. The mucoadhesive I. Buccal delivery system ability of a dosage form is dependent upon a variety of II. Sublingual Delivery system factors, including the nature of the mucosal tissue and III. Nasal delivery system the physicochemical properties of the polymeric IV. Ocular delivery system. formulation (Muraleedharaet al., 2013).Mucoadhesive V. Gastro Intestinal delivery system. drug delivery systems are available in the form of VI. Vaginal delivery system. tablets, films, patches, and gels for oral, buccal, nasal, VII. Rectal delivery system (Alexander et al., ocular, vaginal, rectal and topical routes for both 2011). systemic and local effects. These are evaluated by ex Factors affecting mucoadhesive drug delivery vivo and in vivo.Mucous membranes (mucosae) are the system moist surfaces, lining the walls of various body cavities There are three factors of mucoadhesion drug delivery such as the gastrointestinal and respiratory tracts (Khan system are:- et al., 2014). They consist of a connective tissue layer Polymer related factors (the lamina propria) above which is an epithelial layer, a) Molecular weight- With the increase in the the surface of which is made moist usually by the molecular weight (MW) of the polymer chain, the presence of a mucus layer. mucoadhesiveness of a polymer becomes significantly increases (Dharmendraet al., 2012). b) Chain length- With the increase in the chain length of the polymers there is an increase in the mucoadhesive property of the polymer (Khan et al., * Corresponding Author 2014). E.mail: [email protected] © Sakun Publishing House (SPH): IJPLS 5080 Review Article Nagpal et al., 7(5): May, 2016:5080-5088] CODEN (USA): IJPLCP ISSN: 0976-7126 c) Spatial arrangement- Spatial conformation of a even though they do not have attractive molecule is also important factor.Besides molecular interaction with mucins(Mythriet al., 2011). weight or chain length, spatial conformation of a c) Contact time- With the initial increase in the molecule is also important. The helical confirmation of contact time there is an increase in the hydration dextran may shield many adhesively active groups of the polymer matrix and subsequent primarily responsible for adhesion, unlike PEG interpenetration of the polymer chains. The polymers which have a linear confirmation. (Nikaljeet physiology of the mucosal layer may vary al., 2012). depending on the patho-physiological nature of d) Flexibility- Flexible polymer chains helps in the the human body (Madhavet al., 2014). better penetration and entanglement of the polymer d) Swelling- Swelling depends both on polymer chains with that of mucosal layer thereby improving concentration and on water presence. When the bioadhesive property. The flexibility of the polymer swelling is too great, decrease in bioadhesion chains is generally affected by the crosslinking (Lahotiet al., 2011). reactions and the hydration of the polymer network. Physiological factors Higher the crosslinking density, lower is the flexibility The physiological factors which play an important role of the polymer chains (Harsulkaret al.,2011). in governing the mucoadhesive property of a polymer e) Hydration of polymer- In addition to the reduced matrix include texture and thickness of mucosa. flexibility of the polymer chains, crosslinking results in a) Mucin Turnover- The mucin turnover is the reduced diffusion of water into the crosslinked expected to limit theresidence time of the polymer matrix. Hence highly crosslinked polymeric mucoadhesive on the mucus layer. No matter how matrix limits the interpenetration of polymer and mucin high the mucoadhesive strength is (Siddhaparaet chains amongst themselves which in turn results in the al., 2011). decrease in the mucoadhesive strength (Trivedi et al., b) Disease state -The physicochemical properties of 2011). the mucus are known to change during disease f) Hydrogen bonding- In general, stronger the conditions such as common cold, gastric ulcers, hydrogen bonding stronger is the adhesion. The ulcerative colitis, etc (Shaikhet al., 2011). functional groups responsible for such kind of Theory of mucoadhesive drug delivery system interaction include hydroxyl, carboxyl and amino The concept of mucoadhesive drug delivery system groups (Gandhi et al.,2011). is based upon the following six theories. g) Charge and degree of ionization of polymer- The Electronic theory presence of charged functional groups in the polymer In the electronic transfer theory, mucoadhesion chain has a marked effect on the strength of the occurs as the result of the transfer of electrons bioadhesion. Anionic polyelectrolytes have been found between mucus and the mucoadhesive platform. to form stronger adhesion when compared with neutral The electronic transfer between two different polymers (Asane., 2007). layers results in the formation of a double-layered h) Polymer concentration- In general, polymer electronic charge at the interface. This theory concentration in the range of 1-2.5 wt % may exhibit suggests that the electrostatic forces are critical in sufficient mucoadhesive property for biomedical generating bond adhesions rather than high joint applications (Shijithet al., 2013). strength (Hägerströmet al., 2003). Environmental factors Adsorption theory Apart from the above-mentioned physico-chemical This theory states that bio adhesion bond formed properties of the polymeric network, various between an adhesive substrate and tissue as a environmental factors also play an important role in mucus is due to vanderwall interactions, hydrogen mucoadhesion. bonds and related forces. Although these forces a) pH-Some studies have shown that the pH of the individually weak, the sheer number of medium is important for the degree of hydration interactions a whole produce intense adhesive of cross link (Rajput et al., 2010). strength (Leeet al., 2000). b) Applied strength- The pressure initially applied Diffusion theory to the mucoadhesive tissue contact site can Interpenetrations and entanglement of bio-adhesive affect the depth of interpenetration. If high polymer chains and mucus polymer chains pressure is applied for a satisfactory longer produced semi permeable adhesive bonds and is period of time polymers become mucoadhesive separated by diffusion theory. It is believed that the bond strength increases with degree of penetration © Sakun Publishing House (SPH): IJPLS 5081 Review Article Nagpal et al., 7(5): May, 2016:5080-5088] CODEN (USA): IJPLCP ISSN: 0976-7126 of the polymer chains in to the mucus layer. Greater the individual surface energy of mucus and Penetration of polymer chains into the mucus device in relation to the interfacial energy, greater is network and vice versa is depends upon the the adhesion work, WA(Andrews et al., 2009). concentration gradients and diffusion coefficients. WA= γA + γB - γAB Interpretation is required to produce an effective Techniques to evaluate mucoadhesion bio adhesion bond, it has not been determined Mucoadhesive polymers and drug delivery systems can exactly, but it is believed to be in the range of 0.2- be evaluated by testing theiradhesion strength by both 0.5μm. ex vivo and in vivo tests. The penetration of depth (l) = (t-Db)1/2 a) Ex vivo Study where, t = time of contact ; Db= diffusion 1. Tensile strength measurement. coefficient of the bio adhesive material in mucus 2. Falling liquid film method (Peppaset al., 1996). 3. Viscometric method. Fracture theory 4. Thumb test This is perhaps the most-used theory in studies on the 5. Colloidal
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