Bharadia, vikram pandya and darshan modi department of pharmaceutics, b. This can be achieved by coupling bioadhesion characteristics to microspheres and developing mucoadhesive microspheres. The present study involves preparation and characterization of mucoadhesive microspheres with famotidine as model drug for prolongation of gastric residence time. References powders and granulates free flowing powders and granulates are needed for a variety of industrial processes. Gastroretentive floating microspheres are lowdensity systems that have. Full text preparation, characterization, and potential application of. In some cases, such as for ocular or vaginal formulations, the delivery system is mechanically attached over the membrane. Pegylated chitosan microspheres as mucoadhesive drug. Microsphere are small spherical particles, with diameters in the micrometer range typically 1.
Mucoadhesive microspheres can provide the sustained release of drugs and advantage for pioglitazone hcl in the management of type2 diabetes with a high margin of safety and reduced side effects. Pdf the aim of this study was to investigate the capabilities of chitosan microspheres as drug carrier system in coformulation with polyvinyl alcohol. In recent years such mucoadhesive microspheres have been developed for oral, buccal, nasal, ocular, rectal and vaginal for either systemic or local effects. Pdf mucoadhesive microspheres as carriers in drug delivery. Starch can be used as nasal drug carriers in the form of powder microspheres nanoparticles table 3 among which the degradable starch microspheres dsm, also known as spherexr, is the most widely used and also the first example of mucoadhesive microparticulate nasal delivery system.
Materials used microspheres used usually are polymers. The results of the washoff test indicated that the microspheres had fairly good mucoadhesive properties. Adhesion of microspheres to the intestinal mucosa for a prolonged period is. Pdf mucoadhesive microspheres for gastroretentive delivery. Ph release from these microspheres was slow and extended and dependent on the type of polymer used. Definition mucoadhesive drug delivery system may be defined as a drug delivery system which utilize property of bioadhesion of certain water soluble polymers which become adhesive on hydration and hence can be used for targeting a drug to a particular region of the body for extended periods of time. Such materials can be incorporated in formulations to retain the dosage form at the absorbing epithelial membrane, thereby prolonging drug release and thus decreasing dosage frequency when compared to a more conventional dosage form. Unsurprisingly, the strongest mucoadhesive force would be generated for those microspheres containing 90% ww of chitosan, and the greatest gnp retention rates were 65. Preparation and characterization of mucoadhesive microcapsules. Mucoadhesive microspheres as carriers in drug delivery. With an overwhelming library of mucoadhesive polymers, one practical way to improve mucoadhesion is chemical modification of existing mucoadhesive polymers. Chitosan conjugated dna nanoparticles in gene therapy. The physiochemical characteristics of the prepared mucoadhesive microspheres of simvastatin are shown in table no 3. Optimization of mucoadhesive microspheres of acyclovir by.
Chitosan microspheres of a small particle size and with good sphericity were prepared by a spraydrying method followed by. It is used to deliver chemotherapeutic agent to liver tumor. Microspheres as a promising mucoadhesive drug delivery system. Mucoadhesive microspheres have ability to adheres with gastric mucosa, and thereby they releases drug in continuous manner thus they can be more effective against h.
Microspheres are characteristically free flowing powders consisting of protiens or synthetic polymers which are biodegradable in nature and ideally having a particle size less than 200 m2. One drawback of drugloaded polymeric microspheres is the. The mucoadhesive properties of chitosan microspheres prepared by different method were evaluated by studying the interaction between mucin and microspheres in aqueous solution. Spray drying tenofovir loaded mucoadhesive and phsensitive microspheres. The different types are therapeutic magnetic microspheres and diagnostic microspheres. Pdf influence of glutaraldehyde on drug release and. Jan 20, 2005 the mucoadhesive microspheres were prepared by interpolymer complexation and solvent diffusion method. In other words, the method is based on utilizing the cooperative effect that might be achieved by chemical tethering of a small adhesive moiety to an available mucoadhesive polymer.
Preparation of mucoadhesive formulations, enhancing the. The yield of mucoadhesive microspheres was in the range of 81. Formulation and evaluation of mucoadhesive microspheres of. Jan 22, 2014 contents of the powerpoint on formulation and evaluation of microspheres include. The microspheres were prepared by the wo emulsification solvent evaporation method using mucoadhesive polymers sod. Mucoadhesive microspheres as carriers in drug deliver y. Preparation of mucoadhesive chitosanpolyacrylic acid. Microspheres as a promising mucoadhesive drug delivery. Microspheres are characteristically free flowing powders having particle size ranging. These, however, do not always meet the exacting standards which modern manufacturing. International journal of pharmacy and pharmaceutical sciences.
Mucoadhesive microspheres for gastroretentive delivery of acyclovir. The percent swelling of different microsphere formulation was found to follow the rank order 248 18%, 198 15%, 279 26% and 164 15%, respectively. Formulation and evaluation of mucoadhesive microspheres of ziprasidone hydrochloride for oral controlled release. The microspheres of chitosan or thiolated chitosan were brown in color. The microspheres exhibited good mucoadhesive property in the in vitro washoff test. This pdf is available for free download from a site hosted by medknow publications. Contents of the powerpoint on formulation and evaluation of microspheres include. The rate of enrofloxacin released from the chitosan paa microspheres was slower at higher ph. Preparation and evaluation of the in vitro drug release. The purpose of this research was to formulate and systematically evaluate in vitro and in vivo performances of mucoadhesive microspheres of glipizide. A focus on mucoadhesive polymers and their application in.
Mucoadhesive microspheres are anticipated to take up water from the underlying mucosal tissue by absorbing, swelling, and capillary effects, leading to considerable stronger adhesion. Mucoadhesive chitosan microsphere formulations need. Pdf mucoadhesive microspheres for controlled drug delivery. Pdf oral modified or controlled dosage forms have always proven to be more. Preparation and evaluation of mucoadhesive beadsdiscs of. Mucoadhesive drug delivery systems 3 the contact between the mucoadhesive and the mucous membrane, with spreading and swelling of the formulation, initiating its deep contact with the mucus layer hagerstrom, 2003. Formulation of mucoadhesive microspheres of rosiglitazone. Microspheres with exactly the same size circumvents all of the disadvantages that are encountered while using powders and granulates. Results of preliminary trials indicate that volume of crosslinking agent, time for. Formulation and evaluation of mucoadhesive microspheres of tenofovir disoproxil fumarate for intravaginal use. Thus the drugs can penetrate the microenvironment created by the.
Harikumar and amanpreet kaur rayat and bahra institute of phamacy, sahauran, kharar, district mohali, punjab. The rationale of developing mucoadhesive microspheres are that the formulation will be confined on a biological surface for localized drug delivery and the drug will be released close to the site of action with a consequent enhancement of bioavailability. Mucoadhesive microspheres for gastroretentive delivery of. Mucoadhesive microspheres prepared by interpolymer. The resulting microspheres were spherical and free flowing. Microspheres are characteristically free flowing powders consisting of.
Mucoadhesive drug delivery system copy authorstream. Chitosanbased spraydried mucoadhesive microspheres for. Formulation and characterization of polycarbophil coated. Formulation development and characterization of naproxen. These microspheres are free flowing and roll with practically no friction, that means there is no abrasion, guaranteeing a dust free. It was also observed that alginopectinate microspheres had a better mucoadhesive property table 3 than alginate microspheres, because a combination of both polymers increases the viscosity of the matrix, which helps in increasing adhesion to the intestinal mucosa. Mucoadhesive microspheres for controlled drug delivery. Formulation and evaluation of mucoadhesive glipizide microspheres. A wide range of formulations has been proposed for the delivery of small molecules, but comparatively few have found their way onto the market. Shah, maliba pharmacy college, ukatarsadia university, gopalvidyanagar, bardoli, dist. The spraydried mucoadhesive microspheres appeared as fine powder in white color methocel k15m or pale yellow color carbopol 71g. The present study describes two simultaneous approaches to improve its bioavailability, complexation of rhcl with cyclodextrins, and formulation of mucoadhesive microspheres of the complex using different proportions of carbopol and hpmc.
The interaction was determined by the measurement of mucin adsorbed on the microspheres. The literature survey revealed scanty research on mucoadhesive microspheres of pioglitazone, which were. This combination is useful to provide a greater surface area. Microspheres were pale yellow in color, free flowing, spherical, and porous in outline. Recent advances in mucoadhesive drug delivery system mucoadhesive microspheres. The mucoadhesive microspheres were prepared by interpolymer complexation and solvent diffusion method. Figure 2 ad depict the photomicrographs of microspheres prepared using chitosan, thiolated chitosan, carbopol 71g and methocel k15m. Pdf over the past few decades, the concept of mucoadhesion has gained remarkable interest in the field of pharmaceuticals. Rosiglitazone release from these mucoadhesive microspheres was slow and extended over 12 h duration of time depending on the composition of.
Mucoadhesive microspheres have advantages like efficient absorption and. A strong interaction between chitosan microspheres and mucin was detected. Microspheres prepared with gelatin as the polymer have been found to be highly mucoadhesive and have been used for the controlled release of many drugs. Deshmukh t, deshmukh v, jadhav p, kasat k, and patil r. Pdf international journal of biopharmaceutics recent. Glipizide microspheres containing chitosan were prepared by simple emulsification phase separation technique using glutaraldehyde as a crosslinking agent. Pdf mucoadhesive microspheres of chitosan and polyvinyl.
In vitro and in vivo evaluation article pdf available in the aaps journal 102. The mucoadhesive microspheres were discrete and free flowing. Microspheres were prepared by ionic gelation technique using sodium alginate, carbopol 974, and hydroxyl propyl methyl cellulose k15 m hpmc as a mucoadhesive polymers. Formulation and evaluation of clarithromycin microspheres for. Natural mucoadhesive microspheres of abelmoschus esculentus. Microspheres are multiparticulate drug delivery systems which are prepared to obtain.
Drugs like proteins and peptides can also be targeted through this system. Microspheres prepared from admixtures of gelatin and crosslinked chitosan demonstrated some advantage over that prepared from gelatin alone in terms of better controlled release rate of cemetidine. Mucoadhesive microspheres provide good contact of drugs with mucus. Bioadhesive microspheres for bioavailability enhancement of. The rate of enrofloxacin released from the chitosanpaa microspheres was slower at higher ph. The aim of this present work was to develop prolonged release dosage form to be used for. The microspheres exhibits good mucoadhesive properties and showed high drug entrapment efficiency.
Used to prepare mucoadhesive drug delivery systems, thickening agent, stabilizer. Pdf formulation and evaluation of chitosan microspheres. The microsphere of aceclofenac was prepared by owo. In dilute aqueous acidic solution, the free amino groups of chitosan. Surat gujarat, 394 350, india maliba pharmacy college, ukatarsadia university, gopalvidyanagar, bardoli, dist surat gujarat 394 350 india correspondence. Microspheres composed of hydroxypropyl methylcellulose h, chitosan cs, carbopol 934p cp and various combinations of these mucoadhesive polymers, and maltodextrin m, colloidal silicon dioxide a, and propylene glycol p as filler and shaper, were prepared by spraydrying technique. Evaluation of mucoadhesive properties of chitosan microspheres. Mucoadhesive microspheres exhibit a prolonged residence time at the site of application or absorption and facilitate an intimate contact with the underlying absorption surface and thus contribute to improved andor better therapeutic performance of drugs. Thus the mucoadhesive microspheres will provide greater area more contact time as well as control the drug release7.
Formulation of mucoadhesive microspheres of piroxicam. Optimization of mucoadhesive microspheres of acyclovir by applying 32 full factorial designc. Mucoadhesive microspheres were formulated by emulsification solvent evaporation method using two polymers such as carbopol 974p, hpmc k100m. Mucoadhesion is a topic of current interest in the design of drug delivery systems. Mucoadhesive microspheres provide the ideal topical and oral. Microspheres are free flowing powder that consist of p roteins or synthetic polymers that are biodegradable in nature ranging between 1 nmin size. The microspheres were found spherical and free flowing with emulsion ionic gelation technique with a size range 400600m. In this study, the mucoadhesive biopolymers of chitosan and its derivatives, including high molecular weight, low molecular weight, and carboxylic derivative, were employed as the excipients to prepare spraydried microspheres for the oromucosal drug e.
So to provide prolonged action glipizide microspheres were prepared by ionic gelation technique using different concentration of mucoadhesive polymers. Influence of glutaraldehyde on drug release and mucoadhesive properties of chitosan microspheres. These microspheres are free flowing and roll with practically no friction, that means there is no abrasion, guaranteeing a dust free environment. Microspheres prepared were found discrete, spherical and free flowing.
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