Shah, maliba pharmacy college, ukatarsadia university, gopalvidyanagar, bardoli, dist. Materials used microspheres used usually are polymers. Pdf over the past few decades, the concept of mucoadhesion has gained remarkable interest in the field of pharmaceuticals. A focus on mucoadhesive polymers and their application in. Bioadhesives can be defined as natural or synthetic materials capable of adhering to a biological substrate. Pdf mucoadhesive microspheres as carriers in drug delivery. Microspheres are free flowing powder that consist of p roteins or synthetic polymers that are biodegradable in nature ranging between 1 nmin size. Natural mucoadhesive microspheres of abelmoschus esculentus.
The microspheres were found spherical and free flowing with emulsion ionic gelation technique with a size range 400600m. 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. Microspheres were prepared by ionic gelation technique using sodium alginate, carbopol 974, and hydroxyl propyl methyl cellulose k15 m hpmc as a mucoadhesive polymers. Thus the drugs can penetrate the microenvironment created by the.
Formulation of mucoadhesive microspheres of piroxicam. Chitosan microspheres of a small particle size and with good sphericity were prepared by a spraydrying method followed by. Jan 20, 2005 the mucoadhesive microspheres were prepared by interpolymer complexation and solvent diffusion method. International journal of pharmacy and pharmaceutical sciences.
Evaluation of mucoadhesive properties of chitosan microspheres. 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. Bioadhesive microspheres for bioavailability enhancement of. The mucoadhesive microspheres were discrete and free flowing. These microspheres are free flowing and roll with practically no friction, that means there is no abrasion, guaranteeing a dust free environment. Thus the mucoadhesive microspheres will provide greater area more contact time as well as control the drug release7. 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. Formulation and evaluation of mucoadhesive glipizide microspheres. 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. The microspheres exhibited good mucoadhesive property in the in vitro washoff test. 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 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. The resulting microspheres were spherical and free flowing.
Formulation and evaluation of mucoadhesive microspheres of tenofovir disoproxil fumarate for intravaginal use. Bharadia, vikram pandya and darshan modi department of pharmaceutics, b. Preparation of mucoadhesive chitosanpolyacrylic acid. 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. Formulation development and characterization of naproxen. Mucoadhesive microspheres provide the ideal topical and oral.
The microspheres exhibits good mucoadhesive properties and showed high drug entrapment efficiency. This can be achieved by coupling bioadhesion characteristics to microspheres and developing mucoadhesive microspheres. Microspheres with exactly the same size circumvents all of the disadvantages that are encountered while using powders and granulates. With an overwhelming library of mucoadhesive polymers, one practical way to improve mucoadhesion is chemical modification of existing mucoadhesive polymers. Pdf influence of glutaraldehyde on drug release and. Mucoadhesive microspheres were formulated by emulsification solvent evaporation method using two polymers such as carbopol 974p, hpmc k100m. Microspheres are multiparticulate drug delivery systems which are prepared to obtain.
Pdf mucoadhesive microspheres of chitosan and polyvinyl. It is used to deliver chemotherapeutic agent to liver tumor. A wide range of formulations has been proposed for the delivery of small molecules, but comparatively few have found their way onto the market. The spraydried mucoadhesive microspheres appeared as fine powder in white color methocel k15m or pale yellow color carbopol 71g. Mucoadhesive microspheres prepared by interpolymer. 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 mucoadhesive microspheres were prepared by interpolymer complexation and solvent diffusion method. Formulation and evaluation of clarithromycin microspheres for. This pdf is available for free download from a site hosted by medknow publications. Formulation and evaluation of mucoadhesive microspheres of ziprasidone hydrochloride for oral controlled release. Preparation of mucoadhesive formulations, enhancing the. The microsphere of aceclofenac was prepared by owo. Pegylated chitosan microspheres as mucoadhesive drug. Mucoadhesive microspheres for gastroretentive delivery of.
These, however, do not always meet the exacting standards which modern manufacturing. Gastroretentive floating microspheres are lowdensity systems that have. Contents of the powerpoint on formulation and evaluation of microspheres include. A strong interaction between chitosan microspheres and mucin was detected. Pdf oral modified or controlled dosage forms have always proven to be more. Surat gujarat, 394 350, india maliba pharmacy college, ukatarsadia university, gopalvidyanagar, bardoli, dist surat gujarat 394 350 india correspondence. Glipizide microspheres containing chitosan were prepared by simple emulsification phase separation technique using glutaraldehyde as a crosslinking agent. Pdf international journal of biopharmaceutics recent. Mucoadhesive microspheres as carriers in drug deliver y. Microsphere are small spherical particles, with diameters in the micrometer range typically 1. The percent swelling of different microsphere formulation was found to follow the rank order 248 18%, 198 15%, 279 26% and 164 15%, respectively. Mucoadhesive drug delivery system copy authorstream.
Drugs like proteins and peptides can also be targeted through this system. One drawback of drugloaded polymeric microspheres is the. Results of preliminary trials indicate that volume of crosslinking agent, time for. Pdf formulation and evaluation of chitosan microspheres. 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. Harikumar and amanpreet kaur rayat and bahra institute of phamacy, sahauran, kharar, district mohali, punjab. The aim of this present work was to develop prolonged release dosage form to be used for. Mucoadhesive microspheres for controlled drug delivery.
Mucoadhesive microspheres as carriers in drug delivery. The present study involves preparation and characterization of mucoadhesive microspheres with famotidine as model drug for prolongation of gastric residence 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. Optimization of mucoadhesive microspheres of acyclovir by applying 32 full factorial designc. Full text preparation, characterization, and potential application of. 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. 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. Recent advances in mucoadhesive drug delivery system mucoadhesive microspheres. 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. The rate of enrofloxacin released from the chitosanpaa microspheres was slower at higher ph. The yield of mucoadhesive microspheres was in the range of 81. Mucoadhesive microspheres for gastroretentive delivery of acyclovir. Preparation and characterization of mucoadhesive microcapsules.
Figure 2 ad depict the photomicrographs of microspheres prepared using chitosan, thiolated chitosan, carbopol 71g and methocel k15m. Preparation and evaluation of mucoadhesive beadsdiscs of. Formulation of mucoadhesive microspheres of rosiglitazone. The literature survey revealed scanty research on mucoadhesive microspheres of pioglitazone, which were. Microspheres prepared were found discrete, spherical and free flowing. Mucoadhesive chitosan microsphere formulations need. Microspheres are characteristically free flowing powders consisting of. This combination is useful to provide a greater surface area. The microspheres of chitosan or thiolated chitosan were brown in color. These microspheres are free flowing and roll with practically no friction, that means there is no abrasion, guaranteeing a dust free. Ph release from these microspheres was slow and extended and dependent on the type of polymer used.
The purpose of this research was to formulate and systematically evaluate in vitro and in vivo performances of mucoadhesive microspheres of glipizide. The different types are therapeutic magnetic microspheres and diagnostic microspheres. 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. Glipizide is an oral hypoglycemic drug with short halflife. 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. Chitosan conjugated dna nanoparticles in gene therapy. The primary objective using mucoadhesive microspheres is to achieve a substsntial increase in the length of stay of drug in the gi tract 1. Microspheres were pale yellow in color, free flowing, spherical, and porous in outline. Spray drying tenofovir loaded mucoadhesive and phsensitive microspheres. Mucoadhesive microspheres provide good contact of drugs with mucus. Adhesion of microspheres to the intestinal mucosa for a prolonged period is. The results of the washoff test indicated that the microspheres had fairly good mucoadhesive properties.
Mucoadhesive microspheres have advantages like efficient absorption and. The mucoadhesive properties of chitosan microspheres prepared by different method were evaluated by studying the interaction between mucin and microspheres in aqueous solution. The rate of enrofloxacin released from the chitosan paa microspheres was slower at higher ph. Influence of glutaraldehyde on drug release and mucoadhesive properties of chitosan microspheres. Pdf mucoadhesive microspheres for gastroretentive 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. Optimization of mucoadhesive microspheres of acyclovir by. Mucoadhesion is a topic of current interest in the design of drug delivery systems. References powders and granulates free flowing powders and granulates are needed for a variety of industrial processes. Rosiglitazone release from these mucoadhesive microspheres was slow and extended over 12 h duration of time depending on the composition of. Microspheres as a promising mucoadhesive drug delivery system. In recent years such mucoadhesive microspheres have been developed for oral, buccal, nasal, ocular, rectal and vaginal for either systemic or local effects.
The ir spectra of the free drug and the microspheres are recorded. Pdf mucoadhesive microspheres for controlled drug delivery. Deshmukh t, deshmukh v, jadhav p, kasat k, and patil r. Hence in this study, a mucoadhesive microsphere of biopolymer chitosan was formulated with an aim to enhance the efficacy of the drug.
The interaction was determined by the measurement of mucin adsorbed on the microspheres. 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 evaluation of the in vitro drug release. The purpose of this research was to prepare spraydried mucoadhesive microspheres for nasal delivery. In dilute aqueous acidic solution, the free amino groups of chitosan. The microspheres were prepared by the wo emulsification solvent evaporation method using mucoadhesive polymers sod. Jan 22, 2014 contents of the powerpoint on formulation and evaluation of microspheres include. So to provide prolonged action glipizide microspheres were prepared by ionic gelation technique using different concentration of mucoadhesive polymers. Chitosanbased spraydried mucoadhesive microspheres for. In some cases, such as for ocular or vaginal formulations, the delivery system is mechanically attached over the membrane. Formulation and characterization of polycarbophil coated. Formulation and evaluation of mucoadhesive microspheres of. Microspheres as a promising mucoadhesive drug delivery.
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