Shah, maliba pharmacy college, ukatarsadia university, gopalvidyanagar, bardoli, dist. Microspheres prepared were found discrete, spherical and free flowing. The purpose of this research was to formulate and systematically evaluate in vitro and in vivo performances of mucoadhesive microspheres of glipizide. Surat gujarat, 394 350, india maliba pharmacy college, ukatarsadia university, gopalvidyanagar, bardoli, dist surat gujarat 394 350 india correspondence. Deshmukh t, deshmukh v, jadhav p, kasat k, and patil r. 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. Mucoadhesive microspheres for gastroretentive delivery of acyclovir. Gastroretentive floating microspheres are lowdensity systems that have. The rate of enrofloxacin released from the chitosan paa microspheres was slower at higher ph. Bharadia, vikram pandya and darshan modi department of pharmaceutics, b. Bioadhesive microspheres for bioavailability enhancement of. Evaluation of mucoadhesive properties of chitosan microspheres. Mucoadhesive drug delivery system copy authorstream.
The microspheres were found spherical and free flowing with emulsion ionic gelation technique with a size range 400600m. The microspheres of chitosan or thiolated chitosan were brown in color. Mucoadhesive microspheres as carriers in drug delivery. Mucoadhesive microspheres provide the ideal topical and oral. Mucoadhesive microspheres for controlled drug delivery. Mucoadhesive microspheres prepared by interpolymer. Mucoadhesive microspheres are anticipated to take up water from the underlying mucosal tissue by absorbing, swelling, and capillary effects, leading to considerable stronger adhesion. 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. Microspheres as a promising mucoadhesive drug delivery. Pdf the aim of this study was to investigate the capabilities of chitosan microspheres as drug carrier system in coformulation with polyvinyl alcohol. Results of preliminary trials indicate that volume of crosslinking agent, time for. Pdf mucoadhesive microspheres of chitosan and polyvinyl. The microsphere of aceclofenac was prepared by owo.
The microspheres exhibits good mucoadhesive properties and showed high drug entrapment efficiency. 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. These, however, do not always meet the exacting standards which modern manufacturing. Thus the mucoadhesive microspheres will provide greater area more contact time as well as control the drug release7. 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. These microspheres are free flowing and roll with practically no friction, that means there is no abrasion, guaranteeing a dust free environment. 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 is used to deliver chemotherapeutic agent to liver tumor. Rosiglitazone release from these mucoadhesive microspheres was slow and extended over 12 h duration of time depending on the composition of. The results of the washoff test indicated that the microspheres had fairly good mucoadhesive properties. Preparation and evaluation of the in vitro drug release. Mucoadhesive microspheres have advantages like efficient absorption and. Mucoadhesive microspheres were formulated by emulsification solvent evaporation method using two polymers such as carbopol 974p, hpmc k100m. Spray drying tenofovir loaded mucoadhesive and phsensitive microspheres.
Drugs like proteins and peptides can also be targeted through this system. Mucoadhesive microspheres as carriers in drug deliver y. The ir spectra of the free drug and the microspheres are recorded. Pdf mucoadhesive microspheres for gastroretentive delivery. Formulation of mucoadhesive microspheres of rosiglitazone.
The interaction was determined by the measurement of mucin adsorbed on the microspheres. Bioadhesives can be defined as natural or synthetic materials capable of adhering to a biological substrate. Formulation and evaluation of mucoadhesive microspheres of tenofovir disoproxil fumarate for intravaginal use. Pdf mucoadhesive microspheres as carriers in drug delivery. Formulation and evaluation of mucoadhesive glipizide microspheres. Optimization of mucoadhesive microspheres of acyclovir by. Mucoadhesive chitosan microsphere formulations need. The yield of mucoadhesive microspheres was in the range of 81. These microspheres are free flowing and roll with practically no friction, that means there is no abrasion, guaranteeing a dust free. Materials used microspheres used usually are polymers.
Used to prepare mucoadhesive drug delivery systems, thickening agent, stabilizer. The physiochemical characteristics of the prepared mucoadhesive microspheres of simvastatin are shown in table no 3. Formulation of mucoadhesive microspheres of piroxicam. Jan 22, 2014 contents of the powerpoint on formulation and evaluation of microspheres include. A wide range of formulations has been proposed for the delivery of small molecules, but comparatively few have found their way onto the market. Microspheres are characteristically free flowing powders consisting of. Harikumar and amanpreet kaur rayat and bahra institute of phamacy, sahauran, kharar, district mohali, punjab.
Mucoadhesion is a topic of current interest in the design of drug delivery systems. 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. Figure 2 ad depict the photomicrographs of microspheres prepared using chitosan, thiolated chitosan, carbopol 71g and methocel k15m. 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. Pdf over the past few decades, the concept of mucoadhesion has gained remarkable interest in the field of pharmaceuticals. Hence in this study, a mucoadhesive microsphere of biopolymer chitosan was formulated with an aim to enhance the efficacy of the drug. Chitosanbased spraydried mucoadhesive microspheres for. One drawback of drugloaded polymeric microspheres is the. Unsurprisingly, the strongest mucoadhesive force would be generated for those microspheres containing 90% ww of chitosan, and the greatest gnp retention rates were 65. 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. Formulation and characterization of polycarbophil coated. This combination is useful to provide a greater surface area.
Formulation development and characterization of naproxen. Microspheres were pale yellow in color, free flowing, spherical, and porous in outline. Microspheres are free flowing powder that consist of p roteins or synthetic polymers that are biodegradable in nature ranging between 1 nmin size. Preparation and characterization of mucoadhesive microcapsules. 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.
Pdf influence of glutaraldehyde on drug release and. Recent advances in mucoadhesive drug delivery system mucoadhesive microspheres. A strong interaction between chitosan microspheres and mucin was detected. The rate of enrofloxacin released from the chitosanpaa microspheres was slower at higher ph. The spraydried mucoadhesive microspheres appeared as fine powder in white color methocel k15m or pale yellow color carbopol 71g. The aim of this present work was to develop prolonged release dosage form to be used for. The different types are therapeutic magnetic microspheres and diagnostic microspheres.
Full text preparation, characterization, and potential application of. So to provide prolonged action glipizide microspheres were prepared by ionic gelation technique using different concentration of mucoadhesive polymers. The literature survey revealed scanty research on mucoadhesive microspheres of pioglitazone, which were. Mucoadhesive microspheres provide good contact of drugs with mucus. Thus the drugs can penetrate the microenvironment created by the. 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. The microspheres were prepared by the wo emulsification solvent evaporation method using mucoadhesive polymers sod. In recent years such mucoadhesive microspheres have been developed for oral, buccal, nasal, ocular, rectal and vaginal for either systemic or local effects. Pegylated chitosan microspheres as mucoadhesive drug.
References powders and granulates free flowing powders and granulates are needed for a variety of industrial processes. Pdf international journal of biopharmaceutics recent. With an overwhelming library of mucoadhesive polymers, one practical way to improve mucoadhesion is chemical modification of existing mucoadhesive polymers. 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. Pdf formulation and evaluation of chitosan microspheres.
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. Formulation and evaluation of clarithromycin microspheres for. 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. Mucoadhesive microspheres for gastroretentive delivery of. Optimization of mucoadhesive microspheres of acyclovir by applying 32 full factorial designc.
In dilute aqueous acidic solution, the free amino groups of chitosan. Natural mucoadhesive microspheres of abelmoschus esculentus. Glipizide microspheres containing chitosan were prepared by simple emulsification phase separation technique using glutaraldehyde as a crosslinking agent. Pdf mucoadhesive microspheres for controlled drug delivery. A focus on mucoadhesive polymers and their application in. This pdf is available for free download from a site hosted by medknow publications. Microspheres as a promising mucoadhesive drug delivery system. Preparation and evaluation of mucoadhesive beadsdiscs of. 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. Adhesion of microspheres to the intestinal mucosa for a prolonged period is. Chitosan microspheres of a small particle size and with good sphericity were prepared by a spraydrying method followed by. Chitosan conjugated dna nanoparticles in gene therapy. Formulation and evaluation of mucoadhesive microspheres of.
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. In vitro and in vivo evaluation article pdf available in the aaps journal 102. The mucoadhesive microspheres were discrete and free flowing. Microspheres are characteristically free flowing powders having particle size ranging. Glipizide is an oral hypoglycemic drug with short halflife. The primary objective using mucoadhesive microspheres is to achieve a substsntial increase in the length of stay of drug in the gi tract 1. The mucoadhesive properties of chitosan microspheres prepared by different method were evaluated by studying the interaction between mucin and microspheres in aqueous solution.
Preparation of mucoadhesive formulations, enhancing the. Contents of the powerpoint on formulation and evaluation of microspheres include. Microspheres are multiparticulate drug delivery systems which are prepared to obtain. 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. Influence of glutaraldehyde on drug release and mucoadhesive properties of chitosan microspheres.
This can be achieved by coupling bioadhesion characteristics to microspheres and developing mucoadhesive microspheres. Preparation of mucoadhesive chitosanpolyacrylic acid. The mucoadhesive microspheres were prepared by interpolymer complexation and solvent diffusion method. In some cases, such as for ocular or vaginal formulations, the delivery system is mechanically attached over the membrane. International journal of pharmacy and pharmaceutical sciences. 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. The resulting microspheres were spherical and free flowing.
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