In recent years such mucoadhesive microspheres have been developed for oral, buccal, nasal, ocular, rectal and vaginal for either systemic or local effects. The objective of the present study is to design and evaluate mucoadhesive microspheres for oral controlled release. This can be achieved by coupling bioadhesion characteristics to microspheres and developing mucoadhesive microspheres. Pdf influence of glutaraldehyde on drug release and. Drugs like proteins and peptides can also be targeted through this system. B3 1department of pharmaceutics, oil technological research institute, jnt university anantapur, anantapur 515 002, andhra pradesh, india517 583.
Mucoadhesive agents are usually polymers containing hydrogen bonding groups that can be used in wet formulations or in dry powders for drug. Mucoadhesive microspheres containing antihypertensive agent. Mucoadhesive microspheres were formulated by emulsification solvent evaporation method using two polymers such as carbopol 974p, hpmc k100m. The mucoadhesive microspheres of pioglitazone hydrochloride were formulated by orifice ion gelation technique using sodium alginate as a cell forming polymer and by using a natural bioadhesive polymer viz. Thus the drugs can penetrate the microenvironment created by the. Microspheres as a promising mucoadhesive drug delivery. The cross linking polymer sodium alginate and mucoadhesive polymer were soaked in the water for 24 hours. Formulation and evaluation of mucoadhesive glipizide. 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. Stability and mucoadhesive properties of chitosan microspheres for therap eutic gastric application. 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. Rosiglitazone release from these mucoadhesive microspheres was slow and extended over 12 h duration of time depending on the composition of. Mucoadhesive microspheres phd thesis proposal best essay.
Formulation and evaluation of mucoadhesive microspheres of propranolol hydrochloride for sustained drug delivery akash yadav and dinesh kumar jain department of pharmaceutics, college of pharmacy, indore professional studies ips academy, knowledge village, agrabombay road, rajendra nagar, indore madhya pradesh452012, india. Influence of glutaraldehyde on drug release and mucoadhesive properties of chitosan microspheres article pdf available in carbohydrate polymers 362. The core material simvastatin, 2 g was added to the polymer. Bioadhesive microspheres for bioavailability enhancement of. Pdf mucoadhesive microspheres as carriers in drug delivery. Mucoadhesive microspheres are anticipated to take up water from the underlying mucosal tissue by absorbing, swelling, and capillary effects, leading to considerable stronger adhesion. Microspheres are made from polymeric, waxy or protective materials that is biodegradable synthetic polymers and modified natural products. Formulation development and characterization of naproxen. 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. The prepared mucoadhesive microspheres were subjected for evaluation of various parameters like production yield, particle size, encapsulation efficiency, mucoadhesion test and in vitro dissolution profile studies. Formulation and evaluation of chitosan microspheres containing isoniazid.
The microspheres exhibited good mucoadhesive property in the in vitro washoff test. The composition of irbesartan mucoadhesive microspheres shown in table 1. A well designed controlled drug delivery system can overcome some of the problems of conventional therapy and enhance the therapeutic efficacy of a given drug. The interaction was determined by the measurement of mucin adsorbed on the microspheres. Mucoadhesive microspheres, amoxicillin trihydrate, eudragit, angle of repose, characterizationkeywords. Formulation and in vitro evaluation of acyclovir mucoadhesive. Mtr studies conducted using a frog palate, suggested that ha and hach microspheres were the most mucoadhesive formulation.
Natural polymer based mucoadhesive hydrogel beads of. Formulation and evaluation of mucoadhesive glipizide microspheres. The pure drug such as clopidogrel was dissolved in 10 ml of water and mixed with the above polymer mixture. Development of floatingmucoadhesive microsphere for site. It is used to deliver chemotherapeutic agent to liver tumor. Formulation and evaluation of controlledrelease of. Obtained microspheres were characterized for particle size, surface morphology, entrapment efficiency, drug loading, in vitro drug release and zeta potential.
Mucoadhesive microspheres may be an effective strategy for the development of easy, reproducible and cost effective method for safe and effective oral drug therapy. Weigh amount chitosan and 150 mg of drug was dissolved in 15 ml 5% acetic acid. The purpose of this research was to formulate and systematically evaluate in vitro and in vivo performances of mucoadhesive microspheres of glipizide. Drug action can be improved by developing new drug delivery system, such as the mucoadhesive microsphere drug delivery system 5,6. Mucoadhesive properties were examined by a texture analyser and three types of adhesive layers gelatine discs, mucin gel and porcine stomach mucosa. Formulation and evaluation of invitro characterization of. Results of preliminary trials indicate that volume of crosslinking agent, time for. Preparation and evaluation of chitosan microspheres. Microspheres, in general, have the potential to be used for targeted and controlled release drug delivery. University of baroda, fatehgunj, baroda390002, gujarat, india. Polyurethene, ureaformaldehyde, pmma, polystyrene 10 15 20 ncy % 0.
International journal of engineering science and technology vol. Chitosanbased mucoadhesive microspheres of clarithromycin as a delivery system for antibiotic to stomach volume. Microspheres are manufactured in both solid and hollow form. Mucoadhesive microspheres as carriers in drug delivery. The microspheres were prepared by the wo emulsification solvent evaporation method using mucoadhesive polymers sod. Mucoadhesivetopenetrating controllable peptosomesin. The results of the washoff test indicated that the microspheres had fairly good mucoadhesive properties. Alginate gastroretentive microspheres containing metronidazole were prepared by ionic gelation method using sodium bicarbonate as gas forming agent, guar gum as mucoadhesive polymer, and eudragit l100 as. The purpose of this study was to develop and evaluate metronidazole loaded floating mucoadhesive microsphere for sustained drug release at the gastric mucosa. The literature survey revealed scanty research on mucoadhesive microspheres of pioglitazone, which were. Preparation of mucoadhesive microspheres the mucoadhesive micrrospheres were prepared by the ionic gelation method.
Formulation and evaluation of mucoadhesive microspheres of. 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. Pdf effect of chitosan molecular weight and composition. The particles prepared by the onestep method gave approximately the same particle size and drug content as those prepared by the twostep method p mucoadhesive microparticles. A more specific term than bioadhesion is mucoadhesion. Original article formulation and evaluation of invitro characterization of gastic mucoadhesive microparticlesdiscs containing metformin hydrochloride fatemeh khonsaria, parvin zakerimilanib,c and mitra jelvehgarid,b astudent research committee, tabriz university of medical sciences, tabriz, iran. Microsphere are small spherical particles, with diameters in the micrometer range typically 1.
Preparation and characterization of mucoadhesive microspheres. The release of drug from both biodegradable as well as nonbiodegradable microspheres is influenced by structure or micromorphology of the carrier and the properties of the polymer itself. Vishnubhai patel 2, jayvadan patel 3 and ravi patel 3 1 research scholar in jjt university, jhunjhunu, rajasthan, india 2 apmc college of pharmacy, himmatnagar, gujarat, india. Glipizide microspheres containing chitosan were prepared by simple emulsification phase separation technique using glutaraldehyde as a crosslinking agent. Formulation development and characterization of naproxen sodiumloaded mucoadhesive microspheres saravana kumar. Microspheres as a promising mucoadhesive drug delivery system. Mucoadhesive drug delivery system copy authorstream. Mucoadhesive microsphere application of mucoadhesive microspheres to mucosal tissues causes localized effect, prolong release of drug. Mucoadhesivetopenetrating controllable peptosomesin microspheres coloaded with antimir31 oligonucleotide. Crosslinked mucoadhesive microspheres based on anionic heteropolysaccharide for nasal delivery of felodipine. The present study aims to provide an overview of various aspects of mucoadhesive microsphere based on various polymers, methodology of preparation of. This combination is useful to provide a greater surface area. Galactomannan gum coated mucoadhesive microspheres of. The resulting microspheres were spherical and free flowing.
Sep 30, 2014 formulation and evaluation of microspheres 1. The different types are therapeutic magnetic microspheres and diagnostic microspheres. In turbidimetric titration, a polymer with high affinity to mucin forms aggregates easily, which can be quantitatively determined by light scattering at 600 nm a 600. Nl number of microspheres leached out in vitro drug release study1517 in vitro drug release studies were performed on the beads, using a dissolution apparatus uspxxiii, electro lab, mumbai. Mucoadhesive microspheres, in general, have the potential to be used for controlled release drug delivery, but coupling of mucoadhesive properties to microspheres has additional advantages, e. Mucoadhesive microparticles is an improved drug delivery system which are believed to bind to the mucus layer coating the stomach and other regions of the git.
A strong interaction between chitosan microspheres and mucin was detected. Preparation and in vitro evaluation of mucoadhesive. Process for preparation of microcapsules and microspheres 67. Formulation and invitro evaluation of mucoadhesive floating microspheres of repaglinide using solvent evaporation method k. Mucoadhesive drud delivery system linkedin slideshare. Chitosanbased mucoadhesive microspheres of clarithromycin. E4955 february 2005 with 294 reads how we measure reads.
Turbidimetric titration method was used to compare the mucoadhesive properties of the polymers. Gastroretentive floating microspheres are lowdensity systems that have. Formulation of mucoadhesive microspheres of rosiglitazone maleate. Alginate microspheres obtained by the spray drying. International journal for pharmaceutical research scholars, 20. Pdf formulation and evaluation of chitosan microspheres. The purpose of the research was to formulate microspheres of acyclovir acv using mucoadhesive polymers, sodium alginate and chitosan. Mucoadhesive microspheres provide good contact of drugs with mucus. Mucoadhesive microspheres have advantages such as efficient absorption and enhanced bioavailability of drugs owing to a high surfacetovolume ratio, much more intimate contact with mucus layer, and specific targeting of drugs to absorption site rao and sharma, 1997, lehr et al.
Pesquisaresearch development, optimization and evaluation of alfuzosin hcl mucoadhesive microspheres recebido em 21112012 aceito em 420 hitesh patel 1. Preparation and in vitro evaluation of mucoadhesive chitosan microspheres of amlodipine besylate for nasal administration s. The present study involves preparation and characterization of mucoadhesive microspheres with famotidine as model drug for prolongation of gastric residence time. This test was done with the help of usp disintegration apparatus in which beaker contained 1. Vara lakshmi faculty of pharmaceutical sciences, rajiv gandhi college of pharmacy, rajahmundry, east godavari, andhra pradesh, india. Facile control of the ph of the mucin and mucoadhesive polymer solutions is one advantage of the turbidimetric titration method. Nine formulations were developed with varying concentration of polymers. Evaluation of irbesartan mucoadhesive microspheres. The aim of this work was to design a controlledrelease drugdelivery system for the angiotensinii receptor antagonist drug telmisartan. Murthy pharmacy department, faculty of technology and engineering, m. Mucoadhesive topenetrating controllable peptosomesin microspheres coloaded with antimir31 oligonucleotide and curcumin for targeted colorectal cancer therapy. The mucoadhesive property of the microspheres was evaluated by in vitro adhesion testing methods called invitro wash off test. Formulation and evaluation of mucoadhesive buccal tablets of.
Adhesion of a matter to this layer is hence called mucoadhesion. Solid biodegradable microspheres incorporating a drug. Formulation and evaluation of mucoadhesive micropsheres of. The percent swelling of different microsphere formulation was found to follow the rank order 248 18%, 198 15%, 279 26% and 164 15%, respectively. The tablets were prepared using gum kondagagu, gum olibanum and guar gum as mucoadhesive polymers. Mucoadhesion is a topic of current interest in the design of drug delivery systems. Bioadhesive microspheres for bioavailability enhancement. Formulation and invitro evaluation of mucoadhesive. Thus the mucoadhesive microspheres will provide greater area more contact time as well as control the drug release7.
Telmisartan was encapsulated with different eudragit polymers by an emulsion solvent evaporation technique and the physicochemical properties of the formulations were characterized. Formulation and evaluation of nevirapine mucoadhesive. Formulation of mucoadhesive microspheres of piroxicam. The release profile from the microspheres depends on the nature of the polymer used in the preparation as well as on the nature of the active drug. Crosslinked mucoadhesive microspheres based on anionic. Glipizide is an oral hypoglycemic drug with short halflife. Mucoadhesive microspheres for gastroretentive delivery of. Shobhita mishra, niraj singh patel, manish kumar and kamla pathak affiliation.
Calcium chloride was used as crosslinking, to retard the drug release from the mucoadhesive microspheres. Mucoadhesive microspheres a controlled release system designed to increase its residence time in the stomach with contact with the mucosa was achieved through the preparation of mucoadhesive microspheres microspheres are small spherical particles typically 1. Our result is supported by the report of chowdary and rao who used the microcapsules of glipizide with a coat consisting of alginate and a mucoadhesive polymer n sodium carboxymethyl cellulose, methyl cellulose, carbopol and hydroxypropyl methyl cellulose. Formulation of mucoadhesive microspheres of rosiglitazone. Hollow microspheres are used as additives to lower the density of a material. Microspheres were prepared by ionic gelation technique using sodium alginate, carbopol 974, and hydroxyl propyl methyl cellulose k15 m hpmc as a mucoadhesive polymers. Recent advances in mucoadhesive drug delivery system mucoadhesive microspheres. The mechanism of nevirapine release from the mucoadhesive microsphere was found to be anomalous and super caseii.
Formulation and evaluation of mucoadhesive glipizide microspheres article pdf available in aaps pharmscitech 61. The release profiles of microsphere formulations prepared by solvent evaporation showed that ha and hach microspheres provided release over 3 h. Professor of pharmaceutics, new drug delivery systems laboratory, pharmacy department, donorsplaza, opp. Microspheres were pale yellow in color, freeflowing, spherical, and porous in outline. Most mucosal surfaces such as in the gut or nose are covered by a layer of mucus. So to provide prolonged action glipizide microspheres were prepared by ionic gelation technique using different concentration of mucoadhesive polymers. 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. Mucoadhesive microspheres for controlled drug delivery.
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 mucoadhesive properties of chitosan microspheres prepared by different method were evaluated by studying the interaction between mucin and microspheres in aqueous solution. 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. Microspheres prepared were found discrete, spherical and free flowing.
The crystallinity of nevirapine was found to be reduced in prepared mucoadhesive microspheres f12, which were confirmed by xrd studies. References powders and granulates freeflowing powders and granulates are needed for a variety of industrial processes. 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. Effect of chitosan molecular weight and composition on mucoadhesive properties of mangostinloaded chitosanalginate microparticles. Preparation and evaluation of the in vitro drug release.
Mucoadhesive microspheres containing antihypertensive. The microspheres appeared long drug retention, stable in gastrointestinal conditions, ph responsive and low toxicity. Irbesartan, mucoadhesive microspheres, drug entrapment efficiency, swelling property, in vitro washoff test. Chitosan, thiolated chitosan, carbopol 71g and methocel k15m were used as mucoadhesive polymers. Jan 22, 2014 contents of the powerpoint on formulation and evaluation of microspheres include. Mucoadhesive microspheres as a controlled drug delivery system. These mucoadhesive microparticles bind to the mucus layer leading either to slow release into the git or direct delivery to the gastrointestinal mucosa. Such modifications are provided on surface of microspheres in order to achieve the targeting to the discrete organs and to avoid rapid clearance from the body. Formulation and in vitro characterization of intranasal mucoadhesive microspheres of lamotrigine using chitosan by gluteraldehyde cross linkingcorresponding author. The aim of the present investigation was to evaluate the potential use of mucoadhesive microspheres for gastroretentive delivery of acyclovir. The numbers of microspheres adhering to the tissue were calculated after 30 min, 1 hr and. Introduction i t is the most extensively used method of micro encapsulation. These, however, do not always meet the exacting standards which modern manufacturing.
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