Formulation & Evaluation of Mucoadhesive Microspheres of Carvedilol

Microspheres are important drug delivery systems having small size & efficient carrier properties. These microspheres possess short residence time at the site of action, hence coupling mucoadhesive properties to microspheres lead to a novel DDS i.e., “Mucoadhesive microspheres. Carvedilol loaded alginate microspheres were prepared by ionic gelation technique using calcium chloride as cross linking agent. The ionic gelation technique does not involve the necessity of organic solvents to solubilise the water insoluble polymer as in solvent evaporation /coascervation phase separation technique. The influence of curing time, concentration of calcium chloride used for curing were studied. The polymers used were sodium alginate, HPMC (50cps). The drug entrapment was found to be in the range of 58.82-71.35%.The micromeritic flow properties, moisture content, swelling index, drug content & entrapment efficiency were evaluated for prepared microspheres. The microspheres are spherical and free flowing. Carvedilol release from microspheres followed first order kinetics and was influenced by curing time & concentration of calcium chloride. The drug transport mechanism was fickian as the n value is less than 0.5.

Key words: Mucoadhesive microspheres, sodium alginate, HPMC, Carvedilol.

Author: http://www.pharmainfo.net/bhanunagendla
Guide: http://www.pharmainfo.net/tegkmurthy

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Comments

aravikumar's picture

what are the marketed dosage forms of carvedilol

Averineni Ravi Kumar

bhanunagendla's picture

The conventional type of marketed dosage forms of carvedilol are cardivas, carvadil,carloc. The controlled release formulations are coreg 25, coreg 10, coreg 40.
N.bhanu
snhpratap's picture

carvedilol half life is around 5 hours.As per the presentation u delivered the time taken for 95% of the drug to be released from the microspheres is around 3.5 hours then, how can u say the drug release is sustained.
pratap n h
Balavishnupriya.M's picture

What is the selection criteria for polymer in preparation of Mucoadhesive Microspheres? Is there any dose dumping of drug from mucoadhesive microspheres? What is the effect of viscosity of polymer dispersion on drug entrapment efficiency?

M.Bala Vishnu Priya

bindu's picture

what happens if i overdose the drug?
bhanunagendla's picture

dose of carvedilol for the treatment of mild to moderate heart failure was25 mg twice daily. Symptoms of overdose may include unusually slow heartbeat, severe dizziness, slow or shallow breathing, weakness, or fainting.
N.bhanu
aukunjv's picture

What are the different polymers that have been used for the preparation of mucoadhesive microspheres? Which category do you think is good for the drug of interest of your study?
p.j.subrahmanyam's picture

What is the Y-axis parameter in zero order kinetics graph, is it % drug released or cumulative amount of drug release?
mohinimalla's picture

cum%drug release should be taken on y axis
m.mohini
mohinimalla's picture

cum%drug release should be taken on y axis
m.mohini
mohinimalla's picture

cum%drug release should be taken on y axis
m.mohini
mohinimalla's picture

cum%drug release should be taken on y axis
m.mohini
mohinimalla's picture

cum%drug release should be taken on y axis
m.mohini
mohinimalla's picture

cum%drug release should be taken on y axis
m.mohini
mohinimalla's picture

cum%drug release should be taken on y axis
m.mohini
mohinimalla's picture

cum%drug release should be taken on y axis
m.mohini
bhanunagendla's picture

the cumulative amount of drug release should be on y-axis in case of zero order kinetics
N.bhanu
p.j.subrahmanyam's picture

What are the units of K, t50 and t90?
anil kumar appapurapu's picture

how can we perform bio-adhesion absorption test?

anilkumar

pavan kumar alapati's picture

why the carvidlol is formulated as a mucoadhesive drug delivery system? is there any specific advantage for this system with respect to your drug ?
bhanunagendla's picture

The present research was aimed at development and optimization of alginate mucoadhesive microspheres of carvedilol for oral delivery to improve the therapeutic efficacy in the treatment of hypertension and angina pectoris.Though it is a drug of choice for hypertension it has several drawbacks such as short biological half-life of about 2-8 hours, it is readily metabolized in liver primarily by cytochrome P 450 isoenzyme, CYP 206 and CYP209 and has oral bioavailability as 30%.
N.bhanu
bhanunagendla's picture

sir, the various polymers that are employed for mucoadhesive microspheres are SYNTHETIC POLYMERS Carboxy methyl cellulose +++ Hydroxyl propyl methyl cellulose +++ Carbopol 934 +++ Tragacanth +++ Sodium alginate +++ Polycarbophil +++ Hydroxyl ethyl cellulose +++ Polyvinyl pyrrolidone + NATURAL SOURCE Gelatin ++ Guar gum ++ Gum karaya ++ Pectin + Acacia + NOTE : +++ Excellent ++ Moderate + Poor there fore many polymers have excellent mucoadhesive prpperty but i started with HPMC and still doing with other polymers like guar gum, pectin.
N.bhanu
sowjanya gummalla's picture

Why are you using De-ionised water in the preparation of microcapsules? what is the influence of ions present in that water?
sowjanya gummalla