Release Retarding Polymer Research Articles

Formulation and Evaluation of Domperidone Sustained Release Tablet

In present study, an attempt has been made to design and develop Domperidone matrix tablets using Hydroxypropyl methylcellulose K100M, 5CPS and combination with Acrypol as release retarding polymers by wet granulation method. Domperidone is a peripheral dopamine receptor with blocking properties. Domperidone helps in the gastric emptying and decreases small bowel passing time by increasing esophageal and gastric peristalsis and also by lowering esophageal sphincter pressure. Domperidone sustained release matrix tablet were prepared and evaluated for number of parameters like thickness, diameter, weight variation, swelling index and in vitro release studies. The weights of the tablets were in the range of 125 ± 2 mg. The thickness of the tablet was in the range of 3.25± 0.2 to 3.27 ± 0.2 mm. FT-IR spectral analysis showed that characteristic peak of Domperidone pure drug was retained in the spectra of all the formulations corresponds to the compactness of the drug in all the formulations. The result indicates that Hydroxypropyl Methylcellulose K100M and Acrypol 974p in combination and individual Hydroxy Propyl Methyl Cellulose-5CPS respectively and can be used as an effective matrix former to sustain the release of Domperidone for an extended period of 10 hrs.

Development of Long Acting Depot Injection of Iloperidone by SABER Technology

The present investigations report the application of SABER® technology in the development of a one-month depot injection of iloperidone. SABER® is a new in situ gel formulation technology for sustained release drug delivery, which precludes the use of large amounts of toxic organic solvents in the formulation. Traditionally in the in situ gel forming technology-based depot injections, expensive polymers such as polylactic acid and poly(lactic-co-glycolic acid), and a class 2 solvent like N-methyl-2-pyrrolidone have been used to control the rate of drug release and dissolve the drug and polymer, respectively. In the present investigations, however, no such release retarding polymers were used, moreover, the formulation was developed using a limited amount of dimethylsulphoxide, a class 3 solvent. Formulation variables were optimized by D-optimal mixture design to obtain the depot formulation with a consistent drug release for one month. The composition of sucrose acetate isobutyrate, and dimethylsulphoxide were taken as input variables and cumulative drug release at various time points as response variables. The optimized formulation contained 81.718 % sucrose acetate isobutyrate and 18.282 % dimethylsulphoxide and produced a consistent drug release profile with 85.71 % cumulative drug release in 30 days without any significant burst release.

Formulation of Modified Release Pellets of Montelukast Sodium

The present study was carried out with an aim of preparing modified release pellets of the antiasthma drug montelukast sodium. The patients suffering from chronic asthma many a times suffer from exacerbations during the early morning hours i.e. around 4am to 6 am. Thus the need to take an immediate release medication arises during early morning hours which is not quiet feasible for the patients. The delivery of the drug at this time can be made possible by the use of modified release formulation of montelukast sodium which when taken at the bed time would release the drug as a pulsed delivery without the need of the patient to wake up. The montelukast sodium pellets prepared by extrusion-spheronization were coated with release retarding polymer ethyl cellulose using the Wurster method. The ethyl cellulose coating helped in lag time increase due to prolonged water uptake time. The increase in the coating level increased the lag time sufficiently that might release the drug during the early morning hours. Thus a modified release pellets dosage form to prevent the early morning asthma attacks and exacerbations was developed successfully.

Design and in vivo Evaluation of Gastro-retentive Floating Capsules of Amlodipine Besylate in Healthy Human Volunteers

The aim of this study was to explore the application of Gelucire 43/01 for the design of sustained release gastro retentive drug delivery system of Amlodipine besylate. Gelucire 43/01 has been used in floating sustained release formulations to prolong gastric residence time and increase its bioavailability. Gelucire 43/01 in combination with HPMC and Polyox was used as a release retarding polymer. HPMC of various viscosity grades HPMC K4M, HPMC K15M and HPMC K100M in combination of Gelucire were tested to obtain optimal total floating time as well as controlled drug release for prolonged period. Melt granulation technique has been used to prepare gastro retentive Amlodipine besylate formulations. All the formulations were evaluated in vitro for their floating ability and drug release. The floating times of all tablet formulations were greater than 12h. HPMC K4M in combination with Gelucire as polymeric matrix enhanced the drug release due to addition of hydrophilic polymer facilitated the swelling and erosion of the tablets. Incorporation of low viscosity polymer HPMC K100 M resulted in optimal floating as well as drug release for longer time. In vivo studies of optimized formulation show floating ability for 6 h in stomach. The results indicate that Gelucire 43/01 in combination with dissolution enhancers HPMC increase the permeability of the wax matrix, which provides improved dissolution thereby bioavailability of Amlodipine besylate and can be considered as a carrier for the development of sustained release floating drug delivery systems.

APPLICATION OF SOLID DISPERSION TECHNIQUE IN SOLUBILITY AND DISSOLUTION RATE ENHANCEMENT OF NATEGLINIDE

Objective: Nateglinide (NTG) is a potent short-acting biopharmaceutical classification system class II antidiabetic medication. The primary objective of the present investigation was to prepare and evaluate solid dispersions of NTG to enhance the component solubility and immediate release (IR) profile. The secondary objective was to formulate sustained release (SR) matrix layer of NTG for prolonging its effect in the body and to decrease oscillations in plasma concentration level.Methods: NTG (270 mg) SR layer was formulated using release retardant polymers such as Carbopol, ethyl cellulose (EC), hydroxy EC, hydroxypropyl methylcellulose (HPMC), Kollidon, and locust bean gum at concentrations of 15% and 30%. IR layer of NTG (60 mg) was formulated using drug: Polymer inclusion complexes (1:1 and 1:2) of β-cyclodextrin (CD), HP β-CD, polyvinylpyrrolidone (PVP) K-15, and PVP K-30 by physical mixing and kneading methods (KMs).Results: Among the all the carriers tested HP β-CD at 1:2 ratio prepared by KM (I3) gave highest enhancement of dissolution rate and dissolution efficiency with acceptable f1 (10.5) and f2 (51.0) values in comparison to marketed IR tablets (Starlix-60®). The SR formulation S12 was able to show a minimum amount of drug release (15%) within 1 hr comparatively, with a complete and sustained effect on drug release.Conclusion: Thus, HPMC K-100M at a concentration of 30% in the SR layer in combination with HP β-CD (1:2) solid dispersions in the IR layer may be used in the design of oral controlled drug delivery system for NTG.

A novel co-processed directly compressible release-retarding polymer: In vitro, solid state and in vivo evaluation

Directly compressible (DC) co-processed excipient capable of providing nearly zero order release with improved functionality was developed without any chemical modification by employed various techniques such as physical mixing, high shear mixer granulation and spray drying. Co-processed excipient was developed by using release retarding polymer Eudragit RSPO, separately, in combination with different concentration of hydroxyl propyl methyl cellulose 100 cps (Methocel K100 LV, HPMC), ethyl cellulose (Ethocel N50, EC) and hydroxyl propyl cellulose (Klucel EF, HPC). All co-processed excipients were evaluated for their flow properties in terms of angle of repose, bulk density, tapped density, compressibility index and Hausner's ratio. Out of eighteen combinations, the nine co-processed excipients exhibited promising flow properties were found suitable for direct compression and formulated as tablets. Metoprolol succinate, a BCS Class I drug, was selected as a model drug and the formulation was developed employing direct compression approach. The developed tablets were evaluated for physical parameters like uniformity of weight, thickness, hardness, friability and assay. In vitro dissolution study confirms that formulation prepared using co-processed excipient showed sustained drug release. The optimized tablet formulation was characterized by DSC, FTIR and PXRD which confirms the absence of any chemical change during co-processing. The optimized formulation was kept for stability study for six months as per ICH guidelines and found to be stable. In vivo pharmacokinetic study of optimized formulation in rats showed similar pharmacokinetic behaviour as was observed with the marketed brand. Study revealed that co-processed excipient has advantage over polymers with single property and can be utilised for sustained release formulation.

Development of smart hydrogels of etherified gum ghatti for sustained oral delivery of ropinirole hydrochloride

Gum Ghatti (GG) is a water soluble complex polysaccharide obtained from Anogeissus latifolia. Due to its non toxic and excellent emulsifying characteristics, it was widely used in different pharmaceutical preparations. Currently another facet was explored for its utility as release retardant polymer in oral controlled drug delivery system. As GG solely was incapable of forming microspheres therefore modification of GG to Sodium carboxymethyl (NaCMGG) derivative was done by carboxymethylation process and its gel forming capacity was explored by the use of trivalent cation (Aluminium chloride) which results into complete microbead system in a complete aqueous environment for controlled delivery of Ropinirole Hydrochloride (RHCl). Rheological property of NaCMGG showed pseudoplastic shear thinning behavior. Spherical shape of bead was observed under scanning electron microscope. Depending upon the formulation variables, Drug entrapment efficiency (DEE) varies from 47.66±3.51 % to 71.4±2.65%., and 80 to 90% drug was released in 6h in pH 6.8 phosphate buffer. Drug release was governed by both fickian diffusion and polymer relaxation simultaneously. Compatible environment for drug entrapment was established by Fourier transform infrared (FTIR) spectroscopy and differential scanning calorimetry (DSC). Thus the modified derivative NaCMGG could be a promising polymer in biomedical application.

Formulation and Development of Divalproex Sodium Bi-Layered Tablets using Superdisintegrants and Release Retardant Polymers


 Divalproex sodium is considered as the most important antiepileptic drug and widely used for treatment of epilepsy and bi-polar disorders and prophylaxis of migraine. The present work has been done to formulate bi-layered tablet of Divalproex sodium containing immediate release layer and sustained release layer. The FTIR study revealed that there was no interaction between drug and polymer and combination. Both layers were prepared by wet granulation technique as poor flow property exhibited by pure drug. The immediate release layer was formulated by using superdisintegrants and evaluated for physical parameters, disintegration time and in vitro drug release. The optimized immediate release layer (IF6) with highest in vitro release of 98.11 was selected for bi-layered tablet formulation. HPMC K4M and HPMC K100M polymer were used to retard the drug release from sustained release layer in different proportion and combination and evaluated for physical parameter along with in vitro drug release studies. The optimized sustained release layer (SF8) which extends the Divalproex sodium release more than 18 hrs was selected. Finally, bi-layered tablets were prepared by double compression of selected sustained release layer and immediate release layer of Divalproex sodium. The tablets were evaluated for hardness, thickness, weight variation, friability, drug content uniformity and in vitro drug release. All the physical parameters were in acceptable limit of pharmacopeial specification. The stability studies, shown the bi-layer tablet was stable at 40oC / 75% RH for a period of 3 months.

Investigation and Optimization of the Effect of Polymers on Drug Release of Norfloxacin from Floating Tablets.

Norfloxacin is fluoroquinolone anti-infective used in the treatment of urinary tract infections, prostatitis, gonorrhea and genital tract infections. It has plasma half life of 3 to 4 h requiring multiple dosing in the treatment. Releaseretarding polymers can be used to modulate the drug release of norfloxacin. The objective of this study was to investigate the effect of release-retarding polymers on the drug release of norfloxacin from floating tablets. Norfloxacin was procured as a gift sample from Concept Pharma Ltd. Aurangabad (India) and HPMC K100M was procured as a gift sample from Colorcon Asia Pvt. Ltd., Goa (India). The tablets were prepared by direct compression method and various pharmaceutical parameters were evaluated. It was observed that all tablet formulations F1-F9 retained the drug release up to 12 h with good floating property but only Batch-F4 complies with the USP dissolution limits with a minimum floating lag time. The drug release kinetics were evaluated by the model-dependent (curve fitting) method using PCP Disso v3 software shows Batch-F4 shows to best fit with Peppas model for which R2 value was 0.9921 and the release exponent value was 0.6892. The drug release kinetics study indicates that the floating tablets release the drug by diffusion followed by erosion mechanism. Obtained in-vitro drug release data was analyzed by design expert software for drug release at first hour and at 12th h values and found that release the selected independent variables like HPMC K100M and sodium alginate concentration has a significant effect on drug release.

FORMULATION AND EVALUATION OF PERINDOPRIL MICROENCAPSULES BY USING DIFFERENT POLYMER

Objective: The study was carried out with an objective to achieve a potential sustained release oral drug delivery system of an antihypertensive drug, Perindopril which is a ACE inhibitor having half life of 2 hours. Perindopril is water soluble drug, so we can control or delay the release rate of drug by using release retarding polymers. This may also decrease the toxic side effects by preventing the high initial concentration in the blood.Method: Microcapsules were prepared by solvent evaporation technique using Eudragit L100 and Ethyl cellulose as a retarding agent to control the release rate and magnesium stearate as an inert dispersing carrier to decrease the interfacial tension between lipophilic and hydrophilic phase. Results: Prepared microcapsules were evaluated for the particle size, percentage yield, drug entrapment efficiency, flow property and in vitro drug release for 12 h. Results indicated that the percentage yield, mean particle size, drug entrapment efficiency and the micrometric properties of the microcapsules was influenced by various drug: polymer ratio. The release rate of microcapsules could be controlled as desired by adjusting the combination ratio of dispersing agents to retarding agents.Conclusion:Perindopril microcapsules can be successfully designed to develop sustained drug delivery, that reduces the dosing frequency and their by one can increase the patient compliance.

Alternative approaches in formulating floating hollow tablets via sublimation technique; a platform tailored drug release profile.

The aim of this study was to formulate floating hollow tablets of salbutamol sulphate with a platform tailored drug release profile to attain a controllable drug release. Eight formulations (F1-F8) were prepared using sublimation technique. L-menthol was directly compressed as sublimable core followed by compression coating of hydroxypropylmethyl cellulose (HPMC-K15M) or polyethylene oxide (PEO-WSR301) as release retarding polymer coat. Tablets were then subjected to heat to allow sublimation of the core. The effect of polymer type and that of different drug coat/core distribution on swelling and drug release profile was studied. FTIR and DSC revealed the absence of any drug-excipients interaction. Tablets showed a hollow morphology, resulting in low density tablets that floated for over 24 hours without lag time. Moreover, different drug coat/core distribution resulted in controllable release profiles. Based on these results, an optimum drug release behavior was recorded for HPMC-based hollow tablets consisting of 2:1 drug coat/core distribution ratio (F4), revealing a zero order drug release for over 14 hours. Furthermore, F4 showed no changes in drug content, floating properties and drug release profile upon exposure to accelerated stability conditions.

Design and evaluation of bilayer tablets of metformin hydrochloride and pioglitazone hydrochloride as combination drug therapy

The primary objective of the present investigation was to formulate and evaluate fixed dose bilayer tablet of two antihyperglycemic agents with different mechanisms of action to improve glycemic control in patients with type 2 diabetes. A secondary objective is to ensure that metformin release should be less in stomach and completely released in alkaline pH within the stipulated hours. Hence, metformin hydrochloride (500 mg) sustained release (SR) layer was formulated using various release retardant polymers such as hydroxy propyl methyl cellulose, xanthan gum and sodium carboxy methyl cellulose in three different ratios of 1:0.3, 1:0.4 and 1:0.5, such that therapeutically effective levels can be maintained. Immediate release (IR) layer of pioglitazone hydrochloride (15 mg) was formulated using super disintegrant (crosspovidone) in four different ratios of 1:0.2, 1:0.4, 1:0.6 and 1:0.8. The formulated fixed dose bilayer tablets were subjected to various physiochemical evaluations like weight variation, friability, hardness, drug content, in vitro drug release kinetics and stability studies. The optimized formulation (F8) showed the maximum drug release up to 60 min in IR layer and up to 12 h in SR layer. Formulation F8 was found to be stable at room temperature for a period of 3 months. From the study it is evident that a promising bilayer tablet of pioglitazone hydrochloride and metformin hydrochloride can be developed using crosspovidone (disintegrant) and xanthan gum (release retardant polymer).

Design and statistical optimization of an effervescent floating drug delivery system of theophylline using response surface methodology.

The aim of this research was to formulate effervescent floating drug delivery systems of theophylline using different release retarding polymers such as ethyl cellulose, Eudragit® L100, xanthan gum and polyethylene oxide (PEO) N12K. Sodium bicarbonate was used as a gas generating agent. Direct compression was used to formulate floating tablets and the tablets were evaluated for their physicochemical and dissolution characteristics. PEO based formulations produced better drug release properties than other formulations. Hence, it was further optimized by central composite design. Further subjects of research were the effect of formulation variables on floating lag time and the percentage of drug released at the seventh hour (D7h). The optimum quantities of PEO and sodium bicarbonate, which had the highest desirability close to 1.0, were chosen as the statistically optimized formulation. No interaction was found between theophylline and PEO by Fourier Transformation Infrared spectroscopy (FTIR) and Differential Scanning Calorimetry (DSC) studies.

Novel core in cup (In-lay) tablets of lamotrigine for mucoadhesive drug delivery system

Lamotrigine a BCS class II drug used in treatment of epilepsy has several disadvantages when taken orally (first pass metabolism and increased Cmax). The aim of the study is to design core in cup (In lay) buccoadhesive tablets which aims for controlled, unidirectional release, increased patient compliance and decreased side effects. The present study involves the preparation of core in cup tablets containing release retarding polymers like sodium alginate, xanthan gum and HPMC E 15LV in core and HPMC K 15M in cup for mucoadhesion. L9 orthogonal array Taguchi design was constructed for the study. The dependent variable studied for L9 orthogonal array Taguchi runs include % drug release from which the formulation with highest S/N ratio was optimized. All the runs were evaluated for physical parameters, drug release, mucoadhesive studies and assay. L1, L2, L4 and L8 formulations showed controlled release for up-to 8 hours with good assay values. The model dependent kinetics showed zero order kinetics with super case II transport and Hixson Crowell mechanism which indicates unidirectional drug release.Srinija and Lakshmi, International Current Pharmaceutical Journal, January 2016, 5(2): 9-13

Gastroretentive Sustained Release Floating and Swellable Cefadroxil Formulation: In vitro and in vivo Evaluation

A new Gastroretentive Sustained Release (GRSR) tablet of cefadroxil was developed with floating and swellable properties. Various release retarding polymers, swelling agent, gas generating agent and release modifying agents were evaluated. The optimized formulation was studied for various physical parameters, in vitro drug release profile and for in vitro floating properties. The formulation provided sustained drug release for about 14 h with the floating lag time of 30 s and floating duration of about 14 h. Owing to the promising in vitro floating property, the formulation was explored for in vivo floating performance in healthy human volunteers by radio-analytical technique. The developed formulation of Cefadroxil showed prolonged gastric retention in vivo for 7 h. The tablets also showed significant swelling property with excellent tablet integrity till 7 h. The developed formulation exhibited promising gastroretention in vivo. The radio-analytical technique used to evaluate the in vivo gastroretention was found to be simple, cost-effective and was precisely used for detecting floating time and tablet integrity throughout the study.

Sustained Release Matrix Tablets of Furosemide

Objective: The objective of the present study was to develop and evaluate once-daily sustained release matrix tablets of furosemide using hydroxypropylmethyl cellulose K4M, xanthan gum and sodium alginate as release retarding polymers. Methodology: The matrix tablet formulations were prepared by using different drug: polymer ratios (1:1, 1:2, 1:3, 1:4 and 1:5). The prepared matrix tablets were evaluated for pre-compression parameters like angle of repose, bulk density, tap density and post-compression parameters like hardness, thickness, weight variation, friability, percent drug content and in vitro drug release studies as per USP guidelines. Results: The in vitro drug release data of all the prepared tablet formulations of furosemide were subjected to goodness of fit test by linear regression analysis according to zeroorder and first-order kinetics. Conclusion: The formulation SF 2 containing drug: sodium alginate ratio of 1:2 offered the required in vitro drug release rate according to the official limits of drug release as per USP and selected as a promising formulation among the fifteen formulations which shows 85% drug release in 12 hrs.

Design and Evaluation of Sustained Release Matrix Tablets of Indomethacin by Employing Gelucires and Badam Gum

Sustained release matrix tablets of indomethacin (IM) were developed by employing a relatively less used hydrophilic polymer badam gum and gelucires. The dissolution rate of IM is first improved by dispersing the drug in hydrophilic gelucire (50/13) and the dispersion is then embedded in the matrix of badam gum and hydrophobic gelucire (43/01). Different ratios of IM and gelucire (50/13) were employed, and the solid dispersions were prepared by melting and solvent methods. The dispersion prepared by employing solvent method resulted in much higher dissolving product than was possible with the melting method. The differential scanning calorimetry and infrared spectroscopy (IR) studies revealed that there are no interactions between IM and gelucire and the XRD studies indicated that the drug IM existed in amorphous state in gelucire dispersion. Matrix tablets were prepared by direct compression employing different proportions of badam gum and gelucire (43/01). The prepared tablets were found to be of optimum hardness, uniform weight and acceptable friability. The drug release was found to be dependent on the ratio drug: Gelucire in the solid dispersion and also on the proportion of the release retarding polymer employed – gelucire (43/01) or badam gum. The drug release data suggested that the release of the drug is the first order and is diffusion controlled

Development and in-vitro Evaluation of Once Daily Tablet Dosage Form of Loxoprofen Sodium

Purpose: To formulate and characterize once daily controlled release tablet of loxoprofen sodium. Methods : Eudragit RS-100, hydroxylpropyl methylcellulose (HPMC) and pectin were used as release retarding polymers. All the formulations were prepared by direct compression method. Various precompression studies were carried out to determine Hausner’s ratio, Carr’s index, angle of repose, bulk density and tapped density Differential scanning calorimetry (DSC) studies and also post-compression studies to evaluate hardness, friability, weight variation, drug content, in-vitro drug release were conducted on the tablets. The drug release data were subjected to kinetic models, including zero order, first order, Hixon Crowell, Higuchi and Korsmeyer-Peppas. Results : Compressibility index (7.6 ± 1.32 - 12.5 ± 1.43%), Hausner’s ratio (1.08 ± 0.04 - 1.14 ± 0.03), angle of repose (27.78 ± 0.47 - 30.49 ± 0.46°), hardness (6.25 ± 0.27 - 7.21±0.21 kg/cm2), friability (0.14 ± 0.06 - 0.28 ± 0.0 %), weight variation (249.5 ± 2.09 - 251.35 ± 2.41 mg) and drug content (97.30 ± 0.28 - 103.70 ± 0.31 %) were within generally accepted limits for the pre-and post-compression formulations, respectively. The tablets having the maximum amount of among the three polymers tested as matrix materials, HPMC, represented by F3 tablets, exerted better sustained release properties after 12 h. Release pattern was more of Fickian diffusion followed by Higuchi mechanism. Conclusion : The release of the loxoprofen sodium was optimized up to 12 h. Keywords : Loxoprofen, Sustained release, hydroxypropyl methylcelluose, Pectin, Eudragit, Matrix tablets

Development and in-vitro Evaluation of Once Daily Tablet Dosage Form of Loxoprofen Sodium

Purpose: To formulate and characterize once daily controlled release tablet of loxoprofen sodium.Methods: Eudragit RS-100, hydroxylpropyl methylcellulose (HPMC) and pectin were used as release retarding polymers. All the formulations were prepared by direct compression method. Various precompression studies were carried out to determine Hausner’s ratio, Carr’s index, angle of repose, bulk density and tapped density Differential scanning calorimetry (DSC) studies and also post-compression studies to evaluate hardness, friability, weight variation, drug content, in-vitro drug release were conducted on the tablets. The drug release data were subjected to kinetic models, including zero order, first order, Hixon Crowell, Higuchi and Korsmeyer-Peppas.Results: Compressibility index (7.6 ± 1.32 - 12.5 ± 1.43%), Hausner’s ratio (1.08 ± 0.04 - 1.14 ± 0.03), angle of repose (27.78 ± 0.47 - 30.49 ± 0.46°), hardness (6.25 ± 0.27 - 7.21±0.21 kg/cm2), friability (0.14 ± 0.06 - 0.28 ± 0.0 %), weight variation (249.5 ± 2.09 - 251.35 ± 2.41 mg) and drug content (97.30 ± 0.28 - 103.70 ± 0.31 %) were within generally accepted limits for the pre-and post-compression formulations, respectively. The tablets having the maximum amount of among the three polymers tested as matrix materials, HPMC, represented by F3 tablets, exerted better sustained release properties after 12 h. Release pattern was more of Fickian diffusion followed by Higuchi mechanism.Conclusion: The release of the loxoprofen sodium was optimized up to 12 h.Keywords: Loxoprofen, Sustained release, hydroxypropyl methylcelluose, Pectin, Eudragit, Matrix tablets

Study of the Mucoadhesive Potential of Carbopol Polymer in the Preparation of Microbeads Containing the Antidiabetic Drug Glipizide.

The present investigation was aimed at exploitation of the mucoadhesive potential of carbopol 934P polymer in developing microbeads of glipizide (GLP) for its effectivity in controlling blood sugar in diabetic patients. Various batches of GLP beads were prepared by an emulsion-solvent evaporation technique using the release-retarding polymer carbopol and subjected to a systematic evaluation such as physical characterization, ex vivo mucoadhesion, hydration and erosion test, and in vitro drug release; and instrumental and in vivo studies were performed with the best formulation. The highest yield and loading efficiency were observed as 94 and ∼90%, respectively. The mean particle size of the microbeads ranged from 832 to 742μm. The oval shape of the microbeads with slight roughness was apparent in the SEM micrograph. The release period was extended till 18h. In vitro release of the drug from the beads followed the diffusion and erosion mechanism. In the oral glucose tolerance test (OGTT), there is a significant (p < 0.01) reduction in fasting blood glucose levels in Wistar rat and guinea pig in comparison with that using the marketed product. Results indicated that process parameters-drug-polymer ratio, concentration of the surfactant, and stirring speed-controlled the various characteristics of the microparticles. The mucoadhesivity test ensured strong adherence of the beads to the mucosal membrane in pH 1.2 for a prolonged period. Owing to the mucoadhesivity of carbopol 934P, prolonged release of GLP and reduction of fasting sugar in the animal model were observed to a satisfactory level, and thus, management of diabetes in a better manner is expected with this new formulation.