Mucoadhesive Tablets Research Articles

Carrageenan-Based Acyclovir Mucoadhesive Vaginal Tablets for Prevention of Genital Herpes.

Women are the most affected by genital herpes, which is one of the most common sexually transmitted infections, affecting more than 400 million people worldwide. The application of vaginal microbicides could provide a safe method of protection. Acyclovir is a safe and effective medication for vaginal administration, and numerous benefits have been observed in the treatment of primary or recurrent lesions due to genital herpes. Vaginal tablets based on a combination of the polymers iota-carrageenan and hydroxypropyl methylcellulose were developed for the controlled release of acyclovir. Swelling, mucoadhesion and drug release studies were carried out in simulated vaginal fluid. The tablets, containing a combination of iota-carrageenan and hydroxypropyl methylcellulose, have an adequate uptake of the medium that allows them to develop the precise consistency and volume of gel for the controlled release of acyclovir. Its high mucoadhesive capacity also allows the formulation to remain in the vaginal area long enough to ensure the complete release of acyclovir. These promising formulations for the prevention of genital herpes deserve further evaluation.

Development of Mucoadhesive Buccal Drug Delivery System of Propranolol Hydrochloride Using Aster ericoides Mucilage

Aim: The study was aimed to develop mucoadhesive buccal tablets using Aster ericoides leaves mucilage. Background : Mucilages are naturally occurring high-molecular-weight polyuronides, which have been extensively studied for their application in different pharmaceutical dosage forms. Objective: The objective of the present research was to establish the mucilage isolated from the leaves of Aster ericoides as an excipient for the formulation of the mucoadhesive buccal tablet. Method: The mucilage was isolated from the leaves of Aster ericoides by maceration, precipitated with acetone and characterized. Tablets were prepared using wet granulation technique and evaluated for various official tests. Results: The mucilage was found to be non-toxic on A-431 and Vero cell lines. It was insoluble but swellable in cold and hot water. The results indicate that mucilage can form a three-dimensional network. The pH of the mucilage (6.82 ± 0.13) indicated that it might be non-irritant to the buccal cavity. The mucilage was found to be free from microbes. The release of drug was by Fickian diffusion. The in vivo buccal tablet acceptance was 80%. No significant difference between the diastolic blood pressure of standard and Aster tablets treated volunteer group was recorded. Conclusion: The mucilage was found to be non-toxic on A-431 and Vero cell lines. It was insoluble but swellable in cold and hot water. The results indicate that mucilage can form a three-dimensional network. The pH of the mucilage (6.82 ± 0.13) indicated that it might be non-irritant to the buccal cavity. The mucilage was found to be free from microbes. The release of drug was by Fickian diffusion. The in vivo buccal tablet acceptance was 80%. No significant difference between the diastolic blood pressure of standard and Aster tablets treated volunteer group was recorded. Other: However, to prove the potency of the polymer, in vivo bioavailability studies in human volunteers are needed along with chronic toxicity studies in suitable animal models.

Development of propranolol hydrochloride bilayer mucoadhesive buccal tablets supported by in silico physiologically-based modeling

• A novel in vitro setup for the permeation study: Bio-Dis dissolution apparatus. • Propranolol hydrochloride – specific OCCAT™ pharmacokinetic model was developed. • An in vitro-in silico based strategy was used for the design of intraoral dosage forms. • Established relation between PK parameters and formulation properties: QbD approach.

Formulation Development and <i>In Vitro</i> Evaluation of Buccal Tablets of Ramipril

The main objective of the present investigation was to develop buccal tablets of ramipril, to bypass the first pass metabolism and to improve its oral bioavailability. Ramipril, an ACE inhibitor used in the treatment of hypertension undergoes extensive first pass metabolism and about 25% of the drug reaches the systemic circulation. A unidirectional, bilayered mucoadhesive tablet of ramipril was prepared using HPMC as polymer by direct compression technique. Initially, a backing layer was made by using ethyl cellulose, onto which the drug containing layer as placed and recompressed to get a bilayered tablet. The buccal tablets were evaluated for various parameters such as weight variation test, thickness, hardness, friability, in vitro swelling studies, in vitro mucoadhesion study and in vitro dissolution study. Among the different formulation, the formulation (F1) prepared using 5% HPMC as polymer exhibited satisfactory performance over the other batches and considered as an ideal batch. The release of the drug from the tablets exhibited zero order kinetics and the mechanism of release was governed by diffusion process.

A double-blind randomized clinical trial of novel Ayurvedic muco-adhesive extended release vaginal tablet (NA) for treatment of leucorrhea

A double-blind randomized clinical trial of novel Ayurvedic muco-adhesive extended release vaginal tablet (NA) for treatment of leucorrhea

Validation of a high-performance liquid chromatographic method for the assay and dissolution of captopril in mucoadhesive tablet formulation

Validation of a high-performance liquid chromatographic method for the assay and dissolution of captopril in mucoadhesive tablet formulation

Preparation of mucoahesive tablets of famotidine by wet granulation method and its in-vitro testing

Objective: Famotidine is a histamin H2-receptor antagonist.The aim and objective of the present work is toformulate and evaluate mucoadhesive tablets of famotidine. It is also foused on the selection of mucoadhesivepolymer & its activity in various combinations & ratios. The poor bioavialability & shorter half-life suffice thedevelopment of controlled release mucoadhesive formulation. Method: Mucoadhesive tablets each containing 20mg of famotidine were prepared by conventional wet granulation method employing as mucoadhesive materials. A batch of 50 tablets was prepared, in each case a blend of 1 gm of famotidine with different polymers addition indifferent strengths with required 40mg lactose as diluent achieved after titration which were then grannulated along with a solvent blend if water and ethyl alcohol. Results: The flow properties of all five batches were in between fair and passable. Hardness of tablets ranged from 6.9-8.2 kg/cm2 and the percentage friability was between 0.25-0.79 %. The drug content uniformity in the mucoadhesive tablets was 96.49-104.81%. The surface pH study was within the range from 6.7-7.4. From all formulations, over 20% of the famotidine was release within first hour of dissolution study. In the present study the formulation FT04 (tragacanth & HPMC ) has shown cumulative percent drug release of about 80.762% in 12 h. Conclusion: From the results we concluded that formulation containing famotidine with HPMC & tragacanth has given better drug release property than the other four formulations & the wash-off test has shown that this formulation (FT04) has better mucoadhesive property.

Formulation and Evaluation of Floating and Mucoadhesive tablets containing Glipizide

In the present study, Glipizide, a drug mainly preferred for type-II diabetes, is formulated in the form of floating mucoadhesive tablets to improve its bioavailability. Hydroxy Propyl Methyl Cellulose K200M, Sodium Carboxy Methyl Cellulose, Carbopol 974P, Karaya gum, Chitosan, and Xanthan gum were used as mucoadhesive polymers in designing of the floating mucoadhesive tablets. Different proportions of glipizide and polymer were used to prepare tablets. Pre-compression evaluation studies evaluated the powder blend of Glipizide mucoadhesive tablets (Pre-compression blend). It concluded that the blend had good flow property and better compressibility by interpreting the data obtained from the test. Hence the floating mucoadhesive tablets were prepared by direct compression technique. The results of floating lag time, and buoyancy studies suggested that formulations had a satisfactory floating ability. The release profile of the active pharmaceutical ingredient (glipizide) from the prepared dosage form indicated a controlled and enhanced drug release for a period of 12hrs. An in-vivo study done for selected formulation. By the interpretation of data obtained from all the evaluation studies (Pre-compression test, floating property, drug release profile, & in-vivo study) concluded that formulation GF8 containing drug: Carbopol 974P (1:2) was optimized. The drug release kinetics of the formulation GF8 followed the Higuchi model with a regression value of 0.993.

SYNTHESIS AND CHARACTERIZATION OF THIOLATED GUM KONDAGOGU AND EVALUATION AS MUCOADHESIVE POLYMER

Present work focused on thiolation for enhancing the mucoadhesive potential of Gum kondagogu (GK). Thiolation of GK was done by esterification process with 80 % thioglycolic acid in presence of 7N HCl. Thiolated Gum kondagogu (ThioGK) was determined to possess 1.59 ±0.04 mmol of thiol groups/g of the polymer by Ellman’s method. ThioGK was characterized by FTIR, NMR, DSC, XRD, and FE-SEM. The tablets were prepared by direct compression using 75 mg of ThioGK and GK. Tablets containing ThioGK (F1) and GK (F2) were subjected to evaluation of weight variation, hardness and friability and show enhanced disintegration time, swelling behavior, drug release and mucoadhesion. In vitro drug release of batch F1 exhibits complete release of drug in 24 hr with zero order release kinetics. Comparative mucoadhesive strength was studied using chicken ileum by texture analyzer and revealed higher mucoadhesion of tablet containing ThioGK. From the above study, ThioGK was suitability exploited as mucoadhesive sustained release matrix tablet.

In Vivo Evaluation of a Novel Chitosan-Polycaprolactone Based Mucoadhesive Gastro-Retentive Sustained Release Drug Delivery System for Milnacipran HCl.

The study was aimed to develop a gastro-retentive mucoadhesive sustained release matrix formulation for milnacipran HCl (MCN) by using the design of experiment (DoE). The gastro-retentive swellable mucoadhesive matrix tablets were prepared by modified solvent-based wet granulation through mixing milnacipran (MCN), chitosan low molecular weight (CH-LM), chitosan medium molecular weight (CH-MM), and polycaprolactone (PCL). Optimization of the formulation was carried out via DoE. Formulations were characterized by DSC, FTIR, and in vitro drug release testing. In vitro mucoadhesive studies were performed on rabbit's intestinal mucosa. In vivo drug release studies were performed on dogs. Optimized matrix formulations showed no significant interaction among the polymers and MCN, confirmed by DSC and FTIR, and were characterized as swellable controlled release matrix systems. The optimized formulations MOPT3 and MOPT4 showed significantly improved adhesion time of 12h on the gastric mucosa. Based on the in vivo analysis, the elimination half-life of MCN was increased that proved the matrix formulation to be sustained release DDS. The Tmax was extended from 2 to 12 ± 1.63h for MOPT4. Cmax of matrix was reduced to 121.60 ± 9.496ng/ml as compared to 149.22 ± 9.942ng/ml of solution. The bioavailability of the matrix formulation was significantly improved as compared to the MCN solution by 272.20 ± 48.11%. The controlled drug release and strong mucoadhesive properties of the gastro-retentive matrix formulations suggested the potential application of the formulations for the extended oral delivery of MCN.

Formulation and Evaluation of Floating and Mucoadhesive Tablets containing Repaglinide

In the present study, Repaglinide an anti-diabetic drug is formulated in the form of floating mucoadhesive tablets to improve its bioavailability. Hydroxy Propyl Methyl Cellulose K200M, Sodium Carboxy Methyl Cellulose, Carbopol 974P, Karaya gum, Chitosan, Xanthan gum were used as rate controlling and mucoadhesive polymers in designing the tablets. Various formulations were prepared by using different concentration of polymers. The pre-compression blend of Repaglinide mucoadhesive tablets were characterized with respect to angle of repose, bulk density, tapped density, carr's index and hausner's ratio and all the results indicated that the blend had good flow property and better compressibility. The swelling studies were performed and the results indicated that all the formulations had good swelling index. The results of floating lag time and buoyancy studies suggested that formulations had good floating ability. The drug release studies indicated a controlled and enhanced drug release for a period of 12hrs. In-vivo study was carried out using the optimized formulation. Based on the in-vitro drug release and other related evaluation tests, formulation RT11 containing drug: karaya gum in the ratio 1: 2 was optimized. The drug release of the formulation RT11 followed Higuchi model with regression value of 0.984.

Formulation and evaluation of a mucoadhesive buccal tablet of mefenamic acid

Buccal route of administration has many advantages such as improving patient compliance, bypassing the GIT and hepatic first pass effect. The objectives are to formulate mucoadhesive buccal tablet using Mefenamic acid and compatible excipients, and to evaluate the product using quality control tests and in vitro tests. The ingredients were subjected to Differential Scanning Calorimetry and Fourier Transform Infrared Spectroscopy studies for compatibility test and the results showed no interaction. Two batches of mefenamic buccal tablet were prepared. The tablet thickness and diameter are 3.75 mm and 12 mm respectively. All tablets are within the specification of +/- 5%. The in-house tablet hardness is 6.8-15kg and percent friabilation is not more than 0.8%. The disintegration test showed that all tablets disintegrated within 4 hours. The content uniformity showed that tablets are within the range of 85%-115%. The tablet weight is within the 5% range. The percent swelling is 53.83% to 58.86% and moisture absorption is 14.79% to 15.56%. The surface pH of the tablet is close to the salivary pH, which means that it would not irritate the buccal mucosa. The buccal tablet has a mucoadhesiveness of 0.196 to 0.200. There was no change in pH and size after subjecting it to stability studies in human saliva. Drug release studies showed 80.7% to 83.4% after 3 hours. Even after 3 months of subjecting the tablets to 40 oC and 75% RH, results are within acceptable range. The results show the potential of the formulation as a mucoadhesive buccal tablet.

Development, In-vitro and In-vivo evaluation of gastro retentive formulations for moxifloxacin hcl

The objective of current study is to develop gastro retentive formulation for Moxifloxacin. HCl using various drug release modifiers and performing In-vitro, In-vivo evaluations. Moxifloxacin, novel synthetic fluoro quinolone, antibacterial agent. Floating, Muco Adhesive tablets of Moxifloxacin. HCl were prepared using variable amounts of HPMCK100M, Lannea coromandelica gum (LCG) by direct compression technique, Wet Granulation technique respectively. Amount of release modifiers required to obtain the prolonged release of drug shows impact on objective of the study. Formulations were developed and are checked for pharmacopoeial tests. Results shows that all the formulations were lie within the standard limits. Dissolution parameters of all formulations were subjected to kinetic fitting, various statistical parameters were determined. Formulation GRSOF containing 50mg of HPMCK100M and 50mg of LCG, is the best formulation showing similarity f2=71.734, f1=4.271 with the marketed product (AVELOX). It follows Higuchi’s kinetics, Non-Fickian Diffusion first order kinetics (n= 0.717). In-vivo studies were performed for the GRSOF with 6 healthy rabbits and pharmacokinetic parameters were determined, compared with AVELOX and found that GRSOF produced similar results. GRSOF expected to improve patient compliance by means of providing good clinical outcome.

Formulation Development and Evaluation of Nimesulide Mucoadhesive Tablets using Bael (Aegle marmelos) gum powder as Binder

Formulation Development and Evaluation of Nimesulide Mucoadhesive Tablets using Bael (<i>Aegle marmelos)</i> gum powder as Binder

A Comparative Randomized, Open-label, Multicenter Study of the Efficacy and Safety of Miconazole Mucoadhesive Tablets and Miconazole Gel in the Treatment of Oropharyngeal Candidiasis

A Comparative Randomized, Open-label, Multicenter Study of the Efficacy and Safety of Miconazole Mucoadhesive Tablets and Miconazole Gel in the Treatment of Oropharyngeal Candidiasis

Fabrication and In-vitro Evaluation of Buccal Mucoadhesive Tablet of Meloxicam.

In this study, buccal mucoadhesive tablets of meloxicam were formulated for drug delivery as an alternative route. Direct compression method was applied for the preparation of tablets. Also, different polymers, including hydroxypropyl methyl cellulose (HPMC) 1000, 4000, and 10000, as well as carbopol 934p and carbopol 971p were used as the mucoadhesive polymer and retardant polymer. Thirteen formulations were investigated with various concentrations of polymers. The physicochemical characteristics, in-vitro drug release, swelling index, and taste modification of tablets were evaluated. Also, Carr’s index and Hausner ratio were studied. In addition, zero-order, first-order, and Higuchi kinetics were investigated and the results showed that the highest correlation coefficient (R2) is related to zero-order kinetic for formulations B2 and B3. Furthermore, the highest R2 is related to Higuchi kinetic for formulation C3. Formulation B2 showed the maximum release of 99% in 12 h. The results demonstrated that Formulation B2 can be considered as a proper buccal mucoadhesive tablet of meloxicam with desired property.

ALTERATION OF PHARMACOKINETIC PARAMETERS OF PENTOXIFYLLINE USING NATURAL MUCOADHESIVE POLYMERS

Objective: The present study was aimed to alter the pharmacokinetic parameters of the drug pentoxifylline using a novel natural mucoadhesive polymer from two different plants, Manilkara zapotta Linn and Ocimum basilicum Linn.&#x0D; Methods: The polymer was isolated and six batches of mucoadhesive tablets of pentoxifylline was formulated with 3 different concentrations of each polymer. The best formulation from each of the polymer was selected and administered to rabbits and the plasma drug concentration was compared with the marketed formulation. The pharmacokinetic parameters such as such as Cmax, tmax, AUC, AUMC, λz, t1/2, and MRT were determined.&#x0D; Results: The plasma drug concentration vs time curve shows the extended-release of pentoxifylline when compared with the conventional marketed formulation. The results show that there is no change in the peak plasma concentration, but the significant difference was observed in t½, which showed approximately 2.5 fold increase from 2.44 to 6.87 h and the AUC showed five-fold increase from 22.40 to 117.19 μg*h/ml, and other pharmacokinetic parameters, when compared with the marketed formulation.&#x0D; Conclusion: The isolated polymer from the plants Manilkara zapotta Linn. and Ocimum basilicum Linn can be used as a carrier for developing mucoadhesive formulations and it alter the pharmacokinetic of pentoxifylline positively.

Synergy between surfactants and mucoadhesive polymers enhances the transbuccal permeation of local anesthetics from freeze-dried tablets.

We report on the advance of freeze-dried mucoadhesive orodispersible tablets (ODTs) loaded with prilocaine (PRC) and lidocaine (LDC) hydrochlorides, aiming to promote noninvasive buccal anesthesia. The influences of combining biocompatible polymers (pullulan and HPMC K100 LV) and a blend of surfactants (oleic acid, polysorbate 80 and propylene glycol) acting as chemical enhancers on the permeation of such drugs through the esophageal porcine epithelium and in vitro mucoadhesion were investigated. The ODTs were also characterized in terms of average weight, thickness, pH, drug content, in vitro release, thermal behavior and scanning electronic microscopy. A dissolution test showed fast drug release within one hour. The drug release data for all ODTs fitted first order. No significant influence of the type of mucoadhesive polymer on release was observed, while the drug release from ODTs decreased in the presence of chemical enhancers. For the ODT containing pullulan the drug release mechanism was anomalous transport, whist for all others it was case-II transport. A remarkable synergic effect between pullulan and chemical enhancers on the permeation flux, lag time, and permeability coefficient of both drugs, but mainly for PRC was observed. Pullulan together with permeation enhancers also substantially improved the work of mucoadhesion as compared to HPMC. In contrast, HPMC improved drug retention in the epithelium. The novel drug delivery platform achieved by combining a freeze-drying technique, mucoadhesive biocompatible polymers, and chemical permeation enhancers displayed an effective strategy for the transbuccal delivery of PRC and LDC that can be used to improve needle-free buccal anesthesia.

Randomized Phase 2 Trial of a Novel Clonidine Mucoadhesive Buccal Tablet for the Amelioration of Oral Mucositis in Patients Treated With Concomitant Chemoradiation Therapy for Head and Neck Cancer

Oral mucositis (OM) is a frequent and painful sequela of concomitant chemoradiation (CRT) used for the treatment of head and neck cancer (HNC) for which there is no effective intervention. This randomized, placebo-controlled study evaluated the efficacy of a novel, mucoadhesive topical tablet formulation of clonidine in mitigating CRT-induced OM in patients with HNC. Patients with HNC undergoing adjuvant radiation therapy (60-66 Gy; 5 × 1.8-2.2 Gy/wk) with concomitant platinum-based chemotherapy received daily local clonidine at 50 μg (n = 56), 100 μg (n = 65), or placebo (n = 62) via a topical mucobuccal tablet starting 1 to 3 days before and continuing during treatment. The primary endpoint was the incidence of severe OM (severe OM [SOM], World Health Organization grade 3/4). SOM developed in 45% versus 60% (P = .06) of patients treated with clonidine compared with placebo and occurred for the first time at 60 Gy as opposed to 48 Gy (median; hazard ratio, 0.75 [95% confidence interval, 0.484-1.175], P = .21); median time to onset was 45 versus 36 days. Opioid analgesic use, mean patient-reported mouth and throat soreness, and CRT compliance were not significantly different between treatment arms. Adverse events were reported in 90.8% versus 98.4%, nausea in 49.6% versus 71.0%, dysphagia in 32.8% versus 48.4%, and reversible hypotension in 6.7% versus 1.6% of patients on clonidine versus placebo, respectively. Although the primary endpoint was not met, the positive trends of OM-associated outcomes suggest that the novel mucoadhesive tablet delivery of clonidine might favorably affect the course and severity of CRT-induced SOM and support further evaluation.

Efficacy of Phenytoin Mucoadhesive Tablet versus Mouthwash on Chemotherapy-Induced Oral Mucositis: A Randomized Clinical Trial

Background: Oral mucositis is one of the painful, debilitating and common complications in the patients under chemotherapy for which no certain and effective treatment has not been considered. The aim of this pilot study was to evaluate the efficacy of phenytoin mucoadhesive tablets on treating oral mucositis compared with phenytoin mouthwash. Methods: In this clinical trial, after preparation and in vitro characterization of phenytoin mucoadhesive tablets, 27 patients were enrolled from oncology department of Nemazee Hospital, Shiraz, Iran. 21 patients with oral mucositis, who had the inclusion criteria due to chemotherapy, were divided into two groups of A (11 patients received phenytoin mouthwash 0.5%) and B (10 patients received phenytoin mucoadhesive tablet). Severity of oral mucositis (WHO grading), oral pain Visual Analogue Scale and the extension of lesions (number of involved sites) were assessed on three intervals (at the beginning and one or two weeks after beginning of the study). Results: In the first visit, there was no significant statistical difference between the two groups regarding mean age, mucositis severity and visual analogue scale. However, on first and second weeks after beginning of the study, mucositis severity, extension of lesion and visual analogue scale in both groups were significantly lower than onset of the treatment; however, no significant difference between the two groups was observed. Conclusions: Phenytoin mouthwash and mucoadhesive tablets used for oral mucositis care in patients after chemotherapy showed significant improvement in the lesions. Patients were more satisfied with mouthwash and all the patients in this group were free of lesion after two weeks.