Mucoadhesive Gastroretentive Research Articles

In Vivo Pharmacokinetic Studies of Acyclovir Gastro Retentive Mucoadhesive Microspheres Aided by Azadirachta indica Fruit Mucilage

In Vivo Pharmacokinetic Studies of Acyclovir Gastro Retentive Mucoadhesive Microspheres Aided by Azadirachta indica Fruit Mucilage

DEVELOPMENT OF GASTRORETENTIVE MUCOADHESIVE SOLID DOSAGES FORM CONTAINING AMOXICILLIN TRIHYDRATE AND RANITIDINE HCL FOR THE TREATMENT OF HELICOBACTER PYLORI INFECTIONS

Mucoadhesion can be explored in the design of drug delivery system. Mucoadhesive drug delivery systems interact with the mucus layer covering the mucosal epithelial surface, and mucin molecules, thus increasing the residence time of the dosage form at the site of absorption. The drugs having local action or possessing maximum absorption in gastrointestinal tract (GIT) requires increased duration of stay in GIT. Gastroretentive Mucoadhesive solid dosages form containing Amoxicillin Trihydrate and Ranitidine HCL were formulated to prolong the residence time of the dosage form at the site of application or absorption, and it results in intimate contact of the dosage form with the underline absorption surface. This combination is approved by FDA for the treatment of Helicobacter Pylori Infections. The formulation results in efficient absorption, enhanced bioavailability of the drugs due to a high surface to volume ratio and an improved therapeutic performance of the drug. The prolonged release of drug resulted in reduced frequency of drug administration and improved patient compliance. The optimized formulation was evaluated for various parameters i.e. hardness, friability, thickness, weight variation, drug content, dissolution study and swelling index.

Enhancing Oral Absorption of Orlistat through Gastroretentive Mucoadhesive Pellets: Formulation and Evaluation

Aim: The aim of this study was to develop gastroretentive mucoadhesive pellets of Orlistat to improve its oral bioavailability and enhance its absorption.
 Methods: Orlistat pellets were prepared using Hydroxy Propyl Methyl Cellulose (HPMC) K100M, Sodium Carboxy Methyl Cellulose (NaCMC), Carbopol 934P, and Polyvinyl Pyrrollidone (PVP) K30 in varying ratios. Physical characteristics of the tablets were evaluated, and compatibility studies were performed between Orlistat and the excipients. Swelling index, mucoadhesion strength and drug release were measured for each formulation. Drug release kinetics and stability studies were carried out.
 Results: The combination of HPMC K100M, NaCMC, Carbopol 934P and PVP K30 provided balanced release and mucoadhesion with F13 showing sustained release up to 16 hours. The calibration curve demonstrated a good linear relationship between Orlistat concentration and absorbance over the range of 10 to 50 ?g/ml. Swelling index increased with time and polymer concentration and mucoadhesion strength increased with polymer viscosity and concentration. Drug release from formulations containing HPMC K100M, NaCMC and Carbopol 934P were 12-14 hours, 10-12 hours and 8-11 hours, respectively. Combination polymers in F10-F13 provided balanced release and mucoadhesion, with F13 showing sustained release up to 16 hours. The drug release followed zero order kinetics with non-Fickian diffusion. Stability studies on the optimized F13 formulation showed no significant changes in appearance, hardness, mucoadhesion or drug release over 3 months.
 Conclusion: The combination of HPMC K100M, NaCMC, Carbopol 934P and PVP K30 improved the oral bioavailability and absorption of Orlistat. The study demonstrated the importance of compatibility studies and the use of calibration curves for quantitative analysis. The findings provide valuable insights into the development of drug delivery systems for poorly bioavailable drugs.

Personalised 3D-Printed Mucoadhesive Gastroretentive Hydrophilic Matrices for Managing Overactive Bladder (OAB).

Overactive bladder (OAB) is a symptomatic complex condition characterised by frequent urinary urgency, nocturia, and urinary incontinence with or without urgency. Gabapentin is an effective treatment for OAB, but its narrow absorption window is a concern, as it is preferentially absorbed from the upper small intestine, resulting in poor bioavailability. We aimed to develop an extended release, intragastric floating system to overcome this drawback. For this purpose, plasticiser-free filaments of PEO (polyethylene oxide) and the drug (gabapentin) were developed using hot melt extrusion. The filaments were extruded successfully with 98% drug loading, possessed good mechanical properties, and successfully produced printed tablets using fused deposition modelling (FDM). Tablets were printed with varying shell numbers and infill density to investigate their floating capacity. Among the seven matrix tablet formulations, F2 (2 shells, 0% infill) showed the highest floating time, i.e., more than 10 h. The drug release rates fell as the infill density and shell number increased. However, F2 was the best performing formulation in terms of floating and release and was chosen for in vivo (pharmacokinetic) studies. The pharmacokinetic findings exhibit improved gabapentin absorption compared to the control (oral solution). Overall, it can be concluded that 3D printing technology is an easy-to-use approach which demonstrated its benefits in developing medicines based on a mucoadhesive gastroretentive strategy, improving the absorption of gabapentin with potential for the improved management of OAB.

Karakteristik Granul Gastroretentive Mukoadhesif Amoksisilin dengan menggunakan Kitosan-Alginat, Na.CMC dan HPMC

Gastroretentive Drug Delivery System (GRDDS) is a slow-release preparation that can be bound to the surface of epithelial cells or gastric mucosa, while mucoadhesive is one of the mechanisms of action of the Gastroretentive Drug Delivery System (GRDDS), which is a drug delivery system in which the bio adhesive polymer is combined with the drug. designed to have a longer contact with the mucous membranes in the digestive tract. This study aims to see how the characteristics of the granules that are formulated in the form of mucoadhesive gastroretentive granules. The preparation method used was wet granulation using a mucoadhesive polymer, namely chitosan-alginate with the addition of HPMC and Sodium CMC. The results showed that the velocity test of the flow rate on the granule formula F1-F8 met the flow rate requirements, the results of the F9 velocity had a poor flow rate, while the results of the angle of repose measurement in the F1, F2 and F4 formulas had good flowability, which was below 30o, different with F3, F5, F6, F7, F8, and F9 which have a 30-40o angle of repose with good flowability. The results of the particle size distribution using the stratified sieve method showed that the formulas F1-F9 were mostly retained by a mesh number 20 sieve with a size of 426-850 m. The results of the test results of the gastroretentive mucoadhesive granule preparation of amoxicillin showed that the preparation met the requirements for making granules.

Quality and Release Profile of Captopril from Mucoadhesive Gastroretentive Tablet by Using Matrix Sodium Carboxymethyl Cellulose and Carbopol 934P

Captopril have good absorption in gastric pH and ionized on intestinal pH. It is necessary to keep the drug in the form of molecules in the area of the absoption. The mucoadhesive gastroretensive drug delivery system provides the possibility of controlled release in stomach in a certain amount of time. Research has been conducted to assess the quality and profile of captopril release in of a mucoadhesive gastroretensive tablet. Mucoadhesive tablets (MK) were made in 5 formulas by wet granulation method using carbopol 934P and sodium carboxymethyl cellulose as matrix with ratio 10: 0 (MK1), 0: 10 (MK2), 5: 5 (MK3), 7: 3 (MK4), and 3: 7 (MK5). The parameters which was evaluate were characteristics of granules and tablets and kinetics model of captopril release from tablets in 0,01 N HCl medium. Mucoadhesive tablets had different characteristics for each formula. Mucoadhesive tablets that had good quality and release profile were shown by MK4 and MK5 formula. They had controlled drug release profiles accorded to the Korsmeyer-Peppas and Higuchi kinetics models, respectively.

Antibacterial Activity of Mucoadhesive Gastroretentive Drug Delivery System of Alginate Beads Containing Turmeric Extract - PVP Solid Dispersion.

BACKGROUND:Turmeric extract is less effective because the main ingredient of curcumin has a low solubility. Therefore, it is necessary to convert turmeric extract into a solid dispersion form to increase the dissolution of curcumin.AIM:To determine the antibacterial activity of mucoadhesive gastroretentive drug delivery system of alginate beads containing solid dispersion of turmeric extract.METHODS:Turmeric powder was macerated with 96% ethanol for 8 days. The macerate was evaporated with a rotary evaporator at 50°C to obtain concentrated extract. Solid dispersion of turmeric extract was prepared by solvent method by using polyvinylpyrrolidone (PVP) K30 with a ratio of 1: 1 and 1: 2. The solid dispersion of turmeric extract was encapsulated with alginate gel by gelation method. The antibacterial of alginate beads containing solid dispersion of turmeric extract was tested by using hole agar plate diffusion method against Staphylococcus aureus and Escherichia coli as bacterial models.RESULTS:The size of alginate beads containing turmeric extract-PVP solid dispersion was about 1.3 mm. Antibacterial activity test against Staphylococcus aureus and Escherichia coli showed that alginate beads containing turmeric extract-PVP solid dispersion gave stronger antibacterial activity than those containing turmeric extract without solid dispersion. The antibacterial activity of alginate beads turmeric extract-PVP (1: 2) solid dispersion was stronger than those containing turmeric-extract (1: 1) solid dispersion.CONCLUSION:Based on the results of this study it can be concluded that alginate beads containing turmeric extract-PVP solid dispersion gives the stronger antibacterial activity than those containing turmeric extract without solid dispersion.

Gastroretentive Mucoadhesive Microsphere for the Management of Gastric Infection

Gastric infections are mostly triggered by Helicobacter pylori (H. pylori), a fungus that colonizes the stomach mucosa of more than 50% of the inhabitants of the world. Chronic H. Pylori diseasewas associated with stomach diseases such as peptic ulcer, chronic gastritis and stomach adenoc arcinoma. Current therapy for eradication relies on antibiotic-based therapies that are ineffective in about 20% of patients. Traditional method constraints optimize the creation of new techniques for fast, consistent and cost-effective H diagnosis. Infection with pylori. Wide-ranging study has been carried out over the previous few centuries to create a type of gastro-retentive dosage (GRDF). This sort of dosage form can advance the delivery and efficiency of stomach-active medicines because the GRDF enables the medication to remain in the stomach for a sufficient time period. Various methods were used to develop effective GRDFs such as high-density systems, low-density systems, swelling and expansion systems, hydrodynamically balanced systems, superporous hydrogels,. However, there are both merits and demerits in these kinds of schemes. Intra-individual and inter-individual dissimilarities are obstacles to the growth of effective GRDFs in gastric physiology. Examples of these individual differences include gastric pH and gastric motility that have a notable effect on the moment of stomach retention and delivery of drugs. Some of these obstacles can be overcome by developing a novel mucoadhesive microsphere. The mucoadhesive microsphere is characterized by close contact of the MDF with the mucosal layer, thereby increasing the localized absorption of the drug. H2Receptor antagonists (H2RAs) have become first-line therapy for acid related peptic disease and GRDF especially designed for H2RAs and drugs against H. pylori, including specific targeting systems and leading to a marked development in the quality of life for a large number of patients. In this relationship, new formulations with improved absorption, improved bioavailability and improved acid-suppressing regimens are welcome
 Keywords: H. pylori, gastro-retentive dosage, mucoadhesive microsphere

Design of Experiment (DoE) Approach to Prepare, Characterize and Optimize the Gastroretentive Mucoadhesive Microspheres of Repaglinide

In this present investigation, gastroretentive mucoadhesive microspheres of Repaglinide was formulated, characterized and optimized by applying the design of experiment (DoE) for better release profile and sustain action of the drug. Solvent evaporation technique was used to prepare microspheres, where Methocel K15M CR (X1), Eudragit L 100 (X2) and rpm (X3) were used as independent variables whereas percent cumulative drug release at 8 hours (Y1), bond strength (Y2) and swelling at 8 hours (Y3) were used as dependent variables. Particle size, surface morphology, mucoadhesive bond strength, swelling study, and drug entrapment efficiency were determined to characterize the prepared microspheres. In vitro dissolution study was performed in 0.1N HCl (pH 1.2) media for 8 hours. Response surface of dependent variables was calculated by design expert software and it was found that most of the responses were fitted to the quadratic model. Percent cumulative drug release at 8 hours was found minimum 61.34% and maximum 87.29%, the minimum and maximum range of mucoadhesive bond strength was found 426.02 to 13335.74 N/m2 and in case of swelling at 8 hours, it was found 157.43 and 230.22%. After analyzing the responses, proposed formula was obtained from which minimization of percent cumulative drug release at 8 hours as well as swelling and maximization of bond strength was obtained. Thermal behavior was investigated by DSC study and no interaction was found between drug and excipients from FTIR study. Bangladesh Pharmaceutical Journal 22(2): 135-145, 2019

Formulation and Characterization of Gastroretentive Mucoadhesive Tablets for Treatment of Gastroparesis

The aim of the present research work was to formulate and characterize gastroretentive mucoadhesive tablets of lacidipine (LCDP) intended for the treatment of gastroparesis. Polymers such as sodium alginate, HPMC K4M, carbopol 974P, and chitosan were utilized in LCDP formulation to ensure gastric retention up to 8 h. Direct compression method was adopted in preparation of mucoadhesive tablets. Prior to compression, powder blends were evaluated in order to check their flow and compression properties. Fourier transform infrared spectroscopy and differential scanning calorimetry measurements were performed to assess the compatibility of LCDP with polymers. Tablets were characterized with respect to the uniformity of weight, hardness, friability, drug content, swelling index, surface pH and in-vitro drug release. All formulations exhibited acceptable physicochemical properties. Formulation F4 exhibiting in-vitro drug release of 95.510% was selected as the optimized formulation and was further characterized by scanning electron microscopy. In vitro dissolution data was fitted to various kinetic models, and formulation F4 was found to display non-Fickian mechanism of drug release. No major change was observed in drug release and drug content upon storage of optimized formulation under accelerated aging conditions. The obtained results revealed that carbopol 974P and chitosan can be used in combination to formulate gastroretentive mucoadhesive LCDP tablets.

PREPARATION OF MUCOADHESIVE GASTRORETENTIVE DRUG DELIVERY SYSTEM OF ALGINATE BEADS CONTAINING TURMERIC EXTRACT AND ANTI-GASTRIC ULCER ACTIVITY

Objectives: The objectives of this study were to prepare the mucoadhesive mucoadhesive gastroretentive drug delivery system of alginate beads containing turmeric extract and to evaluate its anti-gastric effect.Methods: Turmeric extract was made by macerating turmeric powder in ethanol 96% and evaporated using rotary evaporator at 50°C to obtained concentrated extract. Then, it was prepared alginate beads containing 5% turmeric extract by gelation method. The mucoadhesive properties of alginate beads containing turmeric extract were tested in vitro in male rats and the anti-gastric ulcer effect was tested on HCl-induced gastric ulcer in rats.Results: The mean diameter of alginate beads obtained was 1.13±0.19 mm. Bioadhesion test showed that alginate beads containing turmeric extract could be attached on gastric rats mucosa. Anti-gastric ulcer test showed that the healing of gastric lesions in rats was faster using alginate beads containing turmeric extract compared to untreated ones.Conclusions: The results of this study suggest that mucoadhesive drug delivery systems of alginate beads containing turmeric extract are potentially developed as an anti-gastric ulcer.

PREPARATION OF MUCOADHESIVE GASTRORETENTIVE DRUG DELIVERY SYSTEM OF ALGINATE BEADS CONTAINING TURMERIC EXTRACT AND ANTI-GASTRIC ULCER ACTIVITY

Objectives: The objectives of this study were to prepare the mucoadhesive mucoadhesive gastroretentive drug delivery system of alginate beads containing turmeric extract and to evaluate its anti-gastric effect.Methods: Turmeric extract was made by macerating turmeric powder in ethanol 96% and evaporated using rotary evaporator at 50°C to obtained concentrated extract. Then, it was prepared alginate beads containing 5% turmeric extract by gelation method. The mucoadhesive properties of alginate beads containing turmeric extract were tested in vitro in male rats and the anti-gastric ulcer effect was tested on HCl-induced gastric ulcer in rats.Results: The mean diameter of alginate beads obtained was 1.13±0.19 mm. Bioadhesion test showed that alginate beads containing turmeric extract could be attached on gastric rats mucosa. Anti-gastric ulcer test showed that the healing of gastric lesions in rats was faster using alginate beads containing turmeric extract compared to untreated ones.Conclusions: The results of this study suggest that mucoadhesive drug delivery systems of alginate beads containing turmeric extract are potentially developed as an anti-gastric ulcer.

Formulation and evaluation sustained release mucoadhesive gastroretentive pantoprazole sodium sesquihydrate tablets for anti–ulcer

Objective: The objective of this research work is to develop and evaluate the mucoadhesive gastroretentive tablets of an anti – ulcer drug for sustain release. Materials and Methods: Mucoadhesive tablets were prepared by direct compression method using Hydroxy propyl methyl cellulose K4M, Carbopol 940 NF and Guar gum in the various drug – polymer ratios. The prepared tablets were evaluated for their pre and post compression parameters. In this study the optimized formulation was obtained within the specified limits. Results: The final optimized formulation was showed mucoadhesion time 12 h, mucoadhesive strength of tablets were ready with HPMC K4M, Carbopol 940 NF and gum were found to be 45 g and the extreme proportion of drug release was obtained 97.11% at the completion of 12 h. The drug release mechanism for optimized formulations of pantoprazole mucoadhesive sustain release tablets was observed to be zero order kinetic model. Conclusion: The formulation of hydroxy propyl methyl cellulose showed excellent mucoadhesive ability and a suitable drug release pattern.
 Keywords: Pantoprazole sodium sesquihydrate, Gastroretentive, mucoadhesive polymers

Complex Hydrogels Composed of Chitosan with Ring-opened Polyvinyl Pyrrolidone as a Gastroretentive Drug Dosage Form to Enhance the Bioavailability of Bisphosphonates

Complex hydrogels formed with chitosan (CS) and ring-opened polyvinyl pyrrolidone (roPVP) as a swellable mucoadhesive gastroretentive drug dosage form (smGRDDF) were prepared and characterized. CS/roPVP hydrogels were produced by blending CS with roPVP obtained by basic treatment of PVP. Effects of the heating time and NaOH concentration employed for preparing roPVP, and CS molecular weights (Mws), and roPVP/CS ratios on the swelling ability of the resultant hydrogels were characterized. Rheological characteristics were further examined. Results demonstrated that roPVP obtained in a 0.5 M NaOH solution heated to 50 °C for 4 h was suitable for producing complex hydrogels with CS. At a roPVP/CS ratio of 20:1, hydrogels composed of three different Mws of CS possessed optimal swelling and mucoadhesive abilities and rheological properties. In vitro dissolution revealed sustained drug release. A pharmacokinetic study exhibited that the plasma profile of alendronate followed a sustained manner with 3-fold enhancement of the oral bioavailability. In conclusion, the smGRDDF composed of CS/roPVP complex hydrogels was successfully developed and is potentially applicable to improve the clinical efficacy of bisphosphonates.

Pharmacokinetic Studies of Gastroretentive Mucoadhesive Matrices for Diltiazem Hydrochloride Using Some Natural Polysaccharides

The objective of this study was to investigate differences in the pharmacokinetic patterns between a gastroretentive mucoadhesive drug delivery system (GRMDDS) and sustained release dosage form of same dose to increase the residence time of the drug in to the stomach and release for extended period of time. Gastroretentive mucoadhesive tablets of diltiazem hydrochloride (DLTH) with hibiscus esculentus mucilage and xanthan gum as natural polysaccharides were developed for mucoadhesive sustained drug release by wet granulation technique. In-vivo gastro retentive mucoadhesion study confirmed stomach retention for more than 10 h. In-vivo pharmacokinetic studies in rabbits showed Cmax of 176.86 ng/ml and Tmax of 13.3 h for GRMDDS. AUC0–t and AUC0–8 for mucoadhesive tablet formulation was 2514.61 and 3145.77 while the marketed formulation was 2220.11 and 2750.36 ng.h/ml respectively. The point estimates (90% CI) of the “test/reference” mean ratio for Cmax, AUC0-t and Tmax were 1.0662, 1.0327 and 1.33. The difference for AUC0–t and AUC0–8 between the test and reference formulation was statistically significant (p<0.05). Non superimposition of the percent in-vivo absorption and in-vitro dissolution curves was observed to investigate a multiple point correlation of in-vivo and in-vitro which might suggest the possibility of the existence of a level A correlation using the optimum dissolution condition. The results of the present study indicate that the oral bioavailability of diltiazem hydrochloride is significant increase when its dosage is provided prolonged gastric residence by GRMDDS.

Development and Clinical Evaluation of Mucoadhesive Gastroretentive Tablets of Dipyridamole

The present research work was focused to develop a mucoadhesive tablet dosage form for dipyridamole, which shows pH dependent solubility, it is highly soluble in acidic pH and as the pH increases the solubility of the drug decreases. Hence it was selected as the drug candidate for the present research. Mucoadhesive tablets of Dipyridamole were successfully prepared by using polymers like HPMC K4M, Chitosan and Isabgul husk by wet granulation method. FT-IR studies showed that there is no incompatibility between drug, polymer and various excipients used in the formulations. Formulated tablets have shown satisfactory results for physical parameters and complied with the pharmacopeial limits. The ex-vivo mucoadhesive strength and mucoadhesive force was found to be in the range of 16.15- 21.20 g and 1.56-2.06 N. Total ex-vivo mucoadhesive time was observed in between 10 to 12 hours. The in-vitro drug release was found to be more than 90% for the formulations FMD2, FMD3 and FMD8, up to 12 hours. Based on in-vitro drug release and mucoadhesive properties, formulation FMD2 was selected as optimized formulation. The dissolution data were further characterized by fitting the data into various kinetic models. The drug release from the matrices followed zero order with non-fickian release (diffusion + erosion controlled) for the optimized formulation. The optimized formulation was further subjected to swelling studies, which showed a swelling index of 286% up to 24 hours. The results indicated that the selected polymers were of swellable type. The stability studies were carried for 6 months as per ICH and WHO guidelines and the results of the stability study revealed that the optimized formulation is stable during the storage period. The in-vivo radiographic studies in fed condition, for the Mucoadhesive tablets (FMD2) showed a gastric residence time of more than 6 hours. When the radiographic images were taken at different time intervals and it was found to be in a particular location, which suggested that the retention of the dosage form might be due to the adhesion of dosage form to the gastric mucosa.

FORMULATION DEVELOPMENT AND EVALUATION OF MUCOADHESIVE TABLETS OF NORFLOXACIN CONTAINING NATURAL POLYMER

The present investigation deals with development and evaluation of mucoadhesive gastroretentive tablet of Norfloxacin using natural polymer from Tamrind seed polysaccharide

Development and Evaluation of Optimized Gastroretentive Mucoadhesive Tablets of Famotidine for Gastro-Esophageal Reflux Disease

The aim of the present investigation was to increase the gastric residence time of Famotidine by designing and optimization of gastroretentive mucoadhesive tablet, thereby improving bioavailability of Famotidine. Famotidine conventional tablets have been reported by many Scientists to exhibit poor oral bioavailability and fluctuations in plasma drug concentration. This results, either in precipitation of side effects or reduction in drug concentration at the target site. Famotidine is a histamine H2-receptor antagonist. It is widely prescribed in active duodenal ulcers, gastric ulcers, Zollinger-Ellison syndrome and gastro esophageal reflux disease. The effective treatment requires administration of 20 mg of Famotidine 4 times a day. A conventional dose of 20 mg can inhibit gastric acid secretion up to 6 hours but not up to 12 hours. An alternative dose of 40 mg leads to plasma fluctuations; thus a sustained release dosage form of famotidine is desirable. The short biological half-life of drug (2.5-4 hours) also favors development of a sustained release formulation. Thus objective of present study to reduce the dosing frequency by developing, optimizing and evaluating gastroretentive mucoadhesive tablet for sustain release. A 32 full factorial design is employed to study the effect of independent variables like Carbopol-940 and HPMC K100M, which significantly influence characteristics like ex-vivo mucoadhesive strength and in-vitro drug release. Tablets were prepared by direct compression technique. No significant change was observed in physical appearance, drug content, hardness, mucoadhesive strength, in vitro dissolution pattern after the stability tasting for one month.&#x0D;

Comparative study of in vitro release and mucoadhesivity of gastric compacts composed of multiple unit system/bilayered discs using direct compression of metformin hydrochloride.

Introduction: Metformin is an oral anti-diabetic drug in the biguanide class. The goal of this study was to develop gastric-retentive MH discs in order to prolong the retention of drug in gastric mucosa. Methods: Two groups of metformin hydrochloride (MH) mucoadhesive gastroretentive discs were prepared: (a) bilayered discs prepared by direct compression of powders containing polymers as Carbopol 934P (CP, mucoadhesive polymer) and ethylcellulose (EC, rotardant polymer), (b) multiple unit system (microparticle) discs prepared by the emulsification, solvent evaporation, and compression technique from microparticles using polymers CP and EC. Gastric-mucoadhesive compacts were evaluated by investigating their release pattern, swelling capacity, mucoadhesion property, surface pH, and in vitro gastro-retentive time. Discs formulation was subjected to disintegration and dissolution tests by placing in 0.1 M hydrochloric acid for 8 h. Results: The production yield showed F2 microparticles of 98.80%, mean particle size of 933.25 µm and loading efficiency of 98.44%. The results showed that prepared microparticle discs had slower release than bilayered discs (p>0.05). The bilayered discs exhibited very good percentage of mucoadhesion. The results also showed a significant higher retention of mucoadhesive bilayered discs in upper gastrointestinal tract (F´1, 1:2 ratio of CP:EC). Histopathological studies revealed no gastric mucosal damage. Conclusion: Mucoadhesive multiple unit system/bilayered discs interact with mucus of gastrointestinal tract and are considered to be localized or trapped at the adhesive site by retaining a dosage form at the site of action as well as improving in the intimacy of contact with underlying absorptive membrane to achieve a better therapeutic performance of anti-diabetic drug.

Screening of Most Effective Variables for Development of Gastroretentive Mucoadhesive Nanoparticles by Taguchi Design

The objective of this study was the selection of the most influential variable for the preparation of gastroretentive mucoadhesive nanoparticles of acyclovir. Nanoparticles were prepared by one-step desolvation method; effect of formulation and processing variables on various response variables were studied by a Taguchi standard orthogonal array L8 design. Independent variables studied were the amount of gelatin, amount of glutaraldehyde, amount of Pluronic F-68, acetone addition rate, pH, stirring time, and stirring speed. The dependent variables studied were the particle size, polydispersity index, amount of drug released in 6 h, time required to release 60% of drug, entrapment efficiency, loading efficiency, and mucoadhesiveness. The size of all nanoparticulate formulations prepared as per the experimental design (Taguchi screening design) varied between 165 and 1610 nm, PDI between 0.360 and 1.00, bioadhesiveness between 3.959 and 11.02 g, cumulative percent drug release in 24 h between 40.74 and 72.48, entrapment efficiency between 15.70 and 83.12, and loading efficiency between 39.72 and 80.49. Pareto ranking analyses showed that the two most important factors affecting the selected responses were amount of gelatin and amount of Pluronic F-68 (P&lt;0.05).