FORMULATION AND EVALUATION OF RACECADOTRIL MUCOADHESIVE MICROSPHERES

Objective: To develop and evaluate the mucoadhesive microsphere using combinations of natural polymers chitosan and xanthan gum for sustained release. Methods: In the present work mucoadhesive microspheres were prepared by using natural polymers like chitosan and xanthan gum by using the emulsion chemical cross-linking method. Chemical cross-linking was done by using glutaraldehyde. The 22 factorial design was employed to show the effect of cross-linking agent and processing factor-like stirring and speed. Prepared microspheres were evaluated for their particle size, surface morphology, drug entrapment efficiency, in vitro drug release, swelling index, and mucoadhesive strength. Results: The size of microspheres of factorial batches were in the range of 26-46 µm. The swelling index was showed in the range of 1.51-1.66 percentage. The equation of multiple regression revealed that there was significant interaction among factors. The glutaraldehyde concentration had a positive effect on % entrapment efficiency, % cumulative drug release and % mucoadhesion. Stirring speed showed a negative impact on % entrapment efficiency, % cumulative drug release and % mucoadhesion. The interactive effect of glutaraldehyde concentration and the stirring speed was found to be positive for % entrapment efficiency and % cumulative drug release. In vitro drug release study of optimized formulation F2 show 96 % of drug release with 6 h indicating sustained release behavior with diffusion mechanism. The SEM image of the optimized batch was spherical with a porous surface. Conclusion: The results obtained in this research work indicated that a promising potential of chitosan and xanthan gum combination for the preparation of the mucoadhesive microsphere of Racecadotril.

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

Formulation and evaluation of deflazacort loaded mucoadhesive microsphere for colon drug delivery system

Irritable bowel disease is very common colon disease. Deflazacort is one of the best drug with clinical activity against Irritable bowel disease. Microsphere system are effectively protect drugs against premature degradation, to localize drug molecules at the target site of action and to control the time and rate of release. Mucoadhesive microspheres enhance the bioavailability of orally given drugs by lengthened contact time of drug with the intestinal mucosa. The main disadvantage of these microspheres is adherence to the substrate by non-specific interaction. To overcome this limitation, microspheres are prepared by emulsification method to treat irritable bowel disease. Chitosan microspheres were prepared by Ionotropic Gelation method. Microspheres were coated with Eudragil S using solvent evaporation method. Keywords: Deflazacort, Mucoadhesive, Microspheres, Irritable bowel disease

MUCOADHESIVE AND MICROSPHERE: A SHORT REVIEW

Microsphere constitutes an important part of novel drug delivery system by virtue of their small size and efficient carrier capacity. Due to their short residence time, bioadhesive characteristics can be coupled to microsphere to develop mucoadhesive microsphere. Bioadhesion defined as state in which two materials, at least one of which is biological in nature, are held together for a prolonged time by the way of interfacial forces. Microsphere are the carrier around drug delivery system in which particle size in ranges from 1-1000 μm range in diameter having a core of drug and entirely outer layers of polymers as coating material. Mucoadhesive microsphere have advantages like efficient absorption and enhanced bioavailability of drugs due to high surface of volume ratio, a much more intimate contact with mucus layer, controlled and sustained release of drug from dosage form and specific targeting of drug to absorption site. This study aim to provide an overview of various aspects of mucoadhesive microsphere based on various polymers, method of preparation of mucoadhesive microsphere, method of evaluation and their applications in drug delivery system.Keywords: Mucoadhesive, microsphere, bioavailability.

FORMULATION ANDCHARACTERIZATION OF OLANZEPINELOADED MUCOADHESIVE MICROSPHERES

Objective: The objective of this research was to formulate and evaluate olanzapine (OLE) mucoadhesive microsphere prepared using carbopol and sodium combination. OLE having extensive hepatic first pass metabolism and low bioavailability problem, determined the need for the development of sustained release formulation.Methods: OLE mucoadhesive microspheres were prepared by ionic gelation method. OLE mucoadhesive microspheres were prepared byionic gelation method by using calcium chloride as crosslinking agent. The OLE mucoadhesive microsphere was characterized by particle sizemeasurement, process yield, morphology of microsphere, drug entrapment efficiency, mucoadhesion test, differential scanning calorimetry, powder X-ray diffraction, Fourier transforms infrared (FTIR) study and in-vitro drug release.Results: The OLE mucoadhesive microsphere having mean particle size ranged from 546.0 µm to 554.3 µm, and the entrapment efficiencies ranged from 73% to 96%. All the olanzapine (OLE) microsphere batches showed good in-vitro mucoadhesive property ranging from 75.89% to 96.47% and in the in-vitro wash off test ranging from 68.12% to 81.3%. FTIR studies indicated the no drug-polymer interactions in the ideal formulation F9. Therewere no compatibility issues, and the crystallinity of OLE was found to be reduced shoeing less intense peak in prepared mucoadhesive microspheres, which were confirmed by differential scanning calorimeter and X-ray diffraction studies. Among different formulations, the OLE microspheres of batch F9 had shown the optimum percent drug entrapment of microspheres. Release pattern of OLE from F9 microspheres batch followed Higuchi kinetic model. Stability studies were carried out for F9 formulation at 4°C/ambient, 25±2°C/60±5%, 40±2°C/75±5% relative humidity revealed that the drug entrapment, mucoadhesive behavior, and drug release were within permissible limits.Conclusion: The results obtained in this work demonstrate the use of carbopol and sodium alginate polymer for preparation of mucoadhesive microsphere.Keywords: Ionic gelation method, Gastroretentive delivery, Mucoadhesive microsphere, Carbopol.