Formulation And Evaluation Of Mucoadhesive Microspheres Of Anti-Emetic Agent For Nasal Delivery.

Abstract

The objective of research work was to develop and optimize mucoadhesive microspheres of anti-emetic agent (Metoclopramide HCL) for nasal delivery with the aim to enhance the residence time and improve therapeutic efficacy and at the same time increase the local absorption of drug and reducing systemic side effects and also to develop unique delivery system for patients suffering from nausea & vomiting. Mucoadhesive microspheres (Chitosan based) of Metoclopramide HCL were prepared by emulsification-crosslinking method in different ratios. Glutaraldehyde was used as crosslinking agent. The mean particle size was significantly increased when high concentration of chitosan was used. Aqueous to oil phase ratio, stirring rate and dioctyl sodium sulfosuccinate (DOSS) concentration also influenced the particle size distribution of the microspheres. Microspheres were evaluated with respect to the production yield, particle size, entrapment efficiency, swelling index, FTIR, in vitro mucoadhesion, cumulative percentage drug release, and stability studies. Formulation F3 was found to be optimized. The optimized formulation F3 was mucoadhesive in nature which adhere on the mucus membrane and increase the residence time within the nasal cavity. Utilizing a high concentration of chitosan resulted in a noticeably larger mean particle size. Particle size distribution of the microspheres was also affected by the concentration of dioctyl sodium sulfosuccinate (DOSS), stirring rate, and aqueous to oil phase ratio. In vitro mucoadhesion, cumulative percentage drug release, swelling index, FT-IR, manufacturing yield, particle size, entrapment efficiency, and stability studies were all taken into consideration when evaluating microspheres. There was an optimized discovered formulation F3. Since it adhered to mucus and lengthened its stay in the nasal cavity, the improved formulation F3 was mucoadhesive in nature