FORMULATION ANDCHARACTERIZATION OF OLANZEPINELOADED MUCOADHESIVE MICROSPHERES

Abstract

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.