Title : Development and In Vitro Evaluation of Chitosan Microspheres of Sertraline hydrochloride for Nasal Delivery
The nasal route has gained tremendous attention for systemic drug delivery by many researchers within the last few decades due to its great potential utility for drug delivery. It offers an attractive alternative for drugs that have limited oral bioavailability, are destroyed by gastrointestinal fluids, or are highly susceptible to hepatic first pass or gut wall metabolism. Nasal drug delivery also offers the convenience and safety of being noninvasive. In addition, nasal drug administration results in quick onset of action as compared to oral, sublingual and transdermal administrations. The aim of the present study was to develop and characterize chitosan mucoadhesive microspheres of sertraline hydrochloride for nasal administration to avoid first pass metabolism and to improve therapeutic efficacy in treatment of depression. Sertraline hydrochloride, a selective serotonin reuptake inhibitor (SSRI), is a drug of choice in the treatment of depression. Sertraline hydrochloride is slowly absorbed following oral administration and undergoes extensively first pass metabolism which results in low bioavailability of 44 %. The chitosan microspheres were prepared by emulsification-cross linking method using glutaraldehyde as a crosslinking agent A 23 factorial design was used with drug: polymer ratio (X1), glutaradehyde concentration (X2) and cross-linking time (X3) as independent variables while mucoadhesive strength (Y1) and particle size (Y2) of the microspheres were the dependent variables. Regression analysis was performed to identify the best formulation conditions. The microspheres were evaluated for morphology and size by SEM, entrapment efficiency, in vitro drug release, differential scanning calorimetry (DSC), X-ray diffraction (XRD), ex vivo permeation studies and stability study. The microspheres were spherical with size of 15-40 μm, which is favorable for intranasal absorption. The shape and surface characteristics were studied by scanning electron microscopy (SEM) which showed that the microspheres were spherical in nature with nearly smooth surface. The entrapment efficiency was observed from 90 to 98% while percentage mucoadhesion was from 78 to 86%. The microspheres released around 87% of drug in 12 h. DSC and XRD studies revealed that sertraline hydrochloride was molecularly dispersed in the microspheres. It was concluded that chitosan microspheres could be used to deliver sertraline hydrochloride following nasal administration for avoiding first pass metabolism and improving the bioavailability.
What will audience learn from your presentation?
- All those who are interested in applications of biomaterials in healthcare will enjoy the presentation.
- The audience will get an overview on biomaterials in development of drug delivery systems.
- The audience will also learn about development of microparticles for nasal administration.
- The talk will help understand the systematic approach for designing the experiment with the help of factorial design.