4.6 Article

Developing Nanosuspension Loaded with Azelastine for Potential Nasal Drug Delivery: Determination of Proinflammatory Interleukin IL-4 mRNA Expression and Industrial Scale-Up Strategy

Journal

ACS OMEGA
Volume 8, Issue 26, Pages 23812-23824

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acsomega.3c02186

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In this study, an azelastine nasal spray based on nanosuspension was created to improve bioavailability and intranasal absorption. Chondroitin was used as a polymer to prepare the nanosuspension through precipitation. The optimized nanosuspension showed a particle size of 500nm, a polydispersity index of 0.276, and a negative potential of -20mV. Characterization tests and assays were conducted to evaluate the properties and performance of the nanosuspension. The results demonstrated that the azelastine nanosuspension had great potential for the intranasal treatment of allergic rhinitis with improved permeability and bioavailability.
In order to increasebioavailability and intranasal absorbance,the current work set out to create azelastine nasal spray based onnanosuspension. Chondroitin was utilized as a polymer to prepare azelastinenanosuspension through the precipitation procedure. A size of 500nm and a polydispersity index of 0.276 with a negative potential (-20mV) were achieved. X-ray diffraction, scanning electron microscopy,Fourier transform infrared spectroscopy, thermal analysis includingdifferential scanning calorimetry and thermogravimetric analysis,in vitro release, and diffusion studies were used to characterizethe optimized nanosuspension. MTT assay was used to assess the viabilityof the cells, and hemolysis assay was used to assess the blood compatibility.Using RNA extraction and reverse transcription polymerase chain reaction,the levels of the anti-inflammatory cytokine IL-4, which is most closelyrelated to cytokines in allergic rhinitis, were measured in mouselungs. The drug dissolution and diffusion study indicated 2.0-foldincrease compared to pure reference sample. Therefore, the azelastinenanosuspension could be suggested as a practical and simple nanosystemfor intranasal delivery with improved permeability and bioavailability.The outcome obtained in this study indicated that azelastine nanosuspensionhas great potential to treat allergic rhinitis as intranasal treatment.

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