Spray-dried alginate microparticles for potential intranasal delivery of ropinirole hydrochloride: development, characterization and histopathological evaluation.
Ropinirole hydrochloride (RH) is an anti-Parkinson drug with relativity low oral bioavailability owing to its extensive hepatic first pass metabolism. Spray-dried mucoadhesive alginate microspheres of RH were developed and characterized followed by histopathological evaluation using nasal tissue isolated from sheep. Spherical microparticles having high product yield (around 70%) were obtained when the inlet temperature of spray drying was 140 °C. Fourier Transform Infrared (FTIR) studies revealed the compatibility of the drug with the polymer, and scanning electron microscopy (SEM) showed that drug-loaded microparticles were spherical, and the apparent surface roughness was inversely related to the ratio of polymer to drug. Furthermore, size of the spray-dried particles were in the range of 2.5-4.37 µm, depending on formulation. All formulations had high drug encapsulation efficiencies (101-106%). Drug loaded into the polymeric particles was in the amorphous state and drug molecules were molecularly dispersed in the polymeric matrix of the microparticles which were revealed by X-ray diffraction and differential scanning calorimetry (DSC), respectively. The in vitro drug release was influenced by polymer concentration. Histopathological study demonstrated that RH-loaded sodium alginate microparticles was safe to nasal epithelium. In conclusion, spray drying of RH using sodium alginate polymer has produced microparticles of suitable characteristics for potential intranasal administration.
['Hussein|Nozad|N|', 'Omer|Huner|H|', 'Ismael|Ava|A|', 'Albed Alhnan|Mohamed|M|', 'Elhissi|Abdelbary|A|', 'Ahmed|Waqar|W|']
D000281:Administration, Intranasal D000464:Alginates D000818:Animals D000978:Antiparkinson Agents D002152:Calorimetry, Differential Scanning D004337:Drug Carriers D016503:Drug Delivery Systems D065546:Drug Liberation D007211:Indoles D008863:Microspheres D009297:Nasal Mucosa D010316:Particle Size D012756:Sheep D013696:Temperature D014961:X-Ray Diffraction
ropinirole hydrochloride microspheres spray drying sodium alginate CNS nose