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Pharm Dev Technol. 2019 Jan 10:1-36. doi: 10.1080/10837450.2019.1567762. [Epub ahead of print]

Spray-Dried Alginate Microparticles for Potential Intranasal Delivery of Ropinirole Hydrochloride: Development, Characterization and Histopathological Evaluation.

Author information

1
a School of Pharmacy and Biomedical Sciences, University of Central Lancashire , Preston , United Kingdom.
2
b College of Pharmacy, Hawler Medical University , Erbil , Iraq.
3
c Institute of Pharmaceutical Science, King's College London , Waterloo , UK.
4
d Office of Vice President for Research and Graduate Studies, Qatar University , Doha , Qatar.
5
e College of Pharmacy, Qatar University , Doha , Qatar.
6
f School of Mathematics and Physics, College of Science, University of Lincoln , UK.

Abstract

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.

KEYWORDS:

CNS; Microspheres; Nose; Ropinirole hydrochloride; Sodium alginate; Spray drying

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