Spray-dried alginate microparticles for potential intranasal delivery of ropinirole hydrochloride: development, characterization and histopathological evaluation

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.

Microencapsulation of Bacteriophages for the Delivery to and Modulation of the Human Gut Microbiota through Milk and Cereal Products

“…Vinner et al, produced Salmonella bacteriophage Felix O1 microcapsules with Eudragit S100 ® and trehalose, with a final humidity of 9% [76]. Hussein et al, obtained 5.5-8.5% humidity in sodium alginate capsules when spray dried at different temperatures [77]. However, it is not the absolute humidity itself that matters, but the storage stability, which is discussed in more detail in Section 3.5.…”

Biocompatible mucoadhesive nanoparticles for brain targeting of ropinirole hydrochloride: Formulations, radiolabeling and biodistribution

“…Polymer ( I ) was prepared via one‐step ring opening polymerization of the monomer using ammonium heptamolybdate as a catalyst and water as an initiator (Figure 1). [ 8 ] The reaction proceeds via in situ formation of ammonium decamolybdate (NH 4 ) 8 ‐[Mo 10 O 34 ] (Dec) at high temperature which is the real catalyst of polymerization process. Characterization of polymer ( I ) was carried out using GPC, FTIR (KBr disk) and DSC measurements.…”

“…This property of chitosan-alginate polyelectrolyte nanocomplex combined with its biocompatibility, mucoadhesivity, and pH sensitivity make this PEC of great interest for controlled release of active agents, specifically for oral delivery of peptide and protein drugs. [7,8] 3.1 | Preparation of HO-PCL-COOH (I)…”

“…Polymer (I) was prepared via one-step ring opening polymerization of the monomer using ammonium heptamolybdate as a catalyst and water as an initiator (Figure 1). [8] The reaction proceeds via in situ formation of ammonium…”

“…[ 7 ] Intranasal delivery of RH as RH‐loaded spray‐dried alginate microparticles was safe to nasal epithelium with enhanced brain targeting. [ 8 ] Chitosan‐alginate polyelectrolyte nanocomplexes represent a special class of polymeric compounds comprising stoichiometric equivalents of oppositely charged polyions (polycation and polyanion) interacting together spontaneously to yield a nanocomplex.…”