Xylometazoline Loaded Chitosan Nanoparticles: Fabrication, Optimization and Evaluation for Nasal Congestion

Abstract

Aim:The present study aims at exploring the development of xylometazoline hydrochloride loaded chitosan nanoparticles (XYL-NP) cross linked with calcium chloride for the treatment of nasal congestion. Materials and Methods: XYL-NP were prepared using different polymer like chitosan, cross linking agent calcium chloride and glacial acetic acid as a solvent enhancer using ionotropic gelation method, which was further optimized and validated by Box-Behnken Design. Further, these particles were characterised for size, morphology and evaluated for its release and permeability studies. Results: XYL-NP showed a particle size of 172+0.4 nm and a PDI of 0.27. The obtained charged nanoparticles showed encapsulation efficiency of 90.5%. Transmission Electron Microscopy (TEM) and Scanning Electron Microscopy (SEM) studies showed nanoparticles have small size and smooth morphology and an in-vitro drug release of 81.2 %, following Peppas-korsemeyer release model.96.3% of the drug was permeated through the nasal mucosa of the goat in a time period of 8 hr. Conclusion: Release and permeation results shows the capability of the nanoparticles to retain large amount of XYL-NP inside the mucosa. Hence XYL-NP can be used in treating nasal congestion as the fabricated formulation has good bioadhesive and mucoadhesive property.

Chitosan Nanoparticles for Intranasal Drug Delivery

“…The table includes details such as the drug delivered, and potential therapeutic benefits, supported by corresponding references. PEG-grafted chitosan nanoparticles for insulin with pure crystalline porcine insulin Improved nasal absorption of insulin in rabbits; size range: 150-300 nm, charge: +16 to +30 mV, loading efficiency: 20-39% [42] Adaptive chitosan-based nano-vehicles with cetirizine Responsive drug release in nasal conditions, suitable for allergic therapy; size: 120 nm, zeta potential: 4 mV [43] Xylometazoline-loaded chitosan nanoparticles Effective treatment for nasal congestion with high mucosal retention; size: 172 nm, PDI: 0.27, encapsulation efficiency: 90.5% [44] Chitosan nanoparticles for galantamine delivery Improved delivery and bioavailability in Alzheimer's disease models; linearity: 0.5-300 ng mL −1 , trueness and precision: acceptable, recoveries: 85.6-114.3% [103] Chitosan nanoparticles for dihydroergotamine delivery Improved systemic absorption for acute migraine treatment via nasal delivery; size: 395 ± 59 nm, 20% loading with 95 ± 13% encapsulation efficiency, bioavailability: 82.5 ± 12.3% [104] Chitosan nanoparticles for didanosine Delivery Enhanced systemic and brain targeting for AIDS-related infections; brain/plasma, olfactory bulb/plasma, CSF/plasma concentration ratios significantly higher (p < 0.05) [105] Chitosan Nanoparticles for zidovudine delivery Improved mucoadhesion and drug flux for nasal administration; Sizes: AZT-loaded NP1 (406 nm), AZT-loaded NP2 (425 nm), Entrapment efficiency: 17.58% ± 1.48 (NP1), 11.02% ± 2.05 (NP2) [106] Silver Favipiravir-loaded chitosan-alginate nanoparticles were expertly engineered using response surface methodology to enhance the transmucosal delivery of Favipiravir (FVR). These mucoadhesive nanoparticles, termed MCS-ALG-NPs, significantly enhanced the antiviral effects of Favipiravir compared to its free form.…”

“…Xylometazoline-loaded chitosan nanoparticles were formulated to address nasal congestion, using calcium chloride cross-linking and optimized through ionotropic gelation. These nanoparticles demonstrated significant drug release and permeation through the nasal mucosa over an 8 h period, supporting their potential for effective mucosal retention and congestion treatment [ 44 ]. Chitosan-coated oil nano capsules for nasal peptide delivery were developed using the solvent displacement technique to enhance the nasal delivery of salmon calcitonin.…”

“…The initial phase of testing should focus on the detailed characterization of nanoparticles. This includes determining particle size, surface charge, and morphology, critical for understanding the basic properties that affect behavior in biological systems [ 24 , 25 , 27 , 41 , 42 , 43 , 44 , 111 , 115 , 116 , 119 , 122 , 123 , 125 , 129 ]. Advanced microscopy and spectroscopy techniques such as Scanning Electron Microscopy (SEM), Dynamic Light Scattering (DLS), and Fourier Transform Infrared Spectroscopy (FTIR) should also be employed to provide deeper insights into the physical and chemical properties of the nanoparticles [ 8 , 20 , 25 , 28 , 44 , 109 ].…”

“…Ex vivo and permeation studies should be included to assess mucoadhesion, transmucosal permeability, and the overall behavior of nanoparticles in interacting with biological barriers. Such studies are essential for applications involving targeted delivery, such as nasal or oral routes [ 22 , 24 , 25 , 27 , 44 , 116 , 120 ].…”

“…This method could offer a less invasive alternative to traditional subcutaneous injections, potentially improving patient adherence and overall quality of life. Moreover, the adaptability of chitosan nanoparticles is being explored in managing allergies, asthma, and nasal congestion, with formulations designed to address issues such as drug hydrophobicity, nasal irritation, and poor mucosal absorption [ 43 , 44 , 45 ].…”