Title : Polysaccharide-based microcarriers for nanoencapsulated galantamine hydrobromide
Abstract:
The treatment of neurodegenerative diseases has always been a significant challenge, with the blood-brain barrier limiting the penetration of various therapeutic molecules into the brain after oral or parenteral administration. Intranasal drug administration is viewed by many researchers as a promising alternative, which can solve problems associated with decreased drug absorption, reduced stability or rapid metabolism.
Aim: The present study aimed at developing polymeric microspheres as a drug delivery system for nasal administration of galantamine hydrobromide pre-incorporated into poly-ε-caprolactone nanostructures.
Materials and Methods: Drug-loaded poly ε-caprolactone nanoparticles were prepared by a double-emulsification technique (W/O/W-type multiple emulsion) with subsequent solvent evaporation. By a spray-drying method, the resulting nanostructures were incorporated into a microsized matrix of fucoidan and sodium alginate. To establish an optimal ratio between the two polysaccharide carriers used, their concentrations in the sprayed solutions were varied by applying a 32 full factorial design. The developed nanocomposite microparticles were characterized in terms of production yield and average particle size, and the influence of fucoidan and alginate concentration on these characteristics was evaluated. The shape and surface morphology of the particles were observed by scanning electron microscopy and the particle size distribution was determined using laser diffraction. The obtained optimal nano- and micro-structures were analyzed for drug loading and drug encapsulation efficiency.
Results and discussion: The solvent evaporation emulsification technique allows the preparation of poly ε-caprolactone nanoparticles with a high yield and suitable dimensions for “nose-to-brain” delivery of galantamine. Spray-dried nanocomposite microspheres of fucoidan and sodium alginate have a medium size in the range of 5 to 10 µm, which can be considered as suitable for nasal administration. The model, obtained by spray-drying a solution with a low level of fucoidan concentration and a high level of sodium alginate concentration was the most optimal in terms of production yield.
Conclusion: In conclusion, the proposed nanocomposite microsphere models can be a promising prerequisite for the development of an innovative and convenient drug-delivery system for the nasal administration of galantamine in the therapy of neurodegenerative diseases.
Acknowledgments: This research was funded by the European Union-NextGenerationEU, through the National Recovery and Resilience Plan of the Republic of Bulgaria project number BG-RRP-2.004-0007-C01.
