Drug delivery to the brain represents a challenge, especially in the therapy of central nervous system malignancies. Simvastatin (SVT), as with other statins, has shown potential anticancer properties that are difficult to exploit in the central nervous system (CNS). In the present work the physico–chemical, mucoadhesive, and permeability-enhancing properties of simvastatin-loaded poly-ε-caprolactone nanocapsules coated with chitosan for nose-to-brain administration were investigated. Lipid-core nanocapsules coated with chitosan (LNCchit) of different molecular weight (MW) were prepared by a novel one-pot technique, and characterized for particle size, surface charge, particle number density, morphology, drug encapsulation efficiency, interaction between surface nanocapsules with mucin, drug release, and permeability across two nasal mucosa models. Results show that all formulations presented adequate particle sizes (below 220 nm), positive surface charge, narrow droplet size distribution (PDI < 0.2), and high encapsulation efficiency. Nanocapsules presented controlled drug release and mucoadhesive properties that are dependent on the MW of the coating chitosan. The results of permeation across the RPMI 2650 human nasal cell line evidenced that LNCchit increased the permeation of SVT. In particular, the amount of SVT that permeated after 4 hr for nanocapsules coated with low-MW chitosan, high-MW chitosan, and control SVT was 13.9 ± 0.8 μg, 9.2 ± 1.2 µg, and 1.4 ± 0.2 µg, respectively. These results were confirmed by SVT ex vivo permeation across rabbit nasal mucosa. This study highlighted the suitability of LNCchit as a promising strategy for the administration of simvastatin for a nose-to-brain approach for the therapy of brain tumors.
Some treatment options available to repair bone defects are the use of autogenous and allogeneic bone grafts. The drawback of the first one is the donor site’s limitation and the need for a second operation on the same patient. In the allograft method, the problems are associated with transmitted diseases and high susceptibility to rejection. As an alternative to biological grafts, polymers can be used in bone repair. Some polymers used in the orthopedic field are poly(methyl methacrylate), poly(ether-ether-ketone), and ultra-high molecular weight polyethylene (UHMWPE). UHMWPE has drawn much attention since it combines low friction coefficient and high wear and impact resistance. However, UHMWPE is a bioinert material, which means that it does not interact with the bone tissue. UHMWPE composites and nanocomposites with hydroxyapatite (HA) are widely studied in the literature to mitigate these issues. HA is the main component of the inorganic phase in the natural bone, and the addition of this bioactive filler to the polymeric matrix aims to mimic bone composition. This brief review discusses some polymers used in orthopedic applications, focusing on the UHMWPE/HA composites as a potential bone substitute.
Drug delivery to the brain represents a challenge especially in the therapy of central nervous system malignancies. Simvastatin (SVT), as other statins, has shown potential anticancer properties that are difficult to exploit in the CNS. In the present work the physico-chemical, mucoadhesive and permeability enhancing properties of simvastatin-loaded poly-ε-caprolactone nanocapsules coated with chitosan for nose-to-brain administration were investigated. Lipid-core nanocapsules coated with different molecular weight (MW) chitosans (LNCchit) prepared by a novel one-pot technique were characterized for particle size, surface charge, particle number density, morphology, drug encapsulation efficiency, interaction between surface nanocapsules with mucin, drug release and permeability across two nasal mucosa models. Results show that all formulations present adequate particle size (below 220 nm), positive surface charge, narrow droplet size distribution (PDI<0.2) and high encapsulation efficiency. Nanocapsules presented controlled drug release and mucoadhesive properties dependent on the MW of the coating chitosan. The results of permeation across RPMI 2650 human nasal cell line evidenced that LNCchit increased the permeation of SVT. In particular, the amount of SVT permeated after 4h for nanocapsules coated with low MW chitosan, high MW chitosan and control SVT was 13.91 ± 0.78 µg, 9.15 ± 1.23 µg and 1.42 ± 0.21 µg respectively. These results were confirmed by the SVT ex vivo permeation across rabbit nasal mucosa. This study highlighted the suitability of LNCchit as promising strategy for the administration of simvastatin for a nose-to-brain approach for the therapy of brain tumors.
Chemically modified natural fibers were introduced into a commercial biodegradable poly(butylene adipate-co-terephthalate) (PBAT) matrix to obtain composite materials in a mini-extruder. Influence of the fiber introduction on thermal and mechanical properties of the composites were studied. A decrease of the crystallinity degree of the composites was observed upon addition of the hydrolyzed-fibers, but the addition of the acetylated ones resulted in the opposite behavior. Thermal stability of the matrix was not affected by introduction of the treated fibers. However, an improvement of mechanical properties of the composites was found by means of dynamic mechanical thermal analysis and tensile tests, particularly for those containing acetylated fibers. Scanning electron micrographs of cryofractured surfaces of the composites showed stronger adhesion of the acetylated fibers to the PBAT matrix. No interfacial gaps or signs of the fiber pullout from the matrix were observed.
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