Ethosomes for skin delivery of ropivacaine: preparation, characterization and ex vivo penetration properties.

Ropivacaine, a novel long-acting local anesthetic, has been proved to own superior advantage. However, Naropin® Injection, the applied form in clinic, can cause patient non-convenience. The purpose of this study was to formulate ropivacaine (RPV) in ethosomes and evaluate the potential of ethosome formulation in delivering RPV transdermally. The RPV-loaded ethosomes were prepared with thin-film dispersion technique and the formulation was characterized in terms of size, zeta potential, differential scanning calorimetry (DSC) analysis and X-ray diffraction (XRD) study. The results showed that the optimized RPV-ethosomes displayed a typical lipid bilayer structure with a narrow size distribution of 73.86 ± 2.40 nm and drug loading of 8.27 ± 0.37%, EE of 68.92 ± 0.29%. The results of DSC and XRD study indicated that RPV was in amorphous state when encapsulated into ethosomes. Furthermore, the results of ex vivo permeation study proved that RPV-ethosomes could promote the permeability in a high-efficient, rapid way (349.0 ± 11.5 µg cm(-2) at 12 h and 178.8 ± 7.1 µg cm(-2) at 0.5 h). The outcomes of histopathology study forecasted that the interaction between ethosomes and skin could loosen the tight conjugation of corneocyte layers and weaken the permeation barrier. In conclusion, RPV-ethosomes could be a promising delivery system to encapsulate RPV and deliver RPV for transdermal administration.

Luteolin-loaded biocomposites containing tantalum and polyimide with antibacterial effects for facilitating osteogenic differentiation and bone bonding.

Polymer-based composites are considered promising candidates for bone repair as they possess some outstanding advantages over ceramic/metallic/polymeric biomaterials. Tantalum (Ta)/polyimide (PI) biocomposites (PT) containing 20 v% (PT20) and 40 v% (PT40) Ta nanoparticles were fabricated, and luteolin (LU) was loaded on PT40 (LUPT40). Compared with PT20 and PI, PT40 with a high Ta content displayed high surface behaviors (e.g., roughness, surface energy, and hydrophilicity). PT40 remarkably improved cell adhesion and multiplication, and LUPT40 with LU displayed further enhancement in vitro. Moreover, LUPT40 evidently boosted osteoblastic differentiation while suppressing osteoclastic differentiation. Furthermore, LUPT40 exhibited good antibacterial effects because of the slow release of LU. The in vivo results confirmed that PT40 markedly promoted bone formation and LUPT40 further enhanced bone formation/bone bonding. In brief, the incorporation of Ta particles improved the surface behaviors of PT40, which stimulated cell response/bone formation. Moreover, the slow release of LU from LUPT40 not only promoted cell response/bone formation but also enhanced bone bonding. The synergistic effects of Ta and LU release from LUPT40 enhanced bone formation/bone bonding. Therefore, LUPT40 would have great potential for the repair of bear-loading bone.

Simultaneous incorporation of gallium oxide and tantalum microparticles into micro-arc oxidation coating of titanium possessing antibacterial effect and stimulating cellular response.

Orthopedic implants with both osteogenesis and antibacterial functions are particularly promising for bone repair and substitutes. In this study, a micro-arc oxidation (MAO) coating containing titanium dioxide (TiO2), gallium oxide (Ga2O3) and tantalum oxide (Ta2O5) on the titanium surface (MGT) was fabricated by dispersing Ga2O3 and Ta microparticles in the electrolyte. The results showed that the simultaneous incorporation of Ga2O3 and Ta microparticles into the MAO coating resulted in optimized surface performance (e.g., micro-topography, roughness, wettability, surface energy, and protein absorption) of MGT compared with pure titanium (pTi). In addition, MGT exhibited outstanding corrosion resistance owing to the presence of both Ga2O3 and Ta microparticles, which exhibit excellent corrosion resistance and their microparticles were incorporated into the micropores of the coating. Moreover, MGT with good cytocompatibility and optimized surface resulted in improved cellular responses (e.g., proliferation and osteogenic differentiation) of rat bone mesenchymal stem cells, which was attributed to Ta microparticles with outstanding osteogenic bioactivity. Furthermore, the excellent antibacterial effect of MGT was attributed to the slow release of Ga3+ from the coating. Thus, the simultaneous incorporation of Ga2O3 and Ta microparticles into the MAO coating of MGT exhibited excellent cytocompatibility, osteogenic bioactivity, antibacterial functions, and corrosion resistance, suggesting that MGT possesses great potential for bone repair applications.