Spray-dried nanoparticle-loaded pectin microspheres for dexamethasone nasal delivery

Abstract

In this study, we present the development of an innovative dry powder dexamethasone (Dex) nasal delivery system comprising Dex-loaded lipid/alginate nanoparticles incorporated within pectin microspheres (Dex/NPs-loaded pectin microspheres; DNM). DNM microspheres were characterized by the mean diameter of 2.76?±?0.10?µm, zeta-potential of –36.2?±?1.1?mV, and drug loading of 3.3?±?0.3%. The morphology study revealed irregular microsphere surface forming external voids. In contact with simulated nasal fluid, DNM microspheres demonstrated desirable property of moderate swelling and ensured stronger mucoadhesion compared with conventional Dex-loaded pectin microspheres. The strategy of Dex incorporation within the lipid/alginate NPs resulted in prolonged Dex release in relation to Dex being directly entrapped within the conventional pectin microspheres. DNM microspheres showed excellent biocompatibility and rendered Dex permeation across the selected epithelial cell model similar to that of Dex solution. In conclusion, balanced biopharmaceutical properties of the proposed nasal Dex delivery system provides the potential for prolonged contact time with nasal mucosa, prolonged therapeutic effect, and improved patient compliance.     

High temperature monoclinic-to-tetragonal phase transition in magnesium doped lanthanum ortho-niobate

Magnesium doped lanthanum ortho-niobate (La_0.98Mg_0.02NbO₄) was prepared by the molten salt synthesis method. X-ray diffraction and dilatometry methods were used to study high temperature behavior of the ceramic material. Special attention was paid to the phase transition between the monoclinic and tetragonal phases. The values of spontaneous strain on the basis of unit cell parameter, obtained by Rietveld refinement, have been calculated as well as Landau order parameter. The thermal expansion coefficient (TEC) of La_0.98Mg_0.02NbO₄ was determined to be 12×10^?6 1/K and 8×10^?6 1/K below and above 500 °C, respectively.     

Influence of Unmodified and β-Glycerophosphate Cross-Linked Chitosan on Anti-Candida Activity of Clotrimazole in Semi-Solid Delivery Systems

The combination of an antifungal agent and drug carrier with adjunctive antimicrobial properties represents novel strategy of complex therapy in pharmaceutical technology. The goal of this study was to investigate the unmodified and ion cross-linked chitosan’s influence on anti-Candida activity of clotrimazole used as a model drug in hydrogels. It was particularly crucial to explore whether the chitosans’ structure modification by β-glycerophosphate altered its antifungal properties. Antifungal studies (performed by plate diffusion method according to CLSI reference protocol) revealed that hydrogels obtained with chitosan/β-glycerophosphate displayed lower anti-Candida effect, probably as a result of weakened polycationic properties of chitosan in the presence of ion cross-linker. Designed chitosan hydrogels with clotrimazole were found to be more efficient against tested Candida strains and showed more favorable drug release profile compared to commercially available product. These observations indicate that novel chitosan formulations may be considered as promising semi-solid delivery system of clotrimazole.     

Synthesis,characterization and in vitro degradation of poly(ester-anhydride)s based on succinic acid and 1,6-bis-p-carboxyphenoxyhexane

This paper describes synthesis and characteristics of functional poly(ester-anhydride)s bearing allyl pendant groups. The polymers were obtained by polycondensation of 1,6-bis-p-carboxyphenoxyhexane (CPH) and oligo(3-allyloxy-1,2-propylene succinate) terminated with carboxyl groups (OSAGE). The carboxyl groups in OSAGE and in CPH were converted to mixed anhydride groups by acetylation with acetic anhydride. After that, prepolymers thus obtained were condensed in vacuum to yield poly(ester-anhydride)s. The structure of copolymers was confirmed by NMR spectroscopy. Influence of molecular weight of OSAGE as well as of the CPH and OSAGE content on selected properties of poly(ester-anhydride)s was examined. Poly(ester-anhydride)s were subjected to hydrolytic degradation at 37 °C, in aqueous phosphate buffer solution of pH 7.41 (PBS). The course of degradation was monitored by determination of weight loss of samples and ¹H NMR. Fracture surfaces of samples during degradation were examined by scanning electron microscopy.     

Shaping Luminescent Properties of Yb3+ and Ho3+ Co‐Doped Upconverting Core–Shell β‐NaYF4 Nanoparticles by Dopant Distribution and Spacing

At the core of luminescence color and lifetime tuning of rare earth doped upconverting nanoparticles (UCNPs), is the understanding of the impact of the particle architecture for commonly used sensitizer (S) and activator (A) ions. In this respect, a series of core@shell NaYF₄ UCNPs doped with Yb³⁺ and Ho³⁺ ions are presented here, where the same dopant concentrations are distributed in different particle architectures following the scheme: YbHo core and YbHo@…, …@YbHo, Yb@Ho, Ho@Yb, YbHo@Yb, and Yb@YbHo core–shell NPs. As revealed by quantitative steady‐state and time‐resolved luminescence studies, the relative spatial distribution of the A and S ions in the UCNPs and their protection from surface quenching has a critical impact on their luminescence characteristics. Although the increased amount of Yb³⁺ ions boosts UCNP performance by amplifying the absorption, the Yb³⁺ ions can also efficiently dissipate the energy stored in the material through energy migration to the surface, thereby reducing the overall energy transfer efficiency to the activator ions. The results provide yet another proof that UC phosphor chemistry combined with materials engineering through intentional core@shell structures may help to fine‐tune the luminescence features of UCNPs for their specific future applications in biosensing, bioimaging, photovoltaics, and display technologies.     

Electrophoretic Deposition,Microstructure, and Corrosion Resistance of Porous Sol–Gel Glass/Polyetheretherketone Coatings on the Ti-13Nb-13Zr Alloy

Metallurgical and Materials Transactions A - In this study, microporous composite sol–gel glass/polyetheretherketone (SGG/PEEK) coatings were produced on the Ti-13Nb-13Zr titanium alloy by...