Thermogelling amphiphilic block copolymers have been widely investigated in the development of pharmaceutical drug carriers. In particular, thermosensitive gels based on poloxamer 407 (P407) have great potential for periodontal disease treatment, thanks to their ability to be liquid at room temperature and become viscous gels at body temperature. However, some problems, related to short in situ residence time, reduce their feasible clinical use. Thus, in order to improve the effective applicability of these materials, we studied how P407 thermogels are affected by the pH and by the inclusion of different hydrophilic polymers, used as excipients for increasing the gel stiffness. For this scope, a complete chemical-physical characterization of the synthesized gels is provided, in terms of determination of sol-gel transition temperature, viscosity and erosion degree. The data are correlated according to a statistical multivariate approach based on Principal Component Analysis and their mucoadhesion properties are also tested by Tapping mode-Atomic Force Microscopy (TM-AFM) imaging. Finally, we studied how the different P407 formulations are able to influence the release pathway of two antibacterial drugs (i.e., chlorhexidine digluconate and doxycycline hyclate) largely used in oral diseases.
24 January 2020 in The Journal of Organic Chemistry
The synthesis of cyclohepta[b]indole derivatives through dearomative (4+3) cycloaddition reaction of 2-vinylindoles or 4H-furo[3,2-b]indoles with in situ generated oxyallyl cations is reported. Oxyallyl cations are generated from α-bromoketones in the presence of a base and a perfluorinated solvent. Cyclohepta[b]indole scaffolds are obtained under mild reaction conditions, in the absence of expensive catalysts, starting from simple reagents, in good to excellent yields and with complete diasteroselectivity. Preliminary expansion of the scope to 3-vinylindoles and to aza-oxyallyl cations is reported.
The development of Fricke gel (FG) dosimeters based on poly(vinyl alcohol) (PVA) as the gelling agent and glutaraldehyde (GTA) as the cross-linker has enabled significant improvements in the dose response and the stability over time of spatial radiation dose distributions. However, a standard procedure for preparing FG in terms of reagent concentrations is still missing in the literature. This study aims to investigate, by means of spectrophotometric analyses, how the sensitivity to the radiation dose and the range of linearity of the dose–response curve of PVA-GTA-FG dosimeters loaded with xylenol orange sodium salt (XO) are influenced by ferrous ammonium sulphate (FAS) and XO concentrations. Moreover, the effect of different concentrations of such compounds on self-oxidation phenomena in the dosimeters was evaluated. PVA-GTA-FG dosimeters were prepared using XO concentrations in the range 0.04–0.80 mM and FAS in the range 0.05–5.00 mM. The optical absorbance properties and the dose response of FG were investigated in the interval 0.0–42.0 Gy. The results demonstrate that the amount of FAS and XO determines both the sensitivity to the absorbed dose and the interval of linearity of the dose–response curve. The study suggests that the best performances of FG dosimeters for spectrophotometric analyses can be obtained using 1.00–0.40 mM and 0.200–0.166 mM concentrations of FAS and XO, respectively.
Biological methods for mosquito larvae control are completely biodegradable and have null or limited effects on nontarget organisms. However, commercially available products have a low residual activity, with the consequent need for multiple applications that inevitably increase costs and the risk of resistance phenomena insurgence. Smart delivery systems made of hydrogels proved their efficacy in increasing the action duration of biolarvicides up to several months, but the lack of an efficient baiting mechanism to strongly attract the target pest remains a problem in practical applications. In this work, we investigated two novel hydrogel-based formulations of completely natural composition for baiting and killing larvae of Aedes albopictus mosquitos. The proposed materials consist of charged crosslinked polysaccharides (chitosan and cellulose) and are specifically manufactured to float in water, simulating organic matter usually present at breeding sites. Within the hydrogels’ matrix, yeast colonies of Saccharomyces cerevisiae were embedded as phagostimulants alongside a biolarvicide (Bacillus thuringiensis var. israelensis (Bti)). Despite the similar chemical nature and structure, chitosan-based hydrogels exhibited a markedly superior baiting potential compared to those made of cellulose and also succeeded in efficiently killing mosquito larvae just after a few hours from administration. We are confident that the proposed smart delivery hydrogel made of chitosan can be an enabling tool to attract mosquito larvae towards biopesticides of different nature without delocalizing active ingredients away from the breeding site and to simultaneously increase their residual activity, thus holding the potential of minimizing environmental pollution related to pest control and vector-borne disease prevention.
21 November 2023 in Journal of Physics D: Applied Physics
A double network hydrogel based on Poly(vinyl-alcohol) (PVA) cross-linked with Glutaraldehyde (GTA) was recently developed by using self-assembling phenylalanine (Phe) peptide derivative (Fmoc-Phe-Phe-OMe), with the aim to improve the mechanical-elastic properties of PVA-GTA hydrogels. In this study, a characterization of the properties of Xylenol Orange based Fricke gel dosimeters obtained by infusing a Fricke solution into the double network hydrogel was performed. The gel dosimeters were irradiated with 6 MV and 15 MV X-rays produced by a medical linear accelerator and investigated by means optical absorbance measurements. The double network hydrogel formulation maintained a satisfactory level of radiological water-equivalence within the investigated radiotherapy range. Fricke gel dosimeters prepared with such network kept the desired properties of independence of the response of the dose rate and energy in the investigated intervals. Furthermore, the addition of self-assembling Phe peptide derivative proved not avoid the motion of radio-inducted ferric ions into the hydrogel, probably maintaining the main characteristics of the standard, no Phe peptide infused, formulation. The time course of formation of the optical response after the irradiation was observed to be similar to what previously measured in traditional PVA-GTA Fricke gel dosimeters, while a decrease of the sensitivity to radiation dose of the order of 30% was found. The extent of the decrease does not seem such as to impair the use of these dosimeters for evaluation of doses typical of radiation therapy applications. The overall dosimetric properties, coupled with the mechanical-elastic characteristics of the double network hydrogel, pave theway to the development of phantoms able both to mimic the deformation of organs possibly occurring during radiotherapy treatments and at the same time to assess the 3D dose distribution within such volumes.
30 March 2020 in European Journal of Organic Chemistry