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Abstract: “Ready to use” products for the coating of solid dosage forms are constituted by film forming polymers and suitable additives in a fixed ratio. Despite the wide literature available for the single polymers and the impact of additives on their properties, the uncertainty on the composition of the “ready to use” products (for patent reasons) make their behaviour still not well known, at least outside the suggested conditions of use. Among the “ready to use” products, some of them, especially those for coloured films, are formed by two different formulated blends to mix together. The aim of this work is the characterization of one of these coating systems, the Sepifilm–Sepisperse platform, in terms of rheological properties of water dispersions and of thermo-mechanical properties of the free films, highlighting the effect of the ratio of the two products that have to be added together. Polymeric water dispersions were prepared with different concentrations of Sepifilm and several ratios of Sepifilm–Sepisperse. The prepared systems were then analysed in terms of viscosity and viscoelasticity. The results highlighted in both cases that it is the film former polymer concentration to mainly influence the system features. Polymeric free films were prepared by casting the water dispersion and drying the films at ambient conditions. The films were analysed by DMA applying tests able to characterize rheological and thermal properties. The results showed that the ratio of the two products influences the final free film properties, both in terms of glassy phase stiffness and transition from glassy to rubbery phase (glass transition, activation energy and fragility). [Copyright &y& Elsevier]

PLGA-PEG-PLGA are copolymers, able to form temperature-dependent hydrogels or sol dispersions at selective conditions. A general overview about the rheological characterization of their aqueous dispersions, focusing how the structural characteristics (e.g. molecular weight, PEG/PLGA ratio) affect their temperature-dependent behaviour, is presented. Different PLGA-PEG-PLGA were synthesized by varying the amount of lactide and glycolide and the amount and molecular weight of PEG. All polymers were characterized by gel-permeation chromatography and differential scanning calorimetry. Then, polymeric dispersions in water (15%–25% w/w) were analysed by oscillatory rheological measurements. At solid state, all copolymers are amorphous and the calculated glass transition temperatures were dependent on PEG/PLGA ratio. As regard aqueous dispersions, the temperature-dependent rheological behaviour named "partially thermogelling" has been described, in addition to the commonly reported thermogelling one. In these samples, the consistency increases over temperature without forming a three-dimensional network as for real hydrogels. All rheological characteristics can be explained according to the proposed categorization (thermogel, partial thermogel and sol dispersion). Image 1 • All PLGA-PEG-PLGA copolymers are amorphous; T g values were dependent on the PEG/PLGA. • Aqueous dispersions were categorised in terms of temperature-dependent behaviour. • Partial thermogelling, thermogelling and sol rheological behaviours were described. • In partially thermogels, consistency increases over temperature without a 3D network. • Thermogels were observed for copolymers having a PEG/PLGA ratio around 0.45–0.5. [ABSTRACT FROM AUTHOR]

High-resolution ultrasound spectroscopy (HR-US) is a spectroscopic technique using ultrasound waves at high frequencies to investigate the structural properties of dispersed materials. This technique is able to monitor the variation of ultrasound parameters (sound speed and attenuation) due to the interaction of ultrasound waves with samples as a function of temperature and concentration. Despite being employed for the characterization of several colloidal systems, there is a lack in the literature regarding the comparison between the potential of HR-US for the determination of phospholipid thermal transitions and that of other common techniques both for loaded or unloaded liposomes. Thermal transitions of liposomes composed of pure phospholipids (dimyristoylphosphatidylcholine, DMPC; dipalmitoylphosphatidylcholine, DPPC and distearoylphosphatidylcholine, DSPC), cholesterol and their mixtures were investigated by HR-US in comparison to the most commonly employed microcalorimetry (mDSC) and dynamic light scattering (DLS). Moreover, tramadol hydrochloride, caffeine or miconazole nitrate as model drugs were loaded in DPPC liposomes to study the effect of their incorporation on thermal properties of a phospholipid bilayer. HR-US provided the determination of phospholipid sol-gel transition temperatures from both attenuation and sound speed that are comparable to those calculated by mDSC and DLS techniques for all analysed liposomal dispersions, both loaded and unloaded. Therefore, HR-US is proposed here as an alternative technique to determine the transition temperature of phospholipid membrane in liposomes. [ABSTRACT FROM AUTHOR]

Graphical abstract Abstract Liposomes are lamellar nanovesicles made of phospholipids of a great interest as drug delivery carriers, able to encapsulate both hydrophilic and lipophilic compounds. Some liposomal formulations have reached the market, including the doxorubicin loaded PEGylated liposomal dispersion Doxil®. The aim of the work was to investigate the possibility of concentrating liposomes through the ultrafiltration process under nitrogen pressure, using Doxil® formulation as a model. The concentrated liposomal dispersions (4x and 8x) obtained from Doxil® were characterised in terms of size evolution (dynamic light scattering), morphology (cryo-TEM) and thermal behaviour (microcalorimetry, mDSC and high-resolution ultrasonic spectroscopy, HR-US) and compared to the unloaded liposomes of the same composition. The ultrafiltration process resulted to be effective in concentrating both loaded and unloaded liposomal dispersions, which showed a particle size and thermal properties comparable to those of the non concentrated ones. Moreover, all liposomal dispersions did not show any remarkable variation in term of particle size distribution and morphology for at least 8 weeks after concentration. Altogether, results demonstrated the effectiveness in using ultrafiltration as a methodology to concentrate both loaded and unloaded liposomes without affecting the quality of the processed product. [ABSTRACT FROM AUTHOR]

[Display omitted] Hand sanitizers represent a primary measure for the prevention of transmissible infections, whose use has been greatly increased during CoViD-19 pandemic. Most of the commercially available products are hydrogels, employing carbomers as thickening agents. However, few information is still available regarding performances of carbomers in hydroalcoholic media containing a percentage of alcohols ≥ 60% v/v as recommended for disinfection. The aim of this study was to investigate the colloidal behaviour of carbomer 974 and carbomer 980 in hydroalcoholic media containing from 50 to 80% w/w of alcohol (ethanol or isopropanol) and neutralised with triethanolamine or aminomethyl propanol. Both carbomers provide transparent hydrogels in water, but carbomer 980 should be preferred for the formulation of hydrogel with a percentage of alcohol ≥ 50% w/w for its better solvation. The critical alcohol concentration (CAlC), above which polymer precipitation occurs, depends on the type of alcohol and base used. Carbomer dispersions with a higher content of alcohol can be prepared using aminomethyl propanol rather than triethanolamine. The choice of the more suitable components is fundamental for the isopropanol-based dispersions since the CAlC is closer to the recommended concentrations for disinfection. Overall, these results provide helpful insights for the correct preparation of alcohol-based hand sanitizers using carbomers. [ABSTRACT FROM AUTHOR]

Soluplus® is a graft copolymer, with PEG and vinylcaprolactam/vinyl acetate side chains, recently available as excipient used to promote fast drug release in pharmaceutical dosage forms and as solubility enhancer. Despite this copolymer is reported to be able to act as a thickening additive and even as gelling agent as a function of temperature, there is a lack of information about the physical-chemical properties of its water dispersions. Thus, the aim of this paper is to investigate the influence of Soluplus® concentration and experimental temperature on the modification of the rheological properties of Soluplus® water dispersions. The results clearly indicated the influence of both the studied parameters and of their interactions on the Soluplus® thickening ability. Although some systems appear gel by human perception at 37 °C, the mechanical spectra demonstrated the lack of the formation of a tridimensional network structure. Overall, in all the analyzed temperatures and concentrations, the systems always behave as a 'rheological' dilute or semidilute polymer solution. [ABSTRACT FROM AUTHOR]