Giulia Di Prima

University of Palermo

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Viviana De

University of Palermo

Giuseppe Angellotti

Institute of Nanostructured Materials

Gaetano Giammona

University of Palermo

Flavia Bongiovì

University of Palermo

Giovanna Pitarresi

University of Palermo

Elena Belfiore

University of Palermo

Mariano Licciardi

University of Palermo

Giuseppina Campisi

University of Palermo

Fabio D’Agostino

National Research Council

Fabio Salvatore Palumbo

University of Palermo

Cooperative Institutions

University of Palermo

National Research Council

University of Palermo

Institute of Nanostructured Materials

National Academies of Sciences, Engineering, and Medicine

Instituto Biofisika

Azienda Ospedaliera Universitaria Policlinico "Paolo Giaccone" di Palermo

Consorzio Roma Ricerche

National Interuniversity Consortium of Materials Science and Technology

Czech Academy of Sciences, Institute of Biophysics

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Grapefruit IntegroPectin isolation via spray drying and via freeze drying: a comparison

Giulia Di Prima Antonino Scurria Giuseppe Angellotti Elena Belfiore Mario Pagliaro

The comparison of grapefruit IntegroPectin powders isolated via spray drying and via freeze drying in terms of phenolic content, quantification of the most representative flavonoids (naringin and hesperidin), radical scavenging activity, total protein content and pH of the aqueous solutions provides relevant information. Except for the protein content, the two drying methods afford largely similar pectins. Optimization of the spray drying parameters allowed to maximize the yield of isolated pectin that nearly approached (>95%) the quantitative yield obtained via freeze drying.

Naringin

Pectin

Vacuum drying

10.26434/chemrxiv-2022-v0mn4

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Citations (0)

Inulin-Based Polymeric Micelles Functionalized with Ocular Permeation Enhancers: Improvement of Dexamethasone Permeation/Penetration through Bovine Corneas

Pharmaceutics (2021)

Giulia Di Prima Mariano Licciardi Flavia Bongiovì Giovanna Pitarresi Gaetano Giammona

Ophthalmic drug delivery is still a challenge due to the protective barriers of the eye. A common strategy to promote drug absorption is the use of ocular permeation enhancers, while an innovative approach is the use of polymeric micelles. In the present work, the two mentioned approaches were coupled by conjugating ocular permeation enhancers (PEG2000, carnitine, creatine, taurine) to an inulin-based co-polymer (INU-EDA-RA) in order to obtain self-assembling biopolymers with permeation enhancer properties for the hydrophobic drug dexamethasone (DEX). Inulin derivatives were properly synthetized, were found to expose about 2% mol/mol of enhancer molecules in the side chain, and resulted able to self-assemble at various concentrations by varying the pH and the ionic strength of the medium. Moreover, the ability of polymeric micelles to load dexamethasone was demonstrated, and size, mucoadhesiveness, and cytocompatibility against HCE cells were evaluated. Furthermore, the efficacy of the permeation enhancer was evaluated by ex vivo permeation studies to determine the performance of the used enhancers, which resulted in PEG2000 > CAR > TAU > CRE, while entrapment ability studies resulted in CAR > TAU > PEG2000 > CRE, both for fluorescent-labelled and DEX-loaded micelles. Finally, an increase in terms of calculated Kp and Ac parameters was demonstrated, compared with the values calculated for DEX suspension.

Penetration (warfare)

10.3390/pharmaceutics13091431

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Spray-Dried Cytisine-Loaded Matrices: Development of Transbuccal Sustained-Release Tablets as a Promising Tool in Smoking Cessation Therapy

Pharmaceutics (2022)

Giuseppe Angellotti Giulia Di Prima Amalia Giulia Scarpaci Fabio D’Agostino Giuseppina Campisi

Cytisine (CYT) has emerged as a promising molecule to treat nicotine addiction, since it acts as a partial agonist of nicotinic acetylcholine receptors. However, its unfavorable pharmacokinetic properties lead to multiple administrations per day, reducing the patient's compliance and increasing the side effects. To overcome these drawbacks, CYT buccal administration is here proposed. Firstly, CYT stability in the buccal environment was assessed and its intrinsic ability to permeate/penetrate the tissue was determined by applying CYT solutions at increasing concentrations. Furthermore, a spray-drying method was selected and optimized as it is an eco-friendly, easily scalable and effective technique to obtain uniform and reproducible CYT-loaded (5% w/w) pharmaceutical powders, which were directly compressed, thus obtaining different buccal delivery systems (BDSs). The obtained BDSs were homogeneous and reproducible and embedded CYT in its amorphous form. The mechanism of CYT release was evaluated in vitro and found to be mainly driven by a Fickian diffusion phenomenon. Predominantly, the ex vivo permeation assays highlighted the ability of the BDSs to enhance CYT permeation, also producing high drug fluxes through the mucosa. Speculative mathematical evaluations based on the already-known CYT pharmacokinetic parameters showed that CYT-loaded BDSs could potentially be sufficient to obtain a therapeutic effect, thus making the reported formulations suitable candidates for further in vivo trials.

Patient Compliance

10.3390/pharmaceutics14081583

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Citations (4)

α_S1-Casein-Loaded Proteo-liposomes as Potential Inhibitors in Amyloid Fibrillogenesis: In Vivo Effects on a C. elegans Model of Alzheimer’s Disease

ACS Chemical Neuroscience (2023)

Angela Paterna Pamela Santonicola Giulia Di Prima Estella Rao Samuele Raccosta

According to the amyloid hypothesis, in the early phases of Alzheimer's disease (AD), small soluble prefibrillar aggregates of the amyloid β-peptide (Aβ) interact with neuronal membranes, causing neural impairment. Such highly reactive and toxic species form spontaneously and transiently in the amyloid building pathway. A therapeutic strategy consists of the recruitment of these intermediates, thus preventing aberrant interaction with membrane components (lipids and receptors), which in turn may trigger a cascade of cellular disequilibria. Milk αs1-Casein is an intrinsically disordered protein that is able to inhibit Aβ amyloid aggregation in vitro, by sequestering transient species. In order to test αs1-Casein as an inhibitor for the treatment of AD, it needs to be delivered in the place of action. Here, we demonstrate the use of large unilamellar vesicles (LUVs) as suitable nanocarriers for αs1-Casein. Proteo-LUVs were prepared and characterized by different biophysical techniques, such as multiangle light scattering, atomic force imaging, and small-angle X-ray scattering; αs1-Casein loading was quantified by a fluorescence assay. We demonstrated on a C. elegans AD model the effectiveness of the proposed delivery strategy in vivo. Proteo-LUVs allow efficient administration of the protein, exerting a positive functional readout at very low doses while avoiding the intrinsic toxicity of αs1-Casein. Proteo-LUVs of αs1-Casein represent an effective proof of concept for the exploitation of partially disordered proteins as a therapeutic strategy in mild AD conditions.

Nanocarriers

Fibrillogenesis

Amyloid (mycology)

10.1021/acschemneuro.3c00239

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Light Scattering as an Easy Tool to Measure Vesicles Weight Concentration

Membranes (2020)

Giulia Di Prima Fabio Librizzi Rita Carrotta

Over the last few decades, liposomes have emerged as promising drug delivery systems and effective membrane models for studying biophysical and biological processes. For all applications, knowing their concentration after preparation is crucial. Thus, the development of methods for easily controlling vesicles concentration would be of great utility. A new assay is presented here, based on a suitable analysis of light scattering intensity from liposome dispersions. The method, tested for extrusion preparations, is precise, easy, fast, non-destructive and uses a tiny amount of sample. Furthermore, the scattering intensity can be measured indifferently at different angles, or even by using the elastic band obtained from a standard spectrofluorimeter. To validate the method, the measured concentrations of vesicles of different matrix compositions and sizes, measured by light scattering with different angles and instruments, were compared to the data obtained by the standard Stewart assay. Consistent results were obtained. The light scattering assay is based on the assessment of the mass fraction lost in the preparation, and can be applied for methods such as extrusion, homogenization, French press and other microfluidic procedures.

Homogenization

Matrix (chemical analysis)

10.3390/membranes10090222

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Citations (8)

Mucoadhesive micelles based on inulin derivative for ocular release of corticosteroids

Gaetano Giammona Giovanna Pitarresi Giulio Ghersi Giorgia Adamo Silvia Saladino

Derivative (finance)

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EPR Spectroscopy Coupled with Spin Trapping as an Alternative Tool to Assess and Compare the Oxidative Stability of Vegetable Oils for Cosmetics

Applied Sciences (2024)

Giulia Di Prima Viviana De Cinzia Cardamone Giuseppa Oliveri Maria Cristina D’Oca

Antioxidants are the most popular active ingredients in anti-aging cosmetics as they can restore the physiological radical balance and counteract the photoaging process. Instead of adding pure compounds into the formulations, some “precious” vegetable oils could be used due to their content of tocopherols, phenols, vitamins, etc., constituting a powerful antioxidant unsaponifiable fraction. Here, electron paramagnetic resonance (EPR) spectroscopy coupled with spin trapping was proven to provide a valid method for evaluating the antioxidant properties and the oxidative resistance of vegetable oils which, following UV irradiation, produce highly reactive radical species although hardly detectable. Extra virgin olive oil, sweet almond oil, apricot kernel oil, and jojoba oil were then evaluated by using N-t-butyl-α-phenylnitrone as a spin trapper and testing different UV irradiation times followed by incubation for 5 to 180 min at 70 °C. The EPR spectra were manipulated to obtain quantitative information useful for comparing the different tested samples. As a result, the knowledge acquired via the EPR analyses demonstrated jojoba oil as the best of the four considered oils in terms of both starting antioxidant ability and oxidative stability overtime. The obtained results confirmed the usefulness of the EPR spin trapping technique for the main proposed purpose.

Spin trapping

Vegetable oil

10.3390/app142210766

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Green next-generation excipients enriched in polyphenols from recovery of grape processing waste black bentonite: Influence of unconventional extraction solvents on antioxidant properties and composition.

Sustainable Chemistry and Pharmacy (2023)

Giulia Di Prima Elena Belfiore Giuseppe Angellotti Viviana De

According to the UN Agenda 2030, several actions could be taken to act synergistically towards various areas of critical importance for both the humanity and the planet. Among them, the application of a circular economy model based on the valorisation of the wastes from the local resources could be a virtuous attitude. In this view, this work proposes a dual green approach for recovery of the waste black bentonite from the fining of organic white grape must. Indeed, this virtuous recovery idea is enhanced by the choice of both eco-friendly extraction method (maceration) and solvents. The latter were unconventional solvents selected among the pharmaceutic/cosmetic liquid hydrophilic excipients (waste-to-market approach) characterized by safety and high solvent power toward polyphenols. PEGs (200, 400, 600), Propylene Glycol and Glycerol were tested and the extracted compared by HPLC-DAD analyses as well as the Folin-Ciocalteu, DPPH and Bradford assays. PEG200 emerged as the best one, leading to coloured extract containing great amount of polyphenols (3.123 ± 0.106 mg/g) and specifically Quercetin (60.778 ± 2.307 μg/mL), which confer it interesting scavenger properties, potentially making it directly useful in a wide range of fields from the pharmaceutic to the cosmetic ones.

Maceration (sewage)

Environmentally Friendly

Bentonite

10.1016/j.scp.2023.101414

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Citations (3)

Core-Shell Arginine-Containing Chitosan Microparticles for Enhanced Transcorneal Permeation of Drugs

Journal of Pharmaceutical Sciences (2018)

Nicolò Mauro Giulia Di Prima Paola Varvarà Mariano Licciardi Gennara Cavallaro

Mucoadhesion

10.1016/j.xphs.2018.09.034

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