maria grazia Sarpietro

maria grazia Sarpietro
University of Catania | UNICT

About

107
Publications
10,288
Reads
How we measure 'reads'
A 'read' is counted each time someone views a publication summary (such as the title, abstract, and list of authors), clicks on a figure, or views or downloads the full-text. Learn more
3,588
Citations
Citations since 2017
27 Research Items
1921 Citations
20172018201920202021202220230100200300
20172018201920202021202220230100200300
20172018201920202021202220230100200300
20172018201920202021202220230100200300

Publications

Publications (107)
Article
Full-text available
Colorectal cancer is one of the most diffused tumoral diseases. Since most medicaments employed for its treatment are debilitating, the use of naturally derived products, which can be effective against the mutated cells and, in addition, can reduce most inflammatory-related effects, could be extremely beneficial for the continued treatment of this...
Article
Full-text available
Investigation of the interaction between drugs and biomembrane models, as a strategy to study and eventually improve drug/substrate interactions, is a crucial factor in preliminary screening. Synthesized peptides represent a source of potential anticancer and theragnostic drugs. In this study, we investigated the interaction of a novel synthesized...
Article
Full-text available
Cell membrane models are useful for obtaining molecular-level information on the interaction of biologically active molecules whose activity is believed to depend also on their effects on the membrane. Cytarabine was conjugated with fatty acids to improve the drug lipophilicity and the interaction with the biomembrane model. Cytarabine was conjugat...
Article
Full-text available
Skin is the first human barrier that is daily exposed to a broad spectrum of physical and chemical agents, which can increase reactive oxygen species (ROS) and lead to the formation of topical disorders. Antioxidant molecules, such as benzo[k,l]xanthene lignans (BXL), are ideal candidates to eliminate or minimize the effects of ROS. Herein, we aime...
Article
Full-text available
Benzo[k,l]xanthene lignans are a group of rare natural products belonging to the class of polyphenols with promising biological activities and are studied as potential chemotherapeutic agents. The lipophilic character of a xanthene core makes these molecules difficult to be used in an aqueous medium, limiting their employment in studies for pharmac...
Article
Full-text available
Histoplasma capsulatum is a dimorphic, thermal, and nutritional fungus. In the environment and at an average temperature of 28 °C, it develops as a mold that is composed of infecting particles. Once in the host or in cultures at 37 °C, it undergoes a transition into the parasitic form. In the present work, we performed chemical extraction and chara...
Article
Full-text available
The interactions of drugs with cell membranes are of primary importance for several processes involved in drugs activity. However, these interactions are very difficult to study due to the complexity of biological membranes. Lipid model membranes have been developed and used to gain insight into drug–membrane interactions. In this study, the intera...
Article
Full-text available
(1) Background: Mangiferin (MGN) is a natural compound, showing anti-inflammatory and antioxidant activities for the potential treatment of eye diseases. The poor physicochemical features of MGN (low solubility and high instability) justify its nanoencapsulation into nanostructured lipid carriers (NLC) to improve its ocular bioavailability. (2) Met...
Article
Full-text available
Naringenin (4′,5,7-trihydroxyflavanone-7-rhamnoglucosideor naringenin-7-rhamnoglucoside), a flavonoid present in large quantities in citrus, has different beneficial effects on human health as an antioxidant, free radical scavenger, anti-inflammatory, carbohydrate metabolism promoter, and immune system modulator. Different studies have shown that t...
Article
Full-text available
A synthetic dual-target mu opioid peptide receptor/delta opioid peptide receptor anti-nociceptive ligand, named LP2, has emerged as a promising candidate for the management of acute and/or persistent pain, but its lipophilicity limits further developments as a therapeutic agent. In this work, to allow designing aqueous formulations of LP2 for paren...
Article
Full-text available
Gastrointestinal cancers, particularly colorectal cancer, are mainly influenced by the dietary factor. A diet rich in fruits and vegetables can help to reduce the incidence of colorectal cancer thanks to the phenolic compounds, which possess antimutagenic and anticarcinogenic properties. Polyphenols, alongside their well-known antioxidant propertie...
Article
Full-text available
Glycyrrhetic acid (GA) and stearyl glycyrrhetinate (SG) are two interesting compounds from Glycyrrhiza glabra, showing numerous biological properties widely applied in the pharmaceutical and cosmetic fields. Despite these appreciable benefits, their potential therapeutic properties are strongly compromised due to unfavourable physical-chemical feat...
Article
Full-text available
Sinapic acid (SA), belonging to the phenylpropanoid family, and its derivatives are secondary metabolites found in the plant kingdom. In recent years, they have drawn attention because of their various biological activities, including neuroprotective effects. In this study, SA was incorporated into two different nanoparticle systems, solid lipid na...
Article
Full-text available
Lipid nanoparticles (LNPs) have been proposed as carriers for drug skin delivery and targeting. As LNPs effectiveness could be increased by the addition of chemical penetration enhancers (PE), in this work, the feasibility of incorporating PE into LNPs to improve idebenone (IDE) targeting to the skin was investigated. LNPs loading IDE 0.7% w/w were...
Article
Full-text available
Several liquid lipids have been proposed to obtain nanostructured lipid carriers (NLC) with improved efficiency. An attractive strategy is the use of oils that could elicit a synergic effect with the loaded drug. In this work, different percentages (0–4% w/w) of tocopheryl acetate (TA), an oily antioxidant, were used as liquid lipid to prepare NLC...
Article
The interaction of limonene, terpineol, and 1,8 cineol with a model of biological membrane and the absorption of the three compounds by the same model of biological membrane were studied. In addition, the possibility to use a lipophilic carrier for the transport and delivery of the compounds to the biomembrane was investigated. Differential scannin...
Article
Full-text available
Alzheimer’s disease (AD) is a neurodegenerative disorder associated with marked oxidative stress at the level of the brain. Recent studies indicate that increasing the antioxidant capacity could represent a very promising therapeutic strategy for AD treatment. Astaxanthin (AST), a powerful natural antioxidant, could be a good candidate for AD treat...
Article
The compound (+)-MR200 [(+)-methyl (1R,2S)-2-{[4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl]methyl}-1-phenylcyclopropanecarboxylate] is a selective sigma 1 (σ1) antagonist with antinociceptive effect, able to increase selective opioid receptor agonist-mediated analgesia. The parent compound (−)-MRV3 [(−)-methyl (1S,2R)-2-[(4-hydroxy-4-phenylpiperidin...
Article
Full-text available
Curcumin (CUR) has a wide range of pharmacological properties, including anti-inflammatory and antioxidant activities, and it can be considered a good candidate for the potential treatment of central nervous system (CNS) pathologies, although its use in clinical practice is compromised due to its high lipophilicity. Solid lipid nanoparticles (SLNs)...
Article
Cytarabine (1-β-d-arabinofuranosylcytosine, Ara-C), a pyrimidine nucleoside analogue, is used for the treatment of both acute and chronic myeloblastic leukemias and non-Hodgkin lymphoma. It has a very short plasma half-life and a very low oral bioavailability. To overcome these disadvantages, much effort has been focused on the design of cytarabine...
Article
Full-text available
Differential scanning calorimetry (DSC) has emerged as a helpful technique both to characterize drug delivery systems and to study their interactions with bio-membranes. In this work, we compared idebenone (IDE)-loaded solid lipid nanoparticle (SLN) interactions with bio-membranes assessed by DSC with previous in vitro skin penetration data to eval...
Article
Objectives Uridine was conjugated with fatty acids to improve the drug lipophilicity and the interaction with phospholipid bilayers. Methods The esterification reaction using carbodiimides compounds as coupling agents and a nucleophilic catalyst allowed us to synthesize tri‐acyl ester derivatives of uridine with fatty acids. Analysis of molecular...
Article
Differential scanning calorimetry (DSC) is a thermoanalytical technique which provides information on the interaction between drugs and models of cell membranes. Studies on the calorimetric behavior of hydrated phospholipids within liposomes are employed to shed light on the changes in the physico- chemical properties when interacting with drugs. I...
Article
Investigating the mechanism of action of drugs whose pharmaceutical activity is associated with cell membranes is fundamental to comprehending the biochemical and biophysical processes that occur on membrane surfaces. In this work, we investigated the interaction of an ester-type derivative of uridine, 3′,4′,6′-trimyristoyl uridine, with models for...
Article
Objectives: Naproxen, a nonsteroid anti-inflammatory drug studied for Alzheimer's disease, was conjugated with lipoamino acids (LAA) directly or through a diethylamine (EDA) spacer to improve the drug lipophilicity and the interaction with phospholipid bilayers. Methods: The interaction of naproxen and its prodrugs with biomembrane models consis...
Article
The degree to which liposomes are PEGylated is the feature, which most influences the length of the presence of stealth liposomes in the bloodstream. In order to thoroughly investigate the maximum amount of DSPE-PEG2000 that can be used to stabilize stealth liposomes, these were synthesized at different concentrations of DSPE-PEG2000 and their phys...
Article
Recent advances in nanotechnology have led to the development of nano-scale drugs and delivery systems to improve drug therapeutic effectiveness. Between the end of ′50 and the beginning of ′60, the first colloidal systems in the nano-metric range were achieved by chance. Several research highlighted the usefulness of these nano-carriers as drug de...
Article
The ability of the naturally derived compound α-hexylcinnamaldehyde (1) to interact with biomembranes and to modulate their permeability has been investigated as a strategy to reverse multidrug resistance (MDR) in cancer cells. Dimyristoylphosphatidylcholine (DMPC) multilamellar vesicles (MLVs) were used as biomembrane models, and differential scan...
Article
The ability of the flavouring sesquiterpenes β-caryophyllene and β-caryophyllene oxide to be absorbed into the cell has been investigated by an in vitro biomembrane model of multilamellar vesicles. Dimyristoylphosphatidylcholine was used as a constituent of the biomembrane and permitted the experiments to be carried out at 37.0 °C, close to body te...
Article
The antimutagenicity of α-hexylcinnamaldehyde (1), a semisynthetic and more stable derivative of cinnamaldehyde, was evaluated against common environmental pollutants in the bacterial reverse mutation assay. The pre-, co-, and post-treatment protocols were applied to assess the involvement of desmutagenic and/or bioantimutagenic mechanisms. Compoun...
Article
Interactions between paclitaxel and its squalenoyl prodrug with dimyristoylphosphatidylcholine (DMPC) monolayer at the air/water interface were studied. Paclitaxel is an antineoplastic drug, largely used as anti-cancer agents. Because its low aqueous solubility, Cremophor EL is used as excipient for its formulation. However, it has been shown that...
Article
In this study we prepared solid lipid nanoparticles (SLN), by the phase inversion temperature (PIT) method, using cetyl palmitate as solid lipid and three different non-ionic emulsifiers of the polyoxyethylene ethers family (ceteth-20, isoceteth-20, oleth-20). These SLN were loaded with different amount of idebenone (IDE), an antioxidant drug usefu...
Article
The interaction between an amphiphilic luteinizing hormone-releasing hormone (LHRH) prodrug that incorporated a lipoamino acid moiety (C12-LAA) with biological membrane models that consisted of multilamellar liposomes (MLVs) and phospholipid monolayers, was studied using Differential Scanning Calorimetry (DSC) and Langmuir-Blodgett film techniques....
Article
The new sigma ligand cis-(±)-methyl (1R,2S/1S,2R)-2-[(4-hydroxy-4-phenylpiperidin-1-yl) methyl]-1-(4-methylphenyl) cyclopropanecarboxylate [(±)-PPCC] is a promising tool for the treatment of various diseases. With the aim to investigate the absorption of (±)-PPCC by the cell membranes, in this study we evaluated the influence on thermotropic behavi...
Article
An emerging approach in pain management is the use of multitarget opioid ligands, owing an improved analgesic effect coupled to a reduced incidence of side effects. With a mu opioid receptor agonist/delta opioid receptor antagonist profile, the benzomorphan-based compound LP1 belongs to multitarget ligands class. Previous in vivo investigations sho...
Article
Full-text available
Metronomic chemotherapy supports the idea that long-term, sustained, constant administration of chemotherapeutics, currently not achievable, could be effective against numerous cancers. Particularly appealing are liposomal formulations, used to solubilize hydrophobic therapeutics and minimize side effects, while extending drug circulation time and...
Article
In this chapter we briefly introduce the main physical principles of DSC as well as related techniques. After a quick survey of the more common experimental techniques, we describe the thermodynamics and kinetics of events accompanying a heating/cooling process. We focus on lipid membranes of one or more components. Both the thermotropic and the ba...
Article
This chapter describes a method for evaluating the release of a drug by different delivery systems to biomembrane models made of multilamellar and unilamellar vesicles, using DSC techniques. First, different delivery systems as well as biomembrane models are described followed by a detailed description of the experimental protocols that are the bas...
Article
The interactions of the two resveratrol analogues 2-hydroxy-3,5,3',5'-tetramethoxystilbene (4) and 2-hydroxy-3,5,3',4'-tetramethoxystilbene (5) with model biomembranes were studied. The aim of this investigation was to highlight possible differences in the interactions with such biomembranes related to the minimal structural differences between the...
Article
Monoterpenes limonene and its metabolic derivatives, α-terpineol and 1,8-cineol, commonly found as aroma wine components, were studied for their antimutagenicity by the bacterial reverse mutation assay on different strains. Substances were also tested for their antioxidant activity, i.e. radical scavenger, chelation, reduction, and lipid peroxidati...
Article
Full-text available
Different anticancer drugs clinically approved by international regulatory organizations present poor water solubility and low stability after systemic injection. Their administration requires suitable carriers capable of maximizing therapeutic efficacy. Lipid and polymeric nanotherapeutics, particularly liposomes, are widely used to deliver chemot...
Article
3,4-Secoisopimar-4(18),7,15-trien-3-oic acid is a diterpenoid contained in the aerial parts of Salvia cinnabarina M. Martens et Galeotti which has been proved to inhibit the effect of some known mutagens, in several bacterial strains, acting as a desmutagenic agent. In order to evaluate if 3,4-Secoisopimar-4(18),7,15-trien-3-oic inactivate the muta...
Article
Full-text available
Bone-seeking (osteotropic) drug delivery systems (ODDS) represent an interesting solution for targeting different types of drugs to the bones. In particular, anticancer and antibacterial agents could take advantage of such therapeutic strategy. We have recently developed an innovative approach to this aim: a new osteotropic biomaterial was prepared...
Article
Full-text available
Differential Scanning Calorimetry was used to study the interaction of new resveratrol derivatives using dimyristoylphosphatidylcholine (DMPC) multilamellar vesicles (MLV) as biomembrane models. MLV prepared in the presence of increasing molar fractions of the following compounds: (A) 3,5,3',5'-tetramethoxystilbene, (B) 3,5,3',4'-tetramethoxystilbe...
Article
The knowledge of the interactions between solid lipid nanoparticles (SLN) and cell membranes is important to develop effective carrier systems for drug delivery applications. Loading idebenone (IDE), an antioxidant drug useful in the treatment of neurodegenerative diseases, into SLN improves IDE antioxidant activity in in vitro biological studies,...
Article
Full-text available
1,1',2-Trisnorsqualenoic acid was conjugated to paclitaxel to obtain the squalenoyl-paclitaxel prodrug with the aim to improve the incorporation in phospholipid bilayers. Differential scanning calorimetry technique was employed to compare the interaction of squalenoyl-paclitaxel prodrug and free paclitaxel with phospholipid bilayers. The possibilit...
Article
The ability of the sodium salt of 3,4-secoisopimar-4(18),7,15-trien-3-oic acid (1), a diterpenoid obtained from Salvia cinnabarina, to inhibit the genotoxic effect of ethyl methanesulfonate (a clastogenic agent) and colcemid (an aneugenic agent), was studied using a micronucleus assay on cultured human lymphocytes. Cells were treated with 1 before...
Article
Anti-inflammatory drugs represent a potential new strategy for the treatment of Alzheimer's disease (AD). The ability to cross the blood-brain barrier and to reach brain tissues is a critical point for these drugs and is strictly related to their lipophilicity. Naproxen (NAP) is a non-steroidal anti-inflammatory drug (NSAIDs) under active investiga...
Article
Nanoparticles (NPs) formed from polymers conjugated with bisphosphonates (BPs) allow the bone targeting of loaded drugs, such as doxorubicin, for the treatment of skeletal tumours. The additional antiosteoclastic effect of the conjugated BP could contribute to the inhibition of tumour-associated bone degradation. With this aim, we have produced NPs...
Article
Solid lipid nanoparticles (SLN) are regarded as interesting carriers to improve sunscreens' safety and effectiveness. In this work, surfactant effects on the physico-chemical properties of SLN loading two of the most widely used UV-filters, octylmethoxycinnamate (OMC) and butylmethoxydibenzoylmethane (BMBM), were evaluated and the interactions betw...
Article
Amphiphilic biodegradable copolymers, for their ability to self-assemble into micelle-like aggregates, with a suitable loading capacity, are of emerging interest for the delivery of water-insoluble drugs. α,β-Poly[(N-hydroxyethyl)-dl-aspartamide] (PHEA) is suitable to obtain amphiphilic graft copolymers. These copolymers can be obtained starting fr...
Article
Full-text available
Solid lipid nanoparticles (SLN) are regarded as interesting drug delivery systems and their preparation techniques have gained a great deal of attention. To evaluate the feasibility of preparing idebenone (IDE) loaded SLN from O/W microemulsions by the phase-inversion temperature (PIT) method. Since SLN have been proposed to improve drug delivery t...
Article
The present study concerns the in vitro and in vivo evaluation of benzocaine (BENZO) and lidocaine (LIDO) topical delivery from nanostructured lipid carriers (NLCs). Morphology and dimensional distribution of NLCs have been, respectively, characterized by differential scanning calorimetry (DSC) and photon correlation spectroscopy. The release patte...
Article
Cytarabine (1-β-D-arabinofuranosylcytosine, Ara-C), a pyrimidine nucleoside analogue, is an attractive therapeutic agent for the treatment of both acute and chronic myeloblastic leukemias. 1,1',2-tris-nor-Squalene acid (squaleneCOOH) has been conjugated to cytarabine with the formation of the squalenoyl-cytarabine prodrug, in order to improve the d...
Article
Insight into the forces governing a system is essential for understanding its behavior and function. Thermodynamic investigations provide a wealth of information that is not, or is hardly, available from other methods. This article reviews thermodynamic approaches and assays to measure collective properties such as heat adsorption / emission and vo...
Article
The release of bioactive molecules by different delivery systems has been studied. We have proposed a protocol that takes into account a system that is able to carry out the uptake of a bioactive molecule released during the time, resembling an in vivo-like system, and for this reason we have used biomembrane models represented by multi-lamellar an...
Article
We derive an elementary phenomenological lattice hole model to describe the complex behavior of the excess surface area as a function of the composition in two-component monolayers. The model accounts for the coupling between the composition fluctuations and the density (holes) concentration in mixed films. When the composition fluctuations are lar...
Chapter
Lipid bilayer is the most simple model of the cell membrane which retains many of its properties even in the absence of proteins. Its formation, structure and properties rely on a subtle combination of different physical forces as well as on the unique chemical nature of the lipid molecules constituted by a polar head covalently linked to a long hy...
Article
Acyclovir has been conjugated to the acyclic isoprenoid chain of squalene to form the squalenoyl-acyclovir prodrug. Its interaction with biomembrane models constituted by dimyristoylphosphatidylcholine (DMPC) monolayers has been studied by employing the Langmuir-Blodgett technique. The aim of the work was to gain information on the interaction of t...
Article
Omega-3 fatty acids, contained in vegetables and fish, exert several beneficial effects on the human health. The interaction of three omega-3 fatty acids (linolenic acid, docosapentaenoic acid and docosahexaenoic acid) with and their absorption by biomembrane models (represented by dimyristoylphosphatidylcholine multilamellar and unilamellar vesicl...
Article
E-3,5,4'-trimethoxystilbene (TMS) is a naturally occurring analog of resveratrol. The anti-neoplastic, antiallergic and anti-angiogenic activities of TMS have been recently reported. From the viewpoint of metabolism, TMS may be more favourable than resveratrol because all of its hydroxyl groups, which are subjected to extensive glucuronide or sulph...
Article
The interaction of eicosapentaenoic acid, a polyunsaturated fatty acid belonging to the omega-3 class, with biomembrane models represented by multilamellar or unilamellar vesicles made of dimyristoylphosphatidylcholine was monitored by means of differential scanning calorimetry technique. The calorimetric analysis of vesicle prepared in the presenc...
Article
Differential scanning calorimetry was used to study the interaction of acyclovir and its prodrug squalenoyl-acyclovir (obtained by conjugation of 1,1',2-tris-nor-squalene acid (squaleneCOOH) with acyclovir) with biomembrane models made of DMPC multilamellar vesicles with the aim to verify whether a stronger interaction of the prodrug with respect t...
Article
Diethyltoluamide and ethylhexyl p-methoxycinnamate (OMC) are two active ingredients in insect repellent and sunscreen products, respectively. The concurrent application of these two substances often increases their systemic absorption, compromising the safety and efficiency of the cosmetic product. In this study, diethyltoluamide and OMC were incor...
Article
The antifungal activity and in vitro toxicity toward animal cells of two inhibitors of oxidosqualene cyclase, squalene bis-diethylamine (SBD) and squalene bis-diethylmethylammonium iodide (SBDI) were studied. Minimum inhibitory concentration (MIC) against dermatophytes and other fungi involved in cutaneous and systemic infections (12 isolates from...
Article
Full-text available
Osteotropic drug-delivery systems have been proposed as a means to provide drugs with affinity to bone tissues. Drugs or proteins have been linked chemically to bone-seeking agents, such as bisphosphonates (BPs); alternatively, drug-loaded nanoparticles have been used to target specific tissues, such as tumor areas. In our current research, these a...
Article
Inulin has been derivatized with methacrylic anhydride (MA) and succinic anhydride (SA) to obtain a methacrylated/succinilated derivative (INU-MA-SA) able to produce a pH sensitive hydrogel after UV irradiation. The hydrogel was characterized and loaded with diflunisal (10.4, 17 and 24%, w/w) chosen as a model drug. The drug release from INU-MA-SA-...
Article
A differential scanning calorimetry study was carried out to investigate the effect exerted by immunogenic synthetic lipopeptides obtained by the conjugation of LCMV33–41 peptide with lipoamino acids (Laas) bearing different alkyl chain lengths (C12 and C16) and number of chains (2 × C12) on the thermotropic behaviour of dimyristoylphosphatidylchol...
Article
Nanoparticles made of a conjugate of poly(D,L-lactide-co-glycolide) with alendronate (PLGA-ALE NPs), were prepared by emulsion/solvent evaporation technique. The conjugation yield, determined by MALDI TOF analysis, was 30-35%. PLGA-ALE NPs size, evaluated by photon correlation spectroscopy, was 198.7+/-0.2 nm. Haemocompatibility studies using diffe...
Article
To demonstrate the relationship between the structure of nitro-polycyclic aromatic hydrocarbons and their effect on biomembranes, we have investigated the influence of three structurally different nitropolycyclic aromatic hydrocarbons, 2-nitrofluorene, 2,7-dinitrofluorene and 3-nitrofluoranthene, on the thermotropic behavior of dimyristoylphosphati...
Article
Molecular interactions between gemcitabine, alone or conjugated with squalene to form the gem-squalene prodrug, with dimyristoylphosphatidylcholine have been investigated by differential scanning calorimetry and Langmuir film balance techniques to gain information about the interaction of gemcitabine and its prodrug with mammalian cell membranes an...