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Publications (87)
Applying a formulation on the skin represents a patient-acceptable and therapeutically effective way to administer drugs locally and systemically. However, the stratum corneum stands as an impermeable barrier that only allows a very limited number of drugs to be distributed in the underlying tissues, limiting the feasibility of this administration...
Liver cancer is one of the most common causes of cancer death worldwide. In recent years, substantial progress has been made in the development of systemic therapies, but there is still the need for new drugs and technologies that can increase the survival and quality of life of patients. The present investigation reports the development of a lipos...
Pomalidomide (POM) is an FDA-approved immunomodulatory imide drug (IMiDs) an it is effectively used in the treatment of multiple myeloma. IMiDs are analogs of the drug thalidomide and they have been repurposed for the treatment of several diseases such as psoriatic arthritis and Kaposi Sarcoma. In recent years, IMiDs have been also evaluated as a n...
Needle-free liquid jet injectors are medical devices used to administer pharmaceutical solutions through the skin. Jet injectors generate a high-speed stream of liquid medication that can puncture the skin and deliver the drug to the underlying tissues. In this work, we investigated the feasibility of using liquid jet injectors to administer nanosu...
Liposomes are one of the most studied and most promising nanocarriers to date, representing a biocompatible, safe, and efficient delivery system for both hydrophilic and lipophilic compounds.
This work aimed to evaluate the efficacy in encapsulating an aqueous extract of Lisosan G (LG), a Triticum aestivum whole grains fermented powder with strong...
Scalability is one of the important factors slowing down or even impeding the clinical translation of nanoparticle-based systems. The latter need to be manufactured at a high level of quality, with batch-to-batch reproducibility, and need to be stable after the manufacturing process, during long-term storage and upon clinical administration. In thi...
Curcumin has shown a potential extraordinary activity as an add-on ingredient in asthma treatment, due to its immunomodulatory and anti-inflammatory mechanism of action. However, its low water solubility and bioavailability lead to a poor therapeutic effect, which can be overcome by its formulation as nanocrystals. The aim of this study was to prep...
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...
In this study, pomegranate peel as a traditional natural remedy was extracted and encapsulated in proniosomal systems in order to improve its stability against harsh environmental conditions. Pomegranate peel was extracted by using sonication as a green extraction technology and the antioxidant activity of the obtained extract was evaluated to be 8...
8-methoxypsoralen is the most common drug in psoralen plus ultraviolet light irradiation therapy for the treatment of severe psoriasis. Despite of the efficacy, its classic oral administration leads to several serious adverse effects. However, the topical psoralen application produces a drug skin accumulation lower than that obtained by oral admini...
Phytosterols are sterols naturally occurring in plant cells and well known for their cholesterollowering activity, as witnessed by the large number of food supplements based on these functional ingredients available on the market. However, the marked hydrophobic character of phytosterols makes their solubility in biological fluids extremely low, wi...
In this work beclomethasone dipropionate was loaded into liposomes and hyalurosomes modified with mucin to improve the ability of the payload to counteract the oxidative stress and involved damages caused by cigarette smoke in the airway. The vesicles were prepared by dispersing all components in the appropriate vehicle and sonicating them, thus av...
The aim of this work was to ascertain the ability of electronic nicotine delivery systems (ENDS) to deliver drug nanocrystals through the produced aerosol. A nanocrystal nanosuspension of beclomethasone dipropionate, a synthetic chlorinated corticosteroid diester commonly used by inhalation in the treatment of asthma and chronic obstructive pulmona...
Topical application of the anti-inflammatory drug diclofenac (DCF) reduces the severity of systemic unwanted effects compared to its oral administration. A number of transdermal formulations are available on the market and routinely used in clinical and home-care settings. However, the amount of DCF delivered across the skin remains limited and oft...
Resveratrol and artemisinin, two naturally occurring compounds with a wide range of biological activities, have been reported to exert antitumor effects against several types of cancer. In this work, Eudragit-coated liposomes were developed to safely transport resveratrol and artemisinin through the gastrointestinal tract and target the intestine....
Topical psoralens plus ultraviolet A radiation (PUVA) therapy consists in the topical application of 8-methoxypsoralen (8-MOP) followed by the skin irradiation with ultraviolet A radiation. The employment of classical 8-MOP vehicles in topical PUVA therapy is associated with poor skin deposition and weak skin permeability of psoralens, thus requiri...
Proniosomes are free-flowing powders composed of water-soluble carriers blended with surfactants, which form niosomes upon hydration. In this work, proniosomal formulations containing the natural antioxidant resveratrol (RSV) were prepared and fully characterized. A pre-formulation study on RSV-loaded niosomes was carried out to determine the most...
Tuberculosis (TB) stands as the second “most deadly infectious disease” behind AIDS. Rifampicin (RIF) represents one of the most effective anti-TB drugs of the “short-term” oral TB therapy. However, the main limitations of the oral treatment are related with the lack of patient adherence and the development of multi-drug resistant Mycobacterium tub...
New three-dimensionally-structured hybrid phospholipid vesicles, able to load clotrimazole in a high amount (10 mg/mL), were obtained for the first time in this work by significantly reducing the amount of water (≤10%), which was replaced with a mixture of glycerol and ethanol (≈90%). A pre-formulation study was carried out to evaluate the effect o...
Quercetin, a natural polyphenol with strong antioxidant activity, was loaded in Eudragit-coated liposomes conceived for intestinal delivery. Eudragit was used to form a protective shell on the surface of liposomes to resist gastric environment and allow the delivery of quercetin to the intestine. The physico-chemical properties of the liposomes wer...
In the present work curcumin loaded hyalurosomes were proposed as innovative systems for the treatment of rheumatoid arthritis. Vesicles were prepared using a one-step and environmentally friendly method. Aiming at finding the most suitable formulation in terms of size, surface charge and stability on storage, an extensive pre-formulation study was...
Chronic obstructive pulmonary disease (COPD) is one of the main health problems worldwide. It is characterised by chronic inflammation in the lungs that leads to progressive, chronic, largely irreversible airflow obstruction. The use of long-acting β agonists remain today the frontline treatment for COPD with the aim of minimizing side effects and...
The use of adrenaline in cardiopulmonary resuscitation is a long-standing medical procedure, recommended by several international guidelines. However, its unspecific action on adrenergic receptors and the need for repeated administrations pose serious concerns about its safety, the balance between benefits and risks being still under debate. To add...
Gellan nanohydrogel and phospholipid vesicles were combined to incorporate baicalin in new self-assembling core-shell gellan-transfersomes obtained by an easy, scalable method. The vesicles were small in size (~107nm) and monodispersed (P.I. ≤ 0.24), forming a viscous system (~ 24mPa/s) as compared to transfersomes (~ 1.6mPa/s), as confirmed by rhe...
The present investigation reports the development of PEG-modified liposomes for the delivery of naturally occurring resveratrol. PEG-modified liposomes were prepared by direct sonication of the phospholipid aqueous dispersion, in the presence of two PEG-surfactants. Small, spherical, unilamellar vesicles were produced, as demonstrated by light scat...
Triiodothyronine (T3), a thyroid hormone synthesized and secreted by the thyroid gland, plays an essential role in morphogenesis and differentiation through interaction with its nuclear receptors (TRs). However, there are increasing evidences for its role in hepatocellular carcinoma (HCC) suppression. The aim of this work was to develop an effectiv...
Results:
demonstrated that the presence of diethylene glycol monoethyl ether influences the Poloxamer 188 ability to stabilize the nanocrystals during the milling process, leading to larger particles as compared to penetration enhancer-free nanosuspensions. As previously reported, the in vitro permeation studies indicate the nanosizing as a key fa...
Glycerosomes were formulated using 1,2-dimyristoyl-sn-glycero-3-phosphatidycholine (DMPC), diclofenac sodium salt and 10, 20 or 30% glycerol in the water phase, while corresponding liposomes were prepared with the same amount of DMPC and diclofenac, without glycerol. The aim of the present work was to evaluate the effect of the used phospholipid on...
Aiming at improving the nebulization performances and lung antioxidant protection of curcumin, chitosan or hyaluronan-coated liposomes were prepared and their characteristics and performances were compared with that of uncoated liposomes. Curcumin loaded liposomes displayed a diameter lower than 100 nm, the coating with both polymers led to a small...
The strategy of formulating poorly soluble actives as nanosuspension has been explored by more than a thousand research papers, with some medicinal products for oral and intravenous use having reached the market or advanced clinical trials. Interestingly, there is a limited number of reports of nanosuspensions formulated for dermal and transdermal...
Resveratrol and gallic acid were co-loaded in phospholipid vesicles aiming at protecting the skin from external injuries, such as oxidative stress and microbial infections. Liposomes were prepared using biocompatible phospholipids dispersed in water. To improve vesicle stability and applicability, the phospholipids and the phenols were dispersed in...
The present investigation reports the development of liposomes for the co-delivery of naturally occurring polyphenols, namely quercetin and resveratrol. Small, spherical, uni/bilamellar vesicles were produced, as demonstrated by light scattering, cryo-TEM, SAXS. The incorporation of quercetin and resveratrol in liposomes did not affect their intrin...
Needle-free liquid jet injectors are devices developed for the delivery of pharmaceutical solutions through the skin. In this paper, we investigated for the first time the ability of these devices to deliver intact lipid vesicles. Diclofenac sodium loaded phospholipid vesicles of two types, namely liposomes and transfersomes, were prepared and full...
In this work, diclofenac was encapsulated, as sodium salt, in glycerosomes containing 10, 20 or 30% of glycerol in the water phase with the aim to ameliorate its topical efficacy. Taking into account previous findings, glycerosome formulation was modified, in terms of economic suitability, using a cheap and commercially available mixture of hydroge...
Resveratrol is a naturally occurring polyphenol with strong antioxidant and free radical scavenging properties, recently proposed as a therapeutic agent for skin diseases. In this study, we investigated the possibility of improving the dermal bioavailability of the poorly water-soluble drug resveratrol by nanocrystal technology. To this purpose, na...
In this work a diclofenac acid nanosuspension formulation was produced as a novel approach for the treatment of skin inflammation. Drug nanocrystals, prepared by the wet media milling technique and stabilized using Poloxamer 188, were characterized by different techniques: scanning electron microscopy, differential scanning calorimetry, X-ray powde...
The aim of this work was to deliver curcumin into the lungs by incorporating it into innovative vesicles obtained using phospholipids and high concentrations of glycerol (50%, v/v), so called glycerosomes, which were then combined with two polymers: sodium hyaluronate and trimethyl chitosan to form polymer-glycerosomes. These systems were prepared...
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...
In the present work new highly biocompatible nanovesicles were developed using polyanion sodium hyaluronate to form polymer immobilized vesicles, so called hyalurosomes. Curcumin, at high concentration was loaded into hyalurosomes and physico-chemical properties and in vitro/in vivo performances of the formulations were compared to those of liposom...
Objectives
The present study was aimed at targeting the skin to deliver lidocaine loaded in surfactant/phospholipid vesicles tailored for improved local delivery. The influence of different formulation parameters was explored to maximise drug efficacy.Methods
The vesicles were prepared using a mixture of soy lipids (Phospholipon 50) and a surfactan...
The aim of this study was to elucidate the influence of the edge activator structure on the properties of novel deformable liposomes, Penetration Enhancer-containing Vesicles (PEVs), capable of delivering drugs to the skin. The PEVs were prepared by testing five different amphiphilic penetration enhancers as edge activators in the bilayer compositi...
Quercetin was incorporated in glycerosomes, new phospholipid-glycerol vesicles, and their protective effect against oxidative stress skin damages was extensively evaluated. In particular, the concentration-dependent effect of glycerol (from 10 to 50%) on vesicle suitability as cutaneous carriers of quercetin was carefully assessed. All vesicles wer...
In the present work biocompatible quercetin and curcumin nanovesicles were developed as a novel approach to prevent and restore skin tissue defects on chronic cutaneous pathologies. Stable and suitable quercetin- and curcumin-loaded phospholipid vesicles, namely liposomes and PEVs (Penetration Enhancer-containing Vesicles), were prepared. Vesicles...
The aims of this work were to improve cutaneous targeting and photostability of tretinoin by using nanosuspension formulation. Tretinoin is a drug widely used in the topical treatment of various dermatological diseases. The tretinoin nanosuspension was prepared by precipitation method and then characterized by photo correlation spectroscopy for mea...
Objectives In this work, a new polymeric microparticle system based on gelatin covalently bound to isoniazid (ISN) and containing rifampicin (RFP) was prepared by spray‐drying technique. Microparticle aptitude to nebulisation and their capability of interacting with A549, alveolar basal epithelial cells, were evaluated in vitro. Methods
Micropartic...
The aim of this work was to develop new microparticles for drug delivery to lungs by coating liposomes with chitosan (CH)–xanthan gum (XG) polyelectrolyte complexes to obtain chitosomes. To this purpose, two groups of liposomes were prepared using a mixture of soy phosphatidylcholine and hydrogenated soy phosphatidylcholine in two different concent...
OBJECTIVES : In this work, a new polymeric microparticle system based on gelatin covalently bound to isoniazid (ISN) and containing rifampicin (RFP) was prepared by spray-drying technique. Microparticle aptitude to nebulisation and their capability of interacting with A549, alveolar basal epithelial cells, were evaluated in vitro.
Microparticles we...
This work describes glycerosomes, vesicles composed of phospholipids, glycerol, and water, as novel vesicular carriers for (trans)dermal drug delivery. In this work, glycerosomes were prepared by hydrating dipalmitoylglycerophosphatidylcholine-cholesterol films with glycerol aqueous solutions (10-30%, v/v). The model drug was diclofenac sodium salt...
In this work we focused on how the concentration of Labrasol® and preparation method of phospholipid vesicles
might influence their physico-chemical features and skin delivery performances. Penetration Enhancer-containing
Vesicles (PEVs) were prepared using caprylcaproyl macrogol-8 glyceride (Labrasol®, HLB 14), a
solubilizer/penetration enhancer f...
In this work, we focused on how composition and preparation method of vesicles might affect their morphological features and delivery performances. Penetration Enhancer-containing Vesicles, PEVs, vesicles containing a water miscible penetration enhancer (Transcutol® P; 10%, 20%, 30% v/v) and encapsulating diclofenac sodium, were formulated and comp...
The aim of this work was to evaluate silica nanocomposites as topical drug delivery systems for the model drug, caffeine. Preparation, characterization, and skin permeation properties of caffeine-silica nanocomposites are described. Caffeine was loaded into the nanocomposites by grinding the drug with mesoporous silica in a ball mill up to 10 h and...
The aim of this work was to develop new microparticles for drug delivery to lungs by coating liposomes with chitosan (CH)-xanthan gum (XG) polyelectrolyte complexes to obtain chitosomes. To this purpose, two groups of liposomes were prepared using a mixture of soy phosphatidylcholine and hydrogenated soy phosphatidylcholine in two different concent...
Quercetin (3,3',4',5,7-pentahydroxyflavone) exerts multiple pharmacological effects: anti-oxidant activity, induction of apoptosis, modulation of cell cycle, anti-mutagenesis, and anti-inflammatory effect. In topical formulations quercetin inhibits oxidative skin damage and the inflammatory processes induced by solar UV radiation. In this work, que...
The aim of the present study was to develop a colon targeted delivery system for metronidazole using polymeric prodrug formulation. Two chitosan amide conjugates of metronidazole were prepared by using two different spacers to covalently link the drug to the amino group of the chitosan glucosamine units. Glutaric and succinic hemiesters of metronid...
The ability of a recently developed novel class of liposomes to promote dermal delivery of tretinoin (TRA) was evaluated. New penetration enhancer-containing vesicles (PEVs) were prepared adding to conventional phosphatidylcholine vesicles (control liposomes) different hydrophilic penetration enhancers: Oramix NS10 (OrNS10), Labrasol (Lab), Transcu...
In vitro study on N-succinyl chitosan and chitosan (control) matrices for selective colon delivery of 5-aminosalicylic acid is described. Matrices containing β-cyclodextrin were also prepared. As shown by DSC analyses, the drug was successfully loaded into the matrices reaching up to 95% entrapment efficiency. Swelling and drug release were studied...
Recently, we described a novel family of liposomes, the Penetration Enhancer-containing Vesicles (PEVs), as carriers for enhanced (trans)dermal drug delivery. In this study, to go deeply into the potential of these new vesicles and suggest the possible mechanism of vesicle-skin interaction, we investigated transcutol containing PEVs as carriers for...
The aim of this work was to evaluate the ability of Transcutol (Trc) to produce elastic vesicles with soy lecithin (SL) and study the influence of the obtained vesicles on in vitro (trans)dermal delivery of minoxidil. To this purpose, so-called penetration enhancer-containing vesicles (PEVs) were prepared using Trc aqueous solutions (5-10-20-30% v/...
The aim of this work was to evaluate the ability of a few different penetration enhancers to produce elastic vesicles with soy lecithin and the influence of the obtained vesicles on in vitro (trans)dermal delivery of minoxidil. To this purpose, so-called Penetration Enhancer-containing Vesicles (PEVs) were prepared as dehydrated-rehydrated vesicles...
This work describes preparation, characterization and properties of nanoemulsion formulations as drug carrier systems for topical application of 8-methoxypsoralen (8-MOP). The lipid emulsions were prepared from soy bean oil, as oil phase, different mixtures of phospholipids as emulsifiers (soy phosphatidylcholine or hydrogenated soy phosphatidylcho...
The influence of drug concentration and vesicle composition on the (trans)dermal delivery of tretinoin (TRA) was studied. To this purpose tretinoin was incorporated at different concentrations in unilamellar liposomes (UVs) prepared by sonication using phospholipids with different transition temperature (7c): hydrogenated soy phosphatidylcholine (T...
In this study the influence of liposomal incorporation on both the stability and the in vitro (trans) dermal delivery of verbascoside was evaluated. The effect of drug entrapment into vesicles on its radical scavenging activity was also studied. Liposomes were obtained from soy phosphatidylcholine and cholesterol according to the film hydration met...
In this work, we investigated the influence of β-cyclodextrin on the photostability of tretinoin and compared the photo-chemical
stability of tretinoin, either in methanol or complexed with β-cyclodextrin, when exposed both to UV and fluorescent light.
The physico-chemical characterization of tretinoin-β-cyclodextrin complexes, prepared by the free...
This work describes the preparation, characterization and properties of niosomal and liposomal carriers for the topical application of 8-methoxypsoralen (8-MOP). Large multilamellar (MLV) and sonicated unilamellar (UV) vesicular systems were prepared from either non-ionic surfactant octyl/decyl polyglucoside (Oramix CG110) or hydrogenated soy phosp...
The influence of drug thermodynamic activity and niosome composition, size, lamellarity and charge on the (trans)dermal delivery of tretinoin (TRA) was studied. For this purpose, tretinoin was incorporated at saturated and unsaturated concentrations in both multilamellar (MLV) and unilamellar (UV) vesicular formulations using two different commerci...
The influence of liposome composition, size, lamellarity and charge on the (trans)dermal delivery of tretinoin (TRA) was studied. For this purpose we studied both multilamellar (MLV) or unilamellar (UV) liposomes. Positively or negatively charged liposomes were obtained using either hydrogenated (Phospholipon90H) or non-hydrogenated soy phosphatidy...
The aim of this work was to study the influence of beta-cyclodextrin (beta-CD) on the biopharmaceutic properties of diclofenac (DCF). To this purpose the physicochemical characterization of diclofenac-beta-cyclodextrin binary systems was performed both in solution and solid state. Solid phase characterization was performed using differential scanni...
The effect of liposomal inclusion on the in vitro antiherpetic activity of Artemisia arborescens L. essential oil was investigated. In order to study the influence of vesicle structure and composition on the antiviral activity of the vesicle-incorporated oil, multilamellar (MLV) and unilamellar (SUV) positively charged liposomes were prepared by th...
The aim of this work is to study liposomes as carriers of nutrients and therapeutic agents in aquaculture with Venerupis decussatus and Venerupis pullastra larvae. Multilamellar (MLVs) and large unilamellar (LUVs) vesicles were prepared from a commercial mixture of soy phosphatidylcholine, rich in unsaturated and polyunsaturated fatty acids, choles...
In this work, we compared the chemical stability of tretinoin (TRA) in methanol and in vesicular suspensions exposed both to UV and artificial daylight conditions with the aim of evaluating the potential of niosomes as topical carriers capable of improving the stability of photosensitive drugs. Tretinoin-loaded niosomes were prepared from polyoxyet...
Tretinoin-loaded niosomes were prepared from polyoxyethylene (4) lauryl ether, sorbitan esters and a commercial mixture of octyl/decyl polyglucosides, in the presence of cholesterol and dicetyl phosphate. Liposomes made of hydrogenated and non-hydrogenated phosphatidylcholine were also prepared as a comparison reference. A study was made of the inf...
A formulation study, using increasing amounts of Sepigel 305 as an emulsifier, has been carried out to find new O/W emulsions and value their stability also in presence of vegetable extracts. Stability results have been compared with those obtained from formulations described in the National Formulary of Italian Pharmacopoeia X and functionalised b...
The effect of liposomal inclusion on the stability and in vitro antiherpetic activity of Santolina insularis essential oil was investigated. In order to study the influence of vesicle structure on the liposome properties, multilamellar and unilamellar vesicles were prepared by the film method and sonication, respectively. Vesicles were obtained fro...
It is well known that surfactants are capable of interacting with phospholipid vesicles leading to different aggregated structures and finally to mixed micellar systems. By means of diffusion experiments with Valia-Chien cells the effect of different vesicular structures (MLV and SUV) and that of three polysorbates on the release of a model drug (c...
The in vitro properties of ten flurazepam capsule formulations marketed in Italy were studied. All studied formulations showed a good agreement with pharmacopoeial requirements. In particular all studied capsules showed a quite fast release of the hypnotic drug even if some differences could be observed. Generally, time dissolution varied between 1...
The biopharmaceutical properties of eight lorazepam tablet formulations, marketed in Italy, were studied and compared. A few significant differences in behaviour were found even among similar formulations. In vitro dissolution patterns vazied on varying pH, technological properties, excipients employed and active ingredient concentrations.
