Pula, Italy
Pula, Italy

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Manca M.L.,University of Cagliari | Marongiu F.,University of Cagliari | Castangia I.,University of Cagliari | Catalan-Latorre A.,University of Cagliari | And 7 more authors.
Industrial Crops and Products | Year: 2016

Grape extract rich in polyphenols (∼129 ± 32 mg of gallic acid equivalents per g of dry extract) was obtained from the pomaces of Cannonau grapes by homogenization in an ethanol/water mixture. The efficacy of ultrasounds in speeding up the extraction kinetics of polyphenols was demonstrated. The extract was incorporated in liposomes and PEVs (penetration enhancer containing vesicles) with Labrasol® or Labrasol®/ethanol. All the vesicles were spherical and predominantly unilamellar: liposomes were large (∼927 nm) and polydispersed (PI ∼0.56), while PEVs were small (∼140 nm) and fairly homogeneous (PI ∼0.3). Moreover, PEVs were able to incorporate a high amount of the extract (∼98% of the extract used for their preparation, 50 mg/ml). The formulations were highly cytocompatible and were able to promote the proliferation of keratinocytes and fibroblasts. In addition, thanks to their antioxidant activity, grape extract formulations provided a cytoprotective effect against oxidative stress damage. Therefore, an efficient, environmentally-friendly extraction strategy is proposed to obtain an extract with high phenolic content from waste grape pomaces, which was incorporated in vesicular systems to maximize the antioxidant power in a cell model of oxidative stress. © 2015 Elsevier B.V.


Manca M.L.,University of Cagliari | Castangia I.,University of Cagliari | Zaru M.,Polytechnic University of Valencia | Nacher A.,Icnoderm Srl | And 6 more authors.
Biomaterials | Year: 2015

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 liposomes having the same lipid and drug content. Vesicles were prepared by direct addition of dispersion containing the polysaccharide sodium hyaluronate and the polyphenol curcumin to a commercial mixture of soy phospholipids, thus avoiding the use of organic solvents. An extensive study was carried out on the physico-chemical features and properties of curcumin-loaded hyalurosomes and liposomes. Cryogenic transmission electron microscopy and small-angle X-ray scattering showed that vesicles were spherical, uni- or oligolamellar and small in size (112-220 nm). The in vitro percutaneous curcumin delivery studies on intact skin showed an improved ability of hyalurosomes to favour a fast drug deposition in the whole skin. Hyalurosomes as well as liposomes were biocompatible, protected in vitro human keratinocytes from oxidative stress damages and promoted tissue remodelling through cellular proliferation and migration. Moreover, in vivo tests underlined a good effectiveness of curcumin-loaded hyalurosomes to counteract 12-O-tetradecanoilphorbol (TPA)-produced inflammation and injuries, diminishing oedema formation, myeloperoxydase activity and providing an extensive skin reepithelization. Thanks to the one-step and environmentally-friendly preparation method, component biocompatibility and safety, good in vitro and in vivo performances, the hyalurosomes appear as promising nanocarriers for cosmetic and pharmaceutical applications. © 2015 Elsevier Ltd.


PubMed | University of Barcelona, University of Valencia, University of Cagliari, University of Rome La Sapienza and 2 more.
Type: Journal Article | Journal: International journal of pharmaceutics | Year: 2016

Allantoin is traditionally employed in the treatment of skin ulcers and hypertrophic scars. In the present work, to improve its local deposition in the skin and deeper tissues, allantoin was incorporated in conventional liposomes and in new argan oil enriched liposomes. In both cases, obtained vesicles were unilamellar, as confirmed by cryo-TEM observation, but the addition of argan oil allowed a slight increase of the mean diameter (130nm versus 85nm). The formulations, especially those containing argan oil, favoured the allantoin accumulation in the skin, in particular in the dermis (8.7g/cm(2)), and its permeation through the skin (33g/cm(2)). The performances of vesicles as skin delivery systems were compared with those obtained by water dispersion of allantoin and the commercial gel, Sameplast(). Moreover, in this work, for the first time, the elastic and viscous moduli of the skin were measured, underlining the different hydrating/moisturizing effects of the formulations. The application of ARG liposomes seems to provide a softening and relaxing effect on the skin, thus facilitating the drug accumulation and passage into and trough it.


PubMed | University of Rome La Sapienza, Icnoderm srl, University of Cagliari and University of Valencia
Type: Journal Article | Journal: International journal of pharmaceutics | Year: 2016

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 hydrogenated soy phosphatidylcholine (P90H). P90H glycerosomes were spherical and multilamellar; photon correlation spectroscopy showed that obtained vesicles were 131nm, slightly larger and more polydispersed than those made with dipalmitoylphosphatidylcholine (DPPC) but, surprisingly, they were able to ameliorate the local delivery of diclofenac, which was improved with respect to previous findings, in particular using glycerosomes containing high amount of glycerol (20 and 30%). Finally, this drug delivery system showed a high in vitro biocompatibility toward human keratinocytes.


Manconi M.,University of Cagliari | Manca M.L.,University of Cagliari | Marongiu F.,University of Cagliari | Caddeo C.,University of Cagliari | And 8 more authors.
International Journal of Pharmaceutics | Year: 2016

The components of pompia, a hybrid Citrus species cultivated only in Sardinia (Italy), were extracted using an environmentally-friendly method and food-grade solvents. Taking into account that only few data are available on pompia composition, the phytochemical fingerprint of its rind extract was obtained by accurate component separation and identification, combining HPLC and mass spectrometry. Different flavones such as naringin (23.77. μg/mg), neoeriocitrin (46.53. μg/mg) and neohesperidin (44.57. μg/mg) were identified. Additionally, the antioxidant activity and phenolic content were confirmed by DPPH and Folin-Ciocalteu assays. The whole extract was incorporated in innovative phospholipid vesicles, namely glycerosomes, hyalurosomes and glycerol containing hyalurosomes, which were prepared using a high ratio of extract/phospholipid (1/3.5. w/w). The in vitro biocompatibility of the nanoincorporated extract and its ability to potentiate the aptitude of the extract to counteract oxidative stress in skin cells were evaluated. The vesicles, especially glycerol containing hyalurosomes, were able to prevent oxidative damage and death of both keratinocytes and fibroblasts, promoting their viability. © 2016 Elsevier B.V.


Manca M.L.,University of Cagliari | Zaru M.,Icnoderm srl | Bacchetta G.,University of Cagliari | Biggio T.,SRL Group | And 5 more authors.
Industrial Crops and Products | Year: 2015

Sardinian folk medicine has given rise to a renewed interest in treatment of different diseases, particularly skin burns and inflammatory disorders. Rubus ulmifolius Schott shoots have been used to treat burns of different degree. During this work, a new and more effective extraction method was developed using olive oil at room temperature for 10 days. The R. ulmifolius oleolite components were mainly represented by polyphenolic compounds and tannins. To obtain a suitable topical formulation, the Rubus oleolite was incorporated in an ointment composed of anhydrous lanolin, white wax, olive oil, and Europhea oil unsaponifiables. Both R. ulmifolius oleolite and ointment were able to scavenge DPPH free radicals in vitro in a way very similar to quercetin, used as reference. In addition, R. ulmifolius ointments were biocompatible in vitro on 3T3 fibroblasts and did not cause any malformation or cell degeneration. Moreover, in vivo studies on Sprague-Dawley rats confirmed the ability of Rubus ointment to improve skin regeneration after burns. © 2014 Elsevier B.V.


PubMed | CNR Institute of Neuroscience, University of Sassari, University of Cagliari and Icnoderm srl
Type: Journal Article | Journal: International journal of pharmaceutics | Year: 2016

The components of pompia, a hybrid Citrus species cultivated only in Sardinia (Italy), were extracted using an environmentally-friendly method and food-grade solvents. Taking into account that only few data are available on pompia composition, the phytochemical fingerprint of its rind extract was obtained by accurate component separation and identification, combining HPLC and mass spectrometry. Different flavones such as naringin (23.77g/mg), neoeriocitrin (46.53g/mg) and neohesperidin (44.57g/mg) were identified. Additionally, the antioxidant activity and phenolic content were confirmed by DPPH and Folin-Ciocalteu assays. The whole extract was incorporated in innovative phospholipid vesicles, namely glycerosomes, hyalurosomes and glycerol containing hyalurosomes, which were prepared using a high ratio of extract/phospholipid (1/3.5w/w). The in vitro biocompatibility of the nanoincorporated extract and its ability to potentiate the aptitude of the extract to counteract oxidative stress in skin cells were evaluated. The vesicles, especially glycerol containing hyalurosomes, were able to prevent oxidative damage and death of both keratinocytes and fibroblasts, promoting their viability.


This invention concerns nanometric vesicles similar to liposomes (hyalurosomes) comprising molecules of hyaluronate, phospholipid molecules and at least one active pharmaceutical or cosmetic ingredient. The invention also concerns the use of hyalurosomes in topical cosmetic or pharmaceutical compositions and their preparation process.


This invention concerns nanometric vesicles similar to liposomes (hyalurosomes) comprising molecules of hyaluronate, phospholipid molecules and at least one active pharmaceutical or cosmetic ingredient. The invention also concerns the use of hyalurosomes in topical cosmetic or pharmaceutical compositions and their preparation process.

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