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Cromolyn sodium, or disodium cromoglycate (CS), is a surface active drug: a pharmacologically active compound with an amphiphilic nature. At certain conditions it is able to self-associate in several kind of supramolecular aggregates. Since CS could play the role of both carrier and drug, bypassing the use of additional excipients and increasing the system biocompatibility, the effects of cromolyn self-aggregates on diffusion and percutaneous permeation across rabbit ear skin were investigated. Niosomes (vesicular systems, 0.5wt% of CS), monomeric and isotropic solutions (0.5 and 5wt% of CS), nematic (15wt% of CS) and hexagonal phases (30wt% of CS) were selected as supramolecular systems and tested as transdermal delivery systems. Results demonstrated that CS was able to form vesicular structures of about 500nm of diameter and this formulation gave the higher percutaneous permeation profile (systemic action), while isotropic solution and liquid crystals mesophases acted as slower release reservoir of drug on the skin surface (local action), as confirmed by diffusion coefficients. Diffusion rates through a synthetic membrane were dependent both on CS concentration present into the formulations and on its structural organization: maximum diffusion was noticed with isotropic solution, a lower amount of diffused cromolyn sodium was achieved by hexagonal phase. Consequently, CS appears as a versatile surfadrug as, depending on the disease degree, it is possible to modulate its permeation profile by choosing the most appropriate formulation., (Copyright © 2015 Elsevier B.V. All rights reserved.)

Ferrogels (or magnetic hydrogels) are cross-linked polymer networks containing magnetic nanoparticles: they are mechanically soft and highly elastic and at the same time they exhibit a strong magnetic response. Our work focuses on an combinatorial strategy to improve the efficacy of 5-Fluorouracil (5-FU) assisted chemotherapy, by developing novel multifunctional pH-sensitive ferrogels. We designed gels based on N,N'-dimethylacrylamide monomers polymerized in presence of methacrylic acid or 2-aminoethyl methacrylate hydrochloride, containing ferro-nanoparticles. The influence of polymeric matrix composition and exposition to magnetic field (MF) on swelling behavior and drugs release were investigated at pH 7.4 and 5. In particular, the magnetic field was obtained by using permanent magnetic bar (0.25 T) or electromagnet (0.5 and 1.2 T), with the aim to analyze quantitatively the magnetic effects. A strong influence of the magnetic field on ferrogels properties have been observed. Swelling analysis indicated a dependence on both pH and network composition, reaching a maximum at pH 7.4, for formulations containing methacrylic acid, while the application of MF appeared to decrease the swelling percentages. Release profiles of 5-FU showed effective modulation in release by application of MF: drug release is always higher in the presence of a magnetic field and generally increases with its intensity. The combining effect of pH sensitive properties and application of MF improved the performance of the systems. Results showed that our ferrogels may be technologically applicable as devices for delivery of 5-FU in a controllable manner., (Copyright © 2015 Elsevier B.V. All rights reserved.)

The aim of this study was to improve the transdermal permeation of sulfadiazine sodium, employing synergistic combination of surfactants (in the form of niosomes) and additives with different number of hydroxylic groups, (following referred to as "alcohol"), as component of the bilayer. In particular the effect of different concentration of each alcohol (ethanol, propylene glycol or glycerol, from 5%, to 40% v/v) on niosomes size and distribution, drug entrapment efficiencies and ex vivo drug percutaneous permeation were evaluated, identifying formulations giving the best performances. The findings revealed that the presence of alcohol critically affect the physico-chemical properties of niosomes, with regards to dimensions, drug encapsulation and permeation. Vesicular size increased with the amount of alcohol and at the same alcohol concentration, follow the sequence ethanol>propylene glycol>glycerol. Loaded niosomes were larger than empty ones. Low E% values were found for ethanol, even less in propylene glycol and glycerol based samples, confirming that the chemical structure of the alcohol and its physico-chemical properties, affected the sulfadiazine entrapment efficiency. The comparative evaluation of percutaneous permeation profiles showed that the cumulative amount of permeated drug increases with alcohol concentration up to 20% v/v. Higher concentration (40% v/v) resulted in a strong decrease of the potential skin permeation. Best performances were obtained with glycerol. In all cases ex vivo sulfadiazine percutaneous permeations are controlled and improved respect to the corresponding free drug solutions and traditional niosomes used as controls., (Copyright © 2014 Elsevier B.V. All rights reserved.)

Niosomes are vesicular systems composed of surfactant molecules, claimed to be used as drug delivery carriers thanks to their physico-chemical and biological properties. The aim of this work was to design niosomes obtained with a surfactant synthesized from glucuronic acid. Doxorubicin and 5FU were used as model drugs. Niosomes were prepared with different ratios between surfactant and cholesterol, and characterized in terms of size, morphology, drugs entrapment efficiency and in vitro releases, to identify the optimal formulation to be used in pharmaceutical fields. In addition, the hemolytic activity of all formulations have been also evaluated. Results showed that dodecylglucuronamide surfactant was able to produce vesicular systems with or without the presence of cholesterol. Niosomes resulted regular in size and shape and they have been found to encapsulate and release in a controlled manner both doxorubicin and 5-fluorouracil. Hemolytic tests showed that the capability of disrupting erythrocyte only depend on the size of colloidal aggregates. Finally, our formulations could be potentially used as antitumoral delivery systems in anticancer therapy., (Copyright © 2014 Elsevier B.V. All rights reserved.)

Niosomal vesicular systems containing resveratrol, alpha-tocopherol and curcumin as single agents and in combination, were designed with the aim to develop novel cosmeceutical formulations. The effects of antioxidants co-encapsulation on the physico-chemical properties of the carriers, their antioxidant properties and in vitro percutaneous permeation profiles were evaluated. Results showed that the co-encapsulation of resveratrol/curcumin and alpha-tocopherol/curcumin affected the physico-chemical properties of niosomes and the entrapment efficiencies values, respect to the formulations containing the single antioxidant. The antioxidants in vitro percutaneous permeations appeared to be controlled and improved respect to the corresponding free solutions used as control. Moreover the antioxidants combinations resulted in a promoted ability to reduce free radicals, due to a synergic antioxidant action., (Copyright © 2013 Elsevier B.V. All rights reserved.)

Recently niosomes have been used as nutraceutical vehicles of functional components, useful in the prevention of many diseases caused by oxidative stress, with the aim to control their delivery into the body and to increase the nutritional quality of food dairy products with which these products can be enriched. We decided to develop novel niosomal formulations containing nutritional supplements such as gallic acid, ascorbic acid, curcumin and quercetin as single agents and in combination, to evaluate the effect of the active molecules co-encapsulation on the physico-chemical properties of the carriers, on their antioxidant properties and capability of releasing the encapsulated materials. Results suggest that the co-encapsulations of gallic acid/curcumin and ascorbic acid/quercetin mix influence their physico-chemical properties and their entrapment efficiencies respect to the formulations containing the single antioxidant; also the antioxidants releases appeared to improve and their combinations resulted in a promoted ability of reducing free radicals, due to a synergic antioxidant action., (Copyright © 2013 Elsevier B.V. All rights reserved.)

In this study, stearic acid- and stearyl ferulate-based solid lipid nanoparticles containing trans-ferulic acid (SLN-FA and SLN-SF-FA, respectively), were prepared and characterized for loading efficiency, size and shape. In addition, by using rat brain microsomes, we evaluated in vitro the antioxidant activity of these formulations against three well known initiators of lipid peroxidation, such as AAPH, NADPH/ADP-Fe(3+) and SIN-1 which in turn generate the peroxyl and perferryl radicals as well as peroxynitrite, respectively. Commercially available FA and its ethyl ester (FAEE) were used as comparators. Both SLN-FA and SLN-SF-FA dose-dependently reduced lipid peroxidation induced by the three oxidants. Interestingly, SLN-SF-FA displayed greater efficacy (EC50) and potency (maximal activity) against AAPH- and NADPH/ADP-Fe(3+)-induced lipid peroxidation. Our results support the idea that this new formulations could facilitate the uptake of FA by the cells because of their lipophilic structure, thus increasing FA bioavailability. Furthermore, stearyl ferulate-based nanoparticles could prevent the degradation of FA entrapped on their structure, making FA almost entirely available to explicate its antioxidant power once released., (Copyright © 2013 Elsevier B.V. All rights reserved.)

The objectives of our study were to evaluate the ability of Pluronic L64 surfactant to give niosomal systems alone or after its functionalization with acrylic groups. The achieved formulations were tested for the percutaneous permeation of Sodium Diclofenac as model drug. In vitro experiments were conducted by Franz diffusion cells, using rabbit ear skin. Data recorded over 24h were compared with those obtained from the drug solution, as control. In addition, the stability of niosomes was improved polymerizing the acryloyl groups of the monomers, because, as reported in the literature, polymerized vesicles maintain their shape for long periods of time, and show remarkable increase in drug encapsulation efficiency. Mean vesicles diameter, drug entrapment efficiency, percutaneous permeation and release profiles were investigated for all vesicles with different composition. The results indicated an increase in mean vesicles diameter and entrapment efficiency with the increase of polymerizable moieties amount. These properties were found to be more evident when the vesicles were polymerized. In addition cytotoxic effects were estimated. The results of this study showed that niosomes based on commercial, functionalized or a mixture of both Pluronic L64 surfactants can be used to achieve retarded release and to enhance the permeation of Sodium Diclofenac, without incurring unacceptable toxicity., (Copyright 2010 Elsevier B.V. All rights reserved.)

A commercial sucrose cocoate surfactant was used to obtain a new vesicular system for transdermal drug delivery. The preparation, the dimensional and morphological characterizations and the skin permeation profile of these new niosomes were evaluated. Moreover we studied the possible employment of mixture of sucrose cocoate and cholesterol at different weigh ratios for the vesicles preparation and we analyzed the influence of cholesterol on niosomes properties. Diclofenac and Sulfadiazine were used as model drugs. Results suggest that sucrose cocoate was able to form vesicles in the presence or not of cholesterol and the addition of cholesterol leads to a variation of size: larger vesicles were obtained in the absence of cholesterol both in empty and drug-loaded niosomes. All vesicles were spherical and regular in shape. In vitro skin permeation profiles were significantly higher than the free drug solution, indicating the favourable relations between skin and niosomes. The faster release of the drug was found for niosomes with no cholesterol or with a reduced amount of this membrane additive, in particular the optimal formulation was that in which the cholesterol content was about 27 wt% of total lipid amount: probably this value is a good compromise between the membrane stability and its deformation capacity, allowing a higher drug permeation across the skin.

UVA exposure induces DNA damage that could result in skin carcinogenesis. Antioxidants are usually employed as protective agents to avoid this problem: in particular, both beta-carotene and alpha-tocopherol can protect the skin against UVA-induced damage. It is well known that the photochemical instability of these compounds has been a limiting factor for their applications to protect skin. In this study, stearyl ferulate-based solid lipid nanoparticles (SF-SLNs), as vehicles for beta-carotene and alpha-tocopherol, were formulated to improve the stability of these compounds. The SF-SLNs were characterized for entrapment efficiency, size and shape together with their cytotoxicity and capability to inhibit lipid peroxidation. After treatment with a pro-oxidant and/or exposition to sunlight the antioxidants entrapped in SF-SLNs were extremely stable. The results highlighted how SF-SLNs represent a suitable vehicle for beta-carotene and alpha-tocopherol stabilizing and protecting them from degradation. A dermatological formulation in order to prevent skin damages is, therefore, suggested.

The synthesis and characterisation of new surfactants with peculiar physical-chemical properties are amongst the most promising and expanding issues in pharmacological colloid science. The most used vesicular carriers are liposomes prepared from a wide variety of natural and synthetic phospholipids, but several ionic and non-ionic amphiphiles have been used to form multilamellar and/or unilamellar vesicles. In the present study the synthesis of alpha,omega-trioxyethylene-bis(sodium 2-dodecyloxy-propylenesulfonate), an anionic Gemini surfactant, and its ability to form niosomes are elucidated. The compound forms vesicles with and without added cholesterol. The vesicular systems were characterized by size, shape and drug entrapment efficiency. The compounds to be incorporated are beta-carotene and ferulic acid, as antioxidants, acetyl salicylic acid, as FANS, and the antineoplastic 5-flurouracil, widely used in dermatological disorders. The results of this study show that alpha,omega-trioxyethylene-bis(sodium 2-dodecyloxy-propylenesulfonate) can be used for the preparation of niosomes entrapping lypophilic, amphiphilic or hydrophilic substances. These niosomes may be promising candidates as percutaneous carriers for the aforementioned drugs.

Niosomes have shown promise as cheap and chemically stable drug delivery systems. In this paper a novel crown ether amphiphile, 1,16-hexadecanoyl-bis-(2-aminomethyl)-18-crown-6 (Bola A-16), has been synthesized with the aim of developing a long time stable controlled release system. Niosomes have been prepared with different molar ratios of amphiphile and cholesterol and their morphological properties have been determined by quasi-elastic light scattering and transmission electron microscopy. The composition of niosomes affects the entrapment efficiency and the release rate of 5-fluorouracil, a well-known antineoplastic molecule. In addition, other two known azacrown ether amphiphiles (4,7,10,13-pentaoxa-16-aza-cyclooctadecane)-hexadecanedioc acid diamide (Bola D-16) and alpha,omega-(4,7,10,13-pentaoxa-16-aza-cyclooctadecane)-hexadecane (Bola C-16), have been synthesized and the obtained vesicles have been characterized for comparison. Furthermore, the release profile of 5-fluorouracil in vitro, from these niosomes, has been studied over a period of 6h in order to simulate a hematic adsorption.

Vesicular formulations (liposomes and niosomes) play an increasingly important role since they can be used as drug delivery and targeting systems. We described the formation of two niosomal systems based on synthetic bolaform surfactants (4,7,10,13-pentaoxa-16-aza-cyclooctadecane)-hexadecanedioc acid diamide (BD-16) and alpha,omega-(4,7,10,13-pentaoxa-16-aza-cyclooctadecane)-hexadecane (BC-16). Systems containing BD-16 or BC-16 and different amount of cholesterol (CH) were prepared by aqueous dispersion of films, followed by examination of methylene blue (MB) entrapment, particle size and morphology. Indeed, we also studied the hydration in the distilled water and physiological solution, in order to investigate the complexing ability on vesicle formation. The results obtained in this study show a high encapsulation capacity and this ability and the size depends on cholesterol content.