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Hypothesis Due to the well-know surfactant-like properties of diclofenac sodium (DS), vesicular systems consisting exclusively of DS, named diclosomes , were designed with the aim to minimize or avoid the use of other excipients and to improve the formulation biocompatibility. Experiments Diclosomes were designed and characterized in terms of dimensions, polydispersity index, ξ-potential, drug retained, stability as a function of storage time and ex-vivo percutaneous permeation profiles. Additionally, diclosomes were incorporated into gel dosage forms and their performance in terms of permeation enhancement were evaluated. Findings DS was found to form nanosized vesicular systems, both alone and in presence of cholesterol. Increasing hydrophobicity (due to the presence of cholesterol) resulted in smaller vesicles, always spherical and homogeneous in shape. Permeation of DS from free solution was found to be lower respect to ones obtained for all diclosomal formulations, allowing these aggregates to be considered as percutaneous permeation enhancers. DS permeated from diclosomal gels was higher than that obtained with traditional niosomal gel, DS plain gel and commercial specialty Voltaren Emulgel ® 1%, while containing a considerably lower drug amount. [ABSTRACT FROM AUTHOR]

Delivering chemotherapy specifically, effectively and safely to tumor remains a significant challenge in recent years. Although cancer cells are more vulnerable than normal to the effect of anticancer agents, these drugs are non-selective and can cause injury to normal tissues. Different approaches i.e. passive, active and magnetic targeting, smart devices with appropriate stimuli-sensitive properties or drugs combinations, have been already proposed as single methods, contributing to minimize severe side effects and enhancing tumor-targeting efficacy. Often, the use of a single strategy is not sufficient, whereby multi-functional approach has been suggested as further evolution of traditional “magic bullet” proposed in the early 1900s by Paul Ehrlich. Among the macromolecular systems useful for targeted drug delivery, liposomes and niosomes are the most extensively studied and they own the most suitable characteristics to be converted in multi-functional devices. Liposomes and niosomes are nanovesicles that contain amphiphilic molecules arranged in concentric bilayers, delimitating an aqueous core. These vesicular carriers are very versatile, since they can be differently designed and modified in such a way that they exhibit combinations of the following properties: longevity in blood, specific target to the tumor, respond to internal/external stimuli, promotion of drug intracellular delivery. This review will focus on the potential of multi-functional vesicular nanocarriers in cancer therapy, analizing each combination of targeting strategies, stimuli-sensitivity and drug combinations and giving an exhaustive collection of recent investigations. Many multi-functional vesicular devices have shown great promise in clinical application, indicating broad potential as therapeutics in the near future, but more needs to be done. The development of more specific and efficient carriers for a personalized cancer therapy is the next challenge. [ABSTRACT FROM AUTHOR]

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, 0.5 wt% of CS), monomeric and isotropic solutions (0.5 and 5 wt% of CS), nematic (15 wt% of CS) and hexagonal phases (30 wt% 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 500 nm 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. [ABSTRACT FROM AUTHOR]

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. [ABSTRACT FROM AUTHOR]

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. [ABSTRACT FROM AUTHOR]

Highlights: [•] Niosomes from glucuronic acid-based surfactant containing doxorubicin or 5FU were prepared. [•] Vesicles were found to encapsulate and release in a prolonged manner both doxorubicin and 5FU. [•] Low toxicity was observed, performing hemolytic tests. [ABSTRACT FROM AUTHOR]

Highlights: [•] Design of niosomal systems containing lipophilic antioxidants for cosmeceutical applications. [•] Evaluation of the effect of antioxidants co-encapsulation on the niosomes properties. [•] Studies of the antioxidant properties and the in vitro percutaneous permeations of antioxidants from the carriers. [Copyright &y& Elsevier]

Highlights: [•] Design of novel niosomal formulations containing nutritional supplements. [•] Evaluation of the effect of the active molecules co-encapsulation on the properties of the carriers. [•] Studies on the antioxidant properties and releasing capability of gallic acid, ascorbic acid, curcumin and quercetin. [Copyright &y& Elsevier]

Highlights: [•] The drugs percutaneous permeation profiles from LC-niosomes formulations as multicomponent systems were investigated. [•] Drugs as third component in the formulations could influence the microstructure of the multicomponent system. [•] Drugs percutaneous permeation from LC-niosomes systems, corresponding niosomal and LC binary systems were compared. [•] All the formulation affected in different way the drugs permeation across the skin. [Copyright &y& Elsevier]

Abstract: In chemotherapy the magnetic drug targeting to a specific organ or tissue is proposed on the assumption that magnetic fields are harmless to biological systems. In this light we have vehiculated doxorubicin as model drug by novel magneto-niosomes in order to evaluate the physico–chemical properties of the obtained formulations and the in vitro release profile. Tween 60 and Pluronic L64 have been used as surfactants and the formulation cytotoxicity has been performed by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolum bromide and trypan blue dye esclusion tests. Results show that niosome dimensions and doxorubicin entrapment efficiencies are influenced by bilayer composition. In addition, formulations are able to control the deliver and release of the drug active form in a retarded manner. No additional toxicity, due to the encapsulation of ferrofluid into niosomes core, has been detected. [Copyright &y& Elsevier]

Abstract: The development of advanced biomaterials and drug-delivery systems has had a significant impact on our ability to treat several diseases. A new study was performed on niosomal formulations obtained from a mixture of commercial surfactants (Tween 80 and Span 80) to be applied topically for the release of Capsaicin. Capsaicin is the pungent principle of red pepper and it has a variety of pharmacological actions on the cardiovascular, respiratory and nervous systems. Niosomal carriers were prepared using a particular ratio between surfactants, to obtain systems with a specific HLB (10,12,14) and characterized in terms of dimension, morphology and their drug entrapment efficiency. Niosomes were compared to microemulsions prepared from the same surfactants in the same ratio, to evaluate their possible use in transdermal drug delivery. As regards the in vitro percutaneous permeation of Capsaicin from both microemulsions and niosomal formulations, it was carried out using diffusion Franz cells. The results indicate that niosomes could better promote the transdermal delivery of Capsaicin, with respect to microemulsions, even if both carriers could be an effective vehicle for topical delivery of this drug. [Copyright &y& Elsevier]

Abstract: 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 &y& Elsevier]

Abstract: 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 27wt% 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. [Copyright &y& Elsevier]

Abstract: 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 α,ω-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 β-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 α,ω-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. [Copyright &y& Elsevier]

pH-responsive polymersomes were obtained by self-assembling of a carboxyl-terminated PEG amphiphile achieved via esterification of PEG diacid with PEG40stearate. The obtained vesicular systems had spherical shape and a mean diameter of 70 nm. The pH sensitivity was assessed by measuring the variations of particles mean diameter after incubation in media mimicking the physiological (pH 7.4) or tumor (pH 5.0) conditions, recording a significant increase of the vesicles dimensions at acidic pH. The ability of the polymersomes to carry both hydrophobic and hydrophilic drugs was evaluated by loading the vesicles with curcumin and methotrexate, respectively, obtaining high encapsulation efficiencies and pH-dependent release profiles. The drug-loaded polymeric vesicles exhibited improved cytotoxic potential against MCF-7 cancer cell line and were found to be highly hemocompatible. Finally, cellular uptake experiments on MCF-7 cancer cells were conducted to demonstrate the ability of the designed polymersomes to enhance drug penetration inside the cells. [ABSTRACT FROM AUTHOR]

Abstract: The role of nonionic vesicles on the rheological behavior of Pluronic F127 is investigated above the dilute regime and below the cloud point of the nonionic surfactant. F127 is a copolymer possessing sol–gel transition by heating attributed to a phase transition from micellar to cubic. The presence of surfactant vesicles is expected to enhance the compartmentalization of a variety of drugs, independently of their affinity to the solvent. Such entrapment would be suitable for controlled release of the drugs in different applications. We address here a mixed Pluronic–nonionic surfactant system with particular emphasis to the effects of the surfactant on the rheological properties of the Pluronics, and the correlation between these properties and drug release control. The results show that the rheological properties of the mixed system are mainly governed by the behavior of the polymer alone and that the mixed system can be useful to control the percutaneous permeation of a small drug, such as Diclofenac Sodium salt. [Copyright &y& Elsevier]