Papers by Eliana B. Souto
Colloids and Surfaces B-biointerfaces, 2011
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Colloids and Surfaces B-biointerfaces, 2010
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Expert Opinion on Drug Delivery, 2009
The scientific literature today provides several systems that can deliver active pharmaceutical i... more The scientific literature today provides several systems that can deliver active pharmaceutical ingredients (APIs) across the skin. These include reservoir matrices, matrix diffusion-controlled devices, multiple polymer devices and multilayer matrix assemblies. Among these, nanostructured lipid carriers (NLC) have emerged as novel systems composed of physiological lipid materials suitable for topical, dermal and transdermal administration. This review focuses on the design characteristics, production and composition of semi-solid formulations containing NLC as API carriers. One of the useful semi-solid systems are hydrogels, which can be used as vehicles to provide appropriate consistency for NLC formulations to be applied onto the skin. In the present review recent developments in the field are highlighted, including examples of APIs successfully entrapped within NLC now amenable for delivery via the skin. Further innovations in NLC composition and formulation, as well as in semi-solid hydrogel assemblies, are likely to expand the number of APIs available for topical, dermal and transdermal delivery.
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Expert Review of Ophthalmology, 2010
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International Journal of Cosmetic Science, 2005
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The main aim of pharmaceutical technology research is the design of successful formulations for e... more The main aim of pharmaceutical technology research is the design of successful formulations for effective therapy, taking into account several issues including therapeutic requirements and patient compliance. In this regard, several achievements have been reported with colloidal carriers, in particular with lipid nanoparticles, due to their unique physicochemical properties. For several years these carriers have been showing potential success for several administration routes, namely oral, dermal, parenteral, and, more recently, for pulmonary and brain targeting. The present chapter provides a review of the use of solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) to modify the release profile and the pharmacokinetic parameters of active pharmaceutical ingredients (APIs) incorporated in these lipid matrices, aiming to modify the API bioavailability, either upwards or downwards depending on the therapeutic requirement. Definitions of the morphological characteristics, surface properties, and polymorphic structures will also be given, emphasizing their influence on the incorporation parameters of the API, such as yield of production, loading capacity, and encapsulation efficiency.
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International Journal of Cosmetic Science, 2008
A detailed review of the literature is presented in attempts to emphasize several advantages of s... more A detailed review of the literature is presented in attempts to emphasize several advantages of solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) for cosmetic applications. Examples of several actives are given and the main features of the solid core of SLN and NLC for topical delivery of cosmetics are discussed. Lipid nanoparticles have been more and more explored in pharmaceutical technology, showing superior advantages for topical purposes over conventional colloidal carriers.Un examen détaillé de la littérature est présenté dans les tentatives de souligner les plusieurs avantages des nanoparticule lipidique solide (SLN) et lipidique nanostructurés (NLC) pour applications cosmétiques. Exemples de plusieurs substances actives sont données et les caractéristiques principales du noyau plein de SLN et de NLC pour la libération topique des produits de beauté sont discutées. Les nanoparticles lipides ont été de plus en plus explorées en technologie pharmaceutique, montrant des avantages supérieurs pour les porteurs colloïdaux conventionnels pour administration topique de buts.
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European Journal of Pharmaceutics and Biopharmaceutics, 2007
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Methods in Enzymology, 2009
Solid lipid nanoparticles (SLNs) have emerged as important tools to modify the release profile fo... more Solid lipid nanoparticles (SLNs) have emerged as important tools to modify the release profile for a large number of drugs including protein and peptide molecules. SLNs are produced from biocompatible and biodegradable lipid materials, making them a promising therapeutic strategy for drug targeting and delivery, and surmounting the inherent limitations of regulation acceptance. Due to their versatility in loading both lipophilic and hydrophilic molecules in the solid lipid matrix, SLNs depict the ability to prolong, extend or sustain the release profile of the loaded molecules, therefore reducing the repeated administration, and increasing the therapeutic value of a certain treatment. Additional advantages include reduction of drug toxicity and increase of drug bioavailability. To develop SLN formulations for drug targeting and delivery, a basic pharmacokinetic understanding of drug distribution is of major relevance, as well as the biopharmaceutical aspects of the administration route. This chapter provides a fundamental understanding of the pharmacokinetic properties of SLNs, which influence both biopharmaceutical and clinical profiles of the loaded molecules.
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European Journal of Pharmaceutics and Biopharmaceutics, 2004
Aqueous dispersions of lipid nanoparticles are being investigated as drug delivery systems for di... more Aqueous dispersions of lipid nanoparticles are being investigated as drug delivery systems for different therapeutic purposes. One of their interesting features is the possibility of topical use, for which these systems have to be incorporated into commonly used dermal carriers, such as creams or hydrogels, in order to have a proper semisolid consistency. For the present investigation four different gel-forming
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Cheminform, 2006
ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was e... more ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
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International Journal of Cosmetic Science, 2007
Incorporation of sunscreens into lipid carriers with an increased sun protection factor (SPF) has... more Incorporation of sunscreens into lipid carriers with an increased sun protection factor (SPF) has not yet been fully accomplished. In the present paper, the effectiveness of a sunscreen mixture, incorporated into the novel topical delivery systems, i.e. solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC), used as ultraviolet (UV) protector enhancers with a distinctly higher loading capacity has been developed and evaluated. SLN and NLC were produced by hot high pressure homogenization technique in lab scale production. Size distribution and storage stability of formulations were investigated by laser diffractometry and photon correlation spectroscopy. Nanoparticles were characterized by their melting and recrystallization behaviour recorded by differential scanning calorimetry. Lipid nanoparticles produced with a solid matrix (SLN and NLC) were established as a UV protection system. The loading capacities for molecular sunscreens reported before now were in the range of 10–15%. It was possible to load NLC with up to 70% with molecular sunscreen, which is appropriate to obtain high SPFs with this novel UV protection system. The developed formulations provide a beneficial alternative to conventional sunscreen formulations. The UV protective efficacy of the lipid particles varied with the nature of lipid and UV wavelength.L'incorporation des protections solaires dans des porteurs de lipide avec un facteur accru de protection du soleil n'a pas été encore entièrement accomplie. Dans le papier de recherches il a été développée et évalué l'efficacité d'un mélange de protection solaire incorporé aux systèmes topiques, c.-à-d. les nanoparticule lipidique solide (SLN) et porteurs lipidique nano-structurés (NLC), utilisés en tant que renforceurs de protection ultra-violets (UV) et possédant une capacité nettement plus élevée de chargement. SLN et NLC ont été produits par une technique d'homogénéisation à haute pression chaude, en production d’échelle de laboratoire. La grandeur de distribution et la stabilité de stockage des formulations ont étéétudiées par difractometrie laser (LD) et spectroscopie de corrélation fotonique (PCS). Les nanoparticules ont été caractérisées par leurs comportement de fusion et de recristallisation, et enregistrées par calorimétrie à balayage différentiel (DSC). Des nanoparticules lipidique produites avec une matrice solide (SLN et NLC) ont étéétablis comme système de protection UV. Les capacités de chargement, pour les protections solaires moléculaires rapportées avant, étaient maintenant dans la gamme de 10–15%. Il a été possible de charger les NLC avec jusqu’à 70% de protection solaire moléculaire, ce qui est appropriée pour obtenir les facteurs élevés de protection solaire (SPF) avec ce système de protection UV. Les formulations développées fournissent une alternative salutaire aux formulations de protection solaire conventionelles. L'efficacité de la protection UV des particules de lipide a changé avec la nature du lipide et la longueur d'onde des UV.
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Journal of Microencapsulation, 2008
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International Journal of Pharmaceutics, 2009
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European Journal of Pharmaceutics and Biopharmaceutics, 2008
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Nanomedicine-nanotechnology Biology and Medicine, 2009
The eyes are among the most readily accessible organs in terms of location in the body, yet drug ... more The eyes are among the most readily accessible organs in terms of location in the body, yet drug delivery to eye tissues is particularly problematic. Poor bioavailability of drugs from ocular dosage forms is mainly due to precorneal loss factors (e.g., tear dynamics, nonproductive absorption, transient residence time in the cul-de-sac, and relative impermeability of the corneal epithelial membrane). There is a clear need for effective topical formulations capable of promoting drug penetration and maintaining therapeutic levels with a reasonable frequency of application--a strategy that can also result in enhancement of side effects that probably would not be acceptable. Delivery of a drug via a nanotechnology-based product fulfills three main objectives: enhancement of drug permeation, controlled release, and targeting. The inflammatory response of the ocular tissues is a common side effect associated with ophthalmic surgery. Together with steroidal agents, nonsteroidal anti-inflammatory drugs are used in eye surgery. In this review we focus on microemulsions, polymeric nanoparticles, liposomes, solid lipid nanoparticles, and drug nanocrystals as formulations incorporating anti-inflammatory drugs for ophthalmic application. This review focuses on microemulsions, polymeric nanoparticles, liposomes, solid lipid nanoparticles, and drug nanocrystals as novel high efficiency delivery systems of anti-inflammatory drugs in ophthalmic applications.
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International Journal of Nanotechnology, 2011
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Nanotechnology, 2011
The purpose of this study was to design and optimize a new topical delivery system for ocular adm... more The purpose of this study was to design and optimize a new topical delivery system for ocular administration of flurbiprofen (FB), based on lipid nanoparticles. These particles, called nanostructured lipid carriers (NLC), were composed of a fatty acid (stearic acid (SA)) as the solid lipid and a mixture of Miglyol® 812 and castor oil (CO) as the liquid lipids, prepared by the hot high pressure homogenization method. After selecting the critical variables influencing the physicochemical characteristics of the NLC (the liquid lipid (i.e. oil) concentration with respect to the total lipid (cOil/L (wt%)), the surfactant and the flurbiprofen concentration, on particle size, polydispersity index and encapsulation efficiency), a three-factor five-level central rotatable composite design was employed to plan and perform the experiments. Morphological examination, crystallinity and stability studies were also performed to accomplish the optimization study. The results showed that increasing cOil/L (wt%) was followed by an enhanced tendency to produce smaller particles, but the liquid to solid lipid proportion should not exceed 30 wt% due to destabilization problems. Therefore, a 70:30 ratio of SA to oil (miglyol + CO) was selected to develop an optimal NLC formulation. The smaller particles obtained when increasing surfactant concentration led to the selection of 3.2 wt% of Tween® 80 (non-ionic surfactant). The positive effect of the increase in FB concentration on the encapsulation efficiency (EE) and its total solubilization in the lipid matrix led to the selection of 0.25 wt% of FB in the formulation. The optimal NLC showed an appropriate average size for ophthalmic administration (228.3 nm) with a narrow size distribution (0.156), negatively charged surface (-33.3 mV) and high EE (~90%). The in vitro experiments proved that sustained release FB was achieved using NLC as drug carriers. Optimal NLC formulation did not show toxicity on ocular tissues.
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Current Eye Research, 2010
Due to the multiple barriers imposed by the eye against the penetration of drugs, the ocular deli... more Due to the multiple barriers imposed by the eye against the penetration of drugs, the ocular delivery and targeting are considered difficult to achieve. A major challenge in ocular drug therapy is to improve the poor bioavailability of topically applied ophthalmic drugs by overcoming the severe constraints imposed by the eye on drug absorption. One of the promising strategies nowadays is the use of colloidal carrier systems characterized by a submicron-meter size. Solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) represent promising alternatives to conventional and very popular ocular carrier systems, such as the nanoemulsions, liposomes, and polymeric nanoparticles. Nevertheless, taking into account the characteristics of the eye, morphometrical properties of the colloidal systems (e.g., average particle size and polydispersion) may represent a limiting factor for topical application without induced corneal irritation, being responsible for the selected system. This review article focuses on the application of lipid nanoparticles (SLN, NLC) as carriers for both non-steroidal and steroidal anti-inflammatory drugs for the treatment of ocular inflammatory disorders. Major benefits, as well as shortcomings, of ocular inflammation conditions are described, in particular upon management of inflammation induced by ocular surgery (e.g., cataracts, refractive surgery). Particular emphasis is given to the clinical choices currently available, while examining the most recent drugs that have been approved.
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Journal of Thermal Analysis and Calorimetry
This article reports the thermodynamic changes of lipid nanoparticles (LN) upon delivery of lipop... more This article reports the thermodynamic changes of lipid nanoparticles (LN) upon delivery of lipophilic vitamin E derivatives to the skin. Skin penetration of α-tocopherol (α-T) and α-tocopherol acetate (α-Ta) into and across porcine ear skin was investigated in vitro using tape-stripping test in modified Franz diffusion cells. Wide angle X-ray scattering (WAXS) and differential scanning calorimetry (DSC) have been used to characterize the polymorphism of the solid matrix of LN before and after in vitro skin penetration assay. Cetyl palmitate LN with a loading capacity of 20% of vitamin E derivatives (with regard to the lipid matrix) have shown the typical β’ modification of waxes, with a crystallinity index (%CI) between 30 and 40%. Mean particle size and shelf life stability was assessed by static (laser diffractometry, LD) and dynamic (photon correlation spectroscopy, PCS) light scattering techniques. Submicron-sized LN were produced, i.e., 99% of LN showed a size below 600 nm immediately after production. A mean size between 180 and 350 nm (polydispersity index < 0.25) was obtained for LN stored at both 8 and 22 °C, and this size range was kept constant for at least 20 days of shelf life. Quantification of α-T and α-Ta in the skin using tape-stripping provided a 3.4-fold increase in the level of actives within the stratum corneum (SC) and 1.3-fold increase in the viable epidermis (VE). LN increased skin penetration of both actives, following a cumulative release during 8 h in modified Franz diffusion cells. The differences in the distribution levels observed between α-T and α-Ta when delivered via LN was due to the different thermodynamic activity of both actives, i.e., following increased partition coefficient of α-Ta into SC and VE, in comparison to α-T.
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Papers by Eliana B. Souto