0000000001319183
AUTHOR
Ana Melero
Nanoencapsulation in Lipid-Core Nanocapsules Controls Mometasone Furoate Skin Permeability Rate and Its Penetration to the Deeper Skin Layers
<b><i>Aims:</i></b> The influence of nanoencapsulation of mometasone furoate (MF) in poly(ε-caprolactone) lipid-core nanocapsules (LNC) on its in vitro human skin permeation and penetration was evaluated. <b><i>Methods:</i></b> Semisolid formulations were prepared by increasing the viscosity of LNC using a carbomer (Carbopol® Ultrez at 0.5% w/v). Two complementary techniques (the static Franz diffusion cell model and the Saarbrücken penetration model) were used to evaluate skin permeation/penetration. <b><i>Results:</i></b> The drug release rate was decreased by nanoencapsulation. The skin permeability of MF was control…
Calcifediol-loaded liposomes for local treatment of pulmonary bacterial infections.
The influence of vitamin D3 and its metabolites calcifediol (25(OH)D) and calcitriol on immune regulation and inflammation is well described, and raises the question of potential benefit against bacterial infections. In the current study, 25(OH)D was encapsulated in liposomes to enable aerosolisation, and tested for the ability to prevent pulmonary infection by Pseudomonas aeruginosa. Prepared 25(OH)D-loaded liposomes were nanosized and monodisperse, with a negative surface charge and a 25(OH)D entrapment efficiency of approximately 23%. Jet nebulisation of liposomes was seen to yield an aerosol suitable for tracheo-bronchial deposition. Interestingly, 25(OH)D in either liposomes or ethanol…
Nortriptyline hydrochloride skin absorption: development of a transdermal patch.
The influence of propylen glycol (PG), ethanol, and oleic acid (OA) on nortriptyline hydrochloride (NTH) penetration through human epidermis was studied in vitro at two different pH values (5.5 and 7.4). The influence of lactic acid and polysorbate 80 was studied for a pH of 5.5. Permeation studies through Heat Separated Epidermis, as well as the enhancing effect of the different vehicles, showed a pH dependency. A pH value of 5.5 in the donor solution decreases significantly the permeability coefficient (Kp) with respect to a pH value of 7.4 (0.011+/-0.004 x 10(-6) versus 0.36+/-0.04 x 10(-6)cm/s). The vehicles showed an increasing enhancement effect in the order: polysorbate 80>ethanol/PG…
3D-Printed Products for Topical Skin Applications: From Personalized Dressings to Drug Delivery.
3D printing has been widely used for the personalization of therapies and on-demand production of complex pharmaceutical forms. Recently, 3D printing has been explored as a tool for the development of topical dosage forms and wound dressings. Thus, this review aims to present advances related to the use of 3D printing for the development of pharmaceutical and biomedical products for topical skin applications, covering plain dressing and products for the delivery of active ingredients to the skin. Based on the data acquired, the important growth in the number of publications over the last years confirms its interest. The semisolid extrusion technique has been the most reported one, probably …
Caffeic acid skin absorption: Delivery of microparticles to hair follicles
Graphical abstract: Emulsions containing CA were prepared, one of which contain free CA and the other microencapsulated CA. They were applied to delimited area of skin. Subsequently the tape stripping and differential striping methods were applied.
Naringenin Nano-Delivery Systems and Their Therapeutic Applications
Naringenin (NRG) is a polyphenolic phytochemical belonging to the class of flavanones and is widely distributed in citrus fruits and some other fruits such as bergamot, tomatoes, cocoa, and cherries. NRG presents several interesting pharmacological properties, such as anti-cancer, anti-oxidant, and anti-inflammatory activities. However, the therapeutic potential of NRG is hampered due to its hydrophobic nature, which leads to poor bioavailability. Here, we review a wide range of nanocarriers that have been used as delivery systems for NRG, including polymeric nanoparticles, micelles, liposomes, solid lipid nanoparticles (SLNs), nanostructured lipid carriers (NLCs), nanosuspensions, and nano…
Nanocarriers for optimizing the balance between interfollicular permeation and follicular uptake of topically applied clobetasol to minimize adverse effects.
The treatment of various hair disorders has become a central focus of good dermatologic patient care as it affects men and women all over the world. For many inflammatory-based scalp diseases, glucocorticoids are an essential part of treatment, even though they are known to cause systemic as well as local adverse effects when applied topically. Therefore, efficient targeting and avoidance of these side effects are of utmost importance. Optimizing the balance between drug release, interfollicular permeation, and follicular uptake may allow minimizing these adverse events and simultaneously improve drug delivery, given that one succeeds in targeting a sustained release formulation to the hair…
Polymeric microcontainers improve oral bioavailability of furosemide.
Microcontainers with an inner diameter of 223 μm are fabricated using the polymer SU-8, and evaluated in vitro, in situ and in vivo for their application as an advanced oral drug delivery system for the poorly water soluble drug furosemide. An amorphous sodium salt of furosemide (ASSF) is filled into the microcontainers followed by applying a lid using Eudragit L100. It is possible to control the drug release in vitro, and in vitro absorption studies show that the microcontainers are not a hindrance for absorption of ASSF. In situ perfusion studies in rats are performed with ASSF-filled microcontainers coated with Eudragit and compared to a furosemide solution. The absorption rate constant …
Caffeine analysis and extraction from a topical cream intended for UV-skin protection
Made available in DSpace on 2021-06-25T10:16:59Z (GMT). No. of bitstreams: 0 Previous issue date: 2020-01-01 This study aimed to develop and validate a method for the analysis of caffeine in complex cosmetic samples, such as sunscreens. Besides, an extraction method of caffeine from coffee oil and from creams, which contains both lipophilic and hydrophilic components, has been developed. The method to analyze caffeine was developed using an isocratic pump, Waters 1515 and an automatic injector Perkin-Elmer Series 200 and an UV detector Perkin-Elmer. As stationary phase, Kromasil C-18 (150 × 4.6 mm ID with particle size of 5 µm) column was used and a mixture of water (pH 4.00)/acetonitrile (…
Cubic Microcontainers Improve In Situ Colonic Mucoadhesion and Absorption of Amoxicillin in Rats
An increased interest in colonic drug delivery has led to a higher focus on the design of delivery devices targeting this part of the gastrointestinal tract. Microcontainers have previously facilitated an increase in oral bioavailability of drugs. The surface texture and shape of microcontainers have proven to influence the mucoadhesion ex vivo. In the present work, these findings were further investigated using an in situ closed-loop perfusion technique in the rat colon, which allowed for simultaneous evaluation of mucoadhesion of the microcontainers as well as drug absorption. Cylindrical, triangular and cubic microcontainers, with the same exterior surface area, were evaluated based on i…
Cranioplasty with autologous bone flaps cryopreserved with Dimethylsulphoxide : does tissue processing matter
Este artículo se encuentra disponible en la siguiente URL: https://www.sciencedirect.com/science/article/abs/pii/S1878875021001625?via%3Dihub En este artículo de investigación también participan: Dolores Ocete, Lucas Aranda, Ana Melero, Antonio J. Guillot, Nuria Yagüe y Carlos Botella. Este es el pre-print del siguiente artículo: Mirabet, V., García, D., Roca, A., Quiroz, A. R., Antón, J., Rodríguez-Cadarso, M., Ocete, D., Aranda, L., Melero, A., Guillot, A. J., Yagüe, N., Guillén, I. & Botella, C. (2021). Cranioplasty with autologous bone flaps cryopreserved with Dimethylsulphoxide: does tissue processing matter. World Neurosurgery, vol. 149 (may.), pp. e582?e591, que se ha publicado de fo…
Lipid Nanoparticles as Potential Gene Therapeutic Delivery Systems for Oral Administration.
Background Gene therapy has experimented an increasing attention in the last decades, due to its enormous potential applications in the medical field. It can be defined as the use of genes or genetic material (DNA, RNA, oligonucleotides) to treat or prevent a disease state, generally a geneticbased one. Application Other applications, like treating viral, bacterial or parasite infections or development of vaccines are gaining also interest. Efficient gene therapy is mainly dependent on the ability of the highly labile genetic material to reach the therapeutic target. For this purpose, different delivery systems have been designed and extensively investigated. Nanoparticles offer a broad ran…
Nortriptyline for smoking cessation: Release and human skin diffusion from patches
Abstract The objective of this work was to develop a simple and inexpensive transdermal formulation containing Nortriptyline Hydrochloride (NTH) for smoking cessation support therapy. Hydroxypropyl-methyl-cellulose was chosen as polymer and a mixture of transdermal enhancers (selected from previous research) was incorporated. The formulations were characterised in terms of appearance, thickness, uniformity of NTH content, release and skin permeation. Release studies demonstrated controlled release for four formulations. Diffusion studies were performed through human heat separated epidermis (HHSE) using Franz Diffusion Cells (FDC). Patches provided different fluxes varying from 20.39 ± 7.09…
Quantification of nortriptyline in plasma by HPLC and fluorescence detection
Abstract A simple, sensitive and specific high-performance liquid chromatography method has been developed for the determination of nortriptyline (NT) in plasma samples. The assay involved derivatization with 9H-fluoren-9-ylmethyl chloroformate (Fmoc-Cl) and isocratic reversed-phase (C 18 ) chromatography with fluorescence detection. The developed method required only 100 μl of plasma sample, deproteinized and derivatized in one step. Calibration curves were lineal over the concentration range of 5–5000 ng/ml. The derivatization reaction was performed at room temperature in 20 min and the obtained NT derivative was stable for at least 48 h at room temperature. The within-day and between-day…
Cyanocobalamin Ultraflexible Lipid Vesicles: Characterization and In Vitro Evaluation of Drug-Skin Depth Profiles
Atopic dermatitis (AD) and psoriasis are the most common chronic inflammatory skin disorders, which importantly affect the quality of life of patients who suffer them. Among other causes, nitric oxide has been reported as part of the triggering factors in the pathogenesis of both conditions. Cyanocobalamin (vitamin B12) has shown efficacy as a nitric oxide scavenger and some clinical trials have given positive outcomes in its use for treating skin pathologies. Passive skin diffusion is possible only for drugs with low molecular weights and intermediate lipophilicity. Unfortunately, the molecular weight and hydrophilicity of vitamin B12 do not predict its effective diffusion through the skin…
Wistar rat skin as surrogate for human skin in nortriptyline hydrochloride patch studies
Six different matrices were prepared containing nortriptyline hydrochloride (NTH) with hydroxypropyl-methyl-cellulose as polymer. A mixture of transdermal enhancers was included as part of the vehicle. Diffusion studies were carried out through Wistar rat full thickness skin using Franz cells. They were compared with previously determined human heat separated epidermis in order to test if this animal can be used as model for in vivo assays. A linear correlation was obtained between NTH diffusion coefficients through both skin types (r2=0.996).
Targeted delivery of Cyclosporine A by polymeric nanocarriers improves the therapy of inflammatory bowel disease in a relevant mouse model
The therapy of inflammatory bowel diseases is still rather inefficient, and about 80% of patients require surgery at some stage. Improving the treatments by more efficient medication is, therefore, an urgent medical need. The objective of this project was to demonstrate targeted delivery of Cyclosporine-A (CYA) to the inflamed areas of the intestinal mucosa after oral administration, enabling improved alleviation of the symptoms and, at the same time, reduced systemic drug absorption and associated adverse effects. As had already been demonstrated in previous studies, nano- to micrometer-sized drug particles will accumulate at inflamed mucosal areas, providing a platform for such purposes. …
Microneedle-Based Delivery: An Overview of Current Applications and Trends
Microneedle arrays (MNA) are considered as one of the most promising resources to achieve systemic effects by transdermal delivery of drugs. They are designed as a minimally invasive, painless system which can bypass the stratum corneum, overcoming the potential drawbacks of subcutaneous injections and other transdermal delivery systems such as chemical enhancers, nano and microparticles, or physical treatments. As a trendy field in pharmaceutical and biomedical research, its applications are constantly evolving, even though they are based on very well-established techniques. The number of molecules administered by MNA are also increasing, with insulin and vaccines administration being the …
Guava: phytochemical composition of a potential source of antioxidants for cosmetic and/or dermatological applications
Made available in DSpace on 2018-11-28T14:21:45Z (GMT). No. of bitstreams: 0 Previous issue date: 2017-01-01. Added 1 bitstream(s) on 2019-10-09T18:26:25Z : No. of bitstreams: 1 S1984-82502017000200612.pdf: 803011 bytes, checksum: 199524e8d40cccb25490594ec61b3ed8 (MD5) Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES) Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq) PADC-FCF-UNESP Fundação para o Desenvolvimento da UNESP (FUNDUNESP) Guava (Psidium guajava L.) is a native fruit of the American tropics with commercial applications for its taste, flavor and aroma. Numerous pharmacological uses have been described for it, such as the antiseptic effect of it…
Guava: phytochemical composition of a potential source of antioxidants for cosmetic and/or dermatological applications
ABSTRACT Guava (Psidium guajava L.) is a native fruit of the American tropics with commercial applications for its taste, flavor and aroma. Numerous pharmacological uses have been described for it, such as the antiseptic effect of its leaves, the use of the fresh fruit and tea from its leaves for the treatment of diarrhea, dysentery, diabetes mellitus, and others. However, considering its rich composition, the guava also is a potential source of antioxidants to be used in the development of new formulations for cosmetic and/or dermatological applications, the main focus of this research. Herein, we describe the study of the phytochemical composition and the antioxidant activity of a guava e…