Artículos (Farmacia y Tecnología Farmacéutica)
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Artículo La presencia de mujeres en los estudios de Farmacia de las universidades peninsulares españolas (1913-1936)(Sociedad Española de Historia de las Ciencias y de las Técnicas (SEHCYT), 2022) González Bueno, Antonio; Nuñez Valdés, Juan; Ramos Carrillo, Antonio; Universidad de Sevilla. Departamento de Farmacia y Tecnología FarmacéuticaLa incorporación de las mujeres a la actividad farmacéutica corre paralela a su actividad social. En este artículo nos ocupamos de describir el proceso que llevó a las mujeres a cursar, en la España metropolitana, los estudios de la Licenciatura en Farmacia. Utilizando los Anuarios Estadísticos de España (Fondo documental del Instituto Nacional de Estadística) cuantificamos la presencia de mujeres entre los inicios de la década de 1910 y el comienzo de la Guerra Civil española (1936), constatando una línea claramente ascendente; el mítico 10% del alumnado femenino se supera, en lo que a los estudios de Farmacia respecta, en el curso 1922/23. Los porcentajes de alumnas matriculadas en las Facultades de Farmacia tienden a la estabilización en el gozne de las décadas de 1920 a 1930; en el curso 1932/33 este porcentaje femenino rozaba un 20% (19.95%). De acuerdo con los datos ofrecidos por los Anuarios Estadísticos de España, fue la Facultad de Farmacia de la Universidad Central la que recibió un mayor número de alumnas; sus valores más altos se alcanzan durante el curso 1928/29 (32.15%); las otras universidades hispanas donde podían cursarse los estudios de Farmacia: Barcelona, Santiago de Compostela y Granada, presenta valores significativamente más bajos que la Central.Artículo Fibrosis Quística: tratamiento actual y avances con la nanotecnología(Universidad de Granada, 2020) Guerra Morillo, María Oliva; Rabasco Álvarez, Antonio María; González Rodríguez, María Luisa; Universidad de Sevilla. Departamento de Farmacia y Tecnología FarmacéuticaIntroducción: Actualmente, los tratamientos existentes para tratar la fibrosis quística (FQ) están diseña-dos para controlar sus síntomas, consistentes principalmente en retención de moco e infección crónica. Se propone la vía pulmonar como alternativa para la administración de los fármacos, principalmente antimicrobianos. Sin embargo, su rápido aclaramiento, que conduce a niveles bajos de fármaco e incremento de los regímenes posológicos, así como la aparición de efectos adversos, hacen de la nanotecnología una estrategia interesante para esta enfermedad. Objetivo: estudiar y analizar los diferentes sistemas nanoparticulares existentes para su uso por vía pulmonar, concretando en el uso de sistemas lipídicos para el tratamiento de la FQ. Método: se realizó una búsqueda no sistemática de artículos en diferentes bases de datos, en los últimos 10 años principalmente, siguiendo pautas establecidas de palabras clave. Resultados: Los progresos que se han conseguido en los últimos años hacen que la FQ pase a ser una enfermedad de adultos. Los tratamientos que se están usando en la actualidad están siendo cada vez más desplazados por otras alternativas, como los sistemas nanoparticulares, siendo idóneos para la administración pulmonar debido a su pequeño tamaño, su liberación sostenida y su elevada biocompatibilidad. Entre éstos, destacan los liposomas por su similitud estructural con el surfactante pulmonar, así como por su capacidad de destruir las biopelículas bacterianas. La mayoría de las formulaciones encontradas contenían un solo fármaco. Conclusión: Existen evidencias científicas que indican que la investigación debe dirigirse hacia el desarrollo de formulaciones que sean capaces de destruir la biopelícula.Artículo Generalidades sobre las vacunas comercializadas en España: estudio monográfico de la vacuna contra el sarampión(Universidad de Granada, 2020) Mejías Padilla, Carmen; Ginés Dorado, Juan Manuel; Universidad de Sevilla. Departamento de Farmacia y Tecnología FarmacéuticaIntroducción: la vacunación es, en la historia de la medicina, una de las actuaciones más significativas en la reducción de la mortalidad infantil y la erradicación de enfermedades. Sin embargo, con el apogeo de los denominados grupos “antivacunas” ha aumentado la incidencia de enfermedades infecciosas, entre ellas, el sarampión, cuya erradicación no ha sido posible para el año 2015, como había propuesto la Organización Mundial de la Salud. Objetivo: hemos estudiado diferentes aspectos tecnológicos de las vacunas comercializadas en España, centrándonos en las utilizadas contra el sarampión, y su problemática actual a la hora de su administración. Método: se ha realizado un estudio de las fichas técnicas de las vacunas recogidas en la Agencia Española de Medicamentos y Productos Sanitarios. Resultados: se obtuvieron resultados sobre diferentes aspectos: tipo de vacuna, sistema fisicoquímico, forma farmacéutica, vía de administración y dispositivo para su administración. Además, se han analizado las formulaciones de las vacunas existentes contra el sarampión, haciendo hincapié en los diversos excipientes que contienen: estabilizadores, antibióticos, medios de cultivo, etc. Conclusiones: la mayoría de las vacunas comercializadas en España se presentan en forma de suspensión para administración intramuscular o subcutánea mediante jeringa precargada. En el caso de la vacuna contra el sarampión, encontramos tres medicamentos de preparación extemporánea, que se presentan en forma de polvo liofilizado en vial y vehículo en jeringa precargada, producidas a partir de diferentes virus vivos o atenuados, siendo por tanto vacunas combinadasArtículo Development of Axitinib-loaded Polymeric Ocular Implants for the Treatment of Posterior Ocular Diseases(Elsevier, 2025) Annuryanti, Febri; Adhami, Masoud; Abdi, Ubah; Domínguez Robles, Juan; Larrañeta, Eneko; Vora, Lalitkumar K.; Raghu Raj Singh, Thakur; Universidad de Sevilla. Departamento de Farmacia y Tecnología Farmacéutica; Wellcome Trust; Ministerio de Ciencia e Innovación (MICIN). EspañaDiabetic retinopathy (DR) and age-related macular degeneration (AMD) are the primary causes of vision impairment and blindness worldwide. The current treatment for these diseases is an intravitreal injection of anti-VEGF agents, which are costly and require frequent injections. Implants can be used to sustain the release of drugs and minimize side effects. Axitinib (AX) is a potent VEGF receptor inhibitor and a promising candidate for treating posterior ocular diseases, such as diabetic retinopathy (DR) and age-related macular degeneration (AMD). A sustained release of AX was successfully achieved from 3D-printed AX-loaded implants fabricated using the well-known 3D printing technique, semi-solid extrusion (SSE). AX at concentrations of 10% w/w and 20% w/w was incorporated within the polycaprolactone (PCL) and Precirol®-based matrix. The fabricated implants were characterized via FTIR spectroscopy, SEM imaging, and thermal analysis. The implants were also evaluated for their drug release and biocompatibility. The AX-loaded implants exhibited thermal stability, and no chemical interactions were found between AX and the matrix components. The release mechanism study of AX revealed that the concentration of drug loading influenced AX release from the implant, with a 10% w/w and 20 %w/w of AX showing first-order and Korsmeyer-Peppas mechanism, respectively. A biocompatibility study using ARPE-19 cells confirmed that AX-loaded implants are nontoxic and safe for ocular use.Artículo Bioinspired Orthogonal-shaped protein–biometal Nanocrystals Enable Oral Protein Absorption(Elsevier, 2025) Durán Lobato, María Matilde; Tovar, Sulay; Cuñarro, Juan; Ramos Membrive, Rocío; Peñuelas, Iván; Marigo, Ilaria; Benetti, Federico; Chenlo, Miguel; Álvarez, Clara V.; Ildikó, Vashegyi; Alonso, María José; Universidad de Sevilla. Departamento de Farmacia y Tecnología Farmacéutica; European Union (UE); Ministerio de Ciencia e Innovación (MICIN). EspañaWith the growing number of marketed biological drugs, the development of technological strategies for their oral systemic absorption, becomes increasingly important. The harsh gastrointestinal environment and low permeability of the intestinal epithelium, represent a huge challenge for their systemic delivery. Herein, bioinspired in the physiological insulin-Zn interaction, the design of orthogonal-shaped protein-biometal hybrid nanocrystals, further enveloped by a bilayer of functional biomaterials, is reported. The nanocrystals exhibited a size of 80 nm, a neutral surface charge and a high insulin loading. In vitro studies showed the capacity of the nanocomplexes to control the release of the associated insulin, while preserving its stability. In vivo evaluation showed sustained blood glucose reductions in both healthy and diabetic rats (up to 40 % and 80 %, respectively), while chronic immunotoxicity studies in mice indicated no toxicity effect. Preliminary efficacy studies in healthy awake pigs following oral capsule administration showed over 20 % absolute bioavailability.Artículo Starch-Based scaffold produced by FDM 3D printing technique as Innovative and biosustainable wound dressing(Elsevier, 2025-05) Dominici, Franco; Imbriano, Anna; Puglia, Debora; Pagano, Cinzia; Luzi, Francesca; Rafanelli, Aurora; Michele, Alessandro Di; Bonacci, Francesco; Melo Barbosa, Raquel de; Perioli, Luana; Universidad de Sevilla. Departamento de Farmacia y Tecnología Farmacéutica; Italian Ministry of University and Research (MUR); Ministerio de Ciencia, Innovación y Universidades (MICIU). España; Junta de AndalucíaStarch is a safe biopolymer, whose use for the production of scaffolds intended for deep wounds treatment is limited, due to its low mechanical and thermal properties. For this reason, until now, it has been used in low amounts and/or in combination with other biopolymers. The aim of the study was to produce thermoplastic filaments (TPS) with high starch content, useful for scaffolds production by Fusion Deposition Modelling 3D printing technique. TPS was obtained by hot melt extrusion from a mixture of starch (70 % w/w) and glycerol (30 % w/w) combined to cationic clay montmorillonite, citric acid and magnesium stearate to improve strength and processability. The prepared scaffold was characterized and compared to other two scaffolds, where the effect of the addition of polycaprolactone (PCL) or methylsulphonylmethane (MSM) (as thermostable model drug) to the blend was evaluated. The mechanical properties were investigated by Brillouin Light Scattering. In vitro studies highlighted that the scaffolds are: i) able to absorb simulated exudates (reaching a hydration of 35 % in 7 days); ii) safe on keratinocytes (viability > 70 %) stimulating their growth; iii) able to inhibit S. pyogenes growth.Artículo Optimising 3D printed medications for rare diseases: In-line mass uniformity testing in direct powder extrusion 3D printing(Elsevier, 2025) Mora Castaño, Gloria; Rodríguez Pombo, Lucía; Carou-Senra, Paola; Januskaite, Patricija; Rial, Carlos; Bendicho-Lavilla, Carlos; Couce, Maria L.; Millán Jiménez, Mónica; Caraballo Rodríguez, Isidoro; Basit, Abdul W.; Alvarez-Lorenzo, Carmen; Goyanes, Alvaro; Universidad de Sevilla. Departamento de Farmacia y Tecnología Farmacéutica; Ministerio de Ciencia, Innovación y Universidades (MICIU). España; Xunta de Galicia; Fundación Mutua Madrileña; Engineering and Physical Sciences Research Council (EPSRC)Biotinidase deficiency is a rare inherited disorder characterized by biotin metabolism issues, leading to neurological and cutaneous symptoms that can be alleviated through biotin administration. Three-dimensional (3D) printing (3DP) offers potential for personalized medicine production for rare diseases, due to its flexibility in designing dosage forms and controlling release profiles. For such point-of-care applications, rigorous quality control (QC) measures are essential to ensure precise dosing, optimal performance, and product safety, especially for low personalized doses in preclinical and clinical studies. In this work, we addressed QC challenges by integrating a precision balance into a direct powder extrusion pharmaceutical 3D printer (M3DIMAKER™) for real-time, in-line mass uniformity testing, a critical quality control step. Small and large capsule-shaped biotin printlets (3D printed tablets) for immediate- and extended-release were printed. The integrated balance monitored and registered each printlet’s weight, identifying any deviations from acceptable limits. While all large printlet batches met mass uniformity criteria, some small printlet batches exhibited weight deviations. In vitro release studies showed large immediate-release printlets releasing 82% of biotin within 45 min, compared to 100% for small immediate-release printlets. For extended-release formulations, 35% of the drug was released from small printlets, whereas 24% was released from large printlets at the same time point. The integration of process analytical technology tools in 3DP shows promise in enhancing QC and scalability of personalized dosing at the point-of-care, demonstrating successful integration of a balance into a direct powder extrusion 3D printer for in-line mass uniformity testing across different sizes of capsule-shaped printlets.Artículo 3D-printed implants loaded with acriflavine for glioblastoma treatment(Elsevier, 2024-09-12) Korelidou, Anna; Domínguez Robles, Juan; Islam, Rayhanul; Donnelly, Ryan F.; Coulter, Jonathan A.; Larrañeta, Eneko; Universidad de Sevilla. Departamento de Farmacia y Tecnología Farmacéutica; European Union (UE). H2020; Agencia Estatal de Investigación. España; Ministerio de Ciencia e Innovación (MICIN). EspañaDrug delivery routes play an essential role in determining the efficacy and safety of medications. This study focused on the development and optimization of 3Dprinted reservoir type implants as a combinational therapy drug delivery system for Glioblastoma Multiforme (GBM) post-surgery, possessing also antibacterial properties. In this study, we used a multimodal agent, Acriflavine (ACF) as an alternative drug to treat GBM. To date, ACF is used only as an antiseptic agent, although it has been shown to possess strong anticancer activities. ACF and a low molecular weight PCL were loaded into 3D-printed reservoir-type implants for sustained drug delivery. The study demonstrated that ACF implants exhibited sustained drug release kinetics, with faster release during the initial 30 days, followed by a gradual decrease over 90 days. This controlled release profile enhances the effectiveness of ACF delivery to tumour targets while minimizing side effects associated with systemic administration. In vitro experiments confirmed the inhibitory activity of ACF against GBM cells compared to non-tumour cells. The study also highlighted the bacteriostatic effects of ACF, making the implants potentially useful for post-surgery infection management, particularly against S. aureus, a common bacterial infection associated with brain surgery. The long-term drug-release capabilities of the implants make them attractive candidates for both tumour inhibition and antibacterial treatment. The study suggests that the developed ACF delivery systems have the potential for future clinical studies. Their ability to provide increased drug efficacy without systemic toxicity makes them promising candidates for cancer therapy and post-surgery infection management.Artículo Halloysite Nanotube-Based Delivery of Pyrazolo[3,4-d]pyrimidine Derivatives for Prostate and Bladder Cancer Treatment(Multidisciplinary Digital Publishing Institute (MDPI), 2024) Massaro, M.; Ciani, R.; Grossi, G.; Cavallaro, G.; Melo Barbosa, Raquel de; Falesiedi, M.; Fortuna, C. G.; Carbone, A.; Schenone, S.; Sánchez Espejo, R.; Viseras, C.; Vago, R.; Riela, S.; Universidad de Sevilla. Departamento de Farmacia y Tecnología FarmacéuticaBackground/Objectives: The development of therapies targeting unregulated Src signaling through selective kinase inhibition using small-molecule inhibitors presents a significant challenge for the scientific community. Among these inhibitors, pyrazolo[3,4-d]pyrimidine heterocycles have emerged as potent agents; however, their clinical application is hindered by low solubility in water. To overcome this limitation, some carrier systems, such as halloysite nanotubes (HNTs), can be used. Methods: Herein, we report the development of HNT-based nanomaterials as carriers for pyrazolo[3,4-d]pyrimidine molecules. To achieve this objective, the clay was modified by two different approaches: supramolecular loading into the HNT lumen and covalent grafting onto the HNT external surface. The resulting nanomaterials were extensively characterized, and their morphology was imaged by high-angle annular dark-field scanning transmission electron microscopy (HAADF-STEM). In addition, the kinetic release of the molecules supramolecularly loaded into the HNTs was also evaluated. QSAR studies were conducted to elucidate the physicochemical and pharmacokinetic properties of these inhibitors, and structure-based virtual screening (SBVS) was performed to analyze their binding poses in protein kinases implicated in cancer. Results: The characterization methods demonstrate successful encapsulation of the drugs and the release properties under physiological conditions. Furthermore, QSAR studies and SBVS provide valuable insights into the physicochemical, pharmacokinetic, and binding properties of these inhibitors, reinforcing their potential efficacy. Conclusions: The cytotoxicity of these halloysite-based nanomaterials, and of pure molecules for comparison, was tested on RT112, UMUC3, and PC3 cancer cell lines, demonstrating their potential as effective agents for prostate and bladder cancer treatment.Artículo Avances terapéuticos en el abordaje de las fisuras anales: explorando la sinergia entre Farmacología y Nanotecnología(Universidad de Granada, 2024) Pazmiño Chiluiza, Carlos Ostwaldo; González Rodríguez, María Luisa; Universidad de Sevilla. Departamento de Farmacia y Tecnología FarmacéuticaIntroducción: La fisura anal es una patología proctológica frecuente, cronificante, caracterizada por la presencia de lesiones dolorosas ocasionadas por la hipertonía del musculo liso del esfínter anal interno. A pesar de su impac-to, los tratamientos convencionales disponibles pueden ser limitados en términos de reproducibilidad, eficacia y tolerabilidad a largo plazo. Debido a ello, la exploración de nuevas terapias farmacológicas, en sincronía con nano-vehículos que permitan su direccionamiento específico al lugar de acción, ofrecen una alternativa potencial para mejorar su tratamiento.Método: Se plantea como un estudio de tipo retrospectivo y longitudinal.Resultados: Se aplican diferentes abordajes terapéuticos, desde medidas higiénico-sanitarias, tratamientos far-macológicos no invasivos, hasta la cirugía, la mayoría de ellos dirigidos a disminuir la hipertonía. Los fármacos habituales a nivel hospitalario son lidocaína, diltiazem, nifedipino, nimodipino, nitrato de isosorbide y la toxina botulínica. Aprovechando las ventajas de la nanotecnología farmacéutica en la mejora de la eficacia terapéutica, disminuyendo los efectos adversos generados en la administración sistémica y aumentando la tasa de curación, se han encontrado estudios sobre la aplicación de nanopartículas poliméricas, vesiculares y micro-nano emulsiones para vehiculizar fármacos para el tratamiento sintomático de la fisura anal. Algunas formulaciones cuentan con autorización sanitaria y otras se encuentran en fase de investigación.Conclusiones: Se ha evidenciado que las nuevas formulaciones, especialmente aquellas basadas en nanotecno-logía, muestran un potencial significativo para mejorar la cicatrización de las fisuras en comparación con los trata-mientos convencionales. No obstante, son necesarios estudios sobre el uso seguro de estos sistemas antes de su implementación clínica generalizada.Artículo Factores asociados a la mortalidad en pacientes hospitalizados por COVID-19 en España: datos del Registro Español de Resultados de Farmacoterapia frente a COVID-19 (RERFAR)(Sociedad Española de Farmacia Hospitalaria, 2022) Olry de Labry Lima, Antonio; Sáez de la Fuente, Javier; Abdel-Kader Martín, Laila; Alegre del Rey, Emilio Jesús; García Cabrera, Emilio; Sierra Sánchez, Jesús F.; Universidad de Sevilla. Departamento de Farmacia y Tecnología Farmacéutica; Universidad de Sevilla. Departamento de Medicina Preventiva y Salud PúblicaObjetivo: Determinar las características basales que se asocian a una mayor mortalidad a los 42 días en aquellos pacientes hospitalizados por COVID-19 en España. Método: Cohorte prospectiva de pacientes COVID-19 hospitalizados. La variable dependiente fue la mortalidad a los 42 días. Además, se recogieron características demográficas, clínicas, comorbilidades, tratamiento habitual, intervenciones de soporte y tratamientos en las primeras 48 horas del ingreso. Para determinar la asociación con la mortalidad, se realizó un análisis multivariante mediante regresión logística. Resultados: Se incluyeron 15.628 pacientes, de ellos falleció el 18,2% (n = 2.806). El análisis multivariante mostró que las variables asociadas significativamente (p < 0,05) con la mortalidad al ingreso fueron: proceder de un centro sociosanitario (odds ratio OR 1,9), frecuencia respiratoria (odds ratio 1,5), gravedad de neumonía (CURB-65) moderada (odds ratio 1,7) o alta (odds ratio 2,9), transaminasa aspartato aminotransferasa ≥ 100 UI/l (odds ratio 2,1), lactato-deshidrogenasa ≥ 360 UI/l (odds ratio 1,6), procalcitonina > 0,5 ng/ml (odds ratio 1,8), creatina- quinasa ≥ 294 U/l (odds ratio 1,5), dímero D > 3.000 ng/ml (odds ratio 1,5), hemoglobina < 11,6 g/dl (odds ratio 1,4) y proteína C reactiva > 120 mg/l (odds ratio 1,2), necesidad de soporte respiratorio en las primeras 48 horas (odds ratio 2,0 de oxigenoterapia; odds ratio 2,8 ventilación no invasiva y odds ratio 3,5 ventilación mecánica) y tratamiento con interferón-beta (odds ratio 1,5). Por el contrario, ser menor de 80 años se asoció a una menor mortalidad. Conclusiones: El análisis del Registro Español de Resultados de farmacoterapia frente a COVID-19 muestra que los factores asociados a peor pronóstico son: mayor edad, valoración mediante la escala CURB‑65, el nivel de requerimiento de soporte respiratorio, neumonía grave (CURB‑65), hipertransaminasemia, elevación de creatina-quinasa, lactato- deshidrogenasa, y dímero-D, anemia y elevación de la frecuencia respiratoria.Artículo Innovations in Cancer Therapy: Endogenous Stimuli-Responsive Liposomes as Advanced Nanocarriers(MDPI, 2025-02-13) Torres, Jazmín; Valenzuela Oses, Johanna Karina; Rabasco Álvarez, Antonio María; González Rodríguez, María Luisa; García, Mónica Cristina; Universidad de Sevilla. Departamento de Farmacia y Tecnología Farmacéutica; Agencia Nacional de Promoción Científica y Tecnológica. Argentina; Consejo Nacional de Investigaciones Científicas y Técnicas (CONICET). Argentina; Universidad de Córdoba. ArgentinaRecent advancements in nanotechnology have revolutionized cancer therapy—one of the most pressing global health challenges and a leading cause of death—through the development of liposomes (L), lipid-based nanovesicles known for their biocompatibility and ability to encapsulate both hydrophilic and lipophilic drugs. More recent innovations have led to the creation of stimuli-responsive L that release their payloads in response to specific endogenous or exogenous triggers. Dual- and multi-responsive L, which react to multiple stimuli, offer even greater precision, improving therapeutic outcomes while reducing systemic toxicity. Additionally, these smart L can adjust their physicochemical properties and morphology to enable site-specific targeting and controlled drug release, enhancing treatment efficacy while minimizing adverse effects. This review explores the latest advancements in endogenous stimuli-responsive liposomal nanocarriers, as well as dual- and multi-responsive L that integrate internal and external triggers, with a focus on their design strategies, mechanisms, and applications in cancer therapy.Artículo Lipid nanoparticles as an emerging platform for cannabinoid delivery: physicochemical optimization and biocompatibility(Taylor & Francis, 2016) Durán Lobato, María Matilde; Martín Banderas, Lucía; Lopes, R.; Gonçalves, L.M.D.; Fernández Arévalo, María Mercedes; Universidad de Sevilla. Departamento de Farmacia y Tecnología Farmacéutica; Junta de Andalucía; Fundação para a Ciência e a Tecnologia. PortugalThis work aims at developing and optimizing a valuable oral delivery carrier for the cannabinoid derivative CB13, which presents a high therapeutic potential in chronic pain states that respond poorly to conventional analgesics, but also shows highly unfavorable physicochemical properties. CB13-loaded lipid nanoparticles (LNP) formulations were developed through solvent-emulsion evaporation and optimized in terms of physicochemical properties, long-term stability, integrity under gastric simulated conditions and in vitro interaction with NIH 3T3, HEK 293T and Caco-2 cells. An optimized formulation of LNP containing CB13 was obtained from a wide range of conditions assayed and analyzed. The selection of the lipid core, production conditions and the inclusion of lecithin proved to be key factors for the final properties of encapsulation, integrity and performance of the carriers. The LNP formulation proposed proved to be a promising carrier for the oral delivery of CB13, a cannabinoid with high therapeutic potential in chronic pain states that currently lack a valid oral treatment.Artículo Comparative study of chitosan- and PEG-coated lipid and PLGA nanoparticles as oral delivery systems for cannabinoids(Elsevier, 2015) Durán Lobato, María Matilde; Martín Banderas, Lucía; Gonçalves, Lídia M.D.; Fernández Arévalo, María Mercedes; Almeida, Antonio J.; Universidad de Sevilla. Departamento de Farmacia y Tecnología Farmacéutica; Junta de Andalucía; imed - Research Institute for Medicines. PortugalThe cannabinoid derivative 1-naphthalenyl[4-(pentyloxy)-1-naphthalenyl]methanone (CB13) has an important therapeutic potential as analgesic in chronic pain states that respond poorly to conventional drugs. However, the incidence of its mild-to-moderate and dose-dependent adverse effects, as well as its pharmacokinetic profile, actually holds back its use in humans. Thus, the use of a suitable carrier system for oral delivery of CB13 becomes an attractive strategy to develop a valuable therapy. Polymeric poly(lactic-co-glycolic) acid (PLGA) and lipid nanoparticles (LNPs) are widely studied delivery vehicles that improve the bioavailability of lipophilic compounds and present special interest in oral delivery. Their surface can be modified to improve the adhesion of particles to the oral mucosa and increase their circulation time in blood with additives such as chitosan (CS) and polyethylene glycol (PEG), which can be feasibly incorporated onto these particles in a post-production step. In this work, CS- and PEG-modified polymeric PLGA and LNPs were successfully obtained and comparatively evaluated under the same experimental conditions as oral carriers for CB13. All the formulations presented adequate blood compatibility and absence of cytotoxicity in Caco-2 cells. Coating with CS led to a higher interaction with Caco-2 cells and a limited uptake in THP1 cells, while coating with PEG led to a limited uptake in Caco-2 cells and strongly prevented THP1 cells uptake. The performance of each formulation is discussed as a comparison of the potential of these carriers as oral delivery systems of CB13.Artículo Engineering of Δ9-tetrahydrocannabinol delivery systems based on surface modified-PLGA nanoplatforms(Elsevier, 2014-11-01) Martín Banderas, Lucía; Muñoz Rubio, Inmaculada; Álvarez Fuentes, Josefa; Durán Lobato, María Matilde; Arias, José L.; Holgado Villafuerte, María Ángeles; Fernández Arévalo, María Mercedes; Universidad de Sevilla. Departamento de Farmacia y Tecnología Farmacéutica; Junta de Andalucía; Instituto de Salud Carlos IIIThe objective of this work is to develop a nanoplatform that can potentiate the oral administration of Δ9-tetrahidrocannabinol, a highly lipophilic active agent with very promising antiproliferative and antiemetic activities. To that aim, colloidal carriers based on the biodegradable and biocompatible poly(d,l-lactide-co-glycolide) were investigated. Such delivery systems were prepared by nanoprecipitation, and nanoparticle engineering further involved surface modification with a poly(ethylene glycol), chitosan, or poly(ethylene glycol)-chitosan shells to assure the greatest uptake by intestinal cells and to minimize protein adsorption. Characterization of the nanoplatforms included particle geometry (size and shape), electrophoretic properties (surface charge). Δ9-tetrahydrocannabinol vehiculization capabilities (loading and release), blood compatibility, and cellular uptake and cytotoxicity. Results were satisfactorily used to define the optimum engineering conditions to formulate surface modified nanoparticles for the efficient oral administration of Δ9-tetrahydrocannabinol. To the best of our knowledge, this is the first time that biocompatible polymeric nanoparticles have been formulated for Δ9-tetrahydrocannabinoldelivery.Artículo Biocompatible gemcitabine-based nanomedicine engineered by Flow Focusing® for efficient antitumor activity(Elsevier, 2013) Martín Banderas, Lucía; Sáez-Fernández, Eva; Holgado Villafuerte, María Ángeles; Durán Lobato, María Matilde; Prados, José C.; Melguizo, Consolación; Arias, José L.; Universidad de Sevilla. Departamento de Farmacia y Tecnología Farmacéutica; Instituto de Salud Carlos IIIWe investigated the incorporation of gemcitabine into a colloidal carrier based on the biodegradable and biocompatible poly(d,l-lactide-co-glycolide) (PLGA) to optimize its anticancer activity. Two synthesis techniques (double emulsion/solvent evaporation, and Flow Focusing®) were compared in terms of particle geometry, electrophoretic properties (surface charge), gemcitabine vehiculization capabilities (drug loading and release), blood compatibility, and in vitro antitumor activity. To the best of our knowledge, the second formulation methodology (Flow Focusing®) has never been applied to the synthesis of gemcitabine-loaded PLGA particles. With the aim of achieving the finest (nano)formulation, experimental parameters associated to these preparation procedures were analyzed. The electrokinetics of the particles suggested that the chemotherapy agent was incorporated into the polymeric matrix. Blood compatibility was demonstrated in vitro. Flow Focusing® led to a more appropriate geometry, higher gemcitabine loading and a sustained release profile. In addition, the cytotoxicity of gemcitabine-loaded particles prepared by Flow Focusing® was tested in MCF-7 human breast adenocarcinoma cells, showing significantly greater antitumor activity compared to the free drug and to the gemcitabine-loaded particles synthesized by double emulsion/solvent evaporation. Thus, it has been identified the more adequate formulation conditions in the engineering of gemcitabine-loaded PLGA nanoparticles for the effective treatment of tumours.Artículo Functional PLGA NPs for Oral Drug Delivery: Recent Strategies and Developments(Bentham Science, 2013) Martín Banderas, Lucía; Durán Lobato, María Matilde; Muñoz Rubio, Inmaculada; Álvarez Fuentes, Josefa; Fernández Arévalo, María Mercedes; Holgado Villafuerte, María Ángeles; Universidad de Sevilla. Departamento de Farmacia y Tecnología Farmacéutica; Junta de AndalucíaThis article presents the potential of PLGA nanoparticles for the oral administration of drugs. Different strategies are used to improve oral absorption of these nanoparticles. These strategies are based on modification of nanoparticle surface properties. They can be achieved either by coating the nanoparticle surface with stabilizing hydrophilic bioadhesive polymers or surfactants, or by incorporating biodegradable copolymers containing a hydrophilic moiety. Some substances such as chitosan, vitamin E, methacrylates, lectins, lecithins, bile salts and RGD molecules are employed for this purpose. Of especial interest are nanoparticles production methods and, in order to improve oral bioavailability, the mechanism of each additive.Artículo Cannabinoids as Emergent Therapy Against COVID-19(Mary Ann Liebert, 2022-10-12) McGrail, Joseph; Martín Banderas, Lucía; Durán Lobato, María Matilde; Universidad de Sevilla. Departamento de Farmacia y Tecnología FarmacéuticaThe coronavirus disease 2019 (COVID-19), caused by the severe acute respiratory distress syndrome coronavirus 2 (SARS-Cov-2), was identified for the first time in late 2019 in China, resulting in a global pandemic of massive impact. Despite a fast development and implementation of vaccination strategies, and the scouting of several pharmacological treatments, alternative effective treatments are still needed. In this regard, cannabinoids represent a promising approach because they have been proven to exhibit several immunomodulatory, anti-inflammatory, and antiviral properties in COVID-19 disease models and related pathological conditions. This mini-review aims at providing a practical brief overview of the potential applications of cannabinoids so far identified for the treatment and prevention of COVID-19, finally considering key aspects related to their technological and clinical implementation.Artículo Preparation and In Vivo Evaluation of Rosmarinic Acid-Loaded Transethosomes After Percutaneous Application on a Psoriasis Animal Model(Springer Nature, 2021) Rodríguez Luna, Azahara María; Talero Barrientos, Elena Mª; Ávila Román, Francisco Javier; Fernández Romero, Ana María; Rabasco Álvarez, Antonio María; Motilva Sánchez, Virginia; González Rodríguez, María Luisa; Universidad de Sevilla. Departamento de Farmacología; Universidad de Sevilla. Departamento de Farmacia y Tecnología Farmacéutica; Junta de Andalucía; Universidad de SevillaThe topical use of rosmarinic acid (RA) in skin inflammatory pathologies is restricted due to its poor water solubility, poor permeability, and chemical instability. In this study, RA-loaded transethosomes-in-Carbopol® formulations have been developed to evaluate its anti-inflammatory activity on imiquimod-induced psoriasis-like skin inflammation in mice. In vitro release profiles demonstrated sustained behavior due to the retentive action of gel and the entrapment of RA into the vesicles. However, the low viscosity of the combined formulation increased the drug release rate. Animal evaluation of anti-inflammatory activity demonstrated that transethosomes-in-gel containing dexamethasone (Dex-TE-Gel), as positive control, showed effect in all the pro-inflammatory parameters evaluated, evidencing that these drug-loaded nanocarriers have been effectively reached the site of action. In addition, transethosomes-in-gel containing RA (RA-TE-Gel) formulations produced a great reduction in the punch edema (P < 0.001) and in TNF-α and IL-6 (P < 0.05). However, non-significant differences were obtained for IL-1β, IL17, and MPO. Despite the protecting effect of Carbopol® and transethosomes on oxidation index and antioxidant activity of RA over the 7 days of treatment, however, a degradation process of this antioxidant to caffeic acid may be the cause of these in vivo results. We have also checked that the pH existing into the intercellular space of damaged cells (pH 6.8) may be affecting. Therefore, our results suggest that RA-TE-Gel could act as an effective RA formulation for skin delivery; further studies will help to understand the loss of activity at the cellular level.Artículo Drug diffusion from disperse systems with a hydrophobically modified polysaccharide: Enhancer (R) vs Franz cells(Elsevier Science Ltd, 2012-09-13) Lucero Muñoz, María Jesús; Claro Cala, Carmen María; Casas Delgado, Marta; Jiménez-Castellanos Ballesteros, María Rosa; Universidad de Sevilla. Departamento de Farmacología, Pediatría y Radiología; Universidad de Sevilla. Departamento de Farmacia y Tecnología FarmacéuticaThis study assesses the capacity of a new hydrophobically modified polysaccharide –hydroxypropyl cellulose–methyl methacrylate – to control drug release in semisolid formulations. The dispersed sys tems contain the new polymer, Igepal®CO520 as surfactant and theophylline as model drug at three concentrations (0.5, 1 and 1.5%, w/w). Drug release study shows that the systems containing 0.5% (w/w) of drug have faster release and higher diffusion coefficient than the other two concentrations. These results can be explained by two different structures (“relaxed” and “structured”) found from a rheologi cal point of view. Also, this paper compares two different devices for testing drug release and diffusion. It has been obtained more reliable and reproducible results with Enhancer Cell®respect to Franz diffusion cell. In both cases, Fickian diffusion was the mechanism predominant for all systems. Finally, the utility of this polymer has been demonstrated to make three-dimensional gel structure and control theophylline release from systems in topical application.