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2.
Int J Nanomedicine ; 16: 2405-2417, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-33814907

RESUMEN

Purpose: Ciprofloxacin (CIP) has poor lung targeting after oral inhalation. This study developed optimized inhalable nanostructured lipid carriers (NLCs) for CIP to enhance deposition and accumulation in deeper parts of the lungs for treatment of noncystic fibrosis bronchiectasis (NCFB). Methods: NLC formulations based on stearic acid and oleic acid were successfully prepared by hot homogenization and in vitro-characterized. CIP-NLCs were formulated into nanocomposite micro particles (NCMPs) for administration in dry powder inhalation (DPI) formulations by spray-drying (SD) using different ratios of chitosan (CH) as a carrier. DPI formulations were evaluated for drug content and in vitro deposition, and their mass median aerodynamic diameter (MMAD), fine particle fraction (FPF), fine particle dose (FPD), and emitted dose (ED) were determined. Results: The CIP-NLCs were in the nanometric size range (102.3 ± 4.6 nm), had a low polydispersity index (0.267 ± 0.12), and efficient CIP encapsulation (98.75% ± 0.048%), in addition to a spherical and smooth shape with superior antibacterial activity. The in vitro drug release profile of CIP from CIP-NLCs showed 80% release in 10 h. SD of CIP-NLCs with different ratios of CH generated NCMPs with good yield (>65%). The NCMPs had a corrugated surface, but with increasing lipid:CH ratios, more spherical, smooth, and homogenous NCMPs were obtained. In addition, there was a significant change in the FPF with increasing lipid:CH ratios (P ˂ 0.05). NCMP-1 (lipid:CH = 1:0.5) had the highest FPD (45.0 µg) and FPF (49.2%), while NCMP-3 (lipid:CH = 1:1.5) had the lowest FPF (37.4%). All NCMP powders had an MMAD in the optimum size range of 3.9-5.1 µm. Conclusion: Novel inhalable CIP NCMP powders are a potential new approach to improved target ability and delivery of CIP for NCFB treatment.


Asunto(s)
Bronquiectasia/tratamiento farmacológico , Ciprofloxacino/uso terapéutico , Portadores de Fármacos/química , Lípidos/química , Nanoestructuras/química , Administración por Inhalación , Antibacterianos/administración & dosificación , Antibacterianos/farmacología , Quitosano/química , Ciprofloxacino/administración & dosificación , Portadores de Fármacos/administración & dosificación , Liberación de Fármacos , Inhaladores de Polvo Seco , Fibrosis , Cinética , Liposomas , Pulmón , Pruebas de Sensibilidad Microbiana , Nanoestructuras/ultraestructura , Tamaño de la Partícula , Electricidad Estática
3.
Adv Exp Med Biol ; 1280: 39-55, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-33791973

RESUMEN

Shotgun lipidomics is an analytical approach for large-scale and systematic analysis of the composition, structure, and quantity of cellular lipids directly from lipid extracts of biological samples by mass spectrometry. This approach possesses advantages of high throughput and quantitative accuracy, especially in absolute quantification. As cancer research deepens at the level of quantitative biology and metabolomics, the demand for lipidomics approaches such as shotgun lipidomics is becoming greater. In this chapter, the principles, approaches, and some applications of shotgun lipidomics for cancer research are overviewed.


Asunto(s)
Lipidómica , Neoplasias , Lípidos , Espectrometría de Masas , Metabolómica , Investigación
4.
Adv Exp Med Biol ; 1280: 173-187, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-33791982

RESUMEN

Lipidomics refers to the large-scale study of pathways and networks of cellular lipids in biological systems. A lipidomic analysis often involves the identification and quantification of the thousands of cellular lipid molecular species within a complex biological sample and therefore requires a well optimized method for lipid profiling. In this chapter, the methods for lipidomic analysis, including sample collection and preparation, lipid derivatization and separation, mass spectrometric identification of lipids, data processing and interpretation, and quality control, are overviewed.


Asunto(s)
Lipidómica , Lípidos , Espectrometría de Masas , Control de Calidad
5.
Adv Exp Med Biol ; 1280: 231-241, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-33791986

RESUMEN

Although normal cells depend on exogenous lipids to function and survive, excessive amount of body fat has been associated with increased risk for certain human cancers. Cancer cells can redirect metabolic pathways to meet energy demands through the regulation of fatty acid metabolism. The importance of de novo fatty acid synthesis and fatty acid oxidation in cancer cells suggests fatty acid metabolism may be targeted for anticancer treatment through the use of pharmacological blockade to limit cell proliferation, growth, and transformation. However, our current knowledge about fatty acid metabolism in cancer cells remains limited, and the investigations of such processes and related pathways are certainly warranted to reveal the clinical relevance of fatty acid metabolism in cancer diagnosis and therapy.


Asunto(s)
Ácidos Grasos , Neoplasias , Proliferación Celular , Metabolismo Energético , Humanos , Metabolismo de los Lípidos , Lípidos
6.
Int J Mol Sci ; 22(6)2021 Mar 12.
Artículo en Inglés | MEDLINE | ID: mdl-33809364

RESUMEN

The conserved VPS13 proteins constitute a new family of lipid transporters at membrane contact sites. These large proteins are suspected to bridge membranes and form a direct channel for lipid transport between organelles. Mutations in the 4 human homologs (VPS13A-D) are associated with a number of neurological disorders, but little is known about their precise functions or the relevant contact sites affected in disease. In contrast, yeast has a single Vps13 protein which is recruited to multiple organelles and contact sites. The yeast model system has proved useful for studying the function of Vps13 at different organelles and identifying the localization determinants responsible for its membrane targeting. In this review we describe recent advances in our understanding of VPS13 proteins with a focus on yeast research.


Asunto(s)
Transporte Biológico/genética , Membrana Celular/genética , Lípidos/genética , Proteínas de Saccharomyces cerevisiae/genética , Membrana Celular/metabolismo , Humanos , Membranas Mitocondriales/metabolismo , Mutación/genética , Saccharomyces cerevisiae/genética , Saccharomyces cerevisiae/metabolismo
7.
Medicine (Baltimore) ; 100(8): e24576, 2021 Feb 26.
Artículo en Inglés | MEDLINE | ID: mdl-33663065

RESUMEN

BACKGROUND: Diabetes is a chronic metabolic disease characterized by elevated blood glucose levels due to insulin resistance and ß-cell dysfunction. In China, Huangyusang decoction (HYS) has been widely used to treat Type 2 diabetes. However, there is no systematic review found. In order to evaluate the efficacy and safety of HYS in the treatment of Type 2 diabetes, we need to conduct a meta-analysis and systematic evaluation. METHODS: We will enroll the randomized controlled trials (RCTs) evaluating the effectiveness and safety of HYS in the treatment of Type 2 diabetes. Data come mainly from 4 Chinese databases (CNKI, Wanfang, CBM, and VIP Database) and 4 English databases (PubMed, Embase, Cochrane Library, and Web of science). The enrollment of RCTs is from the starting date of database establishment till January 30, 2021. Fasting blood glucose is considered as the main indicator of the dyslipidemia, while the body mass index, glycated hemoglobin, fasting insulin, triglycerides, and cholesterol are regarded as the secondary indicators. There are safety indicators including liver enzyme and kidney function. The work such as selection of literature, data collection, quality evaluation of included literature, and assessment of publication bias will be conducted by 2 independent researchers. Meta-analysis will be performed by RevMan 5.0 software. RESULTS: This study will provide high-quality evidence for the effectiveness and safety of HYS in the treatment of type 2 diabetes. CONCLUSION: The results of the study will help us determine whether HYS can effectively treat type 2 diabetes. ETHICS AND DISSEMINATION: This study does not require ethical approval. We will disseminate our findings by publishing results in a peer-reviewed journal. OSF REGISTRATION NUMBER: DOI 10.17605/OSF.IO/AXBRV.


Asunto(s)
Diabetes Mellitus Tipo 2/tratamiento farmacológico , Medicamentos Herbarios Chinos/uso terapéutico , Glucemia , Índice de Masa Corporal , Medicamentos Herbarios Chinos/administración & dosificación , Medicamentos Herbarios Chinos/efectos adversos , Hemoglobina A Glucada , Humanos , Pruebas de Función Renal , Lípidos/sangre , Pruebas de Función Hepática , Ensayos Clínicos Controlados Aleatorios como Asunto , Proyectos de Investigación
8.
Sci Total Environ ; 771: 144700, 2021 Jun 01.
Artículo en Inglés | MEDLINE | ID: mdl-33736139

RESUMEN

The present study has tested the biodiesel potential of two hyper lipid producing strains Chlorella sp. and Scenedesmus sp. in terms of biomass yield, quantity and quality of lipid and fatty acid composition. Biomass yield of Chlorella sp. and Scenedesmus sp. was 1.26 and 1.33 g/L, respectively on day 18 and 20. The lipid content and lipid productivity of Chlorella sp. and Scenedesmus sp. was estimated to be 21.3, 26.5% and 12.33, 14.74 mg/L/d, respectively. Notably, relative abundance of lipid types in both the strains revealed >60% neutral lipids followed by glycolipids and phospholipids in minimal level. Central composite design based optimization revealed 69 and 65.4% FAME yield from Chlorella sp. and Scenedesmus sp. at 3% sulphuric acid and 65 °C reaction temperature. Eventually, higher levels of saturated fatty acids (~45%) and monounsaturated fatty acids (~34%) and make Scenedesmus sp. a promising parent material for workable biodiesel production.


Asunto(s)
Chlorella , Microalgas , Scenedesmus , Biocombustibles , Biomasa , Ésteres , Ácidos Grasos , Lípidos
9.
Adv Exp Med Biol ; 1316: 25-39, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-33740241

RESUMEN

Lipids have many critical biological functions in cancer. There are characteristic changes of lipid metabolism and metabolites in different physiological and pathological processes. Lipidomics is an emerging discipline of metabolomics for systematic analysis of lipids in organisms, tissues, or cells and the molecules that interact with them. With the development of new analytical techniques, especially the application and development of mass spectrometry techniques, the determination of lipids can be carried out quickly and accurately and has a high throughput. A large number of studies have shown that abnormal lipid metabolism is closely related to the occurrence and development of tumors. The application of lipidomics technology can reveal changes in lipids and relative abnormal metabolic pathways associated with tumors. Moreover, it shows a wide range of application prospects in the identification of tumor lipid biomarkers, early tumor diagnosis, and the discovery of antitumor drug targets. This chapter mainly introduces the application and development direction of lipidomics in the diagnosis and therapy of different tumors.


Asunto(s)
Lipidómica , Neoplasias , Humanos , Metabolismo de los Lípidos , Lípidos , Metabolómica , Neoplasias/diagnóstico , Neoplasias/tratamiento farmacológico
10.
Adv Exp Med Biol ; 1316: 1-24, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-33740240

RESUMEN

Lipids are the critical components of cellular and plasma membrane, which constitute an impermeable barrier of cellular compartments, and play important roles on numerous cellular processes including cell growth, proliferation, differentiation, and signaling. Alterations in lipid metabolism have been implicated in the development and progression of cancers. However, unlike other biomolecules, the diversity in the structures and characteristics of lipid species results in the limited understanding of their metabolic alterations in cancers. Lipidomics is an emerging discipline that studies lipids in a large scale based on analytical chemistry principles and technological tools. Multidimensional mass spectrometry-based shotgun lipidomics (MDMS-SL) uses direct infusion to avoid difficulties from alterations in concentration, chromatographic anomalies, and ion-pairing alterations to improve resolution and achieve rapid and accurate qualitative and quantitative analysis. In this chapter, lipids and lipid metabolism relevant to cancer research are introduced, followed by a brief description of MDMS-SL and other shotgun lipidomics techniques and some applications for cancer research.


Asunto(s)
Metabolismo de los Lípidos , Neoplasias , Lipidómica , Lípidos , Espectrometría de Masas , Metabolómica
11.
Adv Exp Med Biol ; 1316: 49-69, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-33740243

RESUMEN

Metabolic reprogramming is one of the most critical hallmarks in cancer cells. In the past decades, mounting evidence has demonstrated that, besides the Warburg Effect, lipid metabolism dysregulation is also one of the essential characteristics of cancer cell metabolism. Lipids are water-insoluble molecules with diverse categories of phosphoglycerides, triacylglycerides, sphingolipids, sterols, etc. As the major utilization for energy storage, fatty acids are the primary building blocks for synthesizing triacylglycerides. And phosphoglycerides, sphingolipids, and sterols are the main components constructing biological membranes. More importantly, lipids play essential roles in signal transduction by functioning as second messengers or hormones. Much evidence has shown specific alterations of lipid metabolism in cancer cells. Consequently, the structural configuration of biological membranes, the energy homeostasis under nutrient stress, and the abundance of lipids in the intracellular signal transduction are affected by these alterations. Furthermore, lipid droplets accumulate in cancer cells and function adaptively to different types of harmful stress. This chapter reviews the regulation, functions, and therapeutic benefits of targeting lipid metabolism in cancer cells. Overall, this chapter highlights the significance of exploring more potential therapeutic strategies for malignant diseases by unscrambling lipid metabolism regulation in cancer cells.


Asunto(s)
Metabolismo de los Lípidos , Neoplasias , Homeostasis , Humanos , Gotas Lipídicas/metabolismo , Lípidos , Neoplasias/metabolismo
12.
Zhonghua Zhong Liu Za Zhi ; 43(3): 318-323, 2021 Mar 23.
Artículo en Chino | MEDLINE | ID: mdl-33752312

RESUMEN

Objective: To investigate the effect of serum lipid level on prognosis of patients with small cell lung cancer (SCLC) at the initial treatment. Methods: The clinical data of patients with SCLC from 2012 to 2017 in our hospital were retrospectively analyzed. According to the standard of appropriate level and abnormal stratification of blood lipid in Chinese population, the lipids included total cholesterol (TC), triglyceride (TG), high-density lipoprotein cholesterol (HDLC) and low-density lipoprotein cholesterol (LDLC) at the time of initial treatment were grouped. Then the relationship between different lipid levels and clinicopathological characteristics was analyzed. Finally, Cox proportional hazard model was used to analyze the independent prognostic factors of patients. Results: A total of 129 patients with SCLC were included in this study. At the time of initial treatment, there were 90 (69.8%) cases whose TC < 5.2 mmol/L, while 39 (30.2%) cases ≥5.2 mmol/L; 95 (73.6%) cases whose TG <1.7 mmol/L, while 34 (26.4%) cases ≥1.7 mmol/L; 27 (20.9%) cases whose HDLC <1.0 mmol/L while 102 cases (79.1%) ≥1.0 mmol/L; 90 (69.8%) cases whose LDLC <3.4 mmol/L while 39 cases (30.2%) ≥3.4 mmol/L. The patients' triglyceride initial treatment was associated with their body mass index (P<0.05). The median disease-free survival (PFS) of SCLC patients was related with their serum TC level and clinical stage (P<0.05) and the overall survival (OS) was related with clinical stage of SCLC patients (P<0.05). The median PFS of SCLC patients in the TC <1.7 mmol/L group at the initial treatment was 10.5 months, significantly longer than 8.8 months of the TC ≥1.7 mmol/L group (P=0.024). The median OS of SCLC patients in the TG <1.7 mmol/L group at the initial treatment was 20.2 months, marginally longer than 15.6 months of the TG ≥1.7 mmol/L group (P=0.097). Multivariate analysis result showed that, the TG level was an independent risk factor of SCLC progression at the time of initial treatment (P=0.024). There was no significant correlation of TC, HDLC, LDLC and SCLC prognosis (P>0.05). Conclusion: TG level is an independent risk factor for the progression of SCLC at the time of initial treatment, and the increase of TG level indicates rapid disease progression and poor prognosis.


Asunto(s)
Neoplasias Pulmonares , Carcinoma Pulmonar de Células Pequeñas , HDL-Colesterol , Humanos , Lípidos , Pronóstico , Estudios Retrospectivos , Carcinoma Pulmonar de Células Pequeñas/tratamiento farmacológico , Triglicéridos
13.
Nat Commun ; 12(1): 1592, 2021 03 11.
Artículo en Inglés | MEDLINE | ID: mdl-33707447

RESUMEN

Parkinson's disease (PD) is a progressive neurodegenerative disorder, which is characterised by degeneration of distinct neuronal populations, including dopaminergic neurons of the substantia nigra. Here, we use a metabolomics profiling approach to identify changes to lipids in PD observed in sebum, a non-invasively available biofluid. We used liquid chromatography-mass spectrometry (LC-MS) to analyse 274 samples from participants (80 drug naïve PD, 138 medicated PD and 56 well matched control subjects) and detected metabolites that could predict PD phenotype. Pathway enrichment analysis shows alterations in lipid metabolism related to the carnitine shuttle, sphingolipid metabolism, arachidonic acid metabolism and fatty acid biosynthesis. This study shows sebum can be used to identify potential biomarkers for PD.


Asunto(s)
Metabolismo de los Lípidos/fisiología , Lípidos/análisis , Enfermedad de Parkinson/patología , Sebo/metabolismo , Anciano , Ácido Araquidónico/metabolismo , Biomarcadores/análisis , Carnitina/metabolismo , Cromatografía Liquida , Ácidos Grasos/biosíntesis , Femenino , Humanos , Masculino , Espectrometría de Masas , Metabolómica/métodos , Persona de Mediana Edad , Esfingolípidos/metabolismo
14.
Medicine (Baltimore) ; 100(13): e25303, 2021 Apr 02.
Artículo en Inglés | MEDLINE | ID: mdl-33787620

RESUMEN

ABSTRACT: This study aimed to investigate the association between mean platelet volume (MPV) and metabolic syndrome (MetS) in patients with type 2 diabetes mellitus (T2DM). Data for 1240 patients with T2DM admitted to the Department of Endocrinology at the First Affiliated Hospital of Guangxi Medical University between January 1, 2017 and June 1, 2020 were collected retrospectively via electronic medical records, including demographic information, complete blood count, lipid profile, and glucose metabolism indexes. MetS was defined according to the Chinese Diabetes Society. Among the 1240 patients enrolled, 873 (70.40%) had MetS. MPV was significantly higher in patients with MetS (P < .001). For individual MetS components, MPV was significantly higher in the presence of abdominal obesity (P = .013) and hypertriglyceridemia (P = .026), but did not differ in the presence of elevated blood pressure (P = .330) or low high-density lipoprotein cholesterol (P = .790). Moreover, MPV was independently associated with MetS after adjustment for sex, smoking, alcohol drinking, white blood cell count, fasting C-peptide, and body mass index (odds ratio 1.174, 95% confidence interval 1.059-1.302). The odds ratio for MetS in the highest tertile, compared with the lowest MPV tertile, was 1.724 (95% confidence interval 1.199-2.479, P for trend = .003) after multiple adjustment. In stratified analyses, the positive correlation of MPV with MetS was significant only in patients who were older, male, or overweight, or who had poor glycemic control. In conclusion, high MPV was positively associated with the presence of MetS in patients with T2DM, particularly older, male, or overweight patients, or those with poor glycemic control.


Asunto(s)
Diabetes Mellitus Tipo 2/sangre , Volúmen Plaquetario Medio , Síndrome Metabólico/sangre , Adulto , Factores de Edad , Anciano , Recuento de Células Sanguíneas , Glucemia , Presión Sanguínea , Índice de Masa Corporal , China , Diabetes Mellitus Tipo 2/complicaciones , Femenino , Humanos , Lípidos/sangre , Masculino , Síndrome Metabólico/etiología , Persona de Mediana Edad , Sobrepeso/sangre , Sobrepeso/complicaciones , Estudios Retrospectivos , Factores Sexuales
15.
Molecules ; 26(4)2021 Feb 13.
Artículo en Inglés | MEDLINE | ID: mdl-33668635

RESUMEN

Launaea nudicaulis is used in folk medicine worldwide to treat several diseases. The present study aimed to assess the antidiabetic activity of L. nudicaulis ethanolic extract and its effect on diabetic complications in streptozotocin-induced hyperglycemic rats. The extract was orally administrated at 250 and 500 mg/kg/day for 5-weeks and compared to glibenclamide as a reference drug at a dose of 5 mg/kg/day. Administration of the extract exhibited a potential hypoglycemic effect manifested by a significant depletion of serum blood glucose concurrent with a significant elevation in serum insulin secretion. After 5-weeks, extract at 250 and 500 mg/kg/day decreased blood glucose levels by about 53.8 and 68.1%, respectively, compared to the initial values (p ≤ 0.05). The extract at the two dosages prevented weight loss of rats from the 2nd week till the end of the experiment, compared to diabetic control rats. The extract further exhibited marked improvement in diabetic complications including liver, kidney and testis performance, oxidative stress, and relative weight of vital organs, with respect to diabetic control. Histopathological examinations confirmed the previous biochemical analysis, where the extract showed a protective effect on the pancreas, liver, kidney, and testis that degenerated in diabetic control rats. To characterize extract composition, UPLC-ESI-qTOF-MS identified 85 chromatographic peaks belonging to flavonoids, phenolics, acyl glycerols, nitrogenous compounds, and fatty acids, with four novel phenolics reported. The potential anti-diabetic effect warrants its inclusion in further studies and or isolation of the main bioactive agent(s).


Asunto(s)
Asteraceae/química , Diabetes Mellitus Experimental/tratamiento farmacológico , Etanol/química , Hipoglucemiantes/uso terapéutico , Extractos Vegetales/química , Extractos Vegetales/uso terapéutico , Animales , Antioxidantes/metabolismo , Biomarcadores/sangre , Glucemia/metabolismo , Peso Corporal/efectos de los fármacos , Diabetes Mellitus Experimental/sangre , Hipoglucemiantes/farmacología , Insulina/sangre , Riñón/efectos de los fármacos , Riñón/fisiopatología , Lípidos/sangre , Hígado/efectos de los fármacos , Hígado/fisiopatología , Masculino , Malondialdehído/sangre , Metabolómica , Tamaño de los Órganos/efectos de los fármacos , Especificidad de Órganos/efectos de los fármacos , Estrés Oxidativo/efectos de los fármacos , Extractos Vegetales/farmacología , Ratas Wistar , Estreptozocina , Pruebas de Toxicidad Aguda
16.
Int J Nanomedicine ; 16: 2247-2269, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-33776431

RESUMEN

Acute lung injury (ALI) or its aggravated stage acute respiratory distress syndrome (ARDS) may lead to a life-threatening form of respiratory failure, resulting in high mortality of up to 30-40% in most studies. Although there have been decades of research since ALI was first described in 1967, the clinical therapeutic alternatives for ALI are still in a state of limited availability. Supportive treatment and mechanical ventilation still have priority. Despite some preclinical studies demonstrating the benefit of pharmacological interventions, none of these has been proved completely effective to date. Recent advances in nanotechnology may shed new light on the pharmacotherapy of ALI. Nanomedicine possesses targeting and synergistic therapeutic capability, thus boosting pharmaceutical efficacy and mitigating the side effects. Currently, a variety of nanomedicine with diverse frameworks and functional groups have been elaborately developed, in accordance with their lung targeting ability and the pathophysiology of ALI. The in-depth review of the current literature reveals that liposomes, polymers, inorganic materials, cell membranes, platelets, and other nanomedicine approaches have conferred attractive therapeutic benefits for ALI treatment. In this review, we explore the recent progress in the study of the nanomedicine-based therapy of ALI, presenting various nanomedical approaches, drug choices, therapeutic strategies, and outcomes, thereby providing insight into the trends.


Asunto(s)
Lesión Pulmonar Aguda/terapia , Nanomedicina , Animales , Humanos , Lípidos/química , Polímeros/química , /terapia
17.
Int J Nanomedicine ; 16: 1977-1992, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-33727810

RESUMEN

Background: Phytostanols are naturally occurring compounds that reduce blood cholesterol levels significantly. However, their aqueous insolubility poses formulation challenges. Aim: To formulate and characterize solid lipid nanoparticle carriers for phytostanol esters to enhance the bioavailability of phytostanols. Methods: Phytostanol ester solid lipid nanoparticles were formulated by the microemulsion method. They were characterized for particle size distribution, polydispersity index, shape, surface charge, entrapment efficiency, stability, chemical structure, and thermal properties. The uptake of the formulation by cell lines, HepG2 and HT-29, and its effect on cell viability were evaluated. Results: The formulation of solid lipid nanoparticles was successfully optimised by varying the type of lipids and their concentration relative to that of surfactants in the present study. The optimised formulation had an average diameter of (171 ± 9) nm, a negative surface charge of (-23.0 ± 0.8) mV and was generally spherical in shape. We report high levels of drug entrapment at (89 ± 5)% in amorphous form, drug loading of (9.1 ± 0.5)%, nanoparticle yield of (67 ± 4)% and drug excipient compatibility. The biological safety and uptake of the formulations were demonstrated on hepatic and intestinal cell lines. Conclusion: Phytostanol ester solid lipid nanoparticles were successfully formulated and characterized. The formulation has the potential to provide an innovative drug delivery system for phytostanols which reduce cholesterol and have a potentially ideal safety profile. This can contribute to better management of one of the main risk factors of cardiovascular diseases.


Asunto(s)
Composición de Medicamentos , Ésteres/química , Hipercolesterolemia/tratamiento farmacológico , Lípidos/química , Nanopartículas/química , Fitosteroles/uso terapéutico , Muerte Celular , Emulsiones/química , Endocitosis , Citometría de Flujo , Células HT29 , Células Hep G2 , Humanos , Tamaño de la Partícula , Polvos , Espectroscopía Infrarroja por Transformada de Fourier , Electricidad Estática , Temperatura
18.
Int J Nanomedicine ; 16: 2013-2044, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-33727812

RESUMEN

Background: Sulpiride (SUL), is a selective antidopaminergic drug that had extensive biological activities. However, its sparingly aqueous solubility and limited gastrointestinal permeability lead to scanty oral bioavailability which hinders its clinical efficacy. Objective: SUL-loaded lipospheres (SUL-LPS) were designed to serve as an oral biocompatible nanovector for improving SUL permeability as well as conquering its low oral absorption and then in turn enhancing its antidepressant action. Methods: SUL-LPS were fabricated via two processing techniques namely, melt emulsification and solvent evaporation. The impact of different lipid cores, phospholipid shells together with various surfactant concentrations and types on the lipospheres properties were screened. Detailed physicochemical elucidations were performed followed by ex vivo permeation appraisal using the non-everted intestine model. The pharmacokinetic parameters of SUL-LPS, free SUL and marketed product were assessed following oral administration to healthy rats. Reserpine-induced depression rat model was used to assess the antidepressant action of SUL-LPS on which full behavioural and biochemical analysis was conducted. Safety attributes of nanoencapsulated SUL on the brain and other internal organs were evaluated. Results: The optimum LPS revealed an excellent nanosize with a narrow PdI, negative zeta potential and acceptable entrapment efficiency of 68.62 nm, 0.242, -30.4 mV and 84.12%, respectively. SUL-LPS showed a sustained release pattern and 2.1-fold enhancement in the intestinal permeation parameters with low mucin interaction. Oral pharmacokinetic appraisal exhibited that LPS provided 3.4-fold improvement in SUL oral bioavailability together with long-circulating properties, relative to the free drug. Pharmacodynamic study confirmed the superior antidepressant action of SUL-LPS as evident by 1.6 and 1.25-fold elevation in the serotonin and dopamine expressions, respectively. Meanwhile, nanotoxicological appraisal proved the biocompatibility of SUL-LPS upon repetitive oral administration. Conclusion: Rationally designed lipospheres hold promising in vitro and in vivo characteristics for efficient delivery of SUL with high oral bioavailability, antidepressant activity together with a good safety profile.


Asunto(s)
Antidepresivos/farmacología , Lípidos/química , Nanopartículas/química , Sulpirida/administración & dosificación , Sulpirida/farmacología , Administración Oral , Animales , Materiales Biocompatibles/química , Disponibilidad Biológica , Cromatografía Líquida de Alta Presión , Composición de Medicamentos , Liberación de Fármacos , Liofilización , Masculino , Mucinas/química , Nanopartículas/ultraestructura , Neurotransmisores/metabolismo , Especificidad de Órganos/efectos de los fármacos , Tamaño de la Partícula , Permeabilidad , Ratas Sprague-Dawley , Ratas Wistar , Sulpirida/química , Sulpirida/farmacocinética , Porcinos
19.
Sci Rep ; 11(1): 5494, 2021 03 09.
Artículo en Inglés | MEDLINE | ID: mdl-33750841

RESUMEN

It is important to pay attention to the indirect effects of the social distancing implemented to prevent the spread of coronavirus disease 2019 (COVID-19) pandemic on children and adolescent health. The aim of the present study was to explore impacts of a reduction in physical activity caused by COVID-19 outbreak in pediatric patients diagnosed with obesity. This study conducted between pre-school closing and school closing period and 90 patients aged between 6- and 18-year-old were included. Comparing the variables between pre-school closing period and school closing period in patients suffering from obesity revealed significant differences in variables related to metabolism such as body weight z-score, body mass index z-score, liver enzymes and lipid profile. We further evaluated the metabolic factors related to obesity. When comparing patients with or without nonalcoholic fatty liver disease (NAFLD), only hemoglobin A1c (HbA1c) was the only difference between the two time points (p < 0.05). We found that reduced physical activity due to school closing during COVID-19 pandemic exacerbated obesity among children and adolescents and negatively affects the HbA1C increase in NAFLD patients compared to non-NAFLD patients.


Asunto(s)
/patología , Intolerancia a la Glucosa/diagnóstico , Obesidad Pediátrica/diagnóstico , Adolescente , Alanina Transaminasa/análisis , Aspartato Aminotransferasas/análisis , Índice de Masa Corporal , Peso Corporal , Niño , Ejercicio Físico , Femenino , Intolerancia a la Glucosa/complicaciones , Hemoglobina A Glucada/análisis , Humanos , Lípidos/análisis , Hígado/enzimología , Masculino , Enfermedad del Hígado Graso no Alcohólico/complicaciones , Enfermedad del Hígado Graso no Alcohólico/diagnóstico , Obesidad Pediátrica/complicaciones , Cuarentena , /aislamiento & purificación
20.
Sheng Wu Gong Cheng Xue Bao ; 37(3): 846-859, 2021 Mar 25.
Artículo en Chino | MEDLINE | ID: mdl-33783154

RESUMEN

Microbial oils are potential resources of fuels and food oils in the future. In recent years, with the rapid development of systems biology technology, understanding the physiological metabolism and lipid accumulation characteristics of oleaginous microorganisms from a global perspective has become a research focus. As an important tool for systems biology research, omics technology has been widely used to reveal the mechanism of high-efficiency production of oils by oleaginous microorganisms. This provides a basis for rational genetic modification and fermentation process control of oleaginous microorganisms. In this article, we summarize the application of omics technology in oleaginous microorganisms, introduced the commonly used sample pre-processing and data analysis methods for omics analysis of oleaginous microorganisms, reviewe the researches for revealing the mechanism of efficient lipid production by oleaginous microorganisms based on omics technologies including genomics, transcriptomics, proteomics (modification) and metabolomics (lipidomics), as well as mathematical models based on omics data. The future development and application of omics technology for microbial oil production are also proposed.


Asunto(s)
Metabolómica , Proteómica , Fermentación , Lípidos , Tecnología
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