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Journal articles on the topic 'Glucocorticoids bioavailabilty'

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Published: 15 February 2025

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1

MacLeod, Clare, Patrick W. F. Hadoke, and Mark Nixon. "Glucocorticoids: Fuelling the Fire of Atherosclerosis or Therapeutic Extinguishers?" International Journal of Molecular Sciences 22, no. 14 (2021): 7622. http://dx.doi.org/10.3390/ijms22147622.

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Glucocorticoids are steroid hormones with key roles in the regulation of many physiological systems including energy homeostasis and immunity. However, chronic glucocorticoid excess, highlighted in Cushing’s syndrome, is established as being associated with increased cardiovascular disease (CVD) risk. Atherosclerosis is the major cause of CVD, leading to complications including coronary artery disease, myocardial infarction and heart failure. While the associations between glucocorticoid excess and increased prevalence of these complications are well established, the mechanisms underlying the

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Mitchell, Brett M., and R. Clinton Webb. "Impaired Vasodilation and Nitric Oxide Synthase Activity in Glucocorticoid-Induced Hypertension." Biological Research For Nursing 4, no. 1 (2002): 16–21. http://dx.doi.org/10.1177/1099800402004001003.

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Synthetic glucocorticoids are among the most widely prescribed medications by physicians. Although they have a vast array of beneficial effects such as immunosuppression and anti-inflammation, excess glucocorticoids can lead to iatrogenic Cushing’s syndrome, which includes hypertension and cardiovascular disease. The exact mechanism by which glucocorticoids elevate blood pressure is not completely understood, but it appears to be a complex pathology that involves increased responsiveness to vasoconstrictors and decreased vasodilator production. Nitric oxide is a vasodilator that plays a key ro

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Petersen, Helle Heibroch, Thomas K. Andreassen, Tilman Breiderhoff, et al. "Hyporesponsiveness to Glucocorticoids in Mice Genetically Deficient for the Corticosteroid Binding Globulin." Molecular and Cellular Biology 26, no. 19 (2006): 7236–45. http://dx.doi.org/10.1128/mcb.00400-06.

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ABSTRACT Corticosteroid binding globulin (CBG) is the carrier for glucocorticoids in plasma. The protein is believed to keep the steroids inactive and to regulate the amount of free hormone acting on target tissues (free hormone hypothesis). Here, we generated a mouse model genetically deficient for CBG to test the contribution of the carrier to glucocorticoid action and adrenocortical stress response. The absence of CBG resulted in a lack of corticosterone binding activity in serum and in an ∼10-fold increase in free corticosterone levels in CBG-null mice, consistent with its role in regulati

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Fowden, A. L., and A. J. Forhead. "Endocrine mechanisms of intrauterine programming." Reproduction 127, no. 5 (2004): 515–26. http://dx.doi.org/10.1530/rep.1.00033.

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Epidemiological findings and experimental studies in animals have shown that individual tissues and whole organ systems can be programmedin uteroduring critical periods of development with adverse consequences for their function in later life. Detailed morphometric analyses of the data have shown that certain patterns of intrauterine growth, particularly growth retardation, can be related to specific postnatal outcomes. Since hormones regulate fetal growth and the development of individual fetal tissues, they have a central role in intrauterine programming. Hormones such as insulin, insulin-li

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WIEDERSBERG, S. "Bioavailability and bioequivalence of topical glucocorticoids." European Journal of Pharmaceutics and Biopharmaceutics 68, no. 3 (2008): 453–66. http://dx.doi.org/10.1016/j.ejpb.2007.08.007.

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Freeman, Lisa, Martin Hewison, Susan V. Hughes та ін. "Expression of 11β-hydroxysteroid dehydrogenase type 1 permits regulation of glucocorticoid bioavailability by human dendritic cells". Blood 106, № 6 (2005): 2042–49. http://dx.doi.org/10.1182/blood-2005-01-0186.

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Abstract Glucocorticoids (GCs) exert powerful anti-inflammatory effects that may relate in part to their ability to restrict the differentiation and function of dendritic cells (DCs). Although these inhibitory effects are dependent upon GCs binding to nuclear glucocorticoid receptors (GRs), fine-tuning of GR signaling is achieved by prereceptor interconversion of cortisol that binds GRs with high affinity and cortisone that does not. We show for the first time that human monocyte-derived DCs are able to generate cortisol as a consequence of up-regulated expression of the enzyme 11β-hydroxyster

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Cattaneo, Dario, Norberto Perico, Flavio Gaspari, Eliana Gotti, and Giuseppe Remuzzi. "Glucocorticoids interfere with mycophenolate mofetil bioavailability in kidney transplantation." Kidney International 62, no. 3 (2002): 1060–67. http://dx.doi.org/10.1046/j.1523-1755.2002.00531.x.

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Hu, Aihua, Sumbul Fatma, Jing Cao та ін. "Th2 cytokine-induced upregulation of 11β-hydroxysteroid dehydrogenase-1 facilitates glucocorticoid suppression of proasthmatic airway smooth muscle function". American Journal of Physiology-Lung Cellular and Molecular Physiology 296, № 5 (2009): L790—L803. http://dx.doi.org/10.1152/ajplung.90572.2008.

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The anti-inflammatory actions of endogenous glucocorticoids (GCs) are regulated by the activities of the GC-activating and -inactivating enzymes, 11β-hydroxysteroid dehydrogenase (11β-HSD)-1 and 11β-HSD2, respectively, that catalyze the interconversion of the inert GC, cortisone, and its bioactive derivative, cortisol. Proinflammatory cytokines regulate 11β-HSD1 expression in various cell types and thereby modulate the bioavailability of cortisol to the glucocorticoid receptor (GR). Since endogenous GCs reportedly attenuate the airway asthmatic response to allergen exposure, we investigated wh

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Kamada, Alan K., Matthew B. Wiener, Nicole M. LaVallee, Maryanne Bartoszek Scott, John C. Seiner, and Stanley J. Szefler. "A Pharmacokinetic Comparison of Two Oral Liquid Glucocorticoid Formulations." Pharmacotherapy: The Journal of Human Pharmacology and Drug Therapy 17, no. 2 (1997): 353–56. http://dx.doi.org/10.1002/j.1875-9114.1997.tb03719.x.

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To compare pharmacokinetics of liquid prednisolone and prednisone solutions and to assess relative bioavailability, six healthy adult men were administered 15 mg of each formulation. Blood samples were obtained and assayed for plasma prednisolone concentrations by high‐performance liquid chromatography. Peak concentration was significantly higher with liquid prednisolone (mean ± SD 430.3 ± 62.5 vs 333.0 ± 27.8 ng/ml, p=0.013), with similar times to peak concentration. Prednisolone liquid gave higher concentrations at every time point (statistically significant for all except 0.25 hrs after the

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Elder, Charlotte J., Ruben Vilela, Trevor N. Johnson, et al. "Pharmacodynamic studies of nasal tetracosactide with salivary glucocorticoids for a noninvasive Short Synacthen Test." Journal of Clinical Endocrinology & Metabolism 105, no. 8 (2020): 2692–703. http://dx.doi.org/10.1210/clinem/dgaa323.

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Abstract Context The Short Synacthen Test (SST) is the gold standard for diagnosing adrenal insufficiency. It requires invasive administration of Synacthen, venous sampling, and is resource-intensive. Objective To develop a nasally administered SST, with salivary glucocorticoids measurement, to assess the adrenal response. Design We conducted 5 studies: 4 open-label, sequence-randomized, crossover, pharmacodynamic studies testing 6 doses/formulations and a repeatability study. Additionally, pharmacokinetic analysis was undertaken using our chosen formulation, 500 µg tetracosactide with mucoadh

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Perogamvros, I., C. Underhill, D. E. Henley, et al. "Novel Corticosteroid-Binding Globulin Variant That Lacks Steroid Binding Activity." Endocrine Reviews 31, no. 4 (2010): 607–8. http://dx.doi.org/10.1210/edrv.31.4.9978.

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Abstract Background: Corticosteroid-binding globulin (CBG) is the principal carrier for glucocorticoids in the circulation and a regulator of their bioavailability. Inherited CBG deficiencies are rarely reported, and only three causative mutations in four families have been described. Patients, Methods, and Results: In a 26-yr-old female with hypotension, fatigue, and undetectable serum cortisol at presentation, we have identified a novel homozygous c.776g&gt;t transversion in exon 3 of the CBG (SERPINA6) gene. This results in a p.Gly237Val substitution that is predicted to influence the p

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Nakhla, Meranda, Andrew E. Denker, James D. Connor, et al. "Bioavailability and Short-Term Tolerability of Alendronate in Glucocorticoid-Treated Children." Clinical Therapeutics 33, no. 10 (2011): 1516–23. http://dx.doi.org/10.1016/j.clinthera.2011.09.001.

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13

Edsb�cker, S., K. E. Andersson, and �. Ryrfeldt. "Nasal bioavailability and systemic effects of the glucocorticoid budesonide in man." European Journal of Clinical Pharmacology 29, no. 4 (1985): 477–81. http://dx.doi.org/10.1007/bf00613465.

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Choudhury, Sirazum, Tricia Tan, Katharine Lazarus, and Karim Meeran. "The use of prednisolone versus dual-release hydrocortisone in the treatment of hypoadrenalism." Endocrine Connections 10, no. 2 (2021): R66—R76. http://dx.doi.org/10.1530/ec-20-0473.

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The introduction of adrenocortical extract in 1930 improved the life expectancy of hyhpoadrenal patients, with further increases seen after the introduction of cortisone acetate from 1948. Most patients are now treated with synthetic hydrocortisone, and incremental advances have been made with optimisation of daily dosing and the introduction of multidose regimens. There remains a significant mortality gap between individuals with treated hypoadrenalism and the general population. It is unclear whether this gap is a result of glucocorticoid over-replacement, under-replacement or loss of the ci

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Vermeer, Harry, Brenda I. Hendriks-Stegeman, Bart van der Burg, Sylvia C. van Buul-Offers, and Maarten Jansen. "Glucocorticoid-Induced Increase in Lymphocytic FKBP51 Messenger Ribonucleic Acid Expression: A Potential Marker for Glucocorticoid Sensitivity, Potency, and Bioavailability." Journal of Clinical Endocrinology & Metabolism 88, no. 1 (2003): 277–84. http://dx.doi.org/10.1210/jc.2002-020354.

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Paglialunga, Musetta, Sara Flamini, Raffaele Contini, et al. "Anti-Inflammatory Effects of Synthetic Peptides Based on Glucocorticoid-Induced Leucine Zipper (GILZ) Protein for the Treatment of Inflammatory Bowel Diseases (IBDs)." Cells 12, no. 18 (2023): 2294. http://dx.doi.org/10.3390/cells12182294.

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Glucocorticoids (GCs) are commonly used to treat autoimmune and inflammatory diseases, but their clinical effects and long-term use can lead to serious side effects. New drugs that can replace GCs are needed. Glucocorticoid-induced leucine zipper (GILZ) is induced by GCs and mediates many of their anti-inflammatory effects, such as inhibiting the pro-inflammatory molecule NF-κB. The GILZ C-terminal domain (PER region) is responsible for GILZ/p65NF-κB interaction and consequent inhibition of its transcriptional activity. A set of five short peptides spanning different parts of the PER region of

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Gouveia, Virgínia M., Loris Rizzello, Claudia Nunes, et al. "Macrophage Targeting pH Responsive Polymersomes for Glucocorticoid Therapy." Pharmaceutics 11, no. 11 (2019): 614. http://dx.doi.org/10.3390/pharmaceutics11110614.

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Glucocorticoid (GC) drugs are the cornerstone therapy used in the treatment of inflammatory diseases. Here, we report pH responsive poly(2-methacryloyloxyethyl phosphorylcholine)–poly(2-(diisopropylamino)ethyl methacrylate) (PMPC–PDPA) polymersomes as a suitable nanoscopic carrier to precisely and controllably deliver GCs within inflamed target cells. The in vitro cellular studies revealed that polymersomes ensure the stability, selectivity and bioavailability of the loaded drug within macrophages. At molecular level, we tested key inflammation-related markers, such as the nuclear factor-κB, t

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Mittal, Shweta, Ishita Kathuria, and Meenakshi K. Chauhan. "IN SILICO STUDIES OF PREDNISOLONE ACETATE DERIVATIVES FOR THE TREATMENT OF DRY EYE DISEASE." Journal of Advanced Scientific Research 12, no. 04 Suppl 1 (2021): 242–49. http://dx.doi.org/10.55218/jasr.s1202112427.

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An attempt was made to find a potential cure for the dry eye syndrome affecting millions of people around the globe eventually leading to inflammation, blurry vision, irritation, redness, and ocular pains. In this condition, the tears are unable to provide enough lubrication either due to the lack of adequate tears or generation of poor-quality tears. The pressing need to find a cure to this chronic disease led to the search for a potential anti-inflammatory drug with the help of molecular studies. Molecular docking studies were used to find the potential anti-inflammatory drug. The study used

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Vermeer, H., B. I. Hendriks-Stegeman, C. E. Van Den Brink, et al. "A novel specific bioassay for the determination of glucocorticoid bioavailability in human serum." Clinical Endocrinology 59, no. 1 (2003): 49–55. http://dx.doi.org/10.1046/j.1365-2265.2003.01793.x.

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Cárdenas, Graciela, Raúl J. Bobes, Gladis Fragoso, et al. "Pharmacokinetic Study of Intranasal Dexamethasone and Methylprednisolone Compared with Intravenous Administration: Two Open-Label, Single-Dose, Two-Period, Two-Sequence, Cross-Over Study in Healthy Volunteers." Pharmaceutics 15, no. 1 (2022): 105. http://dx.doi.org/10.3390/pharmaceutics15010105.

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Dexamethasone (DXM) and methylprednisolone (MEP) are potent glucocorticoids used to control several inflammatory conditions. Evidence of delayed DXM reaching the central nervous system (CNS) as well as tachyphylaxis and systemic, undesirable side effects are the main limitations of peripheral delivery. Intranasal administration offers direct access to the brain as it bypasses the blood–brain barrier. The Mucosal Atomization Device is an optimal tool that can achieve rapid absorption into the CNS and the bloodstream across mucosal membranes. This study was designed to evaluate and compare the b

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Pensado, Andrea, Anita McGrogan, K. A. Jane White, Annette L. Bunge, Richard H. Guy, and M. Begoña Delgado-Charro. "Assessment of dermal bioavailability: predicting the input function for topical glucocorticoids using stratum corneum sampling." Drug Delivery and Translational Research 12, no. 4 (2021): 851–61. http://dx.doi.org/10.1007/s13346-021-01064-8.

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AbstractPredicting the dermal bioavailability of topically delivered drugs is challenging. In this work, minimally invasive stratum corneum (SC) sampling was used to quantify the delivery of betamethasone valerate (BMV) into the viable skin. Betnovate® cream (0.1% w/w BMV) was applied at three doses (2, 5, and 10 mg cm−2) to the ventral forearms of 12 healthy volunteers. The mass of drug in the SC was measured using a validated tape-stripping method (a) after a 4-h “uptake” period, and (b) following a 6-h “clearance” period subsequent to cream removal. Concomitantly, the skin blanching respons

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Rohatagi, Shashank, Gerald R. Rhodes, and Philip Chaikin. "Absolute Oral Versus Inhaled Bioavailability: Significance for Inhaled Drugs with Special Reference to Inhaled Glucocorticoids." Journal of Clinical Pharmacology 39, no. 7 (1999): 661–63. http://dx.doi.org/10.1177/00912709922008281.

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Koszdin, Kari L., Danny D. Shen, and Christopher M. Bernards. "Spinal Cord Bioavailability of Methylprednisolone after Intravenous and Intrathecal Administration." Anesthesiology 92, no. 1 (2000): 156. http://dx.doi.org/10.1097/00000542-200001000-00027.

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Background High-dose intravenously administered methylprednisolone has been shown to improve outcome after spinal cord injury. The resultant glucocorticoid-induced immunosuppression, however, results in multiple complications including sepsis, pneumonia, and wound infection. These complications could be reduced by techniques that increase the spinal bioavailability of intravenously administered methylprednisolone while simultaneously decreasing plasma bioavailability. This study aimed to characterize the spinal and plasma bioavailability of methylprednisolone after intravenous and intrathecal

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Egbuonu, Francis, Farrah A. Antonio, and Mahamood Edavalath. "Effect of Inhaled Corticosteroids on Glycemic Status." Open Respiratory Medicine Journal 8, no. 1 (2014): 101–5. http://dx.doi.org/10.2174/1874306401408010101.

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Although the dysglycemic effects of systemic glucocorticoid therapy are well known, the effect of inhaled corticosteroids (ICS) on carbohydrate metabolism is still a subject of debate. The systemic bioavailability of ICS is claimed to be minimal and the side effects negligible. However, some large retrospective cohort studies showed a definite association between ICS use and incident diabetes or worsening glycemic control in pre-existing diabetes. There are no professional-body recommended guidelines on the diagnosis and management of steroid-induced diabetes for the general population. This r

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Sutariya, Vijaykumar, Jared Tur, Shannon Kelly, et al. "Nanodrug delivery platform for glucocorticoid use in skeletal muscle injury." Canadian Journal of Physiology and Pharmacology 96, no. 7 (2018): 681–89. http://dx.doi.org/10.1139/cjpp-2017-0795.

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Glucocorticoids are utilized for their anti-inflammatory properties in the skeletal muscle and arthritis. However, the major drawback of use of glucocorticoids is that it leads to senescence and toxicity. Therefore, based on the idea that decreasing particle size allows for increased surface area and bioavailability of the drug, in the present study, we hypothesized that nanodelivery of dexamethasone will offer increased efficacy and decreased toxicity. The dexamethasone-loaded poly(lactic-co-glycolic acid) (PLGA) nanoparticles were prepared using nanoprecipitation method. The morphological ch

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Cornejo, Salomon, Kelan Tantisira, Benjamin A. Raby, Scott T. Weiss, and Feige Kaplan. "Nuclear bioavailability of the glucocorticoid receptor in a pediatric asthma cohort with variable corticosteroid responsiveness." Pediatric Research 78, no. 5 (2015): 505–12. http://dx.doi.org/10.1038/pr.2015.148.

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Chen, Hsiao-Jou Cortina, Tsz Yip, Johnny K. Lee, et al. "Restraint Stress Alters Expression of Glucocorticoid Bioavailability Mediators, Suppresses Nrf2, and Promotes Oxidative Stress in Liver Tissue." Antioxidants 9, no. 9 (2020): 853. http://dx.doi.org/10.3390/antiox9090853.

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Hepatic glutathione synthesis and antioxidant protection are critically important for efficient detoxification processes in response to metabolic challenges. However, this biosynthetic pathway, regulated by nuclear factor (erythroid-derived 2)-like 2 (Nrf2), previously demonstrated paradoxical repression following exposure to glucocorticoid stress hormones in cultured hepatic cells. Therefore, the present study used an in vivo model of sub-acute psychological stress to investigate the relationship between hepatic corticosteroid regulation and antioxidant systems. Male Wistar rats were kept und

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Zuo, Xu, Xiaoping Guo, Yinuo Gu, et al. "Recent Advances in Nanomaterials for Asthma Treatment." International Journal of Molecular Sciences 23, no. 22 (2022): 14427. http://dx.doi.org/10.3390/ijms232214427.

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Asthma is a chronic airway inflammatory disease with complex mechanisms, and these patients often encounter difficulties in their treatment course due to the heterogeneity of the disease. Currently, clinical treatments for asthma are mainly based on glucocorticoid-based combination drug therapy; however, glucocorticoid resistance and multiple side effects, as well as the occurrence of poor drug delivery, require the development of more promising treatments. Nanotechnology is an emerging technology that has been extensively researched in the medical field. Several studies have shown that drug d

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Blecharz, Kinga G., Malgorzata Burek, Johann Bauersachs, et al. "Inhibition of proteasome-mediated glucocorticoid receptor degradation restores nitric oxide bioavailability in myocardial endothelial cellsin vitro." Biology of the Cell 106, no. 7 (2014): 219–35. http://dx.doi.org/10.1111/boc.201300083.

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Charmandari, E., A. Johnston, CG Brook, and PC Hindmarsh. "Bioavailability of oral hydrocortisone in patients with congenital adrenal hyperplasia due to 21-hydroxylase deficiency." Journal of Endocrinology 169, no. 1 (2001): 65–70. http://dx.doi.org/10.1677/joe.0.1690065.

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The management of congenital adrenal hyperplasia due to 21-hydroxylase (CYP21) deficiency requires glucocorticoid substitution with oral hydrocortisone given twice or thrice daily. In paediatric practice little is known of the bioavailability of oral hydrocortisone tablets used in these patients. The aim of this study was to assess the bioavailability of oral hydrocortisone and to evaluate current replacement therapy in the light of cortisol pharmacokinetic properties. We determined the bioavailability of hydrocortisone following oral and intravenous administration in sixteen (median age: 10.9

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Längericht, Jan, Irene Krämer, and George J. Kahaly. "Glucocorticoids in Graves’ orbitopathy: mechanisms of action and clinical application." Therapeutic Advances in Endocrinology and Metabolism 11 (January 2020): 204201882095833. http://dx.doi.org/10.1177/2042018820958335.

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Background: Graves’ orbitopathy (GO) is the most frequent extrathyroidal manifestation of the autoimmune Graves’ disease. GO significantly impacts quality of life and has a psycho-social morbidity. Inflammation and swelling of the orbital tissue often leads to proptosis, diplopia, and decrease of visual acuity. Due to the inflammatory background of the disease, glucocorticoids (GC) have been used as a first-line treatment for decades. Methods: PubMed and MeSH database were searched for original articles, clinical trials, reviews, and meta-analyses published between 1 January 2000 and 31 March

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Dubashynskaya, Natallia V., Anton N. Bokatyi, Andrey S. Trulioff, Artem A. Rubinstein, Igor V. Kudryavtsev, and Yury A. Skorik. "Development and Bioactivity of Zinc Sulfate Cross-Linked Polysaccharide Delivery System of Dexamethasone Phosphate." Pharmaceutics 15, no. 10 (2023): 2396. http://dx.doi.org/10.3390/pharmaceutics15102396.

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Improving the biopharmaceutical properties of glucocorticoids (increasing local bioavailability and reducing systemic toxicity) is an important challenge. The aim of this study was to develop a dexamethasone phosphate (DexP) delivery system based on hyaluronic acid (HA) and a water-soluble cationic chitosan derivative, diethylaminoethyl chitosan (DEAECS). The DexP delivery system was a polyelectrolyte complex (PEC) resulting from interpolymer interactions between the HA polyanion and the DEAECS polycation with simultaneous incorporation of zinc ions as a cross-linking agent into the complex. T

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Ciarambino, Tiziana, Pietro Crispino, Giovanni Minervini, and Mauro Giordano. "Vitamin D: Can Gender Medicine Have a Role?" Biomedicines 11, no. 6 (2023): 1762. http://dx.doi.org/10.3390/biomedicines11061762.

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This narrative review aims to shed light on the role of gender differences, on the biological and molecular functions in the main pathological mechanisms that recognize the role of vitamin D. Vitamin D deficiency is widespread worldwide, but it is still very controversial whether the amount of vitamin D taken daily is actually the only problem related to its biological functions. Currently, the plasma concentration of 25-hydroxyvitamin D represents the only indicator of the circulating blood quota. The concept is that the biological function of vitamin D is not only linked to its circulating l

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Bolkenius, Ursula, Daniela Hahn, Axel M. Gressner, Katja Breitkopf, Steven Dooley та Lucia Wickert. "Glucocorticoids decrease the bioavailability of TGF-β which leads to a reduced TGF-β signaling in hepatic stellate cells". Biochemical and Biophysical Research Communications 325, № 4 (2004): 1264–70. http://dx.doi.org/10.1016/j.bbrc.2004.10.164.

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Serra, Magda F., Amanda C. Cotias, Camila R. R. Pão, et al. "Repeated Allergen Exposure in A/J Mice Causes Steroid-Insensitive Asthma via a Defect in Glucocorticoid Receptor Bioavailability." Journal of Immunology 201, no. 3 (2018): 851–60. http://dx.doi.org/10.4049/jimmunol.1700933.

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Clemmons, David R. "40 YEARS OF IGF1: Role of IGF-binding proteins in regulating IGF responses to changes in metabolism." Journal of Molecular Endocrinology 61, no. 1 (2018): T139—T169. http://dx.doi.org/10.1530/jme-18-0016.

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The IGF-binding protein family contains six members that share significant structural homology. Their principal function is to regulate the actions of IGF1 and IGF2. These proteins are present in plasma and extracellular fluids and regulate access of both IGF1 and II to the type I IGF receptor. Additionally, they have functions that are independent of their ability to bind IGFs. Each protein is regulated independently of IGF1 and IGF2, and this provides an important mechanism by which other hormones and physiologic variables can regulate IGF actions indirectly. Several members of the family ar

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Gonzalez, Daniel, and Hartmut Derendorf. "Ciclesonide in the Management of Asthma." Clinical Medicine. Therapeutics 1 (January 2009): CMT.S2133. http://dx.doi.org/10.4137/cmt.s2133.

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Ciclesonide is a novel inhaled corticosteroid (ICSs) approved in most countries for the management of persistent asthma. Although inhaled corticosteroids are first-line therapy in the treatment of asthma, long term use and high-doses of these products may result in significant side effects. When developing a new ICSs, the goal is to identify a drug with comparable (or superior) efficacy to active comparators, and an improved safety profile. Ciclesonide is a prodrug which is administered through a hydrofluoroalkane-propellant metered dose inhaler (HFA-MDI). Once it reaches the lungs, the parent

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Dubashynskaya, Natallia V., Anton N. Bokatyi, Alexey S. Golovkin, et al. "Synthesis and Characterization of Novel Succinyl Chitosan-Dexamethasone Conjugates for Potential Intravitreal Dexamethasone Delivery." International Journal of Molecular Sciences 22, no. 20 (2021): 10960. http://dx.doi.org/10.3390/ijms222010960.

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The development of intravitreal glucocorticoid delivery systems is a current global challenge for the treatment of inflammatory diseases of the posterior segment of the eye. The main advantages of these systems are that they can overcome anatomical and physiological ophthalmic barriers and increase local bioavailability while prolonging and controlling drug release over several months to improve the safety and effectiveness of glucocorticoid therapy. One approach to the development of optimal delivery systems for intravitreal injections is the conjugation of low-molecular-weight drugs with nat

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Zandieh, Iman, Darin Krygier, Victor Wong, et al. "The Use of Budesonide in the Treatment of Autoimmune Hepatitis in Canada." Canadian Journal of Gastroenterology 22, no. 4 (2008): 388–92. http://dx.doi.org/10.1155/2008/509459.

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BACKGROUND: Autoimmune hepatitis (AIH) is a chronic inflammatory disease that is successfully treated with prednisone and/or azathioprine immunosuppressive therapy in 70% to 80% of patients. The remaining patients are intolerant or refractory to these standard medications. Budesonide, a synthetic glucocorticoid, undergoes a high degree of first-pass metabolism, reducing its systemic bioavailability, and has a 15-fold greater affinity for the glucocorticoid receptor than prednisolone. Budesonide may be a potentially useful systemic steroid-sparing immunosuppressive agent in the treatment of AIH

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Patiño-Rodríguez, Omar, Abraham Escobedo-Moratilla, Rosa María Martínez-Medina, Irma Torres-Roque, Maricela Martínez-Delgado, and José Pérez-Urizar. "Development and Validation of a Sensitive LC-MS/MS Method for Determination of Betamethasone in Human Plasma. Application to a Pharmacokinetic Study of Healthy Mexican Subjects." Current Pharmaceutical Analysis 15, no. 1 (2018): 2–8. http://dx.doi.org/10.2174/1573412913666170912111945.

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Background: Synthetic glucocorticoids like Betamethasone (BE) are used in the treatment of inflammatory diseases due to its effective and potent effect. BE is available in three different esters: dipropionate (BD), sodium phosphate (BP), and acetate (BA). BD/BP combined in suspension has antiinflammatory, anti-allergic, and anti-rheumatic effects. The aim of this study was to describe the bioavailability of a single-dose of the injectable formulation of BP/BD in healthy Mexican subjects. Methods: This was a randomized, open-label, longitudinal, not therapeutic, single-dose trial of an intramus

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Desantis, Lanna M., Jeff Bowman, Erin Faught, Rudy Boonstra, Mathilakath M. Vijayan, and Gary Burness. "Corticosteroid-binding globulin levels in North American sciurids: implications for the flying squirrel stress axis." Canadian Journal of Zoology 96, no. 10 (2018): 1090–96. http://dx.doi.org/10.1139/cjz-2017-0300.

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Corticosteroid-binding globulin (CBG) helps to regulate tissue bioavailability of circulating glucocorticoids (GCs), and in most vertebrates, ≥80%–90% of GCs bind to this protein. New World flying squirrels have higher plasma total cortisol levels (the primary corticosteroid in sciurids) than most vertebrates. Recent research suggests that flying squirrels have either low amounts of CBG or CBG molecules that have a low binding affinity for cortisol, as this taxon appears to exhibit very low proportions of cortisol bound to CBG. To test whether CBG levels have been adjusted over evolutionary ti

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Haourigui, M., S. Sakr, M. E. Martin, et al. "Postprandial free fatty acids stimulate activity of human corticosteroid binding globulin." American Journal of Physiology-Endocrinology and Metabolism 269, no. 6 (1995): E1067—E1075. http://dx.doi.org/10.1152/ajpendo.1995.269.6.e1067.

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The effect of postprandial variation of free fatty acids (FFA) on serum corticosteroid binding globulin (CBG) properties and cortisol (hydrocortisone) concentrations were explored in 11 women (20-30 yr) during 8 h after an oral load of tallow (26% C16:0, 18% C18:0, and 43% C18:1), oleic-sunflower (oleic-SF; 73% C18:1), sunflower (SF; 67% C18:2), and mixed oil (MO; 39% C18:1 and 48% C18:2). Serum FFA increased little after SF and MO but more than doubled in the late postprandial period (6 and 8 h) after oleic-SF (due to monounsaturated FFA) or tallow (due to saturated and monounsaturated FFA).

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Guevara-Gordillo, Willams Andrés, Anthony Josué Coloma-León, Paulo Fernando Telenchana-Chimbo, and Carlos Pérez-Salazar. "Actualización en el manejo de gonartrosis: Revisión bibliográfica." Revista Metropolitana de Ciencias Aplicadas 7, no. 3 (2024): 15–25. http://dx.doi.org/10.62452/npqfna86.

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Gonarthrosis is a chronic-degenerative disease that involves the entire joint and its components, mainly affecting the articular cartilage, producing its degeneration and bone hyperplasia. About 50-60% of older adults experience symptoms of OA. The objective of this research is to discover new therapeutic options for gonarthrosis, in addition to expanding knowledge about intra-articular infiltration by describing the substances available for this therapy. An electronic search of scientific articles published from January 2018 to April 2024 was carried out in the PubMed, Scopus, Web of Science

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Gromotowicz-Poplawska, Anna, Piotr Szoka, Agnieszka Zakrzeska, et al. "Hyperglycemia Potentiates Prothrombotic Effect of Aldosterone in a Rat Arterial Thrombosis Model." Cells 10, no. 2 (2021): 471. http://dx.doi.org/10.3390/cells10020471.

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We investigated the role of aldosterone (ALDO) in the development of arterial thrombosis in streptozotocin-induced diabetic rats. To evaluate the effect of endogenous ALDO, the rats underwent adrenalectomy (ADX). ADX reduced the development of arterial thrombosis. A 1 h infusion of ALDO (30 μg/kg/h) enhanced thrombosis in adrenalectomized rats, while this effect was potentiated in diabetic rats. ALDO shortened bleeding time, increased plasma levels of tissue factor (TF) and plasminogen activator inhibitor, decreased plasma level of nitric oxide (NO) metabolites, and increased oxidative stress.

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Qin, Zhenmiao, Baohua Li, Qiyi Deng та ін. "Polymer Nanoparticles with 2-HP-β-Cyclodextrin for Enhanced Retention of Uptake into HCE-T Cells". Molecules 29, № 3 (2024): 658. http://dx.doi.org/10.3390/molecules29030658.

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Triamcinolone acetonide (TA), a medium-potency synthetic glucocorticoid, is primarily employed to treat posterior ocular diseases using vitreous injection. This study aimed to design novel ocular nanoformulation drug delivery systems using PLGA carriers to overcome the ocular drug delivery barrier and facilitate effective delivery into the ocular tissues after topical administration. The surface of the PLGA nanodelivery system was made hydrophilic (2-HP-β-CD) through an emulsified solvent volatilization method, followed by system characterization. The mechanism of cellular uptake across the co

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Shamsher, Ehtesham, Reas S. Khan, Benjamin M. Davis, et al. "Intranasal Resveratrol Nanoparticles Enhance Neuroprotection in a Model of Multiple Sclerosis." International Journal of Molecular Sciences 25, no. 7 (2024): 4047. http://dx.doi.org/10.3390/ijms25074047.

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Purpose: Resveratrol is a natural polyphenol which has a very low bioavailability but whose antioxidant, anti-inflammatory and anti-apoptotic properties may have therapeutic potential for the treatment of neurodegenerative diseases such as multiple sclerosis (MS). Previously, we reported the oral administration of resveratrol nanoparticles (RNs) elicited a neuroprotective effect in an experimental autoimmune encephalomyelitis (EAE) mouse model of MS, at significantly lower doses than unconjugated resveratrol (RSV) due to enhanced bioavailability. Furthermore, we demonstrated that the intranasa

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Forhead, A. J., and A. L. Fowden. "Thyroid hormones in fetal growth and prepartum maturation." Journal of Endocrinology 221, no. 3 (2014): R87—R103. http://dx.doi.org/10.1530/joe-14-0025.

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The thyroid hormones, thyroxine (T4) and triiodothyronine (T3), are essential for normal growth and development of the fetus. Their bioavailabilityin uterodepends on development of the fetal hypothalamic–pituitary–thyroid gland axis and the abundance of thyroid hormone transporters and deiodinases that influence tissue levels of bioactive hormone. Fetal T4and T3concentrations are also affected by gestational age, nutritional and endocrine conditionsin utero, and placental permeability to maternal thyroid hormones, which varies among species with placental morphology. Thyroid hormones are requi

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Mattos, Gabriele E., Jan-Michael Heinzmann, Stefanie Norkowski, et al. "Corticosteroid-binding globulin contributes to the neuroendocrine phenotype of mice selected for extremes in stress reactivity." Journal of Endocrinology 219, no. 3 (2013): 217–29. http://dx.doi.org/10.1530/joe-13-0255.

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Increasing evidence indicates an important role of steroid-binding proteins in endocrine functions, including hypothalamic–pituitary–adrenal (HPA) axis activity and regulation, as they influence bioavailability, local delivery, and cellular signal transduction of steroid hormones. In the plasma, glucocorticoids (GCs) are mainly bound to the corticosteroid-binding globulin (CBG) and to a lesser extend to albumin. Plasma CBG levels are therefore involved in the adaptive stress response, as they determine the concentration of free, biologically active GCs. In this study, we investigated whether m

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Valente, Filippo, Edi Simoni, Erica Gentilin, et al. "Liquid Crystalline Nanoparticles Conjugated with Dexamethasone Prevent Cisplatin Ototoxicity In Vitro." International Journal of Molecular Sciences 23, no. 23 (2022): 14881. http://dx.doi.org/10.3390/ijms232314881.

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The conjugation of drugs with nanoparticles represents an innovative approach for controlled and targeted administration of therapeutic agents. Nanoparticle-based systems have been tested for the inner ear therapy, increasing the drug diffusion and being detected in all parts of the cochlea when locally applied near the round window. In this study, glycerol monooleate liquid crystalline NanoParticles were conjugated with Dexamethasone (NPD), a hydrophobic drug already used for inner ear treatments but defective in solubility and bioavailability. NPD has been tested in vitro in the cell line OC

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Campieri, M., A. Ferguson, W. Doe, T. Persson, and L.-G. Nilsson. "Oral budesonide is as effective as oral prednisolone in active Crohn’s disease." Gut 41, no. 2 (1997): 209–14. http://dx.doi.org/10.1136/gut.41.2.209.

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Background—The use of corticosteroids in active Crohn’s disease often becomes limited by side effects. Budesonide is a potent corticosteroid with low systemic bioavailability due to an extensive first pass liver metabolism.Aims—To compare the efficacy and safety of two dosage regimens of budesonide and prednisolone in patients with active Crohn’s disease affecting the ileum and/or the ascending colon.Patients and methods—One hundred and seventy eight patients were randomised to receive budesonide controlled ileal release (CIR) capsules 9 mg once daily or 4.5 mg twice daily, or prednisolone tab

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