Search Results (22)

The enhancement of drug delivery into the lung surfactant is facilitated by research on the interaction between drugs and the lung surfactant. Drug designers must have a thorough theoretical understanding of a drug before performing clinical tests to reduce the experimental cost. The current study uses a coarse-grained molecular dynamics (MD) approach with the MARTINI force field to parameterize the corticosteroid drug mometasone furoate, which is used to treat lung inflammation. Here, we investigate the accurate parametrization of drug molecules and validate the parameters with the help of umbrella sampling simulations. A collection of thermodynamic parameters was studied during the parametrization procedure. The Gibbs free energy gradient was used to calculate the partition coefficient value of mometasone furoate, which was approximately 10.49 based on our umbrella sampling simulation. The value was then matched with the experimental and predicted the partition coefficient of the drug, showing good agreement. The drug molecule was then delivered into the lung surfactant monolayer membrane at the alveolar air–water interface, resulting a concentration-dependent drop in surface tension while controlling the underlying continual compression–expansion of alveoli that maintains the exhalation–inhalation respiratory cycle. The dynamical properties of the monolayer demonstrate that the drug’s capacity to diffuse into the monolayer is considerably diminished in larger clusters, and this effect is intensified when there are more drug molecules present in the monolayer. The monolayer microstructure analysis shows that the drug concentration controls monolayer morphology. The results of this investigation may be helpful for corticosteroid drug delivery into the lung alveoli, which can be applied to comprehend how the drug interacts with lung surfactant monolayers or bilayers. Full article

Chronic rhinosinusitis (CRS) is a prevalent inflammatory condition of the nasal and paranasal mucosa that significantly impacts the quality of life. Postoperative inflammation and polyp recurrence remain common despite advances in endoscopic sinus surgery (ESS), prompting interest in localized corticosteroid delivery systems. This review analyzes bioresorbable steroid-releasing implants and corticosteroid-impregnated nasal dressings, focusing on their pharmacologic mechanisms, safety, and clinical outcomes. A synthesis of findings from randomized trials and observational studies was performed, with emphasis on devices such as Propel™, NasoPore, Merocel, SinuBand FP, and gel-based dressings. The Propel implant demonstrated robust evidence for reducing adhesions and inflammation with negligible systemic absorption. NasoPore and Merocel provided structural support and localized steroid delivery but lacked controlled-release kinetics. Gel-based dressings and SinuBand FP offered anatomic adaptability, with limited systemic effects. Some methods showed systemic steroid exposure in cortisol monitoring. Corticosteroid-releasing devices enhance ESS outcomes through localized therapy. While Propel is the most validated, other devices remain viable alternatives in specific clinical contexts. Comprehensive safety monitoring and standardized trials are essential to optimize their integration into postoperative care. Full article

Background/Objectives: Mometasone furoate (MF) is a topical corticosteroid used to reduce allergic and inflammation symptoms. In this study, MF was incorporated into the hydrophobic cavities of γ-cyclodextrin metal-organic frameworks (CD-MOFs) to prepare MF@MOF powders for nasal delivery. Methods: MF@MOF particles were characterized by scanning electron microscopy (SEM), powder X-ray diffraction (PXRD), Fourier transform infrared spectroscopy (FTIR), and thermogravimetry. A transparent biomimetic model of the human nasal cavity was produced by 3D printing and used to evaluate intra-nasal depositions patterns. Results: Drug loading was optimized by incubating MF with a CD-MOF at a ratio of 4% for 1 h at 40 °C, and the cubic morphology and particle size of the nanoparticles were not altered using an incubation method. PXRD and FTIR analyses confirmed the successful loading of MF into the CD-MOF. Using a 3D biomimetic nasal cavity model, a 30° administration angle was found to result in reduced drug accumulation in the nasal vestibule and enhanced deposition in the respiratory and olfactory regions, compared with administration at 45°. Approximately 51% of the drug reached the respiratory zone in the model of the nasal cavity from male subjects, while almost 60% of the drug reached this zone in the model associated with female subjects. Compared with nasal sprays, nasal powder sprays had less deposition in the nasal vestibule and more deposits in the middle and inferior nasal concha. Conclusions: MF@MOF is suitable for intranasal administration. Delivery of MF as a nasal powder shows potential in the treatment of chronic rhinosinusitis. Full article

Background and clinical significance: Osteonecrosis of the femoral head (ONFH) is a disease of the epiphysis caused by the death of osteocytes and osteoblasts, resulting in debilitating pain. ONFH can be traumatic or nontraumatic, with prolonged glucocorticoid use being the leading cause of nontraumatic ONFH. Atopic dermatitis (AD) is a chronic inflammatory skin condition typically treated with topical corticosteroids. ONFH following topical corticosteroid treatment is exceedingly rare, with limited documentation in the literature. We present a case of an under-recognized complication of prolonged topical corticosteroid treatment. Case presentation: We report a case of a 29-year-old Caucasian male patient with sharp right hip pain. Plain radiographs, a CT scan, and an MRI indicated Ficat and Arlet stage 3 ONFH. The patient reported the prolonged uncontrolled use of topical mometasone furoate for five years due to AD. Following the diagnosis, topical corticosteroids were discontinued, and the treatment was shifted to tacrolimus and, subsequently, to oral methotrexate with folic acid. The patient underwent a total hip arthroplasty in June 2022. Given his young age and poor response to previous treatments, he was transitioned to upadacitinib, which led to significant improvement without skin flare-ups or postoperative hip pain. Conclusions: This case highlights the rare, but serious, risk of ONFH associated with long-term topical corticosteroid use. It underscores the importance of monitoring systemic side effects in dermatological therapies and educating patients on proper corticosteroid use. Alternative treatments, such as upadacitinib, should be considered in young male patients to prevent severe complications. Full article

Introduction: According to the results of the APRICOT study, airway and respiratory complications constitute 60% of all anesthesia-related complications and may be life-threatening. The primary aim of this study was to evaluate the effect of lidocaine and mometasone spray on the hemodynamic stress response during tracheal intubation and extubation in children. Our secondary aim was to determine its effect on the incidence of postoperative airway complications. Materials and Methods: Following Ethics Committee approval (No: KIIA 2018/489) and clinical trial registration (No: NCT04085744), patient recruitment was initiated only after obtaining parental consent. Children of ASA I-II aged 0 to 16 years and undergoing elective surgery were included. A total of 91 patients were randomly divided into 3 groups. Group M: Patients treated with a topical corticosteroid 0.05% mometasone furoate spray (n = 30). Group L: Patients sprayed with 10% lidocaine (n = 30). Control group: Patients treated with 0.9% normal saline applied around the cuff (n = 31). The systolic, diastolic, and mean blood pressures, heart rate, and SpO₂ values were recorded before operation, after induction, before and after tracheal intubation, and before and after extubation. Patients were followed up for 24 h postoperatively. Results: A statistically significant decrease was found in the lidocaine group for diastolic and mean arterial pressures measured after tracheal intubation (p = 0.018 and p = 0.027, respectively). There was a significant decrease in heart rate values in Group L after extubation (p = 0.024). Cough was observed in 5 patients in the control group at the postoperative 12th hour, but not in the other groups (p = 0.009). The distribution of sore throat severity, dyspnea, and hoarseness and the incidence of early postoperative bronchospasm, recorded in all follow-up periods, decreased; however, it did not show a statistically significant difference. Conclusions: In conclusion, this study revealed that the topical application of lidocaine and mometasone around the tracheal tube cuff in children not only reduces postoperative cough but also, in the case of lidocaine, suppresses the hemodynamic stress response during both tracheal intubation and extubation. Full article

The deposition, residence time, and dissolution profile of nasal suspensions containing corticosteroids play a key role in their in vivo efficacy after administration. However, the conventional methods available to characterize nasal products appear to be unsuitable to exhaustively cover these aspects. The work aims to investigate technological aspects of Ryaltris (mometasone furoate and olopatadine hydrochloride nasal spray) compared to other commercial anti-allergic nasal products, namely, Dymista (azelastine hydrochloride and fluticasone propionate), Nasonex (mometasone furoate), and Avamys (fluticasone furoate). Innovative characterization methods were combined with more traditional approaches to investigate the anti-allergic nasal sprays. These methods applied together allowed to differentiate between the different products and provided a clear picture of the nasal product behavior in terms of drug dissolution and deposition. In particular, the dissolution tests were performed exploiting the Respicell^® apparatus, an innovative technique that allows for the investigation of inhalation products. Then, formulation viscosities were considered along with a formulation flow test on an inclined plane. Finally, the intranasal deposition profile of the commercial formulations was determined using a silicon nasal cast. The results highlight in vitro significant differences in terms of viscosity as well as dissolution rate of the nasal products, with Ryaltris showing a higher viscosity and lower flow compared to other products, which, along with a corticosteroid faster dissolution rate than Dymista, suggest a potential advantage in terms of clinical behavior. Full article

Background: Mometasone furoate nasal spray is efficacious in relieving allergic rhinitis symptoms. The objectives of this study were, firstly, to compare the efficacy of Elonide to Nasonex^® and a placebo and secondly, to investigate the side effects of Elonide. Method: This was a prospective, single-centered, double blinded, randomized, placebo-controlled, non-inferiority trial. A total of 163 participants from the Otorhinolaryngology Clinic, Hospital Canselor Tuanku Muhriz (HCTM), were randomized into three treatment groups receiving Elonide (n = 56), Nasonex^® (n = 54), and placebo (n = 53) nasal sprays using an online randomizer (Random.org). Treatment was administered for 4 weeks. The primary outcome measure was the Total Nasal Resistance (TNR), and the secondary outcomes were the Visual Analogue Score (VAS) and the Rhinoconjunctivitis Quality of Life Questionnaire (RQOLQ) score. Side effects were recorded. Results: There were significant improvements for all groups from baseline. The Elonide group had the greatest mean difference for all primary and secondary outcomes compared to Nasonex^® and the placebo (0.77 ± 2.44 vs. 0.35 ± 1.16, p = 1.00 vs. 0.17 ± 0.82, p = 0.01). Elonide is non-inferior to Nasonex (p = 1.00) and superior to the placebo (p < 0.05). The highest side effects reported were for Nasonex (n = 14, 26%), followed by the placebo (n = 8, 16%) and Elonide (n = 6, 12%); headaches (n = 9, 17%) and sore throat (n = 9, 17%) were the most common. Conclusions: Elonide has similar efficacy to Nasonex^® when compared to a placebo in the treatment of AR in adults. Elonide is safe and tolerable, with fewer side effects and no adverse side effects. Full article

Mometasone furoate is a synthetic corticosteroid used in the treatment of skin inflammatory conditions, hay fever and asthma. The industrial manufacturing routes to mometasone furoate are generally accompanied by the formation of numerous process impurities that need to be detected and quantified, as requested by regulatory authorities. The ready availability of such impurities in the required quantity and purity is therefore essential for toxicological studies, analytical method development and process validation. Herein, we report the multi-gram scale preparation of 21′-chloro-(16′α-methyl-3′,11′,20′-trioxo-pregna-1′,4′-dien-17′-yl)-furan-2-carboxylate (mometasone furoate EP impurity C), one of the known impurities of mometasone furoate. This study also includes the systematic investigation of the final acylation step, as well as the characterization of the difuroate enol ether intermediate and its conversion to the target impurity C. Full article

Mometasone furoate (MF) is a kind of glucocorticoid with extensive pharmacological actions, including inhibiting tumor progression; however, the role of MF in head and neck squamous cell carcinoma (HNSCC) is still unclear. This study aimed to evaluate the inhibitory effect of MF against HNSCC and investigate its underlying mechanisms. Cell viability, colony formation, cell cycle and cell apoptosis were analyzed to explore the effect of MF on HNSCC cells. A xenograft study model was used to investigate the effect of MF on HNSCC in vivo. The core targets of MF for HNSCC were identified using network pharmacology analysis, TCGA database analysis and real-time PCR. Molecular docking was performed to determine the binding energy. Protein tyrosine phosphatase non-receptor type 11 (PTPN11)-overexpressing cells were constructed, and then, the cell viability and the expression levels of proliferation- and apoptosis-related proteins were detected after treatment with MF to explore the role of PTPN11 in the inhibitory effect of MF against HNSCC. After cells were treated with MF, cell viability and the number of colonies were decreased, the cell cycle was arrested and cell apoptosis was increased. The xenograft study results showed that MF could inhibit cell proliferation via promoting cell apoptosis in vivo. PTPN11 was shown to be the core target of MF against HNSCC via network pharmacology analysis, TCGA database analysis and real-time PCR. The molecular docking results revealed that PTPN11 exhibited the strongest ability to bind to MF. Finally, MF could attenuate the effects of increased cell viability and decreased cell apoptosis caused by PTPN11 overexpression, suggesting that MF can inhibit the progression of HNSCC by regulating PTPN11. MF targeted PTPN11, promoting cell cycle arrest and cell apoptosis, and consequently exerting effective anti-tumor activity. Full article

The aim of the study was to develop a sustained-release varnish (SRV) containing mometasone furoate (MMF) for sinonasal stents (SNS) to reduce mucosa inflammation in the sinonasal cavity. The SNS’ segments coated with SRV-MMF or an SRV-placebo were incubated daily in a fresh DMEM at 37 °C for 20 days. The immunosuppressive activity of the collected DMEM supernatants was tested on the ability of mouse RAW 264.7 macrophages to secrete the cytokines’ tumor necrosis factor α (TNFα) and interleukin (IL)-10 and IL-6 in response to lipopolysaccharide (LPS). The cytokine levels were determined by respective Enzyme-Linked Immunosorbent Assays (ELISAs). We found that the daily amount of MMF released from the coated SNS was sufficient to significantly inhibit LPS-induced IL-6 and IL-10 secretion from the macrophages up to days 14 and 17, respectively. SRV-MMF had, however, only a mild inhibitory effect on LPS-induced TNFα secretion as compared to the SRV-placebo-coated SNS. In conclusion, the coating of SNS with SRV-MMF provides a sustained delivery of MMF for at least 2 weeks, maintaining a level sufficient for inhibiting pro-inflammatory cytokine release. This technological platform is, therefore, expected to provide anti-inflammatory benefits during the postoperative healing period and may play a significant role in the future treatment of chronic rhinosinusitis. Full article

Mometasone furoate (MF) is a medium-potency synthetic glucocorticosteroid with anti-inflammatory, antipruritic, and vasoconstrictive properties. However, its role in the treatment of ocular inflammation has not yet been explored. This work investigated the anti-inflammatory activity of MF in ocular tissues. First, the in vivo safety of the intravitreal (IVT) injection of MF (80, 160, and 240 µg) was evaluated via clinical examination (including the assessment of intraocular pressure), electroretinography (ERG), and histopathology. Second, MF was tested in an experimental model of bacillus Calmette–Guérin (BCG)-induced uveitis in Wistar rats. Intraocular inflammation was then evaluated via a slit-lamp and fundus examination, ERG, histopathology, and the quantification of pro-inflammatory markers. Intravitreal MF showed no toxicity in all the investigated doses, with 160 µg leading to attenuated disease progression and improvement in clinical, morphological, and functional parameters. There was a significant reduction in the levels of inflammatory markers (myeloperoxidase, interleukins 6 and 1β, CXCL-1, and tumor necrosis factor-alpha) when compared to the levels in untreated animals. Therefore, MF should be further investigated as a promising drug for the treatment of ocular inflammation. Full article

A pre-formulation study was carried out to obtain liposomal formulations of mometasone furoate as an alternative system to marketed forms of corticosteroid for the treatment of inflammatory skin lesions. Mometasone furoate was loaded in glycerosomes and glyceroethosomes, which were also modified with hyaluronic acid (glyceroethohyalurosomes). Vesicles were designed, elaborated, and characterized, and their biocompatibility, efficacy against oxidative stress and skin lesions were assessed in vitro, in human epidermal cells, and in vivo, in a mouse skin epidermal hyperplasia model. All formulations tested showed great encapsulation efficiency, nanometric size, formed monodispersed systems and a highly negative Z potential. Similar values were obtained over nine months storage at 4 °C, which indicates the great stability of the three types of nanoliposomes at least during the time tested. Among them, 0.1% mometasone furoate glyceroethohyalurosomes were the best formulation to protect cells against oxidative stress and their anti-inflammatory efficacy was confirmed in vivo, being even more effective than the marketed form (Elocom^®), as the reduction in the inflammation was even ~15% higher than that achieved with the commercial cream. Selected formulations could be potential candidates as new vehiculation systems for mometasone furoate. The presence of hyaluronic acid in glyceroethohyalurosomes makes them the best candidates in preventing/treating skin inflammatory lesions. Full article

Persistent olfactory dysfunction is a major concern post-COVID-19, affecting up to 5% of all patients. Different therapeutic options, including mometasone nasal spray, have been recommended, only some of which have been validated for post-COVID-19 olfactory dysfunction. In this study we psychophysically assessed the effect of intranasally applied mometasone furoate on the recovery of olfaction. The spray was applied with a long applicator so that the olfactory cleft could be reached effectively. After olfactory dysfunction had been confirmed psychophysically using Sniffin’ Sticks, patients were randomly assigned to two different treatment arms: the study group (n = 40) underwent olfactory training and intranasal administration of mometasone furoate twice daily, whereas the control group (n = 46) performed olfactory training only. After a study duration of three months, psychophysical testing of olfaction was repeated using Sniffin’ Sticks. We found no benefit of an additional topical administration of mometasone furoate compared to olfactory training alone. These results psychophysically confirm two previous studies which were based on patients’ subjective self-ratings. Our findings are in contrast to current recommendations for the management of olfactory dysfunction post-COVID-19, which might have to be adapted accordingly. Full article

Background: In order to evaluate the efficacy of intranasal mometasone furoate in patients with non-allergic rhinitis (NAR), a real-life, observational, prospective study is performed. Methods: Thirty-one patients (age 18–64 years) receive intranasal (mometasone furoate, 200 µg b.i.d. for 15 consecutive days per month for 6 consecutive months), plus isotonic nasal saline. The cytologic pattern of local inflammation, nasal airflow, through peak nasal inspiratory flow (PNIF), quality of life (QoL), through the rhinitis quality of life questionnaire (RQLQ), the sinonasal outcome test (SNOT-22), the short-form 36-item health survey (SF-36v2), and the combined symptom medication score (CSMS), and, finally, olfactory function, through Sniffin’ sticks-16 identification test (SSIT-16), are evaluated at baseline and after treatment. Results: NARNE is the most frequent cytological pattern (48% of the total sample). The therapeutic response shows improvement in olfactory function and QoL. Conclusions: The results of this study confirm that intranasal mometasone furoate is an effective treatment for patients with NAR. Full article

Background: Local and systemic corticosteroids have long been the workhorse in management of chronic rhinosinusitis with nasal polyps (CRSwNP), although there is no universally accepted modality of prescription. We carried out a survey in Italy to capture current trends in the use of topical and systemic corticosteroids in patients with CRSwNP. Methods: A survey was set up on Survey Monkey^®. Each author distributed the link to the survey in an ad hoc manner and a total of 437 participants filled out the survey. Results: Mometasone furoate (79.3%) was the most frequently prescribed, administered daily by 61.9% of participants; the remaining preferred to discontinue treatment for brief periods to reduce side effects or to modulate the therapy in mild cases. The majority believe that a short cycle of systemic steroids should be prescribed for re-exacerbation of symptoms and that the number of cycles in the previous year should be evaluated to define control of the disease even if international guidelines do not provide clear indications on this topic. A certain degree of divergence emerged from responses regarding how long and the maximal dose of systemic steroids which place patients at high risk for adverse events. Finally, systemic corticosteroids seem to offer only temporary benefit on recovery of smell without guaranteeing long-term control even if the patient is adherent to topical corticosteroids. Conclusions: Our results highlight the need for clear guidelines on oral steroids, which could help supporting the use of a precision medicine approach, including indications for new biological agents. Full article