Our library of drug research abstracts drawn from the medical literature is updated on a regular schedule, and you can be assured that new elocon research articles will be listed here shortly after becoming available to us.
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Medical research on elocon
Int J Pharm. 2008 Jun 4;
James J, Crean B, Davies M, Toon R, Jinks P, Roberts CJ
PURPOSE: This study compares the surface characteristics and surface energetics of two potential bulking excipients, anhydrous sub-micron alpha-lactose and sub-micron sucrose, for use with low-dose, suspension formulations in pressurised metered dose inhalers (pMDIs). Both sub-micron bulking excipients are processed from parent materials (alpha-lactose monohydrate/alpha-lactose monohydrate and silk grade sucrose, respectively) so the surface characteristics of each material were determined and compared. Additionally, the surface energetics and adhesive interactions between each sub-micron bulking excipient and some chosen active pharmaceutical ingredients (APIs) used in pMDI formulations were also determined. From this data, it was possible to predict the potential degree of interaction between the APIs and each sub-micron bulking excipient, thus determining suitable API-excipient combinations for pMDI formulation optimisation. Salmon calcitonin was also investigated as a potential API due to the current interest in, and the potential low-dose requirements for, the pulmonary delivery of proteins. METHODS: The size and morphology of each sub-micron excipient (and parent materials) were determined using scanning electron microscopy (SEM) and the crystalline nature of each sub-micron excipient and parent material was assessed using X-ray diffraction (XRD). The surface chemistry of each sub-micron excipient was analysed using X-ray photoelectron spectroscopy (XPS). The surface energies of each sub-micron excipient, along with their respective parent materials and any intermediates, were determined using two techniques. The surface energies of these materials were determined via (a) single particle adhesive interactions using atomic force microscopy (AFM) and (b) 'bulk' material surface interactions using contact angle measurements (CA). From the CA data, it was possible to calculate the theoretical work of adhesion values for each API-excipient interaction using the surface component approach (SCA). The Young's modulus for each sub-micron excipient and parent material was also determined using AFM. Finally, the adhesive interactions were determined between each sub-micron bulking excipient and five APIs (formoterol fumarate, salmeterol xinafoate, salbutamol sulphate, mometasone furoate and salmon calcitonin). RESULTS: Both sub-micron sucrose and anhydrous sub-micron alpha-lactose exhibited a lower surface free energy than their respective parent materials/intermediates. In addition, both AFM and CA surface energy measurements also showed that sub-micron sucrose has a higher surface energy than anhydrous sub-micron alpha-lactose. Theoretical work of adhesion values between anhydrous sub-micron alpha-lactose and each API are considerably lower than those observed between micronised alpha-lactose monohydrate and each API. Corresponding theoretical work of adhesion values between sub-micron sucrose and each API were almost identical to those observed between silk grade sucrose and each API. Young's modulus determination revealed that sub-micron sucrose has a greater crystal hardness/elasticity ratio than anhydrous sub-micron alpha-lactose. With the exception of salmon calcitonin, sub-micron sucrose showed larger adhesive interactions to the selected APIs than anhydrous sub-micron alpha-lactose. CONCLUSIONS: Anhydrous sub-micron alpha-lactose has been found to have lower adhesive interactions with a range of chosen, low-dose APIs compared to sub-micron sucrose. This could be related to the lower surface energy for anhydrous sub-micron alpha-lactose. Knowledge of the surface free energy and mechanical properties of potential sub-micron bulking excipients and API materials could provide useful information regarding the selection of suitable API-submicron bulking excipient combinations during the development and optimisation stages of suspension pMDI formulations.
Int J Immunopathol Pharmacol. 2008 April-June; 21(2): 333-341
Bernardini R, Pucci N, Rossi ME, Lombardi E, De Martino M, Mori F, Ciprandi G, Novembre E, Marcucci F, Massai C, Azzari C, Vierucci A
There are no data concerning the significance of allergen specific nasal challenge to latex (ASNCL) in the pediatric population and the effect of mometasone furoate nasal spray (MFNS), topic corticosteroid exerting a potent anti-inflammatory activity in children with latex allergic rhinitis. The aims of this study are: to investigate the clinical and immune pathological effects of ASNCL in children with latex allergy; to study the effects of MFNS pre-medication on the clinical and immune pathological effects of ASNCL in children with latex allergy. Thirteen children: 6 male and 7 female, mean (SD) age 9.6 (2.9) years, with latex allergy and seven children: 3 male and 4 female, mean (SD) age 9.9 (3.8) years, without latex allergy underwent ASNCL. Nasal symptoms were recorded, nasal lavage fluid was collected to measure tryptase, eosinophil cationic protein (ECP), interleukin-5, interferon-gamma levels, and spirometric test was performed for each patient without or with premedication with MFNS. ASNCL induced a clinical allergic response and increased tryptase levels only in children with latex allergy. No serious adverse events occurred after ASNCL. MFNS premedication reduced both tryptase and ECP levels only in children with latex allergy. ASNCL is a simple, reliable and useful tool to make or confirm the diagnosis of nasal symptoms due to latex; it allows us to study both clinical symptoms and local immunological changes. MFNS premedication before an ASNCL may prevent some immunological responses induced by ASNCL without clinical allergic modifications.
Eur Respir J. 2008 May 28;
Rytilä P, Ghaly L, Varghese S, Chung W, Selroos O, Haahtela T,
A total of 144 patients with lower airway symptoms suggestive of asthma, but not fulfilling the functional criteria of asthma were included in a randomized, double-blind, placebo-controlled 8-week "proof-of-concept" study with mometasone furoate (MF), 400 microg once daily. The primary efficacy variable was the change from baseline in six mean morning (AM) and evening (PM) weekly symptom scores - cough, sputum production, wheeze, shortness of breath, chest tightness, and exercise-induced cough/wheeze. Total symptom scores were calculated after treatment for 4 and 8 weeks.Compared with placebo MF improved total AM symptom score at 8 weeks. Changes in total PM symptom scores did not differ between treatments. MF improved all individual symptom scores more than placebo although the differences in changes between treatments was not always statistically sig-nificant. Morning and evening peak expiratory flow rates increased with MF compared with placebo. MF reduced eosinophils and the levels of eosinophilic cationic protein in induced sputum.The results show that symptoms suggestive of asthma exist in patients without significant beta2-agonist reversibility or diurnal variability in peak flow. Once-daily MF may benefit some of these patients and a short course with inhaled corticosteroids may be tried. Responders should be identified better in further studies.
Int J Pediatr Otorhinolaryngol. 2008 May 20;
Berlucchi M, Valetti L, Parrinello G, Nicolai P
BACKGROUND: Encouraging results concerning chronic obstructive nasal symptoms due to adenoid in pediatric population were reported by use of intranasal steroid for short period. Up to now, no data are available about outcomes of such therapy after long-term follow-up. We evaluated the utility of mometasone furoate aqueous nasal spray in children with adenoidal hypertrophy in long-term maintenance therapy. METHODS: All children affected by adenoidal hypertrophy and undergoing successful mometasone treatment for 4 months in a preceding trial were reassessed after a mean follow-up of 28 months. Based on the duration of maintenance therapy and eventual adenoid surgical treatment, three subgroups were identified: (1) children voluntarily suspending maintenance therapy and requiring surgery (Group A); (2) children continuing maintenance therapy but undergoing surgery (Group B); and (3) children continuing maintenance therapy but not undergoing surgery (Group C). Clinical and endoscopic evaluation in each group was compared to the assessment performed after the first 4 months of treatment. RESULTS: Six patients (Group A) voluntarily suspended maintenance therapy and underwent adenoidectomy. Either the overall symptom score or choanal obstruction of this group worsened compared to the previous trial. Adenoidal surgery was performed in another three children (Group B) for ear disease. Chronic obstructive nasal symptoms and adenoid size were unchanged compared to the preceding study. Finally, 12 patients were in Group C. The overall symptom score and choanal obstruction of this group showed a further significant improvement at this stage. CONCLUSIONS: This study describes the first long-term follow-up of children undergoing mometasone furoate aqueous nasal spray treatment for adenoidal hypertrophy. Voluntary suspension of maintenance therapy favors surgery of this disorder, whereas its regular administration may lead to successful results.
Antibacterial activity of mometasone furoate.
Arch Otolaryngol Head Neck Surg. 2008 May; 134(5): 519-21
Neher A, Gstöttner M, Scholtz A, Nagl M
OBJECTIVE: To test the antibacterial properties of the topical corticoid mometasone furoate, which is used as a nasal spray. DESIGN: The activity of mometasone (0.01%, 0.1%, and 0.5%) in buffer solution against Staphylococcus aureus, Pseudomonas aeruginosa, Escherichia coli, Streptococcus pyogenes, and Streptococcus milleri was tested by quantitative killing assays. SETTING: In vitro study. MAIN OUTCOME MEASURE: Reduction of viable bacteria and fungi in quantitative killing assays. RESULTS: Mometasone (0.5%) reduced viable counts of S pyogenes and S milleri by 99.99% and 99.00%, respectively, after 24 hours of incubation, whereas colony-forming units (CFUs) of S aureus, P aeruginosa, and E coli were not affected by the corticoid. Mometasone (0.1%) caused a decrease in CFUs of S pyogenes of 99.90% to 99.99%, while it led to a 99.00% reduction in CFUs of S milleri, but only if low bacterial counts of 1 x 10(4) CFUs/mL were incubated. By contrast, the use of mometasone at a low concentration (0.01%) demonstrated an increase in CFUs of S milleri if the baseline bacterial count was low (1 x 10(4) CFUs/mL). CONCLUSION: Mometasone demonstrates antimicrobial activity against streptococci.
Intracellular delivery of nanoparticles of an antiasthmatic drug.
AAPS PharmSciTech. 2008; 9(1): 217-23
Surti N, Naik S, Bagchi T, Dwarkanath BS, Misra A
The aim of the investigation was to prepare and characterize wheat germ agglutinin(WGA)-conjugated poly(D: ,L-lactic-co-glycolic) acid nanoparticles encapsulating mometasone furoate (MF) as a model drug and assess changes in its fate in terms of cellular interactions. MF loaded nanoparticles were prepared using emulsion-solvent evaporation technique. WGA-conjugation was done by carbodiimide coupling method. The nanoparticles were characterized for size, zeta potential, entrapment efficiency and in-vitro drug release. The intracellular uptake of nanoparticles, drug cellular levels, and anti-proliferative activity studies of wheat germ agglutinin-conjugated and unconjugated nanoparticles were assessed on alveolar epithelial (A549) cells to establish cellular interactions. Prepared nanoparticles were spherical with 10-15 microg/mg of WGA conjugated on nanoparticles. The size of nanoparticles increased after conjugation and drug entrapment and zeta potential reduced from 78 +/- 5.5% to 60 +/- 2.5% and -15.3 +/- 1.9 to -2.59 +/- 2.1 mV respectively after conjugation. From the cellular drug concentration-time plot, AUC was found to be 0.4745, 0.6791 and 1.24 for MF, MF-nanoparticles and wheat germ agglutinin-MF-nanoparticles respectively. The in-vitro antiproliferative activity was improved and prolonged significantly after wheat germ agglutinin-conjugation. The results conclusively demonstrate improved availability and efficacy of antiasthmatic drug in alveolar epithelial cell lines. Hence, a drug once formulated as mucoadhesive nanoparticles and incorporated in dry powder inhaler formulation may be used for targeting any segment of lungs for more improved therapeutic response in other lung disorders as well.
Ann Allergy Asthma Immunol. 2008 Mar; 100(3): 272-9
Bielory L
BACKGROUND: Allergic rhinitis (AR) is more appropriately termed allergic rhinoconjunctivitis owing to the equally bothersome nasal and ocular symptoms. Extensive evidence supports the ability of intranasal corticosteroids to reduce nasal symptoms of AR, although less evidence is available to define clearly their impact on allergic conjunctivitis. OBJECTIVE: To determine the effect of the intranasal corticosteroid mometasone furoate nasal spray (NS) on the ocular symptoms of seasonal AR. METHODS: This retrospective pooled analysis of 4 placebo-controlled clinical studies randomized patients 12 years and older with symptomatic seasonal AR to receive mometasone furoate NS, 200 microg once daily (n = 491), or placebo (n = 492). Ocular symptom (eye tearing [epiphora], itching [pruritus], and redness [erythema]) severity was rated by patients twice daily on a 4-point scale (0 = none to 3 = severe) in the morning and evening, with scores averaged to obtain a daily mean score. Efficacy variables were the pooled mean change from baseline in the averaged morning and evening total ocular symptom score (TOSS) and the individual ocular symptom scores. RESULTS: The change in mean TOSS from baseline to days 1 to 15 was -1.33 (-19.8%) with mometasone furoate NS and -0.93 (-5.6%) with placebo (P < .001). Improvements in individual symptoms were significantly better with mometasone furoate NS than with placebo on days 2 (tearing) and 4 (itching and redness). A slightly greater reduction in TOSS was seen with mometasone furoate NS treatment in the evening than in the morning. CONCLUSIONS: This detailed analysis of an intranasal corticosteroid on individual ocular symptoms supports the positive impact of mometasone furoate NS on ocular symptoms.
Suppressive effects of topical mometasone furoate and tacrolimus on skin prick testing in children.
Pediatr Dermatol. 2008 Mar-Apr; 25(2): 269-70
Gradman J, Wolthers OD
Skin prick tests were performed in 12 children with atopic eczema before and after 2 weeks of treatment with topical mometasone furoate and tacrolimus. Both treatments significantly suppressed the allergen wheal size. Mometasone furoate reduced the histamine wheal size as well. Skin prick testing in children treated with topical glucocorticoids or tacrolimus is associated with a risk of false-negative test results.
Ann Allergy Asthma Immunol. 2008 Mar; 100(3): 264-71
Anolik R,
BACKGROUND: Intranasal corticosteroids and nonsedating antihistamines are the drug classes most often prescribed to treat allergic rhinitis (AR). Treatment guidelines recommend a combination of these agents for moderate-to-severe AR. However, clinical studies have found that combining an antihistamine with an intranasal corticosteroid provides few or no advantages over monotherapy with an intranasal corticosteroid. OBJECTIVE: To compare the efficacy of mometasone furoate nasal spray (NS) plus loratadine with that of monotherapy with the individual agents in patients 12 years and older with at least a 2-year history of seasonal AR. METHODS: In a multicenter, randomized, double-blind, parallel-group, placebo-controlled clinical study, 702 patients were randomized to receive mometasone furoate NS, 200 microg, plus loratadine, 10 mg (n = 169); mometasone furoate NS, 200 microg (n = 176); loratadine, 10 mg (n = 181); or placebo (n = 176) once daily for 15 days. Primary efficacy variables were total nasal symptom score (TNSS) and total symptom score (TSS) as recorded on diary cards. RESULTS: No statistically significant differences were observed between mometasone furoate NS plus loratadine and mometasone furoate NS monotherapy for the primary efficacy variables. For TNSS and TSS, all 3 active drug therapies were more effective than placebo (P < or = .02). Both mometasone furoate NS treatment regimens were more effective than loratadine or placebo for TNSS (P < .01 for both) and TSS (P < or = .03 for both), whereas loratadine was more effective than placebo for TNSS only (P = .02). CONCLUSIONS: Combination therapy with mometasone furoate NS and loratadine provided benefits similar to monotherapy with mometasone furoate NS for the symptoms of seasonal AR. Therefore, mometasone furoate NS monotherapy was shown to be an effective treatment for seasonal AR.
Ocular impact of intranasal corticosteroid therapy: all that surprising?
Ann Allergy Asthma Immunol. 2008 Mar; 100(3): 193
Weber RW