scholarly journals What makes flunisolide different among inhaled corticosteroids used for nebulization: a close look at the role of aqueous solubility

2021 ◽  
Vol 16 ◽  
Author(s):  
Ahmad Kantar
Keyword(s):  
Fluticasone Propionate ◽  
Physicochemical Properties ◽  
Beclomethasone Dipropionate ◽  
Water Solubility ◽  
Inhaled Corticosteroids ◽  
Aqueous Solubility ◽  
Pharmacokinetic Profile ◽  
The Elderly ◽  
Metered Dose

Evidence-based management of bronchial asthma and wheezing in children and adults recommends the employment of inhaled corticosteroids (ICSs). Difficulty in using some inhalation devices for ICS delivery, such as pressurized metered-dose and dry-powder inhalers, is common among young children and in the elderly, and for that reason, they are replaced with nebulizers. We reviewed comparative studies that evaluated funisolide with other ICSs currently available on the market, including beclomethasone dipropionate, fluticasone propionate, and budesonide. Moreover, we assessed the physicochemical properties of these ICSs in determining drug fate in the lung. Data indicate that the flunisolide output in respirable particles by any type of pneumatic nebulizer (traditional, open breath or breath-enhanced) is superior to the output of other ICSs. This is principally attributed to the higher water solubility of flunisolide. Furthermore, in vivo simulation studies demonstrate that the intersubject variability of the inhaled dose among asthmatic children was much greater for suspensions of fluticasone propionate and beclomethasone dipropionate than for those of flunisolide. The physicochemical properties and pharmacokinetic profile of flunisolide favor its employment in nebulization.

scholarly journals Investigating the Anti-Inflammatory Activity of Curcumin-Loaded Silica-Containing Redox Nanoparticles

2021 ◽  
Vol 2021 ◽  
pp. 1-11
Author(s):  
Khoa Minh Le ◽  
Nhu-Thuy Trinh ◽  
Vinh Dinh-Xuan Nguyen ◽  
Tien-Dat Van Nguyen ◽  
Thu-Ha Thi Nguyen ◽  
...  
Keyword(s):  
Chronic Inflammation ◽  
Self Assembly ◽  
Water Solubility ◽  
Nitroxide Radical ◽  
Pharmacokinetic Profile ◽  
Ros Scavenging ◽  
Anti Inflammatory ◽  
Inflammatory Effect

Chronic inflammation is considered as one of the challenging diseases, and overproduction of reactive oxygen species (ROS) is strongly related to the onset of chronic inflammation. Therefore, antioxidant and anti-inflammatory approaches are particularly becoming suitable treatment and prevention of inflammation. Curcumin (CUR), a main component of turmeric extract, is well known as an effective agent in both antioxidant and anti-inflammatory activities; however, there are still some limitations of its use including poor water solubility, low bioavailability, and oxidation by ROS. Nanotechnology has been used as a drug delivery system, which is a promising approach in overcoming the aforementioned drawbacks of CUR; hence, it improves the antioxidant and anti-inflammatory effects of conventional medications. In this research, silica-containing redox nanoparticles (siRNP) were designed with the size of several tens of nanometers, prepared by self-assembly of an amphiphilic block copolymer consisting of drug absorptive silica moiety and ROS-scavenging nitroxide radical moiety in the hydrophobic segment. CUR was simply encapsulated into siRNP through the dialysis method, creating CUR-loaded siRNP (CUR@siRNP), which significantly improved the water solubility of CUR. The efficient antioxidant activity and anti-inflammatory effect of CUR@siRNP in vitro were also improved via 2,2-diphenyl-1-picrylhydrazyl assay and lipopolysaccharide-induced macrophage cell line activation, respectively. Oral administration of CUR@siRNP showed improvement in pharmacokinetic profile in vivo including AUC and Cmax values as compared to free CUR. Furthermore, the anti-inflammatory effect of nanoformulation was investigated in the colitis mouse model induced by dextran sodium sulfate.

Lutein encapsulated oleic - linoleic acid nanoemulsion boosts oral bioavailability of retinal protective carotenoid lutein in rat model

2021 ◽  
Author(s):  
Veeresh B Toragall ◽  
Twinkle Godhwani ◽  
V Baskaran ◽  
Naveen Jayapala
Keyword(s):  
Linoleic Acid ◽  
Oral Bioavailability ◽  
Mixed Micelles ◽  
Water Solubility ◽  
Health Benefits ◽  
Aqueous Solubility ◽  
Mean Size ◽  
The Mean

Abstract There is excessive interest in emerging colloidal delivery systems to enhance the water solubility and oral bioavailability of lutein, which is a hydrophobic carotenoid claimed to possess health benefits. The present study aimed to design lutein-enriched nanoemulsions with improved physicochemical properties and to achieve various health benefits of lutein. The prepared lutein nanoemulsion was characterized, and its bioavailability was examined in vitro (simulated gastrointestinal digestion) and in vivo. The mean size, PDI and zeta potential of the lutein nanoemulsion were 110 ± 8 nm, 0.271 and 36 ± 2 mV, respectively. Furthermore, TEM examination revealed that the particles are nanosized and spherical in shape. Notably, the aqueous solubility of the nanoemulsion was 726-fold higher than that of free lutein. The composite nanoemulsion also showed exceptionally higher (87.4%) in vitro bioaccessibility than that of nonencapsulated or free lutein (15%). The in vivo bioavailability of lutein nanoemulsion (112.6 ng/mL) was much higher than that of nonencapsulated lutein (48.6 ng/ml) and mixed micelles (68.5 ng/mL), and the tissue distribution pattern of lutein nanoemulsion showed higher lutein accumulation in the liver (2.80- and 1.70-fold) and eye (1.91- and 1.48-fold) compared to free lutein and mixed micelle-fed groups. These results suggested that oleic acid-linoleic acid composite nanoemulsions may be a promising delivery system for lutein and may help enhance the solubility, oral bioavailability and bioefficacy of lutein and could be used as an ingredient for the formulation of beverages or functional foods.

scholarly journals Efficacy of inhaled corticosteroids for patients with asthma: a descriptive review of randomized controlled trials

2015 ◽  
Vol 5 (1) ◽  
pp. 41-50
Author(s):  
Mostafa Alabousi ◽  
Abdullah Alabousi ◽  
Natalie Ambeault ◽  
John Riva
Keyword(s):  
Fluticasone Propionate ◽  
Full Text ◽  
Beclomethasone Dipropionate ◽  
Search Strategy ◽  
Inhaled Corticosteroids ◽  
Controlled Trials ◽  
Sputum Eosinophil ◽  
Randomized Controlled ◽  
Eosinophil Counts ◽  
Full Text Screening

Objective: To evaluate the efficacy of inhaled corticosteroids (ICS) in patients with asthma based on changes in sputum eosinophil counts, through a review of relevant randomized controlled trials (RCTs).Methods: Studies were retrieved from MEDLINE, EMBASE, the SYSTEM FOR INFORMATION ON GREY LITERATURE, and the INSTITUTE FOR SCIENTIFIC INFORMATION from February 1, 2003 to February 1, 2013 based on a comprehensive search strategy. Articles were screened through two stages: title and abstract; and full-text screening. RCTs enrolling patients with asthma, testing an ICS intervention, and reporting outcomes on changes in sputum eosinophil counts pre- and post-intervention were included. Following screening, data extraction, and quality appraisal, a descriptive synthesis of trials was conducted.Results: The search strategy retrieved 447 articles, of which 66 articles underwent full-text screening, resulting in 37 RCTs that met the inclusion criteria for this review. The articles were stratified according to the type of ICS: budesonide, fluticasone propionate, ciclesonide, beclomethasone dipropionate, and mometasone.  Across trials, 9 of 16 budesonide, 5 of 14 fluticasone propionate, 4 of 9 of nine ciclesonide, 2 of 4 beclomethasone dipropionate, and 1 of 2 mometasone interventions demonstrated a statistically significant (p < 0.05) reduction in sputum eosinophil counts.Conclusion: This study detected differences between ICS treatments however the clinical relevance is uncertain. There is insufficient evidence to suggest the superiority of one ICS treatment over another. Further research needs to be conducted to evaluate the relative impact of ICS products upon eosinophil counts, as well as in clarifying what quantitative level of change in baseline eosinophil counts is required to observe a change in symptom improvement and disease control.

scholarly journals DDIS-21. IN VITRO MICRODIALYSIS RECOVERY OF TRAMETINIB

2019 ◽  
Vol 21 (Supplement_6) ◽  
pp. vi67-vi67
Author(s):  
Carlos Romo ◽  
Nicole Anders ◽  
Morgan Scardina ◽  
Debraj Mukherjee ◽  
Stuart Grossman ◽  
...  
Keyword(s):  
Aqueous Solubility ◽  
Pharmacokinetic Profile ◽  
Primary Objective ◽  
Mitogen Activated Protein Kinase ◽  
In Vivo Studies ◽  
Limit Of Quantification ◽  
Relative Recovery ◽  
Two Samples

Abstract BACKGROUND Dysregulation of the mitogen-activated protein kinase and phosphoinositide 3-kinase (PI3K) pathways is common in several primary brain tumors and metastatic cancers affecting the central nervous system. Trametinib, and oral MEK1/2 inhibitor, has been effective in preclinical studies against a variety of cell lines and improves survival in select patients with gliomas. Unfortunately, limited and often short-lived benefits are frequently seen in patients. A potential explanation for this is insufficient blood brain barrier penetration at therapeutic concentrations. The primary objective of this study is to measure the in vitro relative recovery of trametinib using microdialysis to establish the feasibility of characterizing its intratumoral pharmacokinetics in vivo using this technique. METHODS In vitro recovery experiments were performed utilizing commercially available microdialysis instruments. Two perfusion rates (0.5–1µL/min), the use of iso- and hypertonic perfusates (artificial CSF and 10% bovine serum albumin in PBS), and the addition of dimethyl sulfoxide (DMSO) were evaluated using the extraction efficiency method. Liquid chromatography-tandem mass spectrometry was used to measure the concentrations of trametinib in stock solutions, dialysate samples, and controls over time. RESULTS Dialysate was initially collected from a solution spiked with 15ng/mL at a rate of 1µL/min for 60 minutes, the recovery was 0.3ng/mL (0.2%) in two samples and below the limit of quantification (< 0.2ng/mL) in three. Dialysate samples were then collected from a stock solution with 150ng/mL of trametinib, recovery ranged from 0.3–15.3ng/mL (0.2–10.2%) in nine detectable samples out of sixteen. Recovery was greater with the addition of DMSO to the perfusate and with the use of a hypertonic perfusate. CONCLUSIONS The poor relative recovery of trametinib using microdialysis suggests that this technique would be unreliable in in vivo studies. Trametinib has poor aqueous solubility, limiting the ability of characterizing its pharmacokinetic profile through microdialysis.

scholarly journals Electrospun Resveratrol-Loaded Polyvinylpyrrolidone/Cyclodextrin Nanofibers and Their Biomedical Applications

Pharmaceutics ◽  
2020 ◽  
Vol 12 (6) ◽  
pp. 552 ◽  
Author(s):  
Ying-Cheng Lin ◽  
Stephen Chu-Sung Hu ◽  
Pao-Hsien Huang ◽  
Tzu-Ching Lin ◽  
Feng-Lin Yen
Keyword(s):  
Antioxidant Activity ◽  
Physicochemical Properties ◽  
Water Solubility ◽  
Skin Penetration ◽  
Aqueous Solubility ◽  
Amorphous Structure ◽  
Penetration Ability ◽  
Potential Applications ◽  
Anti Inflammatory ◽  
Franz Diffusion Cells

Resveratrol is a naturally occurring polyphenol compound which has been shown to possess antioxidant and anti-inflammatory properties. However, its pharmaceutical applications are limited by its poor water solubility. In this study, we used electrospinning technology to synthesize nanofibers of polyvinylpyrrolidone (PVP) and hydroxypropyl-β-cyclodextrin (HPBCD) loaded with resveratrol. We used X-ray diffractometry to analyze crystalline structure, Fourier transform infrared spectroscopy to determine intermolecular hydrogen bonding, antioxidant assays to measure antioxidant activity, and Franz diffusion cells to evaluate skin penetration. Our results showed that the aqueous solubility of resveratrol nanofibers was greatly improved (by more than 20,000-fold) compared to the pure compound. Analysis of physicochemical properties demonstrated that following nanofiber formation, resveratrol was converted from a crystalline to amorphous structure, and resveratrol formed new intermolecular bonds with PVP and HPBCD. Moreover, resveratrol nanofibers showed good antioxidant activity. In addition, the skin penetration ability of resveratrol in the nanofiber formulation was greater than that of pure resveratrol. Furthermore, resveratrol nanofibers suppressed particulate matter (PM)-induced expression of inflammatory proteins (COX-2 and MMP-9) in HaCaT keratinocytes. Therefore, resveratrol-loaded nanofibers can effectively improve the solubility and physicochemical properties of resveratrol, and may have potential applications as an antioxidant and anti-inflammatory formulation for topical skin application.

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