Gentamicin and leucine inhalable powder: What about antipseudomonal activity and permeation through cystic fibrosis mucus?

The aim of this study was to evaluate the permeation properties of gentamicin (G) in a novel dry powder form for inhalation through an artificial mucus model. Moreover, since respiratory infections sustained by Pseudomonas are a major cause of sickness and death in CF patients, the susceptibility of P. aeruginosa to engineered G powders was investigated.     

Synthesis and Fluorescent Properties of Carbazole‐Substituted Hydroxyethylcelluloses

Carbazole‐substituted hydroxyethylcelluloses (Cz‐HECs) are homogeneously synthesized by reacting hydroxyethylcellulose (HEC) with N‐3′‐bromopropyl carbazole (Br‐Cz). The structure of Cz‐HECs is characterized with elemental analysis and NMR, and the DS of the carbazole is in the range 0.11–0.43, determined from nitrogen content. The fluorescent properties of Cz‐HECs are measured using a spectrofluorimeter. The results show that the fluorescence lifetime increases as the DS increases, and the fluorescent intensity of Cz‐HECs is stronger than that of Br‐Cz. All samples exhibit concentration self‐quenching properties. The addition of acrylonitrile, as an electron acceptor, quenches the emission spectra of Cz‐HECs, and the fluorescence quenching is found to be a dynamic quenching by analyzing with the Stern–Volmer equation.     

Semisynthetic Derivative of Artemisia annua-Loaded Transdermal Bioadhesive for the Treatment of Uncomplicated Malaria Caused by Plasmodium falciparum in Children

According to the most recent World Health Organization statistics, malaria infected approximately 219 million people in 2017, with an estimate of 435,000 deaths (World Health Organization, 2018). Communities isolated from cities are the most deprived of access to the necessary hospital facilities. Herein we report the development of a transdermal bioadhesive containing artemether (ART), an alternative, potentially lifesaving, treatment regimen for malaria in low-resource settings. Bioadhesives were prepared from an aqueous blend of hydroxyethylcellulose (4.5% w/w), ART, propoxylated-ethoxylated-cetyl-alcohol, polysorbate 80, propyleneglycol, glycerine, mineral oil, and oleic acid. In this study, the average pore size of bioadhesive 5.5b was 52.6 ± 15.31 μm. Differential scanning calorimetry and thermogravimetric analyses confirm the thermal stability of ART bioadhesives at room temperature. Tensile tests indicated good mechanical properties for bioadhesive 5.5b, when compared to 5.5a, where 5.5b showed elastic modulus 0.19 MPa, elongation at break 204%, tensile stress 0.31 MPa, tensile strength at break 0.23 MPa. Bioadhesion assays suggested that formulations containing surfactants had higher detachment forces. Permeation studies demonstrated that the best outcome was achieved with a bioadhesive containing 25 mg ART (5.5b) that after 24 h released 6971 ± 125 μg, which represents approximately 28% of drug permeation. Data reported presents a promising candidate for a new antimalarial transdermal formulation.     

Open evaluation of a new non-preserved artificial tear

In an open, one-eye controlled study the efficacy of a new, non-preserved artificial tear (sodium chloride 0.34% W/W, hydroxyethylcellulose 0.44% W/W), stored in single-use disposable units (Minims, Smith and Nephew) was compared to a variety of other tear substitutes in 30 patients who were currently applying artificial tears to both eyes. It was found that the new drop was tolerated well by the majority of patients with 19 subjects (63%) preferring them to their existing medication. There was a significant reduction in the overall rose bengal staining pattern and also in the stain uptake of the medial conjunctiva between the first and second visits in the Minims treated eyes, but not in the eyes treated with the other drops ( P < 0.05). There was also a significant improvement in the patients' subjective feelings of dryness and grittiness in the Minims treated eyes, but not in the other eyes ( P < 0.05).     

Effect of Hydrogen Peroxide on the Viscosity of a Hydroxyethylcellulose-Based Gel

Pharmaceutical Research -     

羟乙基纤维素接枝聚丙烯酸纳米颗粒的制备及药物缓释

羟乙基纤维素接枝聚丙烯酸共聚物(HEC g PAA)在选择性溶剂中进行自组装,制备了具有良好分散稳定性的纳米颗粒,用动态激光光散射和透射电子显微镜对纳米颗粒大小分布和形态进行了表征.以生物可降解的HEC g PAA接枝共聚物负载模型药物布洛芬(Ibuprofen),制备载药纳米颗粒(Ib HEC g PAA).在37℃于不同pH的缓冲溶液中进行了体外释放研究.药物释放速率的测定结果表明,以HEC g PAA作为布洛芬的载体,可以在选择性条件下实现药物可控释放的目的.     

Trehalose Versus Hyaluronan or Cellulose in Eyedrops for the Treatment of Dry Eye

Purpose Trehalose eyedrops were found by a previous study to be safe and effective compared with saline in the treatment of moderate-to-severe dry eye syndrome. The present study was designed to compare the efficacy of trehalose eyedrops with that of the commercially available eyedrops containing hyaluronan or cellulose now used in the treatment of moderate-to-severe dry eye syndrome.Methods In a randomized, double-masked, 4-week crossover, controlled clinical trial, 36 patients with moderate-to-severe dry eye syndrome were divided into two groups: the hyaluronan (Hyalein)-comparison group (18 patients) and the hydroxyethylcellulose (Mytear)-comparison group (18 patients). Each group used either trehalose or one of the commercially available medications contained in a masked eyedrop container for the first 4 weeks, and then for the second 4 weeks, switched to either trehalose or the commercial eyedrop not used for the first 4 weeks. Symptoms and signs in both eyes were recorded at the baseline, at 4 weeks, and at 8 weeks.Results At 4 weeks after the treatment, fluorescein and rose bengal staining scores of the ocular surface as well as the tear film breakup time had improved significantly with trehalose eyedrops compared with the commercially available eyedrops containing either hyaluronan or hydroxyethylcellulose (P < 0.001, Wilcoxon signed ranks test). In addition, all the objective signs were significantly better in patients who finished with trehalose at the end of the 8-week trial compared with those who finished with either of the two commercially available drugs. A larger number of patients evaluated trehalose as a better treatment than the commercially available eyedrops.Conclusions Trehalose solution was a better treatment for moderate-to-severe dry eye syndrome in comparison with two commercially available eyedrops containing hyaluronan or hydroxyethylcellulose. Jpn J Ophthalmol 2004;48:321–327 © Japanese Ophthalmological Society 2004Presented in part at the annual meeting of the American Academy of Ophthalmology, Orlando, Florida, October 2002. Toshihiko Matsuo is the inventor of Trehalose Eyedrops for Dry Eye Syndrome. The patent rights are held by Hayashibara Biochemical Laboratories, Okayama, Japan, in which Dr. Matsuo has no financial interest.