PEGylated liposomes of anastrozole for long-term treatment of breast cancer: in vitro and in vivo evaluation

The aim of present study was to develop conventional and PEGylated (long circulating), liposomes containing anastrozole (ANS) for effective treatment of breast cancer. ANS is a third-generation non-steroidal aromatase inhibitor of the triazole class used for the treatment of advanced and late-stage breast cancer in post-menopausal women. Under such disease conditions the median duration of therapy should be prolonged until tumor regression ends (>31 months). Liposomes were prepared by the thin film hydration method by using ANS and various lipids such as soyaphosphatidyl choline, cholesterol and methoxy polyethylene glycol distearoyl ethanolamine in different concentration ratios and evaluated for physical characteristics, in vitro drug release and stability. Optimized formulations of liposome were studied for in vitro cytotoxic activity against the BT-549 and MCF-7 cell lines and in vivo behavior in Wistar rats. Preformulation studies, both Fourier transform infrared study and differential scanning calorimetry analysis showed no interaction between the drug and the excipients used in the formulations. The optimized formulations AL-07 and AL-09 liposomes showed encapsulation efficiencies in the range 65.12?±?1.05% to 69.85?±?3.2% with desired mean particle size distribution of 101.1?±?5.9 and 120.2?±?2.8?nm and zeta potentials of ?43.7?±?4.7 and ?62.9?±?3.5 mV. All the optimized formulations followed Higuchi-matrix release kinetics and when plotted in accordance with the Korsemeyer–Peppas method, the n-value 0.5?n?in vitro cytotoxicity studies (p?(0–∞) values when compared to pure drug (p?相似文献   

New molecular data favour an anthropogenic introduction of the wood mouse (Apodemus sylvaticus) in North Africa

According to fossil data, the wood mouse arrived in North Africa 7500 ya, while it was present in Europe since Early Pleistocene. Previous molecular studies suggested that its introduction in North Africa probably occurred via the Strait of Gibraltar more than 0.4 Mya ago. In this study, we widely sampled wood mice to get a better understanding of the geographic and demographic history of this species in North Africa and possibly to help resolving the discrepancy between genetic and palaeontological data. Specifically, we wanted to answer the following questions: (1) When and how did the wood mouse arrive in North Africa? and (2) What is its demographic and geographic history in North Africa since its colonization? We collected in the field 438 new individuals and used both mtDNA and six microsatellite markers to answer these questions. Our results confirm that North African wood mice have a south‐western European origin and colonized the Maghreb through the Strait of Gibraltar probably during the Mesolithic or slightly after. They first colonized the Tingitana Peninsula and then expanded throughout North Africa. Our genetic data suggest that the ancestral population size comprised numerous individuals reinforcing the idea that wood mice did not colonize Morocco accidentally through rafting of a few individuals, but via recurrent/multiple anthropogenic translocations. No spatial structuring of the genetic variability was recorded in North Africa, from Morocco to Tunisia.     

A promising RVO4:Eu3+,Li+@SiO2 (R = Gd,Y and Gd/Y) red‐emitting phosphor with improved luminescence (cd/m2) and colour purity for optical display applications

Red emission intensity was optimized in three stages, by investigating the effects of: (i) host composition (Gd, Y and Gd/Y), (ii) codoping Li⁺ as a sensitizer and, finally, (iii) with a SiO₂ shell coating as a protecting layer. Lanthanide vanadate powder phosphors were synthesized using a modified colloidal precipitation technique. The effects of SiO₂ coating on phosphor particles were characterized using scanning electron microscopy (SEM)‐EDAX, transmission electron microscopy (TEM), Fourier transform infrared (FTIR) and photoluminescence (PL) measurements. An improvement in the PL intensity on Li codoping was due to improved crystallinity, which led to higher oscillating strengths for the optical transitions, and also a lowering of the inversion symmetry of Eu³⁺ ions. Red emission intensity due to ⁵D₀ → ⁵D₂ transition of the phosphor Y_0.94VO₄:Eu³⁺_0.05,Li⁺_0.01 was enhanced by 22.28% compared with Y_0.95VO₄:Eu³⁺_0.05, and was further improved by 58.73% with SiO₂ coating. The luminescence intensity (I) and colour coordinates (x, y) of the optimized phosphor Y_0.94VO₄:Eu³⁺_0.05,Li⁺_0.01@SiO₂, where I = 13.07 cd/m² and (x = 0.6721, y = 0.3240), were compared with values for a commercial red phosphor (Y₂O₂S:Eu³⁺), where I = 27 cd/m² and (x = 0.6522, y = 0.3437). The measured colour coordinates are superior to those of the commercial red phosphor, and moreover, match well with standard NTSC values (x = 0.67, y = 0.33). Copyright © 2015 John Wiley & Sons, Ltd.     

Design and synthesis of pyridazinone-substituted benzenesulphonylurea derivatives as anti-hyperglycaemic agents and inhibitors of aldose reductase – an enzyme embroiled in diabetic complications

Thirty new aryl-pyridazinone-substituted benzenesulphonylurea derivatives (I–XXX) were synthesized and evaluated for their anti-hyperglycaemic activity in glucose-fed hyperglycaemic normal rats. Twenty-three compounds (III–XI, XIV–XVII, XIX–XXIV, XXVI and XXVIII–XXX) showed more or comparable area under the curve (AUC) reduction percentage (ranging from 21.9% to 35.5%) as compared to the standard drug gliclazide (22.0%). On the basis of docking results, 18 compounds were screened for their in vitro ability to inhibit rat lens aldose reductase. Ten compounds (III–VI, XII, XVI–XVIII, XXI and XXVII) showed ARI activity with IC50 ranging from 34 to 242?μM. Out of these, two compounds IV and V showed best ARI activity which is comparable with that of quercetin. As a result, two compounds (IV and V) possessing significant dual action (anti-hyperglycaemic and aldose reductase inhibition) were identified and may be used as lead compounds for developing new drugs.     

Seasonal incidence of aphid,Amphorophora ampullata Bukton (Homoptera: Aphididae) on fern,Hypolepis polypodioides (Blume) Hook (Hypolepidaceae) from Western Himalaya

Seasonal incidence of aphid, Amphorophora ampullata on Hypolepis polypodioides was recorded throughout the year from November 2012 to November 2013 at weekly interval. Peak incidence of aphid was recorded during third week of November 2012 (25.94 ± 2.39 aphids/pinna), later the aphid population gradually decreased from December 2012 onwards and reached below threshold level during the last week of January (0.1 ± 0 aphids/pinna). The aphid population starts building up again from first week of February 2013 (1.6 ± 0.13 aphids/pinna) and attained its peak in the last week of August (32.17 ± 1.22 aphids/pinna) then decreased gradually in the first week of September (20.82 ± 4.70 aphids/pinna). Aphid densities again increased gradually from second week of September (21.62 ± 3.02 aphids/pinna) to November 2013 and reached maximum aphid densities during November (56.55 ± 4.34 aphids/pinna). Among weather parameters, aphid population showed significant positive correlation with relative humidity during morning hours.     

Assessing the applicability of phytoremediation of soils with mixed organic and heavy metal contaminants

Soil pollution is a major environmental problem and many contaminated sites are tainted with a mixture of organic and heavy metal contaminants. Compared to other remedial strategies, phytoremediation is a low cost, environmentally-friendly, sustainable means of remediating the contamination. This review first provides an overview of phytoremediation studies where the soil is contaminated with just one type of pollutant (heavy metals or organics) and then critically evaluates the applicability of phytotechnologies for the remediation of contaminated sites where the soil is polluted by a mixture of organic and heavy metal contaminants. In most of the earlier research studies, mixed contamination was held to be detrimental to plant growth, yet there were instances where plant growth was more successful in soil with mixed contamination than in the soil with only individual contaminants. New effective phytoremediation strategies can be designed for remediation of co-contaminated sites using: (a) plants species especially adapted to grow in the contaminated site (hyperacumulators, local plants, transgenic plants); (b) endophytic bacteria to enhance the degradation in the rizhosphere; (c) soil amendments to increase the contaminants bioavailability [chelating agents and (bio)surfactants]; (d) soil fertilization to enhance the plant growth and microbial activity in the soil; and (e) coupling phytoremediation with other remediation technologies such as electrokinetic remediation or enhanced biodegradation in the rhizosphere.