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Context and objective: The aim of this study was to develop, characterize and evaluate a mucoadhesive caplet resulting from a polymeric blend (polymeric caplet) for intravaginal anti-HIV-1 delivery.

Materials and methods: Poly(lactic-co-glycolic) acid, ethylcellulose, poly(vinylalcohol), polyacrylic acid and modified polyamide 6, 10 polymers were blended and compressed to a caplet-shaped device, with and without two model drugs 3′-azido-3′-deoxythymidine (AZT) and polystyrene sulfonate (PSS). Thermal analysis, infrared spectroscopy and microscopic analysis were carried out on the caplets employing temperature-modulated DSC (TMDSC), Fourier transform infra-red (FTIR) spectrometer and scanning electron microscope, respectively. In vitro and in vivo drug release analyses as well as the histopathological toxicity studies were carried out on the drug-loaded caplets. Furthermore, molecular mechanics (MM) simulations were carried out on the drug-loaded caplets to corroborate the experimental findings.

Results and discussion: There was a big deviation between the Tg of the polymeric caplet from the Tg's of the constituent polymers indicating a strong interaction between constituent polymers. FTIR spectroscopy confirmed the presence of specific ionic and non-ionic interactions within the caplet. A controlled near zero-order drug release was obtained for AZT (20 d) and PSS (28 d). In vivo results, i.e. the drug concentration in plasma ranged between 0.012–0.332?mg/mL and 0.009–0.256?mg/mL for AZT and PSS over 1–28 d.

Conclusion: The obtained results, which were corroborated by MM simulations, attested that the developed system has the potential for effective delivery of anti-HIV-agents.  相似文献   
3.
Fretting fatigue is one of the most important phenomena for inducing a significant reduction of fatigue strength and consequently, leading to unexpected failure accidents of the engineering structures even at very low stresses. In the present study, both plain and fretting fatigue tests with zero mean stress were carried out on two different types of steel, low-carbon steel and martensitic stainless steel, by means of a reversed bending fatigue testing machine. The drop in the fatigue strengths through fretting at vise clamp-specimen interface were significant for both tested steels. The fretting processes produced a reduction in fatigue strength of about 27% for low-carbon steel and 16% for martensitic stainless steel.  相似文献   
4.
The influence of noncompetitive (MK-801), competitive (AP-7) and the antagonist of polyamines site of NMDA receptor (arcaine) on the central activity of angiotensin II (A II) was studied. The open field test, conditioning of active avoidance responses (CARs) and passive avoidance situation was used to investigate learning and memory in rats. All used antagonists decreased beneficial action of A II on these processes.  相似文献   
5.
Quantities of attractive (exo-brevicomin and frontalin) and inhibitory (trans-verbenol, verbenone, and ipsdienol) pheromones were monitored in both sexes ofDendroctonus brevicomis during their colonization of a ponderosa pine. Verbenone was found in males in the greatest amounts at the time of landing, and it declined more rapidly than the other pheromones in either sex. The amounts of frontalin andexo-brevicomin in males and females, respectively, increased after initial boring within the host but began to decline after mating. The quantity oftrans-verbenol in both sexes (females had significantly more) declined more gradually thanexo-brevicomin, frontalin, and verbenone. Ipsdienol was found only in males during the initial stages of attack when encountering the resin. It is suggested that along with a general decline in all pheromonal components, a sufficient change in the ratio of the attractive pheromones to an inhibitory pheromone,trans-verbenol, may play a role in termination of aggregation.trans-Verbenol may also function along with verbenone and ipsdienol in limiting the density of attack and thus intraspecific competition. These inhibitory pheromones also appear to cause several competing species of bark beetle to avoid landing in areas infested withD. brevicomis, even when their own pheromone is present.Coleoptera:Scolytidae. These studies were supported in part by the Rockefeller Foundation, USDA Forest Service, Regional research project W-110, SEA/ USDA, and the National Science Foundation and Environmental Protection Agency through a grant (NSF GB-34719/BMS 75-04223) to the University of California.  相似文献   
6.
The major sex attractant of the oak leaf roller (Archips semiferanus Walker),cis-10-tetradecenyl acetate (I), was synthesized in 55–62% overall yield by a highly economical route from inexpensive azelaic acid (II).Authorized as Paper No. 4779 in the Journal Series of the Pennsylvania Agricultural Experiment Station.  相似文献   
7.
The Journal of Supercomputing - Smart services are a concept that provides services to the citizens in an efficient manner. The online shopping and recommender system can play an important role for...  相似文献   
8.
Stratified concrete poses a promising alternative for construction. Its fresh and hardened properties have been studied at the material level; however, structural behavior in steel reinforced specimens has not been studied. This paper focuses on the flexural behavior of eight stratified reinforced concrete (SRC) specimens representing slices from a slab or non-bearing wall. Specimens with two stratified concrete designs and three steel ratios were tested and compared to estimates from a fiber element numerical model and rectangular stress-block design methods from ACI 318 and Eurocode 2. The results suggest that SRC has similar damage modes as ordinary reinforced concrete (ORC). The fiber element model accurately estimated the measured behavior, while ACI 318 and Eurocode 2 differed from the experimental results by <25%. These prediction accuracies are similar to those for ORC. Therefore, the flexural design of SRC can be done using both fiber element and rectangular stress-block approaches.  相似文献   
9.
In this study, larvicidal activity of silver nanoparticles (AgNPs) synthesised using apple extract against fourth instar larvae of Aedes aegypti was determined. As a result, the AgNPs showed moderate larvicidal effects against Ae. aegypti larvae (LC50  = 15.76 ppm and LC90  = 27.7 ppm). In addition, comparison of larvicidal activity performance of AgNPs at high concentration prepared using two different methods showed that Ae. aegypti larvae was fully eliminated within the duration of 2.5 h. From X‐ray diffraction, the AgNP crystallites were found to exhibit face centred cubic structure. The average size of these AgNPs as estimated by particle size distribution was in the range of 50–120 nm. The absorption maxima of the synthesised Ag showed characteristic Ag surface plasmon resonance peak. This green synthesis provides an economic, eco‐friendly and clean synthesis route to Ag.Inspec keywords: silver, nanofabrication, X‐ray diffraction, zoology, particle size, nanoparticles, biomedical materials, nanomedicineOther keywords: time 2.5 h, size 50 nm to 120 nm, silver nanoparticle, larvicidal property, instar larvae, Aedes aegypti, larvicidal effect, larvicidal activity performance, X‐ray diffraction, nanoparticle particle size distribution, absorption maxima, silver surface plasmon resonance peak  相似文献   
10.
Unmanned aerial vehicles (UAVs) have shown promising benefits in many applications. This has been enabled by the emergence of additive manufacturing (AM), which give the designers a large amount of geometrical freedom. In this paper, a novel design process of fused deposition modeling (FDM) combining both topology and infill optimization is introduced for AM of high performance porous structures. Tensile testing of FDM printed samples is first carried out to study the effect of the build orientation on the mechanical properties of acrylonitrile butadiene styrene (ABS) samples. It is found that samples built perpendicular to the load axis are the weakest with a tensile strength of 29 MPa and Young's modulus of 1960 MPa. The materials properties are fed to the finite elements analysis (FEA) for geometrical topology optimization, aiming to maximize stiffness and reduce weight of those parts. Afterwards, an infill optimization is carried out on the topology optimized parts using different mesostructures such as honeycomb, triangular, and rectangular to achieve high structural performance. The results showed that triangular pattern with 50% infill density had the lowest developed stresses, less mass, and strain energy when compared to other structures. Optimum UAVs parts of a quadcopter are successfully manufactured, assembled, and tested.
  相似文献   
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