Notes

Aftereffect of Biomodulina-T® and VA-MENGOC-BC® upon lymphocyte subpopulations within older adults.
the validity of s-IgA as an acute stress biomarker, including additional measures during stress exposure.
Acute psychosocial stress stimulates s-IgA secretion, but only after puberty. However, children with a history of maltreatment exhibited a response resembling that of adolescents, suggesting an early maturation of the immune system. Further studies are needed to clarify the validity of s-IgA as an acute stress biomarker, including additional measures during stress exposure.Structure-guided isolation of a CH2Cl2-soluble fraction of the heartwood of Catalpa bungei "Jinsi" provided two new naphthoquinones, 9-hydroxy-4-oxo-α-lapachone (1) and 6-hydroxy-4-oxo-α-lapachone (2), together with three undescribed ones (3-5) and six known ones (6-11). The structures were elucidated on the basis of spectroscopic methods including electronic circular dichroism calculation. The antiproliferative effects of these isolates were evaluated in human breast adenocarcinoma cells MCF7. (4R)-4,9-dihydroxy-α-lapachone (5) and (4S)-4,9-dihydroxy-α-lapachone (6) exhibited the significant activities with IC50 values of 2.19 and 2.41 μM, respectively. The structure-activity relationship of 1-11 in the antiproliferative assay was then discussed. The most potent 5 and 6 were found to induce cell arrest in G1 phage through DNA damage. AP-III-a4 research buy The findings provided some valuable insights for the discovery and structural modification of α-lapachone as antiproliferative lead compounds against human breast adenocarcinoma cells.Two new polycyclic diterpenoids, euphkanoids H and I (1 and 2), along with 6 known analogues (2-8) were isolated from the roots of Euphorbia fischeriana, a traditional Chinese medicine. Their structures were identified by spectral methods, and the absolute configurations of 1 and 2 were determined by ECD calculation and single crystal X-ray diffraction, respectively. Compound 1 represents the first example of C-17 norcassane indole-diterpenes. All the isolates were screened for antiproliferative activity against a panel of human cancer cell lines using the MTT assay, and 1 showed significant cytotoxicity against HEL cells (IC50 = 3.2 μM). Simple mechanistic study revealed that 1 could induce cell cycle arrest at G0/G1 phase and apoptosis in HEL cells.Seven previously undescribed oleanane-type glycosides were isolated from the trunk barks of a Central African tree named Millettia laurentii De Wild (Fabaceae). After the extraction from the barks, the isolation and purification of these compounds were achieved using various solid/liquid chromatographic methods. Their structures were established mainly by 1D and 2D NMR (COSY, TOCSY, ROESY, HSQC, HMBC) and mass spectrometry (ESI-MS), as 3-O-β-D-glucuronopyranosyl-(1 → 2)-β-D-glucuronopyranosylechinocystic acid, 3-O-β-D-apiofuranosyl-(1 → 3)-β-D-glucuronopyranosyl-(1 → 2)-β-D-glucuronopyranosylechinocystic acid, 3-O-β-D-apiofuranosyl-(1 → 3)-β-D-galactopyranosyl-(1 → 2)-β-D-glucuronopyranosylechinocystic acid, 3-O-β-D-apiofuranosyl-(1 → 3)-[β-d-xylopyranosyl-(1 → 2)]-β-D-galactopyranosyl-(1 → 2)-β-D-glucuronopyranosylechinocystic acid, 3-O-β-D-apiofuranosyl-(1 → 3)-[α-L-arabinofuranosyl-(1 → 2)]-β-D-galactopyranosyl-(1 → 2)-β-D-glucuronopyranosylechinocystic acid, 3-O-α-L-arabinofuranosyl-(1 → 2)-β-D-galactopyranosyl-(1 → 2)-β-D-glucuronopyranosyloleanolic acid, 3-O-β-D-apiofuranosyl-(1 → 3)-[α-L-arabinofuranosyl-(1 → 2)]-β-D-galactopyranosyl-(1 → 2)-β-D-glucuronopyranosyloleanolic acid. In addition, the cytotoxicity of six glycosides among the isolated ones, was evaluated against 4 T1 cell line from a mouse mammary gland tissue, using MTS method.The work aims to explore the feasibility of Raman mapping in predicting the dissolution profiles of solid oral dosage form. In this study, N = 36 batches of representative sinomenine hydrochloride sustained-release tablets were prepared, using a D-optimal design, to introduce adequate variability, and the Raman mapping data of each tablet were acquired. The partial least squares regression models were established using three kinds of different modes, named single point mode, average mode and multi-point mode, to predict the dissolution profiles based on Raman mapping data. The percent dissolutions at specific time points and the parameters of an exponential function, which was employed to fit the dissolution profiles, were predicted, and the accuracy and precision of prediction were tested. The results showed that the multi-point mode displayed the best accuracy and precision in the prediction of both the dissolutions at the specific time points and the function parameters. In summary, the established method based on Raman mapping avoids the shortcomings of traditional dissolution testing protocols, such as complex operation, time-consuming and high analysis cost, thus has great potential of application and popularization.The most common treatment for obstructive coronary artery disease (CAD) is the implantation of a permanent drug-eluting stent (DES). Not only has this permanency been associated with delayed healing of the artery, but it also poses challenges when treating subsequent re-narrowing due to in-stent restenosis (ISR). Drug-coated balloons (DCBs) provide a potential solution to each of these issues. While their use has been primarily limited to treating ISR, in recent years, DCBs have emerged as an attractive potential alternative to DESs for the treatment of certain de novo lesions. However, there remain a number of concerns related to the safety and efficacy of these devices. Firstly, unlike DESs, DCBs necessitate a very short drug delivery window, favouring a higher drug loading. Secondly, while the majority of coronary DCBs in Europe are coated with paclitaxel, the potential mortality signal raised with paclitaxel DCBs in peripheral interventions has shifted efforts towards the development of limus-eluting balleover, indicate the potential for designing a DCB that gives rise to sufficiently similar safety and efficacy indicators as current commercial DESs.Physical instability remains a major concern with amorphous solid dispersions (ASDs). In addition to bulk crystallization inhibition, another potential strategy to improve the physical stability of ASDs is surface engineering. However, coating processes are extremely challenging for ASD microparticles. Herein, we describe for the first time the application of atomic layer coating (ALC), a solvent-free technique, to deposit a pinhole-free, ultra-thin film of aluminum oxide onto the surface of spray-dried ASD particles containing high drug loadings of ezetimibe with hydroxypropyl methylcellulose acetate succinate. ALC affords excellent control over the thickness, uniformity and conformality of the coating at the atomic scale. The freshly prepared coated ASD powders exhibited less agglomeration, a lower hygroscopicity, as well as improved wettability, flowability and compressibility compared to the uncoated samples. Under accelerated storage conditions, crystallization was detected in the uncoated 50% and 70% drug loading ASDs after only a few days, whereas the coated samples showed no evidence of physical instability for two years. Consequently, there was a dramatic decrease in the drug release from the uncoated ASDs during storage, while little change was observed for the coated samples. Using ALC for surface nanocoating of ASD paves the way for the development of higher drug loading ASD without compromising physical stability, thereby reducing the pill burden.Drug release from microparticle-based topical gels may affect their bioavailability, safety and efficacy. This work sought to elucidate spatial distribution of the drug within the microparticle matrix and how this impacts the product's critical performance attributes. The purpose of this research was to inform the development of in vitro characterization approaches to support a demonstration of bioequivalence. Drug-free microparticles were loaded with tretinoin or drug-loaded microparticles were separated from purchased Retin-A Micro® (tretinoin) topical gel drug products. The resultant microparticles were analyzed for tretinoin content, drug loading efficiency, morphology, surface topography, surface pore size distribution, particle size distribution and tretinoin release. The solid-state characteristics and chemical interaction of tretinoin with the microparticles were also investigated. Microparticles loaded with tretinoin made in-house and those separated from Retin-A Micro® (tretinoin) topical gel were spherical, polydisperse and free of aggregates. The surface porosity of the microparticles was ∼19.8% with an average pore size of ∼327 nm. Microparticles loaded with tretinoin in-house were smaller in size and exhibited faster drug release than those separated from Retin-A Micro® (tretinoin) topical gel. Tretinoin release was found to increase with an increase in the drug loading. Based on XRD and DSC data, tretinoin was present in an amorphous state. The FTIR spectra indicated a disappearance of carbonyl band of microparticles and shifting of the hydroxyl band of tretinoin due to hydrogen bonding. The extent of drug loading and the solid-state interaction of tretinoin with the microparticles may be critical for drug release. Additional characterization of the drug products is necessary to understand the effect of the factors examined in this work on the bioavailability and efficacy of tretinoin gels.Drug-coated balloons (DCB) have emerged as the alternative procedure for restenosis because of their ability to treat a variety of occlusion types with a uniform dose of anti-proliferative drugs. DCB are balloons coated with antiproliferative drugs encapsulated in a polymer matrix. There are several types of coating matrices used to produce DCB. In this study, the relationship between coating composition and drug release under physiologically relevant conditions was examined to understand how differences in coating composition impacts the drug transfer from the balloon surface to the simulated body fluids. To conduct the experiments, the balloons were coated with different paclitaxel (drug)-to-iopromide (excipient) ratios (31, 32 and 12) using an in-house developed micro-pipetting method. Scanning electron microscopy (SEM) images showed that the 31 PTXIOP ratio produced a more uniform, crystalline microstructure with a thinner coating throughout the balloon surface compared to the other drug-to-excipient ratios. The 12 PTXIOP ratio showed the least crystalline microstructure among the three ratios evaluated in this study. Three different drug elution conditions were tested. The amount of drug released to the medium was quantified by high performance liquid chromatography (HPLC). Our soaking study and submerge & deploy study showed that ∼20% of the drug transferred to the target site under physiological conditions. A track and deploy method was performed using a "mock" artery, to simulate an in vitro environment. Coated balloons were passed through the mock artery to mimic tracking turns the balloon within the arteries during the angioplasty procedures. Seven elution samples were collected at different stages of the procedure. Drug release results suggest that the higher excipient ratio helps to deliver the lipophilic drug to the target site under simulated conditions but causes higher drug loss during the balloon transfer process.
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