STRUCTURAL ELUCIDATION OF GLYCOSIDES FROM THE SEEDS OF Entada phaseoloides GROWING IN THUA THIEN HUE

Entada phaseoloides (L.) Merr. belongs to Fabaceae family and widely distributes throughout Vietnam, Thailand, Malaysia, Indonesia, Philippines, China, New Guinea, and Australia. In Vietnamese traditional medicine, the seeds of Entada phaseoloides were used for the treatment of stomachache, haemorrhoids, and hernia diseases. In this article, we report the isolation and structural elucidation of four glycosides from the water extract of seeds of E. phaseoloides including phaseoloideside C (1), phaseoloideside E (2), acanthoside D (3), and 1-(3,4,5-trimethoxyphenyl)prop-7-en-9-ol-O-(6ʹʹ-O-α-L-arabinopyranosyl)-β-D-glucopyranoside (4). To the best of our knowledge, compounds 3-4 were isolated from E. phaseoloides for the first time

Superior performance of aptamer in tumor penetration over antibody : implication of aptamer-based theranostics in solid tumors

Insufficient penetration of therapeutic agents into tumor tissues results in inadequate drug distribution and lower intracellular concentration of drugs, leading to the increase of drug resistance and resultant failure of cancer treatment. Targeted drug delivery to solid tumors followed by complete drug penetration and durable retention will significantly improve clinical outcomes of cancer therapy. Monoclonal antibodies have been commonly used in clinic for cancer treatment, but their limitation of penetrating into tumor tissues still remains because of their large size. Aptamers, as "chemical antibodies", are 15-20 times smaller than antibodies. To explore whether aptamers are superior to antibodies in terms of tumor penetration, we carried out the first comprehensive study to compare the performance of an EpCAM aptamer with an EpCAM antibody in theranostic applications. Penetration and retention were studied in in vitro three-dimensional tumorspheres, in vivo live animal imaging and mouse colorectal cancer xenograft model. We found that the EpCAM aptamer can not only effectively penetrate into the tumorsphere cores but can also be retained by tumor sphere cells for at least 24 h, while limited tumor penetration by EpCAM antibody was observed after 4 h incubation. As observed from in vivo live animal imaging, EpCAM aptamers displayed a maximum tumor uptake at around 10 min followed by a rapid clearance after 80 min, while the signal of peak uptake and disappearance of antibody appeared at 3 h and 6 h after intravenous injection, respectively. The signal of PEGylated EpCAM aptamers in xenograft tumors was sustained for 26 h, which was 4.3-fold longer than that of the EpCAM antibody. Consistently, there were 1.67-fold and 6.6-fold higher accumulation of PEGylated aptamer in xenograft tumors than that of antibody, at 3 h and 24 h after intravenous administration, respectively. In addition, the aptamer achieved at least a 4-time better tumor penetration in xenograft tumors than that of the antibody at a 200 μm distances from the blood vessels 3 h after intravenous injection. Taken together, these data indicate that aptmers are superior to antibodies in cancer theranostics due to their better tumor penetration, more homogeneous distribution and longer retention in tumor sites. Thus, aptamers are promising agents for targeted tumor therapeutics and molecular imaging

The epidemiology and aetiology of diarrhoeal disease in infancy in southern Vietnam: a birth cohort study.

OBJECTIVES: Previous studies indicate a high burden of diarrhoeal disease in Vietnamese children, however longitudinal community-based data on burden and aetiology are limited. The findings from a large, prospective cohort study of diarrhoeal disease in infants in southern Vietnam are presented herein. METHODS: Infants were enrolled at birth in urban Ho Chi Minh City and a semi-rural district in southern Vietnam, and followed for 12 months (n=6706). Diarrhoeal illness episodes were identified through clinic-based passive surveillance, hospital admissions, and self-reports. RESULTS: The minimum incidence of diarrhoeal illness in the first year of life was 271/1000 infant-years of observation for the whole cohort. Rotavirus was the most commonly detected pathogen (50% of positive samples), followed by norovirus (24%), Campylobacter (20%), Salmonella (18%), and Shigella (16%). Repeat infections were identified in 9% of infants infected with rotavirus, norovirus, Shigella, or Campylobacter, and 13% of those with Salmonella infections. CONCLUSIONS: The minimum incidence of diarrhoeal disease in infants in both urban and semi-rural settings in southern Vietnam was quantified prospectively. A large proportion of laboratory-diagnosed disease was caused by rotavirus and norovirus. These data highlight the unmet need for a rotavirus vaccine in Vietnam and provide evidence of the previously unrecognized burden of norovirus in infants

Overseas Treatment of Latent Tuberculosis Infection in US-Bound Immigrants.

Seventy percent of tuberculosis (TB) cases in the United States occur among non-US-born persons; cases usually result from reactivation of latent TB infection (LTBI) likely acquired before the person's US arrival. We conducted a prospective study among US immigrant visa applicants undergoing the required overseas medical examination in Vietnam. Consenting applicants >15 years of age were offered an interferon-γ release assay (IGRA); those 12-14 years of age received an IGRA as part of the required examination. Eligible participants were offered LTBI treatment with 12 doses of weekly isoniazid and rifapentine. Of 5,311 immigrant visa applicants recruited, 2,438 (46%) consented to participate; 2,276 had an IGRA processed, and 484 (21%) tested positive. Among 452 participants eligible for treatment, 304 (67%) initiated treatment, and 268 (88%) completed treatment. We demonstrated that using the overseas medical examination to provide voluntary LTBI testing and treatment should be considered to advance US TB elimination efforts

Developmental strategies of curcumin solid dispersions for enhancing bioavailability

Background:Although curcumin has been demonstrated to be beneficial in treating various diseases,its low solubility, chemical stability and bioavailability limit its application, especially in cancer therapy.Methods:Solid dispersions have been utilized in the last few decades to improve the bioavailability and stabilityof curcumin.Results:However, there is a lack of summaries and classifications of the methods for preparing curcumin withthis technology. The current review aims to overview the strategies used to develop solid dispersions containingcurcumin for improving drug delivery. The classification of techniques for creating solid dispersions for curcuminwas summarized, including systems for protecting curcumin degradation despite its chemical stability. Theapplications of advanced nanotechnologies in recent studies of solid dispersions were also discussed to explainthe roles of nanoparticles in formulations.Conclusion:This overview of recent developments in formulating solid dispersions for improving curcuminbioavailability will contribute to future studies of curcumin for clinical development.</jats:sec

Lead compounds in the context of extracellular vesicle research

Studies of small extracellular vesicles (sEVs), known as exosomes, have been flourishing in the last decade with several achievements, from advancing biochemical knowledge to use in biomedical applications. Physiological changes of sEVs due to the variety of cargos they carry undoubtedly leave an impression that affects the understanding of the mechanism underlying disease and the development of sEV-based shuttles used for treatments and non-invasive diagnostic tools. Indeed, the remarkable properties of sEVs are based on their nature, which helps shield them from recognition by the immune system, protects their payload from biochemical degradation, and contributes to their ability to translocate and convey information between cells and their inherent ability to target disease sites such as tumors that is valid for sEVs derived from cancer cells. However, their transport, biogenesis, and secretion mechanisms are still not thoroughly clear, and many ongoing investigations seek to determine how these processes occur. On the other hand, lead compounds have been playing critical roles in the drug discovery process and have been recently employed in studies of the biogenesis and secretion of sEVs as external agents, affecting sEV release and serving as drug payloads in sEV drug delivery systems. This article gives readers an overview of the roles of lead compounds in these two research areas of sEVs, the rising star in studies of nanoscale medicine.</jats:p

Mucoadhesive Formulation Designs for Oral Controlled Drug Release at the Colon

:Mucoadhesive formulations have been demonstrated to result in efficient drug delivery systems with advantagesover existing systems such as increased local retention and sustained drug release via adhesiveness to mucosal tissues. Thecontrolled release of colon-targeted, orally administered drugs has recently attracted a number of studies investigatingmucoadhesive systems. Consequently, substantial designs, from mucoadhesive cores to shells of particles, have been studiedwith promising applications. This review will provide an overview of and discuss specific strategies for developingmucoadhesive systems for colon-targeted oral delivery with controlled drug release, including mucoadhesive matrices,cross-linked mucoadhesive microparticles, coatings and mucoadhesive nanoparticles. The understanding of the basicprinciple of these designs and advanced formulations throughout will lead to the development of products with efficientdrug delivery at the colon for therapies for different diseases.</jats:sec

Insoluble polymers in solid dispersions for improving bioavailability of poorly water-soluble drugs

In recent decades, solid dispersions have been demonstrated as an effective approach for improving the bioavailability of poorly water-soluble drugs, as have solid dispersion techniques that include the application of nanotechnology. Many studies have reported on the ability to change drug crystallinity and molecular interactions to enhance the dissolution rate of solid dispersions using hydrophilic carriers. However, numerous studies have indicated that insoluble carriers are also promising excipients in solid dispersions. In this report, an overview of solid dispersion strategies involving insoluble carriers has been provided. In addition to the role of solubility and dissolution enhancement, the perspectives of the use of these polymers in controlled release solid dispersions have been classified and discussed. Moreover, the compatibility between methods and carriers and between drug and carrier is mentioned. In general, this report on solid dispersions using insoluble carriers could provide a specific approach and/or a selection of these polymers for further formulation development and clinical applications