Rubusoside-assisted solubilization of poorly soluble C6-Ceramide for a pilot pharmacokinetic study

In this study we explored the use of a natural compound rubusoside (RUB) as a solubilizer to enhance the solubility of a fluorescence-labeled C6-Ceramide (NBD C6-Ceramide) and to characterize its pharmacokinetics and tissue distribution in an animal model. RUB significantly enhanced the solubility of NBD C6-Ceramide by forming nanomicelles, and efficiently delivered NBD C6-Ceramide in rats by oral and intravenous administration. RUB loaded 1.96% of NBD C6-Ceramide in the nanomicelles and solubilized it to a concentration of 3.6 mg/mL in water. NBD C6-Ceramide in nanomicelles remained stable in aqueous solutions, allowing intravenous administration without the use of any organic solvents or surfactants. After oral administration, NBD C6-Ceramide rapidly rose to peak plasma concentrations within the first 90 min, distributed to tissues, and remained in vivo for more than 24 hours. Tissular levels of NBD C6-Ceramide from high to low were associated with heart, lung, cerebellum, testicle, spleen, liver, kidney, and brain. Altogether, our study demonstrated that RUB-assisted nanomicelles can serve as an efficient and convenient delivery system for short-chain C6-Ceramide and enable in vivo evaluation of potential new cancer treatments.Graphic AbstractNatural rubusoside (RUB) efficiently encapsulates NBD C6-Ceramide, a short chain ceramide to form RUB-assisted nanomicelles (∼29 nm) in aqueous solution. This novel nanomicelles can make water insoluble...
Source: Prostaglandins and Other Lipid Mediators - Category: Lipidology Source Type: research

Related Links:

Publication date: Available online 22 January 2020Source: The Lancet NeurologyAuthor(s): Jeremy Chataway, Floriana De Angelis, Peter Connick, Richard A Parker, Domenico Plantone, Anisha Doshi, Nevin John, Jonathan Stutters, David MacManus, Ferran Prados Carrasco, Frederik Barkhof, Sebastien Ourselin, Marie Braisher, Moira Ross, Gina Cranswick, Sue H Pavitt, Gavin Giovannoni, Claudia Angela Gandini Wheeler-Kingshott, Clive Hawkins, Basil SharrackSummaryBackgroundNeurodegeneration is the pathological substrate that causes major disability in secondary progressive multiple sclerosis. A synthesis of preclinical and clinical re...
Source: The Lancet Neurology - Category: Neurology Source Type: research
This study provides strong evidence that following a healthy lifestyle can substantially extend the years a person lives disease-free." Commentary on Recent Evidence for Cognitive Decline to Precede Amyloid Aggregation in Alzheimer's Disease https://www.fightaging.org/archives/2020/01/commentary-on-recent-evidence-for-cognitive-decline-to-precede-amyloid-aggregation-in-alzheimers-disease/ I can't say that I think the data presented in the research noted here merits quite the degree of the attention that it has been given in the popular science press. It is interesting, but not compelling if its role...
Source: Fight Aging! - Category: Research Authors: Tags: Newsletters Source Type: blogs
CONCLUSIONS: GDC-0084 demonstrated classic PI3K/mTOR-inhibitor related toxicities. FDG-PET and concentration data from brain tumor tissue suggest that GDC-0084 crossed the blood-brain barrier. PMID: 31937616 [PubMed - as supplied by publisher]
Source: Clinical Cancer Research - Category: Cancer & Oncology Authors: Tags: Clin Cancer Res Source Type: research
This study presents the effects of berberine (BBR) on the aging process resulting in a promising extension of lifespan in model organisms. BBR extended the replicative lifespan, improved the morphology, and boosted rejuvenation markers of replicative senescence in human fetal lung diploid fibroblasts. BBR also rescued senescent cells with late population doubling (PD). Furthermore, the senescence-associated β-galactosidase (SA-β-gal)-positive cell rates of late PD cells grown in the BBR-containing medium were ~72% lower than those of control cells, and its morphology resembled that of young cells. Mechanistically...
Source: Fight Aging! - Category: Research Authors: Tags: Newsletters Source Type: blogs
Publication date: Available online 12 November 2019Source: Colloids and Surfaces B: BiointerfacesAuthor(s): Suma Saad, Iqbal Ahmad, Syed M. Kawish, Urooj A. Khan, Farhan J. Ahmad, Asgar Ali, Gaurav K. JainAbstractDoxorubicin (DOX) is commonly used for the treatment of many types of cancers but its cardiotoxicity, owing to free radical formation, limits its clinical use. Hesperidin (HES), a flavanone glycoside, has been shown to exert multiple pharmacological actions including cardioprotective effects. Herein, we aim to formulate HES loaded solid lipid nanoparticles (SLNs) using supercritical antisolvent (SAS) technology to...
Source: Colloids and Surfaces B: Biointerfaces - Category: Biochemistry Source Type: research
The dangers of alcohol begin at the first sip of the first drink. Although most responsible drinking habits shouldn’t be cause for major concern, everyone who drinks runs the risk of encountering the negative effects of alcohol. The Dietary Guidelines for Americans defines moderate drinking as up to 1 drink per day for women and up to 2 drinks per day for men.  A single drink is considered as: 12 ounces of beer (5% alcohol content) 8 ounces of malt liquor (7% alcohol content) 5 ounces of wine (12% alcohol content) 1.5 ounces of 80-proof (40% alcohol content) distilled spirits or liquor (e.g., gin, rum, vodka, ...
Source: Cliffside Malibu - Category: Addiction Authors: Tags: Alcohol Alcohol Rehab Information Alcoholism alcohol abuse alcohol dependence alcohol dependency alcohol detox alcohol treatment alcohol treatment center alcohol treatment facility Alcoholics Anonymous Source Type: blogs
Measuring lipid and glutamine levels predicts how fast a tumour will grow Related items fromOnMedica Sentinel node biopsy first to check spread of oral cancer NHS annual cancer checks top two million Cancer research funding boost following death of Tessa Jowell Nanoparticle drug delivery system could help fight brain cancer Men ’s dementia risk higher after androgen deprivation therapy
Source: OnMedica Latest News - Category: UK Health Source Type: news
In this study, by adenovirus-mediated delivery and inducible transgenic mouse models, we demonstrate the proliferation of both HCs and SCs by combined Notch1 and Myc activation in in vitro and in vivo inner ear adult mouse models. These proliferating mature SCs and HCs maintain their respective identities. Moreover, when presented with HC induction signals, reprogrammed adult SCs transdifferentiate into HC-like cells both in vitro and in vivo. Finally, our data suggest that regenerated HC-like cells likely possess functional transduction channels and are able to form connections with adult auditory neurons. Epige...
Source: Fight Aging! - Category: Research Authors: Tags: Newsletters Source Type: blogs
UCLA began observing its 100th birthday this year and delivered new  advances in research, health care, the arts, community service and teaching. These are some of the top stories from UCLA Newsroom in 2019 — those which made news and engaged the community of Bruins and beyond.UCLA Newsroom will resume publishing on Jan. 2, 2020. For more, be sure toperuse the archives and to followUCLA Newsroom on Twitter. UCLA turns 100UCLA ArchiveUCLA from overhead in the 1930s.Founders of UCLA would marvel at their creationIn just 100 years, UCLA has grown into a respected center of learning, research and health ca...
Source: UCLA Newsroom: Health Sciences - Category: Universities & Medical Training Source Type: news
Abstract PURPOSE: Pediatric low-grade glioma (pLGG) is the most prevalent childhood brain tumor. Patients with BRAF V600 mutation-positive pLGG may benefit from treatment with dabrafenib. Part 2 of a phase I/IIa study, open-label study (NCT01677741) explores the activity and safety of dabrafenib treatment in these patients. PATIENTS AND METHODS: Patients ages 1 to
Source: Clinical Cancer Research - Category: Cancer & Oncology Authors: Tags: Clin Cancer Res Source Type: research
More News: Brain | Brain Cancers | Cancer | Cancer & Oncology | Cardiology | Cerebellum | Heart | Lipidology | Liver | Nanotechnology | Neurology | Oral Cancer | Organic | Study | Urology & Nephrology