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https://www.readbyqxmd.com/read/28627455/gemcitabine-vitamin-e-conjugates-synthesis-characterization-entrapment-into-nanoemulsions-and-in-vitro-deamination-and-antitumor-activity
#1
Ahmed Abu-Fayyad, Sami Nazzal
Gemcitabine is the first line therapy for pancreatic cancer. It is, however, extensively metabolized to the inactive form by deamination enzymatic reaction. Conjugation of gemcitabine with fatty acids on its 4-amino group was found to protect it from deamination deactivation reaction. The objective of the present study was to test the in-vitro anticancer activity of gemcitabine conjugated to the γ-tocotrienol isomer of vitamin E against pancreatic tumor cells. This objective was based on reported studies in which it was demonstrated that free tocotrienol isomers of vitamin E can potentiate the anticancer activity of gemcitabine...
June 13, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28622558/photodynamic-therapy-treatment-of-onychomycosis-with-aluminium-phthalocyanine-chloride-nanoemulsions-a-proof-of-concept-clinical-trial
#2
Luciano Ferreira Morgado, Ana Regina Franchi Trávolo, Luís Alexandre Muehlmann, Paulo Souza Narcizo, Rodrigo Barbosa Nunes, Pedro Alencar Gomes Pereira, Karen Rapp Py-Daniel, Cheng-Shi Jiang, Jinsong Gu, Ricardo Bentes Azevedo, João Paulo Figueiró Longo
The conventional treatment of onychomycosis, a common fungal infection, consists in the use of local and systemic drugs for 4-6 months. This long protocol is often ineffective due to patient compliance, and usually promotes important collateral effects such as liver and kidney failure. As the alternative, Photodynamic Therapy (PDT) has been used as a noninvasive alternative local treatment for onychomycosis due to the reduction of systemic side effects, fact indicates their use for patients undergoing other systemic treatments...
June 8, 2017: Journal of Photochemistry and Photobiology. B, Biology
https://www.readbyqxmd.com/read/28616962/size-dependent-translocation-of-nanoemulsions-via-oral-delivery
#3
Fei Xia, Wufa Fan, Sifan Jiang, Yuhua Ma, Yi Lu, Jianping Qi, Ejaj Ahmad, Xiaochun Dong, Weili Zhao, Wei Wu
The in vivo translocation of nanoemulsions was tracked by imaging tools with emphasis on the size effect. To guarantee accurate identification of nanoemulsions in vivo, water-quenching environment-responsive near-infrared fluorescent probes were used to label nanoemulsions. Imaging evidence confirms prominent digestion in gastrointestinal tract and oral absorption of integral nanoemulsions that survive digestion by enteric epithelia in a size-dependent way. In general, reducing particle size leads to slowed in vitro lipolysis and in vivo digestion, prolonged lifetime in small intestine, increased enteric epithelial uptake, and enhanced transportation to various organs...
June 15, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28605186/synthesis-of-oil-laden-poly-ethylene-glycol-diacrylate-hydrogel-nanocapsules-from-double-nanoemulsions
#4
Mengwen Zhang, Maksymilian Nowak, Paula Malo de Molina, Michael Abramovitch, Katherine Santizo, Samir Mitragotri, Matthew E Helgeson
Multiple emulsions have received great interest due to their ability to be used as templates for the production of multicompartment particles for a variety of applications. However, scaling these complex droplets to nanoscale dimensions has been a challenge due to limitations on their fabrication methods. Here, we report the development of oil-in-water-in-oil (O1/W/O2) double nanoemulsions via a two-step high-energy method and their use as templates for complex nanogels comprised of inner oil droplets encapsulated within a hydrogel matrix...
June 12, 2017: Langmuir: the ACS Journal of Surfaces and Colloids
https://www.readbyqxmd.com/read/28604104/intranasal-delivery-of-quercetin-loaded-mucoadhesive-nanoemulsion-for-treatment-of-cerebral-ischaemia
#5
Niyaz Ahmad, Rizwan Ahmad, Atta Abbas Naqvi, Md Aftab Alam, Mohammad Ashafaq, Rehan Abdur Rub, Farhan Jalees Ahmad
BACKGROUND: Quercetin (QUR), as an antioxidant flavonoid, exhibits potential role in the amelioration of cerebral ischaemia; however, poor solubility as well as oral absorption results low serum and tissue levels for this drug. PURPOSE OF THE STUDY: To enhance bioavailability, this study aims to prepare QUR nanoemulsions and administer via non-invasive nasal route in order to evaluate the drug targeting in brain. METHODS: Quercetin mucoadhesive nanoemulsion (QMNE) was prepared (ionic gelation method) and optimized using various parameters, that is, particle size, entrapment efficiency, zeta potential and ex vivo permeation study...
June 12, 2017: Artificial Cells, Nanomedicine, and Biotechnology
https://www.readbyqxmd.com/read/28603605/phase-behavior-of-mixed-lipid-monolayers-on-perfluorocarbon-nanoemulsions-and-its-effect-on-acoustic-contrast
#6
Rajarshi Chattaraj, Galen M Goldscheitter, Adem Yildirim, Andrew P Goodwin
Lipid-stabilized nanoemulsions containing a volatile liquid perfluorocarbon core have been studied as ultrasound contrast agents owing to their ability to transform into high-contrast microbubbles when subjected to high intensity focused ultrasound (HIFU). However, while there have been several studies on the effect of acoustic parameters on contrast, the effect of the droplet's stabilizing shell has not been studied as extensively. Inspired by previous studies showing lateral phase separation in microbubbles and vesicles, nanodroplets were formulated with a perfluorohexane core and a shell composed of varying amounts of saturated (DPPC) phospholipids, unsaturated (DOPC) phospholipids, and cholesterol, which were fractionated to obtain nanodroplets of mean diameter 300-400 nm and were stable over one week...
December 4, 2016: RSC Advances
https://www.readbyqxmd.com/read/28599959/photodynamic-process-induced-by-chloro-aluminum-phthalocyanine-nanoemulsion-in-glioblastoma
#7
Andrielle Castilho-Fernandes, Tácila G Lopes, Fernando L Primo, Marcelo R Pinto, Antonio C Tedesco
BACKGROUND: Glioblastoma multiforme (GBM) is a tumor characterized by rapid cell proliferation and migration. GBM constitutes the most aggressive and deadly type of brain tumor and is classified into several subtypes that show high resistance to conventional therapies. There are currently no curative treatments for malignant glioma despite the numerous advances in surgical techniques, radiotherapy, and chemotherapy. Therefore, alternative approaches are required to improve GBM treatment...
June 6, 2017: Photodiagnosis and Photodynamic Therapy
https://www.readbyqxmd.com/read/28597364/potential-application-of-nanoemulsions-for-skin-delivery-of-pomegranate-peel-polyphenols
#8
Thaisa Baccarin, Elenara Lemos-Senna
Pomegranate peel and seeds have demonstrated to possess antioxidant compounds with potential application to protect the skin against the ultraviolet radiation damage. However, the photoprotection activity is dependent on the amount of these compounds that reach the viable skin layers. In this paper, we describe the in vitro skin permeation and retention of the major pomegranate peel polyphenols using Franz diffusion cells, after entrapping a ethyl acetate fraction (EAF) from Punica granatum peel extract into nanoemulsions (NEs) prepared with pomegranate seed oil (PSO) or medium chain triglyceride oil (MCT)...
June 8, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28596014/designing-food-structure-and-composition-to-enhance-nutraceutical-bioactivity-to-support-cancer-inhibition
#9
REVIEW
David Julian McClements, Hang Xiao
Many types of bioactive molecules found in foods ("nutraceuticals") have been shown to exert anticancer activities, including curcumin, resveratrol, polyphenols, sulforaphane, anthocyanins, genistein, quercetin and lycopene. The potential health benefits of nutraceuticals are often not realized because of their poor water solubility, chemical instability, adverse taste profile, and low oral bioavailability. Carefully designed food matrices are being developed to overcome these problems. Nutraceuticals can be isolated from their natural environment, and then incorporated into functional foods, often with the help of delivery systems (such as emulsions, nanoemulsions, liposomes, biopolymer nanoparticles, and microgels)...
June 5, 2017: Seminars in Cancer Biology
https://www.readbyqxmd.com/read/28590938/combined-passive-acoustic-mapping-and-magnetic-resonance-thermometry-for-monitoring-phase-shift-nanoemulsion-enhanced-focused-ultrasound-therapy
#10
Calum Crake, F Can Meral, Mark Burgess, Iason Papademetriou, Nathan McDannold, Tyrone Porter
Focused ultrasound (FUS) has the potential to enable precise, image-guided noninvasive surgery for the treatment of cancer in which tumors are identified and destroyed in a single integrated procedure. However, success of the method in highly vascular organs has been limited due to heat losses to perfusion, requiring development of techniques to locally enhance energy absorption and heating. In addition, FUS procedures are conventionally monitored using MRI, which provides excellent anatomical images and can map temperature, but is not capable of capturing the full gamut of available data such as the acoustic emissions generated during this inherently acoustically-driven procedure...
June 7, 2017: Physics in Medicine and Biology
https://www.readbyqxmd.com/read/28585133/therapeutic-effects-of-curcumin-nanoemulsions-on-prostate-cancer
#11
Yan-Bin Guan, Shu-Yao Zhou, Yu-Qiong Zhang, Jia-le Wang, Yu-Dong Tian, Yong-Yan Jia, Yan-Jun Sun
The therapeutic potential of curcumin (Cur) is hampered by its poor aqueous solubility and low bioavailability. The aim of this study was to determine whether Cur nanoemulsions enhance the efficacy of Cur against prostate cancer cells and increase the oral absorption of Cur. Cur nanoemulsions were developed using the self-microemulsifying method and characterized by their morphology, droplet size and zeta potential. The results showed that the cytotoxicity and cell uptake were considerably increased with Cur nanoemulsions compared to free Cur...
June 2017: Journal of Huazhong University of Science and Technology. Medical Sciences
https://www.readbyqxmd.com/read/28583444/nanomedicine-for-prostate-cancer-using-nanoemulsion-a-review
#12
REVIEW
Aravindsiva Sasikumar, Kaladhar Kamalasanan
Prostate cancer (PCa) is a worldwide issue, with burgeoning rise in prevalence, morbidity and mortality. Targeted drug delivery, a long sort solution in this regard using controlled release (CR) - nanocarriers, is still a challenge. There is an emerging criticism that, the challenges are due to less appreciation for the biological barriers and lack of corresponding newer technologies. Over the years, more understanding about the biological barriers has come with the progress in characterization techniques. Correspondingly, there is a change in opinion about approaches in clinical trial that; focus of the end point need to be shifted towards disease stabilization for these explorative technologies...
June 2, 2017: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/28572727/organic-effects-of-associating-paclitaxel-with-a-lipid-based-nanoparticle-system-on-a-nonhuman-primate-cebus-apella
#13
Danielle Cristinne Azevedo Feio, Nayara Cristina Lima de Oliveira, Edmundo Luis Rodrigues Pereira, Aleksandra Tiemi Morikawa, José Augusto Pereira Carneiro Muniz, Raquel Carvalho Montenegro, Ana Paula Negreiros Nunes Alves, Patrícia Danielle Lima de Lima, Raul Cavalcante Maranhão, Rommel Rodríguez Burbano
Lipid-based nanoparticle systems have been used as vehicles for chemotherapeutic agents in experimental cancer treatments. Those systems have generally been credited with attenuating the severe toxicity of chemotherapeutic agents. This study aimed to investigate the effects of associating paclitaxel (PTX) with a lipid-based nanoparticle system on a nonhuman primate, Cebus apella, documenting the toxicity as measured by serum biochemistry, which is a detailed analysis of blood and tissue. Eighteen C. apella were studied: three animals were treated with cholesterol-rich nanoemulsion (LDE) only, without PTX, administered intravenously every 3 weeks, during six treatment cycles; six animals were treated with PTX associated with LDE at the same administration scheme, three with lower (175 mg/m(2)) and three with higher (250 mg/m(2)) PTX doses; and six animals were treated with commercial PTX, three with the lower and three with the higher doses...
2017: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/28571549/nanoemulsion-based-transdermal-drug-delivery-system-for-the-treatment-of-tuberculosis
#14
Mohammad Wais, Mohd Aqil, Ashish Kumar Sharma, Jaya Agnihotri
BACKGROUND: The nanoemulsion based carriers are the most suitable delivery systems for poorly soluble drugs to improve the solubility of drugs, permeation of drugs and ultimately increase bioavailability by transdermal therapeutic system. The nanoemulsion for poorly soluble drugs is the excellent and offered several advantages over others carriers. METHODS: For the nanoemulsions formulation they have to deliver the energetic element at the specific organ with nominal uneasiness...
June 1, 2017: Recent Patents on Anti-infective Drug Discovery
https://www.readbyqxmd.com/read/28562041/preparation-and-characterization-of-controlled-release-avermectin-castor-oil-based-polyurethane-nanoemulsions
#15
Hong Zhang, He Qin, Lingxiao Li, Xiaoteng Zhou, Wei Wang, Chengyou Kan
Avermectin (AVM) is a low-toxic and high-active biopesticide, but it can be easily degraded by UV light. In this paper, biodegradable castor oil-based polyurethanes (CO-PU) are synthesized and used as carriers to fabricate a new kind of AVM/CO-PU nanoemulsion through an emulsion solvent evaporation method, and the chemical structure, colloidal property, AVM loading capacity, controlled-release behavior, foliar adhesion, and photostability of the AVM/CO-PU drug delivery systems are investigated. Results show that AVM is physically encapsulated in the CO-PU carrier nanospheres, the diameter of the AVM/CO-PU nanoparticles is <50 nm, and the AVM/CO-PU films are flat and smooth without any AVM aggregate...
June 12, 2017: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/28561230/enhancement-of-quercetin-oral-bioavailability-by-self-nanoemulsifying-drug-delivery-system-and-their-quantification-through-ultra-high-performance-liquid-chromatography-and-mass-spectrometry-in-cerebral-ischemia
#16
Niyaz Ahmad, Rizwan Ahmad, Atta Abbas Naqvi, Md Aftab Alam, Rehan Abdur Rub, Farhan Jalees Ahmad
Background Quercetin (Qur) and its major in vivo bioactive metabolites i. e., 3'-O-methyl quercetin, 4'-O-methyl quercetin and quercetin 7-O-β-D-glucuronide, may be used to treat cerebral ischemia however the poor aqueous solubility and less intestinal absorption of Qur results low bioavailability. Purpose To improve Qur bioavailability through preparation of nanoformulation and to develop and validate a sensitive quantification method for Qur detection in brain homogenate. Methods Qur-containing self-nanoemulsifying drug delivery system (Qur-SNEDDS) was developed to form oil-in-water nanoemulsions in situ...
May 23, 2017: Drug Research
https://www.readbyqxmd.com/read/28559042/self-assembled-core-shell-type-lipid-polymer-hybrid-nanoparticles-intracellular-trafficking-and-relevance-for-oral-absorption
#17
Qiuxia Li, Dengning Xia, Jinsong Tao, Aijun Shen, Yuan He, Yong Gan, Chi Wang
Lipid-polymer hybrid nanoparticles (NPs) are advantageous for drug delivery. However, their intracellular trafficking mechanism and relevance for oral drug absorption are poorly understood. In this study, self-assembled core-shell lipid-polymer hybrid NPs made of PLGA and various lipids were developed to study their differing intracellular trafficking in intestinal epithelial cells, and their relevance for oral absorption of a model drug saquinavir (SQV). Our results demonstrated that the endocytosis and exocytosis of hybrid NPs could be changed by varying the kind of lipid...
May 27, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28552767/parenteral-nanoemulsions-of-risperidone-for-enhanced-brain-delivery-in-acute-psychosis-physicochemical-and-in-vivo-performances
#18
Sanela M Đorđević, Anja Santrač, Nebojša D Cekić, Bojan D Marković, Branka Divović, Tanja M Ilić, Miroslav M Savić, Snežana D Savić
This work aimed to deepen the lately acquired knowledge about parenteral nanoemulsions as carriers for brain delivery of risperidone, a poorly water-soluble antipsychotic drug, through establishing the prospective relationship between their physicochemical, pharmacokinetic, biodistribution, and behavioral performances. For this purpose, two optimized risperidone-loaded nanoemulsions, stabilized by lecithin or lecithin/polysorbate 80 mixture, and costabilized by sodium oleate, were produced by high-pressure homogenization...
May 25, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28551576/light-triggered-release-from-dye-loaded-fluorescent-lipid-nanocarriers-in-vitro-and-in-vivo
#19
Redouane Bouchaala, Nicolas Anton, Halina Anton, Thierry Vandamme, Julien Vermot, Djabi Smail, Yves Mély, Andrey S Klymchenko
Light is an attractive trigger for release of active molecules from nanocarriers in biological systems. Here, we describe a phenomenon of light-induced release of a fluorescent dye from lipid nano-droplets under visible light conditions. Using auto-emulsification process we prepared nanoemulsion droplets of 32nm size encapsulating the hydrophobic analogue of Nile Red, NR668. While these nano-droplets cannot spontaneously enter the cells on the time scale of hours, after illumination for 30s under the microscope at the wavelength of NR668 absorption (535nm), the dye showed fast accumulation inside the cells...
May 15, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/28545970/chitosan-stabilized-camptothecin-nanoemulsions-development-evaluation-and-biodistribution-in-preclinical-breast-cancer-animal-mode
#20
Subramanian Natesan, Abimanyu Sugumaran, Chandrasekar Ponnusamy, Vignesh Thiagarajan, Rajaguru Palanichamy, Ruckmani Kandasamy
Clinical use of camptothecin (CPT) is hindered due to its poor water and oil solubility, active lactone ring instability and non-targeted toxicity. Recently we reported formulation of camptothecin microemulsions with increased solubility for the improved treatment of breast cancer. In this research chitosan stabilized camptothecin nanoemulsions (CHI-CPT-NEs) were formulated improve the cancer targeting efficiency of CPT. The developed NEs were characterized for their droplet size distribution, stability in plasma and evaluated for in-vitro drug release, in-vivo targeting potential, in-vitro hemolytic potential, cytotoxicity, genotoxicity and in-vivo biodistribution...
May 22, 2017: International Journal of Biological Macromolecules
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