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Danieli Urach Monteiro, Maria Isabel Azevedo, Carla Weiblen, Sônia DE Avila Botton, Nadine Lysyk Funk, Cristiane DE Bona DA Silva, Régis Adriel Zanette, Thiago Guilherme Schwanz, Mário Luiz DE LA Rue
Cystic echinococcosis is a zoonotic disease of difficult diagnosis and treatment. The use of protoscolicidal agents in procedures is of utmost importance for treatment success. This study was aimed at analysing the in vitro and ex vivo activity of Melaleuca alternifolia oil (tea tree oil - TTO), its nanoemulsion formulation (NE-TTO) and its major component (terpinen-4-ol) against Echinococcus ortleppi protoscoleces obtained from cattle. Concentrations of 2·5, 5 and 10 mg mL-1 of TTO, 10 mg mL-1 of NE-TTO and 1, 1·5 and 2 mg mL-1 of terpinen-4-ol were evaluated in vitro against protoscoleces at 5, 10, 15 and 30 min...
October 20, 2016: Parasitology
Sun-Hyung Kim, Yeun-Sun Ji, Eui-Seok Lee, Soon-Taek Hong
Curcumin is a flavonoid found in the rhizome of the turmeric plant (Curcuma longa L.) and has recently attracted interest because it has numerous biological functions and therapeutic properties. In the present study, we attempted to incorporate curcumin into medium-chain triglyceride (MCT) nanoemulsions (0.15 wt% curcumin, 10 wt% MCT oil, and 10 wt% emulsifiers) with various emulsifiers [polyoxyethylene (20) sorbitan monolaurate (Tween-20), sorbitan monooleate (SM), and soy lecithin (SL)]. The physicochemical properties of the nanoemulsions including the Ostwald ripening stability were investigated...
September 2016: Preventive Nutrition and Food Science
Yanan Gao, Xuejing Qi, Yiping Zheng, Hongyu Ji, LinhuaWu, Nannan Zheng, Jingling Tang
The vitamin E analogue, α-tocopherol succinate (α-TOS), has a broad anti-tumor effect. α-TOS can induce cancer cells apoptosis and suppress tumor growth by targeting mitochondria. Low bioavailability of α-TOS is the major problem encountered with formulation development. In our study, α-TOS nanoemulsion (α-TOS-NE) was demonstrated as a new drug delivery system of α-TOS to increase the bioavailability. MTT-based cytotoxicity assay and mitochondrial membrane potential (ΔY) were performed on human breast cancer cell lines MCF-7 and human oral epithelial cancer cell lines KB to evaluate in vitro anticancer efficacy of α-TOS-NE...
October 13, 2016: International Journal of Pharmaceutics
Matteo Ciocci, Egidio Iorio, Felicia Carotenuto, Haneen A Khashoggi, Francesca Nanni, Sonia Melino
The improvement of solubility and/or dissolution rate of poorly soluble natural compounds is an ideal strategy to make them optimal candidates as new potential drugs. Accordingly, the allyl sulfur compounds and omega-3 fatty acids are natural hydrophobic compounds that exhibit two important combined properties: cardiovascular protection and antitumor activity. Here, we have synthesized and characterized a novel formulation of diallyl disulfide (DADS) and α-linolenic acid (ALA) as protein-nanoemulsions (BAD-NEs), using ultrasounds...
October 12, 2016: Oncotarget
Ankur Gupta, Vivek Narsimhan, T Alan Hatton, Patrick S Doyle
The evolution of droplet size during nanoemulsion formation is critical for the ra- tional design of nanoemulsions in areas such as drug delivery and materials synthesis. In this article, we discuss the relative importance of various time scales involved in nanoemulsion formation and propose a population balance model for droplet breakup that takes into account the droplet's internal viscosity. The proposed model gives a qualitative agreement with average droplet size and polydispersity data for nanoemul- sions prepared by high pressure homogenization and ultrasonication...
October 11, 2016: Langmuir: the ACS Journal of Surfaces and Colloids
Éverton da Silva Santos, Francielle Pelegrin Garcia, Priscila Miyuki Outuki, Jaqueline Hoscheid, Paulo Roberto Nunes de Goes, Lúcio Cardozo-Filho, Celso Vataru Nakamura, Mara Lane Carvalho Cardoso
Currently, leishmaniasis is difficult to manage owing to the limited choice and high toxicity of available drugs, and emergence of drug-resistant protozoa. Medicinal plants, which produce various bioactive molecules, can help counter this global shortage. In this study, we prepared Pterodon pubescens fruit extracts, which show antileishmanial activity, and developed a nanoemulsion of the optimized extract to improve its performance. The extracts were prepared using conventional methods and a supercritical fluid method and were tested for activity against Leishmania amazonensis promastigotes and amastigotes...
October 7, 2016: Experimental Parasitology
Michelle Y Chan, Dawn M Fedor, Tony Phan, Lucien Barnes V, Ryan M Kramer
Determining the association of vaccine components in a formulation is of interest for designing and optimizing well characterized vaccines. Three methods are described to assess interactions between protein antigens and oil-in-water nanoemulsion adjuvants. The methods include (1) ultracentrifugation to measure free versus adjuvant-associated protein, (2) size exclusion chromatography (SEC) to qualitatively assess existing interactions, and (3) Native PAGE as a means to visualize the formulation run in its native state on a polyacrylamide gel...
2017: Methods in Molecular Biology
Alicia M Schwartz, Michelle Y Chan, Dawn M Fedor, Sandra J Sivananthan, Ryan M Kramer
Adjuvants in modern vaccines boost and shape immune responses and allow for antigen dose-sparing. Analysis of protein antigens in the presence of adjuvants can prove challenging, especially if the adjuvant interferes with visualization of the protein band on an SDS-PAGE gel. In this chapter, a variety of different techniques are presented to mitigate the interference of a nanoemulsion adjuvant, GLA-SE, with different recombinant proteins of varying molecular weight by addressing sample preparation and staining methods...
2017: Methods in Molecular Biology
Michelle Y Chan, Quinton M Dowling, Sandra J Sivananthan, Ryan M Kramer
Dynamic light scattering (DLS) and nanoparticle tracking analysis (NTA) are two orthogonal and complementary methods of measuring size of particles in a sample. These technologies use the theory of Brownian motion by analyzing the random changes of light intensity scattered by particles in solution. Both techniques can be used to characterize particle size distribution of proteins and formulations in the nanometer to low micron range.Each method has benefits over the other. DLS is a quick and simple measurement that is ideal for monodisperse particles and can also analyze a distribution of particles over a wide range of sizes...
2017: Methods in Molecular Biology
Doris Hinger, Susanna Gräfe, Fabrice Navarro, Bernhard Spingler, Devaraj Pandiarajan, Heinrich Walt, Anne-Claude Couffin, Caroline Maake
BACKGROUND: Photodynamic therapy (PDT) as promising alternative to conventional cancer treatments works by irradiation of a photosensitizer (PS) with light, which creates reactive oxygen species and singlet oxygen ((1)O2), that damage the tumor. However, a routine use is hindered by the PS's poor water solubility and extended cutaneous photosensitivity of patients after treatment. In our study we sought to overcome these limitations by encapsulation of the PS m-tetrahydroxyphenylchlorin (mTHPC) into a biocompatible nanoemulsion (Lipidots)...
October 3, 2016: Journal of Nanobiotechnology
Kartika Pidaparthi, Divya Suares
The objective of the study was to develop and compare the efficiency of nanoemulsion and aqueous micelle system of Paliperidone on intranasal administration. Both the formulations were evaluated for physical parameters such as globule size, pH, viscosity, conductivity and in vitro drug release studies. The reduction in spontaneous motor activity of L-dopa and Carbidopa-treated Swiss Albino mice on intranasal administration of nanoemulsion and micellar system of Paliperidone was compared with plain drug suspension...
October 6, 2016: AAPS PharmSciTech
Laura De Matteis, Maria Alleva, Inés Serrano-Sevilla, Sonia García-Embid, Grazyna Stepien, María Moros, Jesús M de la Fuente
The tunability of the properties of chitosan-based carriers opens new ways for the application of drugs with low water-stability or high adverse effects. In this work, the combination of a nanoemulsion with a chitosan hydrogel coating and the following poly (ethylene glycol) (PEG) grafting is proven to be a promising strategy to obtain a flexible and versatile nanocarrier with an improved stability. Thanks to chitosan amino groups, a new easy and reproducible method to obtain nanocapsule grafting with PEG has been developed in this work, allowing a very good control and tunability of the properties of nanocapsule surface...
September 30, 2016: Marine Drugs
Viorel Simion, Cristina Ana Constantinescu, Daniela Stan, Mariana Deleanu, Monica Madalina Tucureanu, Elena Butoi, Ileana Manduteanu, Maya Simionescu, Manuela Calin
Inflammation is a common process associated with numerous vascular pathologies. We hypothesized that targeting the inflamed endothelium by coupling a peptide with high affinity for P-selectin to the surface of dexamethasone-loaded lipid nanoemulsions will highly increase their specific binding to activated endothelial cells (EC) and reduce the cell activation. We developed and characterized dexamethasone-loaded lipid nanoemulsions directed towards P-selectin (PLN-Dex) and monitored their anti-inflammatory effects in vitro using cultured EC (EA...
2016: Mediators of Inflammation
Nirav Patel, Happy Nakrani, Mihir Raval, Navin Sheth
A novel cationic nanoemulsified in-situ ophthalmic gel of loteprednol etabonate (LE) was developed to improve the permeability and retention time of formulations for overall improvement of drug's ocular bioavability. Capryol 90 (oil phase), tween 80 (surfactant) and transcutol P (cosurfactant) was selected as formulation excipients to construct pseudoternary phase diagrams and nanoemulsion region was recognized from diagrams. Spontaneous emulsification method was used to manufacture LE nanoemulsion and it was optimized using 3(2) factorial design by considering the amount of oil and the ratio of surfactant to cosurfactant (Smix) as independent variables and evaluated for various physicochemical properties...
September 30, 2016: Drug Delivery
Vianney Díaz-Blancas, Dora I Medina, Erika Padilla-Ortega, Raquel Bortolini-Zavala, Melissa Olvera-Romero, Gabriel Luna-Bárcenas
Tebuconazole (TBZ) nanoemulsions (NEs) were formulated using a low energy method. TBZ composition directly affected the drop size and surface tension of the NE. Water fraction and the organic-to-surfactant-ratio (RO/S) were evaluated in the range of 1-90 and 1-10 wt %, respectively. The study was carried out with an organic phase (OP) consisting of an acetone/glycerol mixture containing TBZ at a concentration of 5.4 wt % and Tween 80 (TW80) as a nonionic and Agnique BL1754 (AG54) as a mixture of nonionic and anionic surfactants...
2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Abeer Khattab, Lobna Hassanin, Nashwah Zaki
The aim of our investigation is to develop and characterize self-nanoemulsifying drug delivery systems (SNEDDS) of CoQ10 to improve its water solubility, dissolution rate, and bioavailability, and then evaluate its biochemical and physiological effect on liver cirrhosis in rats compared with CoQ10 powder. SNEDDS are isotropic and thermodynamically stable mixture of oil, surfactant, co-surfactant, and drug that form an oil/water nanoemulsion when added to aqueous phases with soft agitation. Upon administration, self-nanoemulsifying system becomes in contact with gastrointestinal fluid and forms o/w nanoemulsion by the aid of gastrointestinal motility...
September 27, 2016: AAPS PharmSciTech
Mariem Ben Jemaa, Hanen Falleh, Marcos A Neves, Hiroko Isoda, Mitsutoshi Nakajima, Riadh Ksouri
The objective of this study is to evaluate the effect of either a solution of Thymus capitatus essential oil or its nanoemulsion on the quality of milk contaminated by bacteria. After 24h of S. aureus inoculation, bacterial growth reached 202×10(3)CFU/ml in the presence of the essential oil while it was limited to 132×10(3)CFU/ml when treated with nanoemulsion. The reduction of antioxidant capacity of milk treated with essential oil was higher when treated with nanoemulsion. Moreover, free essential oil was more efficient in protecting proteins from degradation than the nanoemulsion...
February 15, 2017: Food Chemistry
Juarana Dal Mas, Tailyn Zermiani, Liliani C Thiesen, Joana Lm Silveira, Kathryn Abs da Silva, Márcia M de Souza, Angela Malheiros, Tania Mb Bresolin, Ruth M Lucinda-Silva
The aim of this study was to develop nanoemulsion containing soft extract of stem bark of Rapanea ferruginea to improve the topical delivery and anti-inflammatory activity. The extract of R. ferruginea stem bark was incorporated into the oily phase of the nanoemulsion by the method of phase inversion at low energy. The developed nanoemulsion had an average droplet size of 47.88±8.20 nm and a polydispersibility index of 0.228. Uniformity of size, spherical shape of droplet, and absence of clusters were confirmed by transmission electronic microscopy...
2016: International Journal of Nanomedicine
Pulkit Khatri, Jun Shao
The aim of this study is to develop a simple, reliable, timesaving and cost-effective method for separation of the external aqueous phase from o/w nanoemulsions. The method is based on centrifugation through a hydrophilic membrane. Five o/w nanoemulsions (droplet size of 20-200nm) with radio-labeled C18 triglyceride were prepared. These nanoemulsions were placed in tubes with cellulose membranes (10-50K molecular weight cut-off) and centrifuged at 250-3000g for 5-15min. The filtrates were analyzed for the presence of lipid droplets and radioactivity...
September 16, 2016: European Journal of Pharmaceutical Sciences
Afonso A Shiozaki, Tiago Senra, Aleksandra T Morikawa, Débora F Deus, Antonio T Paladino-Filho, Ibraim M F Pinto, Raul C Maranhão
OBJECTIVE: The toxicity of anti-cancer chemotherapeutic agents can be reduced by associating these compounds, such as the anti-proliferative agent paclitaxel, with a cholesterol-rich nanoemulsion (LDE) that mimics the lipid composition of low-density lipoprotein (LDL). When injected into circulation, the LDE concentrates the carried drugs in neoplastic tissues and atherosclerotic lesions. In rabbits, atherosclerotic lesion size was reduced by 65% following LDE-paclitaxel treatment. The current study aimed to test the effectiveness of LDE-paclitaxel on inpatients with aortic atherosclerosis...
August 2016: Clinics
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