Effects of Lipids on in Vitro Release and Cellular Uptake of β-Carotene in Nanoemulsion-Based Delivery Systems

2015 ◽  
Vol 63 (50) ◽  
pp. 10831-10837 ◽  
Author(s):  
Jiang Yi ◽  
Fang Zhong ◽  
Yuzhu Zhang ◽  
Wallace Yokoyama ◽  
Liqing Zhao
2010 ◽  
Vol 13 (2) ◽  
pp. 286 ◽  
Author(s):  
Tailane Sant´Anna Moreira ◽  
Valéria Pereira De Sousa ◽  
Maria Bernadete Riemma Pierre

Abstract PURPOSE: Transdermal delivery of anti-inflammatory lumiracoxib (LM) could be an interesting strategy to avoid the side effects associated with systemic delivery, but it is ineffective due to the drug poor skin penetration. We have investigated the effects of oleic acid (OA), a lipid penetration enhancer, on the in vitro release of LM from poloxamer-based delivery systems (PBDS). The rheological behavior (shear rate dependent viscosity) and gelation temperature through measurements of optimal sol-gel transition temperatures (Tsol-gel) were also carried out in these systems. METHODS: In vitro release studies of LM from PBDS were performed using cellulose acetate as artificial membrane mounted in a diffusion system. The amount of LM released was divided by exposition area (µg/cm2) and these values were plotted as function of the time (h). The flux of the drug across the membrane (J) was calculated from the slope of the linear portion of the plot and expressed as µg/cm2. h -1. The determination of viscosity was carried out at different shear rates (γ) between 0.1- 1000 S-1 using a parallel plate rheometer. Oscillatory measurements using a cone-plate geometry rheometer surrounded by a double jacket with temperature varying 4-40°C, was used in order to determine Tsol-gel. RESULTS: Increase of both polymer and OA concentrations increases the viscosity of the gels and consequently reduces the in vitro LM release from the PBDS, mainly for gels containing OA at 10.0% compared to other concentrations of the penetration enhancer. Tsol-gel transition temperature was decreased by increasing viscosity; in some cases the formulation was already a gel at room temperature. Rheological studies showed a pseudoplastic behavior, which facilitates the flow and improves the spreading characteristics of the formulations. CONCLUSIONS: Taken together, the results showed that poloxamer gels are good potential delivery systems for LM, leading to a sustained release, and also have appropriate rheological characteristics. Novelty of the work: A transdermal delivery of non-steroidal antinflammatory drugs like lumiracoxib (LM) can be an interesting alternative to the oral route of this drug, since it was recently withdraw of the market due to the liver damage when systemically administered in tablets as dosage form. There are no transdermal formulations of LM and it could be an alternative to treat inflammation caused by arthritis or arthrosis. Then, an adequate delivery system to LM is necessary in order to release the drug properly from the PBDS as well as have good characteristics related to semi-solid preparations for transdermal application, which were evaluated through in vitro release studies and rheological behavior in this paper, respectively.


2015 ◽  
Vol 485 (1-2) ◽  
pp. 202-214 ◽  
Author(s):  
Maja Lusina Kregar ◽  
Marjana Dürrigl ◽  
Andrea Rožman ◽  
Želimir Jelčić ◽  
Biserka Cetina-Čižmek ◽  
...  

2012 ◽  
Vol 32 (11) ◽  
pp. 2679-2690 ◽  
Author(s):  
Hiva Baradari ◽  
Chantal Damia ◽  
Maggy Dutreih-Colas ◽  
Etienne Laborde ◽  
Nathalie Pécout ◽  
...  

2020 ◽  
Vol 10 (1) ◽  
Author(s):  
Ye Yuan ◽  
Jia-Xing Song ◽  
Mei-Na Zhang ◽  
Bao-Shan Yuan

Abstract Osteosarcoma is a malignant condition affecting adolescents and children more than adults. Nanobiomedicine has opened up several avenues which have increased therapeutic efficiencies than the conventional treatment for the same. In the current study, a novel organic nanoparticle was devised conjugated with bisphosphonate zoledronic acid which has an affinity for bone tissues. Moreover, the nanoparticle was loaded with multiple anti-cancer drugs like gemcitabine and epirubicin. The nanoparticles were characterized by microscopic analysis, entrapment and loading efficiencies, bone affinity studies, in-vitro release studies, cytotoxicity studies and finally in-vivo tumor regression studies. Bone affinity studies depicted a high affinity of zoledronic acid towards bone powder. The nanoparticle exhibited a nanosize dimension, high entrapment and loading efficiencies with uniform symmetry devoid of agglomeration. The in-vitro release experiments showed a measured release of drugs over a longer time without any hint of burst release. However, the release was comparatively for a longer duration in acidic pH and normal physiological pH which may be excellent for therapeutic efficiency. The cytotoxicity studies revealed enhanced cytotoxic effect for MG-63 cell lines in comparison of free drug or single drug combinations. Nonetheless, they proved to be cytocompatible with primary bone cells. Additionally, cellular uptake of nanoparticle was appreciably improved. Significant tumor (250%) regression was seen upon treatment with multiple drug loaded zoledronic acid conjugated nanoparticle, along with epigenetic changes affecting microRNA expressions. The increased cytotoxicity and increased cellular uptake may be of greater advantage in systemic osteosarcoma therapy. Combining all results, our study demonstrated substantial potential towards management of osteosarcoma.


2019 ◽  
Vol 20 (8) ◽  
Author(s):  
Brock Matter ◽  
Alireza Ghaffari ◽  
David Bourne ◽  
Yan Wang ◽  
Stephanie Choi ◽  
...  

2019 ◽  
Vol 15 (4) ◽  
pp. 373-409 ◽  
Author(s):  
Emirhan Nemutlu ◽  
İpek Eroğlu ◽  
Hakan Eroğlu ◽  
Sedef Kır

Background:Nanotech products are gaining more attention depending on their advantages for improving drug solubility, maintenance of drug targeting, and attenuation of drug toxicity. In vitro release test is the critical physical parameter to determine the pharmaceutical quality of the product, to monitor formulation design and batch-to-batch variation.Methods:Spectrophotometric and chromatographic methods are mostly used in quantification studies from in vitro release test of nano-drug delivery systems. These techniques have advantages and disadvantages with respect to each other considering dynamic range, selectivity, automation, compatibility with in vitro release media and cost per sample.Results:It is very important to determine the correct kinetic profile of active pharmaceutical substances. At this point, the analytical method used for in vitro release tests has become a very critical parameter to correctly assess the profiles. In this review, we provided an overview of analytical methods applied to the in vitro release assay of various nanopharmaceuticals.Conclusion:This review presents practical direction on analytical method selection for in vitro release test on nanopharmaceuticals. Moreover, precautions on analytical method selection, optimization and validation were discussed.


2011 ◽  
Vol 56 (2) ◽  
pp. 137-143 ◽  
Author(s):  
Wagner L. Priamo ◽  
Alana M. de Cezaro ◽  
Stéphani C. Benetti ◽  
J. Vladimir Oliveira ◽  
Sandra R.S. Ferreira

Sign in / Sign up

Export Citation Format

Share Document