Formulation of Polymeric Nanoparticles of Lercanidipine by Two Bottom Down Techniques Optimized by Design of Experiment

2020 ◽  
Vol 57 (3) ◽  
pp. 1-18
Author(s):  
Alicia Menezes ◽  
Shanthi Lysetty ◽  
Anup Naha

Lercanidipine has found to be effective in lowering blood pressure among the potent calcium channel blockers, through its action on L- type calcium channels. However, the major disadvantage associated with Lercanidipine is, it is a BCS class II drug having low solubility bioavailability is around 10% through oral route due of extensive first pass metabolism. The present study is aimed to prepare and evaluate polymeric nanoparticles of Lercanidipine using a combination of two bottom down techniques, High speed homogenizer and Probe sonication. Preformulation studies like, DSC, FTIR using surfactants such as Tween 80, Sodium Lauryl sulphate, Polyvinyl Alcohol, singely and in combination were used. A full factorial method was utilized to study the effect of various factors such as surfactant concentration, homogenization speed, sonication amplitude and sonication time on Lercanidipine nanoparticles in two levels. Optimized nanoparticles (with PVA as surfactant) showed an average particle size of 141 nm, PDI 0.248 and zeta potential +6.46. Formulation was further optimized using Design Expert 10 software. Optimized formulation was found to be stable during 3 months stability studies as per ICH guidelines.

Pharmaceutics ◽  
2019 ◽  
Vol 11 (5) ◽  
pp. 213 ◽  
Author(s):  
Evi Christodoulou ◽  
Maria Nerantzaki ◽  
Stavroula Nanaki ◽  
Panagiotis Barmpalexis ◽  
Kleoniki Giannousi ◽  
...  

Magnetic hybrid inorganic/organic nanocarriers are promising alternatives for targeted cancer treatment. The present study evaluates the preparation of manganese ferrite magnetic nanoparticles (MnFe2O4 MNPs) encapsulated within Paclitaxel (PTX) loaded thioether-containing ω-hydroxyacid-co-poly(d,l-lactic acid) (TEHA-co-PDLLA) polymeric nanoparticles, for the combined hyperthermia and chemotherapy treatment of cancer. Initially, TEHA-co-PDLLA semitelechelic block copolymers were synthesized and characterized by 1H-NMR, FTIR, DSC, and XRD. FTIR analysis showed the formation of an ester bond between the two compounds, while DSC and XRD analysis showed that the prepared copolymers were amorphous. MnFe2O4 MNPs of relatively small crystallite size (12 nm) and moderate saturation magnetization (64 emu·g−1) were solvothermally synthesized in the sole presence of octadecylamine (ODA). PTX was amorphously dispersed within the polymeric matrix using emulsification/solvent evaporation method. Scanning electron microscopy along with energy-dispersive X-ray spectroscopy and transmission electron microscopy showed that the MnFe2O4 nanoparticles were effectively encapsulated within the drug-loaded polymeric nanoparticles. Dynamic light scattering measurements showed that the prepared nanoparticles had an average particle size of less than 160 nm with satisfactory yield and encapsulation efficiency. Diphasic PTX in vitro release over 18 days was observed while PTX dissolution rate was mainly controlled by the TEHA content. Finally, hyperthermia measurements and cytotoxicity studies were performed to evaluate the magnetic response, as well as the anticancer activity and the biocompatibility of the prepared nanocarriers.


2020 ◽  
Vol 18 ◽  
Author(s):  
Yanfang Zhang ◽  
Rina Du ◽  
Pengwei Zhao ◽  
Sha Lu ◽  
Rina Wu ◽  
...  

Background: Quercetin is the main active ingredient of Xanthoceras sorbifolia Bunge. Traditional compatibility theory of traditional Chinese medicine has typically reported a synergistic interaction among multiple components, while the synergistic effects of nanoemulsion have not been fully clarified. Objective: To study preparation and characterization of quercetin-based Mongolia Medicine Sendeng-4 nanoemulsion (NQUE-NE) and its antibacterial activity and mechanisms. Methods: The morphology of the nanoemulsion was observed by transmission electron microscopy (TEM), and the zeta potential, polydispersity index (PDI), and particle size distribution were determined by the nanometer particle size analyze. The stability of nanoemulsion was investigated by light test, high speed centrifugal test and storage experiment at different temperature. The combined bacteriostatic effect of N-QUE-NE was studied in vitro by double-dilution method and checkerboard dilution method. Results: The appearance of N-QUE-NE was pale yellow, clear and transparent. The nanoemulsion particles were spherical and uniformly distributed under TEM. The PDI was 0.052, the average particle size was 19.6nm, and the Zeta potential was -0.2mV. When quercetin nanoemulsion (QUE-NE) was used in combination with tannin nanoemulsion (TAN-NE) and toosendanin nanoemulsion (TOO-NE), it exhibited a synergistic antibacterial effect. However, the combination of QUE-NE and geniposide nanoemulsion (GEN-NE) exhibited an antagonistic effect. It was revealed that the antibacterial effect was in order of quercetin-tannin-toosendanin nanoemulsion (QUE-TAN-TOO-NE) > quercetin-tannin nanoemulsion (QUE-TANNE) > QUE-NE > quercetin-tannin-toosendanin-geniposide nanoemulsion (QUE-TAN-TOO-GEN-NE). Conclusion: This study explored the preparation and efficacy of N-QUE-NE, and the results showed that quercetin, tannin and toosendanin had satisfactory synergistic antibacterial effects. The antagonistic effect of quercetin and geniposide in nanoemulsion indicated that it is not beneficial to the antibacterial effect of Sendeng-4, and further research needs to be conducted to clarify its antibacterial effect.


2016 ◽  
Vol 2016 ◽  
pp. 1-10 ◽  
Author(s):  
C. Arancibia ◽  
R. Navarro-Lisboa ◽  
R. N. Zúñiga ◽  
S. Matiacevich

Carboxymethyl cellulose (CMC) is a hydrocolloid with surface activity that could act as emulsifiers in oil-in-water emulsions; however the principal role is that it acts as structuring, thickening, or gelling agent in the aqueous phase. This study aims to evaluate the application of CMC as thickener into nanoemulsions based on olive oil and their influence on particle characteristics, flow behavior, and color. Four nanoemulsions with different oil (5% and 15% w/w olive oil) and CMC (0.5% and 0.75% w/w) concentration and two control samples without CMC added were prepared using Tween 80 as emulsifier. All physical properties studied on nanoemulsions were depending on both oil and CMC concentration. In general, z-average particle size varied among 107–121 nm and those samples with 5% oil and CMC were the most polydisperse. The addition of CMC increased anionic charge of nanoemulsions obtaining zeta potential values among −41 and −55 mV. The oil concentration increased both consistency and pseudoplasticity of samples, although samples were more stable to gravitational separation at the highest CMC concentration. Color of nanoemulsions was affected principally by the oil concentration. Finally, the results showed that CMC could be applied in nanoemulsions as thickener increasing their physical stability although modifying their physical properties.


2008 ◽  
Vol 1103 ◽  
Author(s):  
Aniruddha Subhash Deshpande ◽  
Ramdas B. Khomane ◽  
Bhalchandra K. Vaidya ◽  
Renuka M. Joshi ◽  
Arti S. Harle ◽  
...  

AbstractSulfur nanoparticles were synthesized from hazardous H2S gas by desulfurization based on liquid redox process [1]. The use of novel biodegradable iron chelates, in particular, FeCl3-malic acid chelate system has been extensively studied in various aqueous surfactant systems of Tween 80, SDS, CTAB for catalytic oxidation of H2S gas at ambient conditions of temperature, pressure and neutral pH. The structural features of sulfur nanoparticles have been characterized by XRD, TEM, and DLS measurements. XRD analysis indicates the presence of Metal-sulfur (JCPDS-08247). TEM analysis shows that the morphology of sulfur nanoparticles synthesized in aqueous surfactant system of Tween 80 is nearly uniform in size of 12nm average particle size, in SDS surfactant system shows 15nm average particle size, where as sulfur nanoparticles synthesized in CTAB shows average particle size of 7nm. The DLS result shows the mono-dispersity of the sulfur nanoparticles in the aqueous surfactant systems. The described process serves mainly two objectives; (a) waste utilization for preparation of commercially important nano-sulfur product and (b) reduction in environmental pollution. 1. G. Nagal, Chem. Eng. 104, 125 (1997).


2017 ◽  
Vol 731 ◽  
pp. 29-36 ◽  
Author(s):  
Jan Suda ◽  
Jan Valentin

This paper presents an experimental verification of the alternative options for using by-products or mineral waste materials applied to cold recycled mixtures with low level of stabilisation intended for low-volume road structures. To achieve the necessary refinement and a certain level of reactivity potential, the by-products were activated mechanically, i.e. pulverized in a high-speed disintegrator with respect to the lowest possible energy demands of the process and to the level of wear-and-tear of the working components in the milling machine. Such refined material, with average particle size of 10-15 μm, is applies as an active filler component allowing to partly substitute hydraulic binder in cold recycled mixtures. The application of such materials in structural pavement layers should increase the environmental benefits and result in added economic value. The experimental measurements taken focused on cold recycled mixtures with low level of stabilisation, modified by a combination of binders, or namely cement, mechanically activated concrete from reclaimed concrete pavement slabs originating from the Czech backbone D1 highway modernisation, mechanical-chemically activated fluid ashes from the Pilsen heat plant and foamed bitumen. Both basic volumetric properties and strength and deformation parameters were set for the purposes of evaluation of the characteristic measured in the experimental mixes.


2017 ◽  
Vol 139 (8) ◽  
Author(s):  
Seongchul Juna ◽  
Jinsub Kima ◽  
Hwan Yeol Kimb ◽  
Seung M. Youa

The growth of hovering bubbles on Copper, High-Temperature Thermally-Conductive Microporous Coating (Cu-HTCMC) and plain surface were compared at 1,000 kW/m2 in nucleate boiling with different subcoolings. Images obtained by a high speed camera operating at 2,000 frames per second were used. The Cu-HTCMC was created by sintering copper powders with the average particle size of 67 μm and ∼300 μm thickness, which showed the optimized nucleate boiling and critical heat flux enhancement. The hovering bubble size became smaller as subcooling increased for both Cu-HTCMC and plain surface due to condensation by surrounding subcooled water. At 30 K subcooling, big hovering bubbles disappeared on both surfaces. Small bubbles were shown on plain surface and mists were shown on Cu-HTCMC surface. The hovering bubble sizes were close and the growth times were comparable for both surfaces in saturated and 10 K subcooling cases. However, the bubbles on Cu-HTCMC surface were smaller than those of plain surface at 20 K and 30 K subcoolings. This is believed to be due to the microporous structures shown in the SEM image (top left figure). The heat transfer coefficients of Cu-HTCMC were ∼300 kW/m2K for various subcoolings, about 6 times higher than those of plain surface (top right figure). The figure indicates slightly increasing trend of the heat transfer coefficient with subcooling. This is believed to be the result of the disappearance of relatively big size bubbles in Cu-HTCMC case.


2009 ◽  
Vol 79-82 ◽  
pp. 1987-1990
Author(s):  
Xun Lei Gu ◽  
Yu Qiao Shan ◽  
Chang Sheng Liu

The Al-Mg coatings were deposited on high-speed electro-galvanizing steel by using double-target DC magnetron sputtering. Numerous Al-Mg coatings were prepared with a range of different Mg-target power at different substrate temperatures. The morphologies and compositions were analyzed by SEM, EDS and XRD, the corrosion-resistance properties with different sputtering parameters were discussed by electrochemical measurement. It was found that with the substrate temperature increasing, the porosity decreased, meanwhile, higher substrate temperature resulted in more granular particles and an increased average particle size, but that did not affect corrosion properties obviously. The corrosion-resistance properties were found to be significantly affected by the targets power. As the power of Al-target and Mg-target were 900W and 200W respectively, the film acted the best corrosion-resistance property. Corrosion current density was approximately 4μA/cm2, decreased significantly compared with galvanized sheet. After analysis, the coating was mainly composed of Al12Mg17 which afforded sacrificial anode protection. As the Mg-target power over high relative to Al-target, the coating was composed of Al12Mg17 and MgZn2, the latter can cause micro-galvanic acceleration of corrosion.


2019 ◽  
Vol 7 (22) ◽  
pp. 3757-3761
Author(s):  
Anayanti Arianto ◽  
Cindy Cindy

BACKGROUND: There are a lot of different types of sunscreen products (oils, sticks, gels, creams, lotions) which can be found on the world's market. Sunscreen product that contains active chemical ingredients sometimes has harmful effects on the skin. Sunflower oil contains vitamin E and acts as a natural sunscreen which can absorb UVB light. The average droplet size of nanoemulsion is between 100 and 500 nm and do not show the problems of stability (creaming, flocculation, coalescence, and sedimentation), which are commonly associated with macroemulsions. AIM: The aim of this study was to prepare and evaluate the sunflower oil nanoemulsion as a sunscreen. METHODS: Sunflower oil nanoemulsions were prepared by spontaneous emulsification method with 3 formulas F1 (Tween 80 38%, sorbitol 22%), F2 (Tween 80 36%, sorbitol 24%), F3 (Tween 80 34%, sorbitol 26%) and 5% sunflower oil as a sunscreen substance. The nanoemulsions were evaluated for particle size, physical stability in room temperature (25 ± 2°C), low temperature (4 ± 2°C) and high temperature (40 ± 2°C) during experiment for 12 weeks of storage, centrifugation at 3750 rpm for 5 hours, viscosity, pH, freeze-thaw test and sun protection value (SPF) value by in vitro. RESULTS: The results of nanoemulsion evaluation showed that nanoemulsion formula F1 had the smallest average particle size of 124.47 nm with yellowish colour, clear, transparent, pH value (6.5 ± 0.1), viscosity value (225 ± 25 cP), did not show any separation or creaming in the centrifugation, and stable during experiment for 12 weeks of storage at room temperature, low temperature and high temperature. The SPF value of all nanoemulsion preparations was higher than that of the emulsion. CONCLUSION: The preparation of the sunflower oil nanoemulsion with a ratio of Tween 80 and sorbitol (38: 22) produces a stable nanoemulsion during the experiment for 12 weeks storage at the room, low and high temperature. The nanoemulsion preparation has higher SPF values compared to the emulsion. This nanoemulsion formulation could be considered more effective in sunscreen cosmetic use compare to the emulsion.


2019 ◽  
Vol 22 (6) ◽  
pp. 421-427
Author(s):  
Seyyed Jalal Roudbaraki ◽  
Sadaf Janghorban ◽  
Majid Ghashang

Aim and Objective: The aim of this paper is to introduce HSBM as a green and environmentally friendly technique for the synthesis of thiochromeno[4,3-b]pyran and benzo[h]thiazolo[2,3-b]quinazoline derivatives over ZnAl2O4 nanopowders as an efficient catalyst. Materials and Methods: ZnAl2O4 nanopowders were synthesized via a co-precipitation of Zn(NO3)2 and Al(NO3)3 salts and were characterized by XRD, FE-SEM, TEM and DLS techniques. The as-prepared ZnAl2O4 nano-powders have been used as a catalyst on the synthesis of pyran nucleus using high-speed ball milling (HSBM) technique. The structure of products was confirmed with NMR analysis. Results: ZnAl2O4 exhibits a cubic crystal structure (Space group: Fd-3m) with the average crystallite size of 41 nm. The average particle size of ZnAl2O4 nano-powders determined by DLS technique is 55 nm. The catalytic activity of nano-powders was examined on the synthesis of 2- amino-4,5-dihydro-4-arylthiochromeno[4,3-b]pyran-3-carbonitriles, (8Z)-2-amino-8-arylidene-4,5, 7,8-tetrahydro-4-arylthiopyrano[4,3-b]pyran-3-carbonitriles, 4-aryl-3,4,5,6-tetrahydrobenzo[h]quinazoline- 2(1H)-thiones and 4-aryl-1,3,4,5-tetrahydro-2H-thiochromeno[4,3-d]pyrimidine-2-thione derivatives. All products were obtained in high yields with short reaction times. Conclusion: ZnAl2O4 nanopowders were prepared via a cost-effective co-precipitation method and showed good potential for the synthesis of 4H-pyran analogous in good yields. The salient advantages of HSBM technique include environmentally friendly with reduced solvents, is a simple technique and has low energy costs.


2014 ◽  
Vol 136 (4) ◽  
Author(s):  
Deepak Kumar Goyal ◽  
Harpreet Singh ◽  
Harmesh Kumar ◽  
Varinder Sahni

Degradation of surfaces of hydroturbine components caused by impact of abrasive particles carried by flowing water is a serious issue. To counteract the same, surface modification of turbine materials by the application of protective coatings is gaining popularity these days. In this work, Cr3C2–NiCr coating was deposited on CA6NM turbine steel by the HVOF spray process and studied with regard to its performance under different slurry erosion conditions. The effect of three parameters, namely average particle size of slurry particles, speed (rpm), and slurry concentration on slurry erosion of this coating material, was studied by using a high speed erosion test rig. The analysis of the surfaces of the samples before and after slurry erosion tests was done by using SEM. The HVOF sprayed Cr3C2–NiCr coating showed very good performance under slurry erosion in comparison with uncoated CA6NM steel.


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