scholarly journals Formulation and Characterization of Polyurethane Microstructures with Propolis Extract

2019 ◽  
Vol 56 (2) ◽  
pp. 321-323
Author(s):  
Alexandra Duca ◽  
Florin Borcan ◽  
Danina M. Muntean ◽  
Ersilia C. Alexa ◽  
Codruta M. Soica

Propolis is a natural apicultural product derived from plant resins with impressive health benefits. Its major biologically active substances are barely soluble in water, but this could be increased by proper formulations.The aim of the present study was to obtain a transmembrane delivery system based on polyurethane microstructures for eight propolis samples collected from different regions of Western Romania and to characterize them by differential scanning calorimetry (DSC); the assessed parameters were the particle size, the polydispersity index and their clustering tendency. Polyurethane polymers based on isophorone-diisocyanate and polyethylene glycol 200/ethylene glycol were chosen as carriers for the propolis extract. A perfect inclusion of propolis inside the structures was observed for half of the samples. Particle size ranged between 504 and 621 nm and was confirmed by the low stability against aggregation (Zeta potential: 16.3-19.8 mV). The polydispersity index was between 0.4 and 0.7.

2018 ◽  
Vol 18 (14) ◽  
pp. 1167-1174 ◽  
Author(s):  
Petra Lovecka ◽  
Jan Lipov ◽  
Kamila Thumova ◽  
Anna Macurkova

Pharmaceutics ◽  
2020 ◽  
Vol 12 (2) ◽  
pp. 182 ◽  
Author(s):  
Bwalya A. Witika ◽  
Vincent J. Smith ◽  
Roderick B. Walker

Lamivudine (3TC) and zidovudine (AZT) are antiviral agents used orally to manage HIV/AIDS infection. A pseudo one-solvent bottom-up approach was used to develop and produce nano co-crystals of 3TC and AZT. Equimolar amounts of 3TC dissolved in de-ionized water and AZT in methanol were rapidly injected into a pre-cooled vessel and sonicated at 4 °C. The resultant suspensions were characterized using a Zetasizer. The particle size, polydispersity index and Zeta potential were elucidated. Further characterization was undertaken using powder X-ray diffraction, Raman spectroscopy, Fourier transform infrared spectroscopy, differential scanning calorimetry, and energy dispersive X-ray spectroscopy scanning electron microscopy. Different surfactants were assessed for their ability to stabilize the nano co-crystals and for their ability to produce nano co-crystals with specific and desirable critical quality attributes (CQA) including particle size (PS) < 1000 nm, polydispersity index (PDI) < 0.500 and Zeta potential (ZP) < −30 mV. All surfactants produced co-crystals in the nanometer range. The PDI and PS are concentration-dependent for all nano co-crystals manufactured while only ZP was within specification when sodium dodecyl sulfate was used in the process.


2020 ◽  
Vol 10 (1) ◽  
pp. 57-67 ◽  
Author(s):  
Durga Puro ◽  
Rajani Athawale ◽  
Anjali Pandya

Introduction: Raloxifene Hydrochloride (RXL), a BCS class II drug, is used for the treatment of invasive breast cancer and osteoporosis in post menopausal women. Even though the drug is highly efficient, it shows poor bioavailability of 2% when administered orally. The aim of the study was to develop, statistically optimize, and characterize Raloxifene Hydrochloride loaded Nanostructured Lipid Carriers (NLC) for transdermal delivery to overcome the bioavailability issue. Methods: The RXL-NLC’s were developed using glyceryl behenate (Compritol® 888 ATO), glyceryl monostearate (GMS), and capric triglyceride (Miglyol® 810) as solid and liquid lipids, and Polysorbate 80 (Tween 80) and cremophor EL were used as surfactants and co-surfactant. A response surface methodology was applied for the optimization of NLC, using Box-Behnken experimental design. Amount of the drug, tween 80 and polyethoxylated castor oil (cremophor EL), each at three levels, were selected as independent variables, while particle size and polydispersity index were identified as dependent variables. The optimized batch was characterized for Particle size (79.8 nm±3), Polydispersity index (0.229±0.05), Zeta potential (-12.3±5) and Entrapment efficiency (79.14%±5). Surface morphology of the NLC’s were studied using Transmission Electron microscopy (TEM) and the shift in the endotherm of Differential scanning calorimetry confirmed the entrapment of the drug within NLC. In vitro drug release studies were performed using dialysis bag (12000-14000 Da) method. The optimized NLC dispersion was then incorporated into gel and characterized for gel uniformity, spreadability, pH, viscosity and drug content. Results: In vivo skin penetration study was carried out by tape stripping method, which showed increase in penetration when incorporated into nanogel as compared to plain drug gel. Conclusion: Based on the above result it can be concluded that transdermal delivery of NLC’s can be a superior alternative for orally low bioavailable drugs such as RXL which undergoes rapid first pass metabolism.


Author(s):  
Amruta Papdiwal ◽  
Kishor Sagar ◽  
Vishal Pande

Poor water solubility and slow dissolution rate are major issues for the majority of upcoming and existing biologically active pharmaceutical compounds. Nateglinide is Biopharmaceutical Classification System Class-II drug that has low solubility and high permeability. The purpose of the present study was to improve the solubility and dissolution rate of Nateglinide by the preparation of nanosuspension by the nanoprecipitation technique. Nateglinide nanosuspension was evaluated for its particle size, in vitro dissolution study, and characterized by differential scanning calorimetry and scanning electron microscopy. The optimized formulation showed an average particle size of 207 nm and zeta potential of -25.8 mV. The rate of dissolution of the optimized nanosuspension was enhanced by 83% in 50 min relative to micronized suspension of nateglinide (37% in 50 min). This improvement was mainly due to the formulation of nanosized particles of Nateglinide. Stability study revealed that nanosuspension was more stable at room temperature and refrigerator condition with no significant change in particle size distribution. These results indicate that the nateglinide loaded nanosuspension may significantly improve in vitro dissolution rate and thereby possibly enhance the onset of therapeutic effect.


Separations ◽  
2021 ◽  
Vol 8 (7) ◽  
pp. 89
Author(s):  
Jan Javorský ◽  
Martin Král ◽  
Marek Šnirc ◽  
Július Árvay ◽  
Bohuslava Tremlová ◽  
...  

Knowledge of analytical values in wines is essential to ensure product safety and compliance with legislation, and it is also essential to understand the various technologies in wine production. The aim of this work was to evaluate the analytical parameters of bottled Moravian wines from the Znojmo sub-region, from harvests 2015 and 2016. Basic oenological parameters and biologically active substances were evaluated. Moreover, we evaluated conditions during bottle aging in wines from harvest 2016. The results of the basic analytical values such as total phenolic acid (TPA), total sulfur dioxide (SO2), pH, actual alcohol content (EtOH), and titratable acidity (TA) were in accordance with generally known values in wines and met the legislative requirements within oenological practices. Biologically active substances, such as gallic acid, trans-caffeic acid (TCA), trans-p-coumaric acid (TPCA), rutin, ferulic acid (FA), myricetin, resveratrol, and quercetin were identified. Comparing the analytical values of individual types of wine leads to a better understanding of winemaking technology and the development of wine as such. The subject of the study was also the monitoring of produced grape pomace incurred during wine production harvest 2015 with the indication of possibilities of its further use.


2021 ◽  
pp. 207-215
Author(s):  
Arsen Shamsudinovich Ramazanov ◽  
Shamsiyat Abdulmejidovna Balayeva ◽  
Oleg Borisovich Rudakov ◽  
Igor' Aleksandrovich Saranov

The object of the study was the fruits of milk thistle [Silybum marianum (L) Gaertn.] and fatty oil obtained from them by hexane extraction in the Soxlet apparatus. The aim of the study was to study the influence of natural and climatic conditions on the accumulation of fatty oil and other biologically active substances in the fruits of milk thistle growing on the territory of the Republic of Dagestan. It was found that the content of fatty oil and proteins in the fruits of milk thistle increases with a decrease in air temperature, an increase in the amount of precipitation and soil moisture at the place of growth; the content of carbohydrates and flavolignans in the studied samples of milk thistle fruits is inversely dependent on the content of fatty oil. It was revealed that with an increase in the amount of precipitation and a decrease in the amount of active temperatures during the change of the natural and climatic zone from the foothill Kaitagsky to the high-mountain Kulinsky district, the total content of unsaturated fatty acids, primarily linoleic acid, in milk thistle oil samples decreases. The method of differential scanning calorimetry has been used to study the thermophysical properties of the fatty oil of milk thistle growing in the Kulinsky, Levashinsky and Kaitagsky districts of Dagestan. The results of the thermal analysis are in good agreement with the conclusions obtained from the results of chemical and chromatographic analysis, differential scanning calorimetry allows us to identify trends in the change in the fatty acid and triglyceride composition of milk thistle fatty oil, depending on the natural and climatic conditions of the growth of milk thistle.


2014 ◽  
Vol 1015 ◽  
pp. 713-720
Author(s):  
Si Tao Yang ◽  
Hui Tang ◽  
Yan Fang Liu ◽  
Xue Ying

Gossypol (GP) is a kind of poorly water-soluble polyphenolic compounds. In this study, freeze dried gossypol nanosuspensions (GP-NS) were prepared by high-pressure homogenization and Freeze-drying technique. Bovine serum albumin (BSA) and D-alpha-tocopheryl polyethylene glycol succinate (TPGS) were used as stabilizing agents for the nanosuspensions while mannitol were used as lyophilized protecting medium. The physicochemical characteristics of the GP-NS were investigated when it was found that the mean particle size and zeta potential of the GP-NS were 217±23 nm and-21.4±2.7 mV, respectively, and the saturation solubility was 586.48±23.03 μg.mL-1. Differential scanning calorimetry and X-Ray Diffraction indicated that GP was in a crystalline state in nanosuspensions. GP-NS with a small particle size, and high saturation solubility, can be produced by the method described in this study.


Molecules ◽  
2021 ◽  
Vol 26 (5) ◽  
pp. 1485
Author(s):  
Yogeeta O. Agrawal ◽  
Umesh B. Mahajan ◽  
Vinit V. Agnihotri ◽  
Mayur S. Nilange ◽  
Hitendra S. Mahajan ◽  
...  

Ezetimibe (EZE) possesses low aqueous solubility and poor bioavailability and in addition, its extensive hepatic metabolism supports the notion of developing a novel carrier system for EZE. Ezetimibe was encapsulated into nanostructured lipid carriers (EZE-NLCs) via a high pressure homogenization technique (HPH). A three factor, two level (23) full factorial design was employed to study the effect of amount of poloxamer 188 (X1), pressure of HPH (X2) and number of HPH cycle (X3) on dependent variables. Particle size, polydispersity index (PDI), % entrapment efficiency (%EE), zeta potential, drug content and in-vitro drug release were evaluated. The optimized formulation displays pragmatic inferences associated with particle size of 134.5 nm; polydispersity index (PDI) of 0.244 ± 0.03; zeta potential of −28.1 ± 0.3 mV; % EE of 91.32 ± 1.8% and % CDR at 24-h of 97.11%. No interaction was observed after X-ray diffraction (XRD) and differential scanning calorimetry (DSC) studies. EZE-NLCs (6 mg/kg/day p.o.) were evaluated in the high fat diet fed rats induced hyperlipidemia in comparison with EZE (10 mg/kg/day p.o.). Triglyceride, HDL-c, LDL-c and cholesterol were significantly normalized and histopathological evaluation showed normal structure and architecture of the hepatocytes. The results demonstrated the superiority of EZE-NLCs in regard to bioavailability enhancement, dose reduction and dose-dependent side effects.


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