scholarly journals Evaluation of physicochemical and antioxidant properties of nanosized copolymeric micelles loaded with kaempferol

Pharmacia ◽  
2020 ◽  
Vol 67 (2) ◽  
pp. 49-54
Author(s):  
Krassimira Yoncheva ◽  
Nadia Hristova-Avakumova ◽  
Vera Hadjimitova ◽  
Trayko Traykov ◽  
Petar Petrov
Keyword(s):  
Antioxidant Activity ◽  
Propylene Oxide ◽  
Encapsulation Efficiency ◽  
Antioxidant Properties ◽  
In Vitro Release ◽  
Before And After ◽  
Poly Propylene ◽  
Vitro Release

The study was focused on the evaluation of two copolymers as micellar carriers for kaempferol delivery. The copolymers comprised identical hydrophilic blocks of poly(2-(dimethylamino)ethyl methacrylate and different hydrophobic blocks of either poly(ε-caprolactone) (PDMAEMA9-b-PCL70-b-PDMAEMA9) or poly(propylene oxide) (PDMAEMA13-b-PPO69-b-PDMAEMA13). The calculation of Flory-Huggins parameters and determination of encapsulation efficiency showed that PDMAEMA-b-PCL-b-PDMAEMA copolymer possessed higher capacity for kaempferol loading. The diameter of the micelles before and after lyophilization was not changed, suggesting that the micelles could be lyophilized and redispersed before administration. The in vitro release of kaempferol from PDMAEMA-b-PPO-b-PDMAEMA micelles was faster than the release from PDMAEMA-b-PCL-b-PDMAEMA micelles, probably due to the higher affinity of kaempferol to this copolymer. Further, the higher affinity resulted in a retention of antioxidant activity of kaempferol in the presence of DPPH and KO2 radicals. Thus, PDMAEMA-PCL-PDMAEMA was considered more appropriate carrier because of the higher encapsulation efficiency and preservation of antioxidant activity of the drug.

Thyme essential oil loaded in nanocochleates: Encapsulation efficiency, in vitro release study and antioxidant activity

LWT ◽  
2017 ◽  
Vol 77 ◽  
pp. 497-502 ◽  
Author(s):  
Martina Asprea ◽  
Isabella Leto ◽  
Maria Camilla Bergonzi ◽  
Anna Rita Bilia
Keyword(s):  
Antioxidant Activity ◽  
Essential Oil ◽  
Encapsulation Efficiency ◽  
In Vitro Release ◽  
Thyme Essential Oil ◽  
Release Study ◽  
Vitro Release

Optimization and Characterization of Aqueous Micellar Formulations for Ocular Delivery of an Antifungal Drug, Posaconazole

2020 ◽  
Vol 26 (14) ◽  
pp. 1543-1555 ◽  
Author(s):  
Meltem E. Durgun ◽  
Emine Kahraman ◽  
Sevgi Güngör ◽  
Yıldız Özsoy
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Size Distribution ◽  
Encapsulation Efficiency ◽  
Fungal Infections ◽  
In Vitro Release ◽  
Pluronic F127 ◽  
Glycol Succinate ◽  
Vitro Release

Background: Topical therapy is preferred for the management of ocular fungal infections due to its superiorities which include overcoming potential systemic side effects risk of drugs, and targeting of drugs to the site of disease. However, the optimization of effective ocular formulations has always been a major challenge due to restrictions of ocular barriers and physiological conditions. Posaconazole, an antifungal and highly lipophilic agent with broad-spectrum, has been used topically as off-label in the treatment of ocular fungal infections due to its highly lipophilic character. Micellar carriers have the potential to improve the solubility of lipophilic drugs and, overcome ocular barriers. Objective: In the current study, it was aimed optimization of posaconazole loaded micellar formulations to improve aqueous solubility of posaconazole and to characterize the formulations and to investigate the physical stability of these formulations at room temperature (25°C, 60% RH), and accelerated stability (40°C, 75% RH) conditions. Method: Micelles were prepared using a thin-film hydration method. Pre-formulation studies were firstly performed to optimize polymer/surfactant type and to determine their concentration in the formulations. Then, particle size, size distribution, and zeta potential of the micellar formulations were measured by ZetaSizer Nano-ZS. The drug encapsulation efficiency of the micelles was quantified by HPLC. The morphology of the micelles was depicted by AFM. The stability of optimized micelles was evaluated in terms of particle size, size distribution, zeta potential, drug amount and pH for 180 days. In vitro release studies were performed using Franz diffusion cells. Results: Pre-formulation studies indicated that single D-ɑ-tocopheryl polyethylene glycol succinate (TPGS), a combination of it and Pluronic F127/Pluronic F68 are capable of formation of posaconazole loaded micelles at specific concentrations. Optimized micelles with high encapsulation efficiency were less than 20 nm, approximately neutral, stable, and in aspherical shape. Additionally, in vitro release data showed that the release of posaconazole from the micelles was higher than that of suspension. Conclusion: The results revealed that the optimized micellar formulation of posaconazole offers a potential approach for topical ocular administration.

scholarly journals Enhanced Lymphatic Delivery of Methotrexate Using W/O/W Nanoemulsion: In Vitro Characterization and Pharmacokinetic Study

Pharmaceutics ◽  
2020 ◽  
Vol 12 (10) ◽  
pp. 978 ◽  
Author(s):  
Ji-Hun Jang ◽  
Seung-Hyun Jeong ◽  
Yong-Bok Lee
Keyword(s):  
Plasma Concentration ◽  
Zeta Potential ◽  
Intravenous Administration ◽  
Half Life ◽  
Encapsulation Efficiency ◽  
In Vitro Release ◽  
Lymphatic Delivery ◽  
Vitro Release ◽  
Lymphatic Targeting

Methotrexate, which is widely used in the treatment of cancer and immune-related diseases, has limitations in use because of its low bioavailability, short half-life, and tissue toxicity. Thus, in this study, a nano-sized water-in-oil-in-water (W/O/W) double emulsion containing methotrexate was prepared to enhance its lymphatic delivery and bioavailability. Based on the results from solubility testing and a pseudo-ternary diagram study, olive oil as the oil, Labrasol as a surfactant, and ethanol as a co-surfactant, were selected as the optimal components for the nanoemulsion. The prepared nanoemulsion was evaluated for size, zeta potential, encapsulation efficiency, pH, morphology, and in vitro release profiles. Furthermore, pharmacokinetics and lymphatic targeting efficiency were assessed after oral and intravenous administration of methotrexate-loaded nanoemulsion to rats. Mean droplet size, zeta potential, encapsulation efficiency, and pH of formulated nanoemulsion were 173.77 ± 5.76 nm, −35.63 ± 0.78 mV, 90.37 ± 0.96%, and 4.07 ± 0.03, respectively. In vitro release profile of the formulation indicated a higher dissolution and faster rate of methotrexate than that of free drug. The prepared nanoemulsion showed significant increases in maximum plasma concentration, area under the plasma concentration-time curve, half-life, oral bioavailability, and lymphatic targeting efficiency in both oral and intravenous administration. Therefore, our research proposes a methotrexate-loaded nanoemulsion as a good candidate for enhancing targeted lymphatic delivery of methotrexate.

Fabrication of curcumin-loaded whey protein microgels: Structural properties, antioxidant activity, and in vitro release behavior

LWT ◽  
2019 ◽  
Vol 103 ◽  
pp. 94-100 ◽  
Author(s):  
Mehdi Mohammadian ◽  
Maryam Salami ◽  
Shima Momen ◽  
Farhad Alavi ◽  
Zahra Emam-Djomeh
Keyword(s):  
Antioxidant Activity ◽  
Whey Protein ◽  
Structural Properties ◽  
In Vitro Release ◽  
Release Behavior ◽  
Vitro Release

Development and Characterization of Olanzapine Loaded Poly(lactide-co-glycolide) Microspheres for Depot Injection: In vitro and In vivo Release Profiles

2019 ◽  
Vol 16 (4) ◽  
pp. 375-383 ◽  
Author(s):  
Fahad Pervaiz ◽  
Mahmood Ahmad ◽  
Lihong Li ◽  
Ghulam Murtaza
Keyword(s):  
Bulk Density ◽  
Encapsulation Efficiency ◽  
In Vitro Release ◽  
Infrared Spectrometry ◽  
Burst Release ◽  
In Vivo Release ◽  
Depot Injection ◽  
Vitro Release

Purpose: The purpose of this study was to develop a new PLGA based microsphere formulation aimed to release the olanzapine for the period of one month which will result in increased compliance. Methods: Microspheres loaded with olanzapine were prepared using oil in water emulsion and solvent evaporation technique. The microspheres were characterized by surface morphology, shape, size, bulk density, encapsulation efficiency, and Fourier transform infrared spectrometry. In vitro release studies were performed in phosphate buffer at 37°C and in vivo studies were conducted on male Sprague- Dawley rats. Results: The morphological results indicated that microspheres produced were having a smooth surface, spherical shape and the size in the range from 9.71 to 19.90 μm mean diameter. Encapsulation efficiency of olanzapine loaded microspheres was in the range of 78.53 to 96.12% and was affected by changing the ratio of lactic to glycolic acid in copolymer PLGA. The properties of PLGA and other formulation parameters had a significant impact on in vitro and in vivo release of drug from microspheres. In vitro release kinetics revealed that release of drug from microspheres is by both non-Fickian diffusion and erosion of PLGA polymer. In vivo data indicated an initial burst release and then sustained release depending on properties of PLGA, microsphere size, and bulk density. Conclusion: This study indicates that microsphere formulations developed with PLGA (75:25) and PLGA (85:15) have provided a sufficient steady release of drug for at least 30 days and can be potential candidates for 30-day depot injection drug delivery of olanzapine.

scholarly journals Encapsulation of Olive Pomace Extract in Rocket Seed Gum and Chia Seed Gum Nanoparticles: Characterization, Antioxidant Activity and Oxidative Stability

Foods ◽  
2021 ◽  
Vol 10 (8) ◽  
pp. 1735
Author(s):  
Alican Akcicek ◽  
Fatih Bozkurt ◽  
Cansu Akgül ◽  
Salih Karasu
Keyword(s):  
Encapsulation Efficiency ◽  
In Vitro Release ◽  
Olive Pomace ◽  
Pickering Emulsions ◽  
Chia Seed ◽  
Oil In Water ◽  
Wall Materials ◽  
Seed Gum ◽  
Vitro Release

The aim of this study was to determine the potential use of rocket seed and chia seed gum as wall materials, to encapsulate and to prevent degradation of olive pomace extract (OPE) in polymeric nanoparticles, and to characterize olive pomace extract-loaded rocket seed gum nanoparticles (RSGNPs) and chia seed gum nanoparticles (CSGNPs). The phenolic profile of olive pomace extract and physicochemical properties of olive pomace, rocket seed gum (RSG), and chia seed gum (CSG) were determined. The characterization of the nanoparticles was performed using particle size and zeta potential measurement, differential scanning calorimeter (DSC), Fourier-transform infrared spectroscopy (FTIR), scanning electron microscope (SEM), encapsulation efficiency (EE%), in vitro release, and antioxidant activity analyses. Nanoparticles were used to form oil in water Pickering emulsions and were evaluated by oxitest. The RSGNPs and CSGNPs showed spherical shape in irregular form, had an average size 318 ± 3.11 nm and 490 ± 8.67 nm, and zeta potential values of-22.6 ± 1.23 and -29.9 ± 2.57, 25 respectively. The encapsulation efficiency of the RSGNPs and CSGNPs were found to be 67.01 ± 4.29% and 82.86 ± 4.13%, respectively. The OPE-RSGNP and OPE-CSGNP presented peaks at the 1248 cm−1 and 1350 cm−1 which represented that C-O groups and deformation of OH, respectively, shifted compared to the OPE (1252.53 cm−1 and 1394.69 cm−1). The shift in wave numbers showed interactions of a phenolic compound of OPE within the RSG and CSG, respectively. In vitro release study showed that the encapsulation of OPE in RSGNPs and CSGNPs led to a delay of the OPE released in physiological pH. The total phenolic content and antioxidant capacity of RSGNPs and CSGNPs increased when the OPE-loaded RSGNPs and CSGNPs were formed. The encapsulation of OPE in RSGNPs and CSGNPs and the IP values of the oil in water Pickering emulsions containing OPE-RSGNPs and OPE-CSGNPs were higher than OPE, proving that OPE-loaded RSGNPs and CSGNPs significantly increased oxidative stability of Pickering emulsions. These results suggest that the RSG and CSG could have the potential to be utilized as wall materials for nanoencapsulation and prevent degradation of cold-pressed olive pomace phenolic extract.

scholarly journals Development and Validation of HPTLC Method for Estimation of Carbamazepine in Formulations and Its In Vitro Release Study

2011 ◽  
Vol 2011 ◽  
pp. 1-8 ◽  
Author(s):  
Rashmin B. Patel ◽  
Mrunali R. Patel ◽  
Kashyap K. Bhatt ◽  
Bharat G. Patel
Keyword(s):  
High Performance ◽  
Linear Regression Analysis ◽  
In Vitro Release ◽  
Analysis Data ◽  
Limit Of Quantitation ◽  
Bulk Drug ◽  
Development And Validation ◽  
Vitro Release

A new, simple, and rapid high-performance thin-layer chromatographic method was developed and validated for quantitative determination of Carbamazepine. Carbamazepine was chromatographed on silica gel 60 F254 TLC plate using ethyl acetate-toluene-methanol (5.0 + 4.0 + 1.0 v/v/v) as mobile phase. Carbamazepine was quantified by densitometric analysis at 285 nm. The method was found to give compact spots for the drug (Rf=0.47 ± 0.01). The linear regression analysis data for the calibration plots showed good linear relationship with r2=.9995 in the concentration range 100–600 ng/spot. The method was validated for precision, recovery, repeatability, and robustness as per the International Conference on Harmonization guidelines. The minimum detectable amount was found to be 16.7 ng/spot, whereas the limit of quantitation was found to be 50.44 ng/spot. Statistical analysis of the data showed that the method is precise, accurate, reproducible, and selective for the analysis of Carbamazepine. The method was successfully employed for the estimation of equilibrium solubility, quantification of Carbamazepine as a bulk drug, in commercially available preparation, and in-house developed mucoadhesive microemulsion formulations and solution.

scholarly journals Application of Molecularly Structured Ben Oil in Gentamicin Entrapped Lipospheres

2019 ◽  
pp. 262-270 ◽  
Author(s):  
Salome A. Chime ◽  
Ikechukwu V. Onyishi ◽  
Ifeoma O. Eze
Keyword(s):  
Particle Size ◽  
Encapsulation Efficiency ◽  
Moringa Oleifera ◽  
Extended Release ◽  
In Vitro Release ◽  
Antimicrobial Studies ◽  
Microbial Inhibition ◽  
Vitro Release ◽  
Moringa Oleifera Seed

Objective: To formulate extended release gentamicin-entrapped lipospheres using natural lipids from Irvingia wombolu (IWF) and Moringa oleifera seed (MO) popularly known as Ben oil. Methods: Different lipid combinations including IWF and Phospholipon 90H (P90H) and IWF and MO were employed in the formulation of lipospheres. The formulations were analysed for particle size, encapsulation efficiency (EE), pH stability and antimicrobial studies amongst other tests. Also the in vitro release properties were studied in Phosphate buffer pH 7.2. Results: High EE of up to 90 % were obtained for the various LM combinations. The pH was stable over 30 days and the formulations showed about 93 % release of gentamicin at 12 h. Lipospheres formulated with MO matrices showed synergism in the microbial inhibition than other formulations. Conclusion: Natural lipids from Irvingia wombolu and Moringa oleifera seed could be used in formulating oral extended release gentamicin lipospheres.

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