scholarly journals An In-Vitro Evaluation of the Characteristics of Zein-Based Films for the Release of Lactobionic Acid and the Effects of Oleic Acid

Polymers ◽  
2021 ◽  
Vol 13 (11) ◽  
pp. 1826
Author(s):  
Alessandro Coroli ◽  
Roberta Romano ◽  
Andrea Saccani ◽  
Noura Raddadi ◽  
Elisa Mele ◽  
...  
Keyword(s):  
Oleic Acid ◽  
Water Solubility ◽  
Antioxidant Properties ◽  
Precursor Solution ◽  
Physiological Solution ◽  
Burst Release ◽  
Lactobionic Acid ◽  
Industrial Sectors ◽  
Total Extraction

Lactobionic acid (LBA) is widely used in different industrial sectors owing to its biocompatibility characteristics as well as antioxidant and antimicrobial properties. In this study, mixtures of the protein zein with LBA and with the addition of oleic acid (OA) as a ternary system were investigated as drug delivery films for the release of LBA. The chosen combinations exploit the vast difference in water solubility between LBA and the other two components (zein and OA). DSC thermograms and dynamic mechanical spectra, alongside electron microscopy images, were used to describe the microstructural features of the films and were found to provide insights for the release of LBA from the two examined zein-based films immersed in an aqueous physiological solution. For both film systems, a burst release behavior was observed, followed by a rapid and total extraction of LBA. The required immersion time for the total extraction of LBA was greatly reduced when oleic acid was added to the precursor solution mixture for producing the films. The LBA released from the zein-based films was found to exhibit both the expected antioxidant properties as well as exerting bacteriostatic effects towards Escherichia coli and Staphylococcus epidermidis.

scholarly journals Formulation and Characterization of Felodipine as an Oral Nanoemulsions

2021 ◽  
Vol 30 (1) ◽  
pp. 209-217
Author(s):  
Sumaya B. Hamed ◽  
Shaimaa N. Abd Alhammid
Keyword(s):  
Particle Size ◽  
Oleic Acid ◽  
Zeta Potential ◽  
Water Solubility ◽  
Tween 80 ◽  
Aqueous Solubility ◽  
Compatibility Study ◽  
Drug Content ◽  
Drug Molecules

            Felodipine is a calcium-channel blocker with low aqueous solubility and bioavailability. Lipid dosage forms are attractive delivery systems for such hydrophobic drug molecules. Nanoemulsion (NE) is one of the popular methods that has been used to solve the dispersibility problems of many drugs. Felodipine was formulated as a NE utilizing oleic acid as an oil phase, tween 80 and tween 60 as surfactants and ethanol as a co-surfactant. Eight formulas were prepared, and different tests were performed to ensure the stability of the NEs, such as particle size, polydispersity index, zeta potential, dilution test, drug content, viscosity and in-vitro drug release. Results of characterization showed that felodipine nanoemulsion (F3) with (oleic acid 10%) ,(Smix 60% of tween80 :ethanol in a ratio of 3:1), (DDW 30%) was selected as the best formula, since it has a particle size of (17.01)nm, low PDI (0.392), zeta potential (-22.34mV), good dilution without drug precipitation , higher percent of drug content (99.098%) with  acceptable viscosity , and complete release of the drug after (45 min.) with significantly higher (P<0.05)   dissolution  rate in comparison with the pure drug powder. The selected formula (F3) subjected to further investigations as drug and excipient compatibility study by Fourier transform infrared spectroscopy (FTIR) The outcomes of the (FTIR) explain that the distinctive peaks for felodipine were not affected by other components and displayed the same functional group's band with very slight shifting. This indicates that there was no interaction between felodipine and other NE components. Therefore, these excipients were found to be compatible with felodipine. In conclusion, the NE was found to be an efficient method to enhance the dispersibility and permeatioins of drugs that have poor water solubility (lipophilic drugs).

scholarly journals Formulation Design, Statistical Optimization, and In Vitro Evaluation of a Naringenin Nanoemulsion to Enhance Apoptotic Activity in A549 Lung Cancer Cells

2020 ◽  
Vol 13 (7) ◽  
pp. 152 ◽  
Author(s):  
Shadab Md ◽  
Nabil A. Alhakamy ◽  
Hibah M. Aldawsari ◽  
Mohammad Husain ◽  
Sabna Kotta ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Cancer Cells ◽  
Water Solubility ◽  
Spherical Surface ◽  
Physical Stability ◽  
Lung Cancer Cells ◽  
Enzyme Linked Immunosorbent Assay ◽  
Burst Release ◽  
A549 Lung

Naringenin (NAR), a flavonoid mainly found in citrus and grapefruits, has proven anti-cancer activities. However, the poor water solubility and low bioavailability of NAR limits its use as a therapeutic agent. The aim of this study was to develop and optimize stable naringenin nanoemulsions (NAR-NE) using a Box–Behnken experimental design to obtain a formulation with a higher efficiency. Anticancer activity of optimized NAR-NE was evaluated in A549 lung cancer cells using cell viability, flow-cytometric assays, and enzyme-linked immunosorbent assay. The stabilized nanoemulsion, which showed a spherical surface morphology, had a globule size of 85.6 ± 2.1 nm, a polydispersity index of 0.263 ± 0.02, a zeta potential of −9.6 ± 1.2 mV, and a drug content of 97.34 ± 1.3%. The NAR release from the nanoemulsion showed an initial burst release followed by a stable and controlled release for a longer period of 24 h. The nanoemulsion exhibited excellent thermodynamic and physical stability against phase separation and storage. The NAR-NE showed concentration-dependent cytotoxicity in A549 lung cancer cells, which was greater than that of free NAR. The percentage of apoptotic cells and cell cycle arrest at the G2/M and pre-G1 phases induced by NAR-NE were significantly higher than those produced by free NAR (p < 0.05). NAR-NEs were more effective than the NAR solution in reducing Bcl2 expression, while increasing pro-apoptotic Bax and caspase-3 activity. Therefore, stabilized NAR-NE could be a suitable drug delivery system to enhance the effects of NAR in the treatment of lung cancer.

scholarly journals Curcumin In Situ Gelling Polymeric Insert with Enhanced Ocular Performance

Pharmaceutics ◽  
2020 ◽  
Vol 12 (12) ◽  
pp. 1158
Author(s):  
Hamdy Abdelkader ◽  
David Wertheim ◽  
Barbara Pierscionek ◽  
Raid G. Alany
Keyword(s):  
Ocular Surface ◽  
Water Solubility ◽  
Molecular Form ◽  
Antioxidant Properties ◽  
In Vitro Release ◽  
Duration Of Action ◽  
Corneal Permeability ◽  
In Situ Gelling

The search for an ocular drug delivery system that could provide long-acting effects without a detriment to the anatomy and physiology of the eye remains a challenge. Polyphenolic compounds (curcumin in particular) have recently gained popularity due to their powerful antioxidant properties; yet curcumin suffers poor stability and water solubility. A conventional eye drop formulation of curcumin in the form of a suspension is likely to suffer a short duration of action requiring multiple instillations. On the other hand, polymeric in-situ gelling inserts offer the prospect of overcoming these limitations. The aim of this study was to prepare, characterize and evaluate in vivo, polymeric, in-situ gelling and mucoadhesive inserts for ocular surface delivery of curcumin. Different types and ratios of biocompatible polymers (HPMC, CMC, PL 127 and PVA) and three plasticizers along with the solvent casting method were adopted to prepare curcumin inserts. The inserts were investigated for their physicochemical characteristics, applicability, and suitability of use for potential placement on the ocular surface. The prepared inserts revealed that curcumin was mainly dispersed in the molecular form. Insert surfaces remained smooth and uniform without cracks appearing during preparation and thereafter. Improved mechanical and mucoadhesive properties, enhanced in vitro release (7.5- to 9-fold increases in RRT300 min) and transcorneal permeation (5.4- to 8.86-fold increases in Papp) of curcumin was achieved by selected in-situ gelling inserts compared to a control curcumin suspension. The developed inserts demonstrated acceptable ocular tolerability, enhanced corneal permeability, and sustained release of curcumin along with retention of insert formulation F7 on the ocular surface for at least two-hours. This insert provides a viable alternative to conventional eye drop formulations of curcumin.

Physicochemical, Nutritional and Antioxidant Properties of Tempeh Flour from Common Bean ( Phaseolus vulgaris L.)

2010 ◽  
Vol 16 (5) ◽  
pp. 427-434 ◽  
Author(s):  
M. Reyes-Bastidas ◽  
E.Z. Reyes-Fernández ◽  
J. López-Cervantes ◽  
J. Milán-Carrillo ◽  
G.F. Loarca-Piña ◽  
...  
Keyword(s):  
Common Bean ◽  
G Protein ◽  
Water Solubility ◽  
Antioxidant Properties ◽  
Protein Digestibility ◽  
Essential Amino Acids ◽  
Efficiency Ratio ◽  
Bean Flour ◽  
Phenolics Content

The effects of solid state fermentation (SSF) on physicochemical, nutritional and antioxidant properties of common bean flour were studied. SSF increased protein content (21.7%) and decreased lipids (-38.4%), carbohydrates (-3.5%) and phytic acid (-58.3%). Fermented (tempeh) flour showed higher dispersability, lower water solubility index and pH than unfermented flour. Fermentation also increased an average of 0.21 g/100 g protein, six of the essential amino acids (EAAs), including total sulfur (Met + Cys), the limiting EAAs in unfermented flour (score = 0.91); Lys and Trp decreased 0.21 and 0.09 g/100 g protein, respectively. SSF improved the in vitro protein digestibility and the calculated protein efficiency ratio. Tempeh flour had 2.2-fold more phenolics than the bean flour and exhibited antiradical activity (43%) and antioxidant activity (38%) correlated with total phenolics content. Common bean tempeh flour may be considered for the fortification of widely consumed legume-based food products and also for the prevention of pathologies associated with oxidative stress.

scholarly journals Evaluation of Oleic Acid and Polyethylene Glycol Monomethyl Ether Conjugate (PEGylated Oleic Acid) as a Solubility Enhancer of Furosemide

Processes ◽  
2019 ◽  
Vol 7 (8) ◽  
pp. 520
Author(s):  
Rahul S. Kalhapure ◽  
Pradeep Kumar Bolla ◽  
Sai HS. Boddu ◽  
Jwala Renukuntla
Keyword(s):  
Oleic Acid ◽  
In Vitro Release ◽  
Aqueous Solubility ◽  
Fold Increase ◽  
Monomethyl Ether ◽  
New Drugs ◽  
Burst Release ◽  
Investigational Drugs ◽  
Solubility Enhancers

Poor aqueous solubility limits the therapeutic efficacy of many marketed and investigational drugs. Synthesis of new drugs with improved solubility is challenging due to time constraint and expenses involved. Therefore, finding the solubility enhancers for existing drugs is an attractive and profitable strategy. In this study, PEGylated oleic acid (OA-mPEG5000), a conjugate of oleic acid and mPEG5000 was synthesized and evaluated as a solubilizer for furosemide. OA-mPEG5000 was evaluated as a nanocarrier for furosemide by formulating polymersomes. Solubility of furosemide in milli-Q water and aqueous OA-mPEG5000 solution was determined using shake flask method. At 37 °C, the solubility of furosemide in OA-mPEG5000 (1% w/w) and milli-Q water was 3404.7 ± 254.6 µg/mL and 1020.2 ± 40.9 µg/mL, respectively. Results showed there was a 3.34-fold increase in solubility of furosemide in OA-mPEG5000 compared to water at 37 °C. At 25 °C, there was a 3.31-fold increase in solubilization of furosemide in OA-mPEG5000 (1% w/w) (90.0 ± 1.45 µg/mL) compared to milli-Q water (27.2 ± 1.43 µg/mL). Size, polydispersity index and zeta potential of polymersomes ranged from 85–145.5 nm, 0.187–0.511 and −4.0–12.77 mV, respectively. In-vitro release study revealed a burst release (71%) within 1 h. Significant enhancement in solubility and formation of polymersomes suggested that OA-mPEG5000 could be a good solubilizer and nanocarrier for furosemide.

Functional and In Vitro Antioxidant Properties of Wild and Insect-Cultured Cordyceps Cicadae Polysaccharides

2021 ◽  
Vol 20 (2) ◽  
pp. 229-238
Author(s):  
Shun-ming Tang ◽  
Jiao Xu ◽  
Nabilla Joshua Abdulai ◽  
Lang Zhou ◽  
Shan-shan Wang ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Water Solubility ◽  
Antioxidant Properties ◽  
Reducing Power ◽  
Bioactive Substances ◽  
Entomogenous Fungus ◽  
Foaming Property ◽  
Silkworm Pupae ◽  
Cordyceps Cicadae

Cordyceps cicadae is an entomogenous fungus, which is used as both medicine and food due to the presence of rich bioactive substances. Currently, most studies focus on the pharmacological effects of the bioactive components of C. cicadae, but the research on their processing is still in its infancy. In this study, polysaccharides were extracted from insect-cultivated C. cicadae (tussah pupae C. cicadae and domestic silkworm pupae C. cicadae) and wild C. cicadae. The functional properties of C. cicadae polysaccharides were evaluated. At the same time, the in vitro antioxidant activity of the insect-cultivated C. cicadae was determined and compared with the wild C. cicadae. The results showed that the cultivated C. cicadae polysaccharides and the wild one had similar structures, and both had appreciable water solubility, oilholding capacity, thermal stability, and emulsifying property compared to foaming property and foaming stability. Further, the C. cicadae polysaccharides cultured on silkworm pupae and tussah pupae showed comparable antioxidant and reducing power to the wild C. cicadae. Our data indicates that the C. cicadae polysaccharides have the potential as a food additive, among which the domestic silkworm pupae C. cicadae showed the best outcome, and the C. cicadae polysaccharides cultured by bionic method have the same antioxidant activity as the wild one.

scholarly journals Integration of Oyster and Milky Mushroom Flour to Underutilized Pulses for the Development of Mushroom Analogues

2020 ◽  
pp. 7-15
Author(s):  
T. R. Thirumuruga Ponbhagavathi ◽  
S. Kanchana ◽  
G. Hemalatha ◽  
S. Vellaikumar ◽  
K. Kalpana
Keyword(s):  
Water Solubility ◽  
Antioxidant Properties ◽  
Added Value ◽  
In Vitro Digestibility ◽  
Horse Gram ◽  
Extrusion Processing ◽  
Nutritional Factor ◽  
Feed Moisture ◽  
Protein Rich

Mushrooms are considered to be a healthy food as they are low in fat, high in protein with good biological value and antioxidant properties. Mushrooms also contain appreciable amounts of dietary fiber. But their quality starts deteriorating immediately after the harvest. On the other hand, horse gram and cowpea have limited utilization due to the presence of anti nutritional factor. In order to extend the shelf life of mushrooms with added value and breakdown the limit of utilization of horse gram and cowpea, extrusion processing has been carried out to develop mushroom analogues through the combination of mushrooms with those underutilized pulses. A formulation comprising 50-75% of pulses and 25-50% mushrooms was made up and extruded with feed moisture content of 12%, an extrusion temperature of 120°C and a screw speed of 150 rpm. The developed products had protein content ranging from 23.01 to 24.56% with increased antioxidant and in-vitro- digestibility properties. Addition of mushroom flour increased the Water Absorption Index (WAI) and decreased the Water Solubility Index (WSI). Incorporation of oyster mushroom powder at 25% and 50% along with cowpea and horse gram flour was found most acceptable in terms of texture and other organoleptic attributes. Developed mushroom analogues can act as a novel vegetarian protein rich convenience product in the market to improve nutritional status of the population.

QUALITATIVE AND QUANTITATIVE PHYTOCHEMICAL SCREENING AND IN VITRO ANTIOXIDANT EVALUATION OF PERGULARIA DAEMIA

2018 ◽  
Vol 24 (2) ◽  
Author(s):  
GITA MISHRA ◽  
HEMESHWER KUMAR CHANDRA ◽  
NISHA SAHU ◽  
SATENDRA KUMAR NIRALA ◽  
MONIKA BHADAURIA
Keyword(s):  
Reducing Sugars ◽  
Antioxidant Properties ◽  
Phytochemical Analysis ◽  
Phytochemical Screening ◽  
Qualitative And Quantitative ◽  
The Family ◽  
Ethanolic Extracts ◽  
Antioxidant Evaluation ◽  
In Vitro Antioxidant Activity

Pergularia daemia belongs to the family Asclepiadaceae, known to have anticancer, anti-inflammatory activity. Aim of the present study was to evaluate qualitative and quantitative phytochemical and antioxidant properties of ethanolic extracts of leaf, stem and root parts of P. daemia . Preliminary phytochemical analysis and in vitro antioxidant properties were evaluated by standard methods. The qualitative phytochemical analysis of P. daemia showed presence of flavonoids, tannins, alkaloid, phytosterol, carbohydrate, phenol, saponin, glycosides, terpenoids, steroids proteins and reducing sugars. Quantitative analysis showed polyphenol, flavonoid, flavonone, flavone and flavonol in P. daemia leaves, stem and root in considerable quantity. The in vitro antioxidant activity of P. daemia clearly demonstrated that leaf, stem and root parts have prominent antioxidant properties and was effective in scavenging free radicals.

Preparation and In Vitro Evaluation of Resealed Erythrocytes as A New Trend in Treatment of Asthma

2016 ◽  
Vol 6 (3) ◽  
Author(s):  
Mohammed Ibrahim ◽  
Alaa Zaky ◽  
Mohsen Afouna ◽  
Ahmed Samy
Keyword(s):  
In Vitro Release ◽  
Human Erythrocytes ◽  
The Body ◽  
Blood Levels ◽  
Time Interval ◽  
Burst Release ◽  
Prolonged Release ◽  
Nocturnal Asthma ◽  
Carrier Erythrocytes

Carrier erythrocytes are emerging as one of the most promising biological drug delivery systems investigated in recent decades. Beside its biocompatibility, biodegradability and ability to circulate throughout the body, it has the ability to perform extended release system of the drug for a long period. The ultimate goal of this study is to introduce a new carrier system for Salbutamol, maintaining suitable blood levels for a long time, as atrial to resolve the problems of nocturnal asthma medication Therefore in this work we study the effect of time, temperature as well as concentration on the loading of salbutamol in human erythrocytes to be used as systemic sustained release delivery system for this drug. After the loading process is performed the carrier erythrocytes were physically and cellulary characterized. Also, the in vitro release of salbutamol from carrier erythrocytes was studied over time interval. From the results it was found that, human erythrocytes have been successfully loaded with salbutamol using endocytosis method either at 25 Co or at 37 Co . The highest loaded amount was 3.5 mg/ml and 6.5 mg/ml respectively. Moreover, the percent of cells recovery is 90.7± 1.64%. Hematological parameters and osmotic fragility behavior of salbutamol loaded erythrocytes were similar that of native erythrocytes. Scanning electron microscopy demonstrated that the salbutamol loaded cells has moderate change in the morphology. Salbutamol releasing from carrier cell was 43% after 36 hours in phosphate buffer saline. The releasing pattern of the drug from loaded erythrocytes showed initial burst release in the first hour followed by a very slow release, obeying zero order kinetics. It concluded that salbutamol is successfully entrapped into erythrocytes with acceptable loading parameters and moderate morphological changes, this suggesting that erythrocytes can be used as prolonged release carrier for salbutamol.

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