scholarly journals Development, Characterization, Stability and Bioaccessibility Improvement of 7,8-Dihydroxyflavone Loaded Zein/Sophorolipid/Polysaccharide Ternary Nanoparticles: Comparison of Sodium Alginate and Sodium Carboxymethyl Cellulose

Foods ◽  
2021 ◽  
Vol 10 (11) ◽  
pp. 2629
Author(s):  
Yufeng Chen ◽  
Jingchong Peng ◽  
Yueqi Wang ◽  
Daniel Wadhawan ◽  
Lijun Wu ◽  
...  
Keyword(s):  
Sodium Alginate ◽  
Carboxymethyl Cellulose ◽  
Electrostatic Interactions ◽  
Storage Stability ◽  
Amorphous State ◽  
Sodium Carboxymethyl Cellulose ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
In Vitro Bioaccessibility

In this study, two polysaccharides [sodium alginate (ALG) and sodium carboxymethyl cellulose (CMC)] were selected to establish zein/sophorolipid/ALG (ALG/S/Z) and zein/sophorolipid/ALG (CMC/S/Z) nanoparticles to encapsulate 7,8-dihydroxyflavone (7,8-DHF), respectively. The results showed that polysaccharide types significantly affected performance of ternary nanoparticles, including CMC/S/Z possessed lower polydispersity index, particle size and turbidity, but higher zeta potential, encapsulation efficiency and loading capacity compared to ALG/S/Z. Compared to zein/sophorolipid nanoparticles (S/Z), both ALG/S/Z and CMC/S/Z had better stability against low pH (pH 3~4) and high ionic strengths (150~200 mM NaCl). Hydrophobic effects, electrostatic interactions and hydrogen bonding were confirmed in ternary nanoparticles fabrication via Fourier-transform infrared spectroscopy. Circular dichroism revealed that CMC and ALG had no evident impact on secondary structure of zein in S/Z, but changed surface morphology of S/Z as observed by scanning electron microscope. Encapsulated 7,8-DHF exhibited an amorphous state in ternary nanoparticles as detected by X-ray diffraction and differential scanning calorimetry. Furthermore, compared to S/Z, ALG/S/Z, and CMC/S/Z remarkably improved the storage stability and bioaccessibility of 7,8-DHF. CMC/S/Z possessed a greater storage stability for 7,8-DHF, however, ALG/S/Z exhibited a better in vitro bioaccessibility of 7,8-DHF. This research provides a theoretical reference for zein-based delivery system application.

scholarly journals Establishment and Characterization of Stable Zein/Glycosylated Lactoferrin Nanoparticles to Enhance the Storage Stability and in vitro Bioaccessibility of 7,8-Dihydroxyflavone

2022 ◽  
Vol 8 ◽  
Author(s):  
Yufeng Chen ◽  
Xiaojing Gao ◽  
Shucheng Liu ◽  
Qiuxing Cai ◽  
Lijun Wu ◽  
...  
Keyword(s):  
Encapsulation Efficiency ◽  
Storage Stability ◽  
Hydrophobic Interactions ◽  
Amorphous State ◽  
Spherical Shape ◽  
Low Ph ◽  
In Vitro Bioaccessibility ◽  
Ph Conditions

In this work, the lactoferrin (LF) was glycosylated by dextran (molecular weight 10, 40, and 70 kDa, LF 10K, LF 40K, and LF 70K) via Maillard reaction as a stabilizer to establish zein/glycosylated LF nanoparticles and encapsulate 7,8-dihydroxyflavone (7,8-DHF). Three zein/glycosylated LF nanoparticles (79.27–87.24 nm) with low turbidity (<0.220) and polydispersity index (PDI) (<0.230) were successfully established by hydrophobic interactions and hydrogen bonding. Compared with zein/LF nanoparticles, zein/glycosylated LF nanoparticles further increased stability to ionic strength (0–500 mM NaCl) at low pH conditions. Zein/glycosylated LF nanoparticles had nanoscale spherical shape and glycosylated LF changed surface morphology of zein nanoparticles. Besides, encapsulated 7,8-DHF exhibited an amorphous state inside zein/glycosylated LF nanoparticles. Most importantly, zein/glycosylated LF nanoparticles had good water redispersibility, high encapsulation efficiency (above 98.50%), favorable storage stability, and bioaccessibility for 7,8-DHF, particularly LF 40K. Collectively, the above research provides a theoretical reference for the application of zein-based delivery systems.

Role of polymer/polymer and polymer/drug specific interactions in drug delivery systems

2019 ◽  
Vol 39 (6) ◽  
pp. 534-544
Author(s):  
Farid Ouazib ◽  
Naima Bouslah Mokhnachi ◽  
Nabila Haddadine ◽  
Regis Barille
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Polymer System ◽  
Amorphous State ◽  
Delivery Systems ◽  
Release Mechanism ◽  
Release Kinetic ◽  
X Ray Diffraction ◽  
Scanning Calorimetry

Abstract Drug delivery systems based upon the blending of Arabic gum and poly(N-vinylpyrrolidone) (AG/PVP) were prepared for the controlled release of acebutolol (Acb) hydrochloride. The prepared blends containing Acb were characterized using different techniques. The presence of physical interactions between the drug and polymer matrices was observed with Fourier-transform infrared spectroscopy. These interactions resulted in the transition of the drug from a crystalline to an amorphous state into the polymeric matrices, as demonstrated by differential scanning calorimetry and X-ray diffraction analysis. The thermogravimetric analysis study confirmed the presence of these interactions, which had a stabilizing effect on the drug against both thermal degradation and crystallinity. The in vitro release of Acb from the AG/PVP polymer system was investigated. Each drug-loaded system was used in a tablet formulation. Moreover, an in vitro dissolution study was carried out in three different dissolution media, and comparison of the dissolution profiles of the different dosage forms revealed that the polymer blend matrix had a better release-retarding efficiency. To better understand the release mechanism, the dissolution data were fitted to various release kinetic models.

scholarly journals Formulation and development of metformin-loaded microspheres using Khaya senegalensis (Meliaceae) gum as co-polymer

2020 ◽  
Vol 6 (1) ◽  
Author(s):  
Chukwuebuka H. Ozoude ◽  
Chukwuemeka P. Azubuike ◽  
Modupe O. Ologunagba ◽  
Sejoro S. Tonuewa ◽  
Cecilia I. Igwilo
Keyword(s):  
Controlled Release ◽  
Sodium Alginate ◽  
Release Kinetics ◽  
Drug Carrier ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Metformin Hydrochloride ◽  
Scanning Calorimetry ◽  
Khaya Senegalensis

Abstract Background Khaya gum is a bark exudate from Khaya senegalensis (Maliaecae) that has drug carrier potential. This study aimed to formulate and comparatively evaluate metformin-loaded microspheres using blends of khaya gum and sodium alginate. Khaya gum was extracted and subjected to preformulation studies using established protocols while three formulations (FA; FB and FC) of metformin (1% w/v)-loaded microspheres were prepared by the ionic gelation method using 5% zinc chloride solution as the cross-linker. The formulations contained 2% w/v blends of khaya gum and sodium alginate in the ratios of 2:3, 9:11, and 1:1, respectively. The microspheres were evaluated by scanning electron microscopy, Fourier transform-infrared spectroscopy, differential scanning calorimetry, entrapment efficiency, swelling index, and in vitro release studies. Results Yield of 28.48%, pH of 4.00 ± 0.05, moisture content (14.59% ± 0.50), and fair flow properties (Carr’s index 23.68 ± 1.91 and Hausner’s ratio 1.31 ± 0.03) of the khaya gum were obtained. FTIR analyses showed no significant interaction between pure metformin hydrochloride with excipients. Discrete spherical microspheres with sizes ranging from 1200 to 1420 μm were obtained. Drug entrapment efficiency of the microspheres ranged from 65.6 to 81.5%. The release of the drug from microspheres was sustained for the 9 h of the study as the cumulative release was 62% (FA), 73% (FB), and 80% (FC). The release kinetics followed Korsmeyer-Peppas model with super case-II transport mechanism. Conclusion Blends of Khaya senegalensis gum and sodium alginate are promising polymer combination for the preparation of controlled-release formulations. The blend of the khaya gum and sodium alginate produced microspheres with controlled release properties. However, the formulation containing 2:3 ratio of khaya gum and sodium alginate respectively produced microspheres with comparable controlled release profiles to the commercial brand metformin tablet.

scholarly journals Eudragit S-100 coated sodium alginate microspheres of naproxen sodium: Formulation, optimization and in vitro evaluation / Alginatne mikrosfere naproksen natrija obložene Eudragitom S-100: Priprava, optimizacija i in vitro vrednovanje

2012 ◽  
Vol 62 (4) ◽  
pp. 529-545 ◽  
Author(s):  
Anuj Chawla ◽  
Pooja Sharma ◽  
Pravin Pawar
Keyword(s):  
Drug Release ◽  
Sodium Alginate ◽  
Naproxen Sodium ◽  
Drug Loading ◽  
Size Analysis ◽  
Scanning Calorimetry ◽  
Sem Images ◽  
S 100 ◽  
Eudragit S 100

The aim of the study was to prepare site specific drug delivery of naproxen sodium using sodium alginate and Eudragit S-100 as a mucoadhesive and pH-sensitive polymer, respectively. Core microspheres of alginate were prepared by a modified emulsification method followed by cross-linking with CaCl2, which was further coated with the pH dependent polymer Eudragit S-100 (2.5 or 5 %) to prevent drug release in the upper gastrointestinal environment. Microspheres were characterized by FT-IR spectroscopy, X-ray diffraction, differential scanning calorimetry and evaluated by scanning electron microscopy, particle size analysis, drug loading efficiency, in vitro mucoadhesive time study and in vitro drug release study in different simulated gastric fluids. Stability studies of the optimized formulation were carried out for 6 months. SEM images revealed that the surface morphology was rough and smooth for core and coated microspheres, respectively. Core microspheres showed better mucoadhesion compared to coated microspheres when applied to the mucosal surface of freshly excised goat colon. The optimized batch of core microspheres and coated microspheres exhibited 98.42 ± 0.96 and 95.58 ± 0.74 % drug release, respectively. Drug release from all sodium alginate microsphere formulations followed Higuchi kinetics. Moreover, drug release from Eudragit S-100 coated microspheres followed the Korsmeyer-Peppas equation with a Fickian kinetics mechanism. Stability study suggested that the degradation rate constant of microspheres was minimal, indicating 2 years shelf life of the formulation.

Mannosylated Solid Lipid Nanocarriers Of Chrysin To Target Gastric Cancer: Optimization and Cell line Study.

2021 ◽  
Vol 18 ◽  
Author(s):  
Sonia S. Pandey ◽  
Farhinbanu I. Shaikh ◽  
Arti R. Gupta ◽  
Rutvi J. Vaidya
Keyword(s):  
Gastric Cancer ◽  
Particle Size ◽  
Ex Vivo ◽  
Biological Effects ◽  
Entrapment Efficiency ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Solid Lipid ◽  
Lipid Nanocarriers

Background: Despite significant biological effects, the clinical use of chrysin has been restricted because of its poor oral bioavailability. Objective: The purpose of the present research was to investigate the targeting potential of Mannose decorated chrysin (5,7- dihydroxyflavone) loaded solid lipid nanocarrier (MC-SLNs) for gastric cancer. Methods: The Chrysin loaded SLNs (C-SLNs) were developed optimized, characterized and further mannosylated. The C-SLNs were developed with high shear homogenizer, optimized with 32 full factorial designs and characterized by Fourier Transform Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), X-ray Diffraction (XRD) and Scanning Electron Microscope (SEM) and evaluated for particle size/polydispersity index, zeta-potential, entrapment efficiency, % release and haemolytic toxicity. The ex-vivo cytotoxicity study was performed on gastric cancer (ACG) and normal cell lines. Results: DSC and XRD data predict the chrysin encapsulation in lipid core and FTIR results confirm the mannosylation of C-SLNs. The optimized C-SLNs exhibited a narrow size distribution with a particle size of 285.65 nm. The % Entrapment Efficiency (%EE) and % controlled release were found to be 74.43% and 64.83%. Once C-SLNs were coated with mannose, profound change was observed in dependent variable - increase in the particle size of MC-SLNs (307.1 nm) was observed with 62.87% release and 70.8% entrapment efficiency. Further, the in vitro studies depicted MC- SLNs to be least hemolytic than pure chrysin and C-SLNs. MC-SLNs were most cytotoxic and were preferably taken up ACG tumor cells as evaluated against C-SLNs. Conclusion: These data suggested that the MC-SLNs demonstrated better biocompatibility and targeting efficiency to treat the gastric cancer.

scholarly journals A study of the effects of sodium alginate and sodium carboxymethyl cellulose on the growth of the common duckweed (Lemna minor L.)

2021 ◽  
pp. 82-82
Author(s):  
Bianca Boros ◽  
Nathalie Grau ◽  
Adriana Isvoran ◽  
Adina Datcu ◽  
Nicoleta Ianovici ◽  
...  
Keyword(s):  
Sodium Alginate ◽  
Carboxymethyl Cellulose ◽  
Water Solubility ◽  
Lemna Minor ◽  
Sodium Carboxymethyl Cellulose ◽  
Log P ◽  
Growth Inhibitory ◽  
Wide Range ◽  
The Common ◽  
High Doses

Sodium alginate (ALG) and sodium carboxymethyl cellulose (CMC) are two polysaccharides that have a wide range of applications which could lead to accidental pollution of the environment, making the assessment of their potential ecotoxicity imperative. The present study assesses the ALG and CMC effects on the growth response of the common duckweed (Lemna minor L.). The results emphasize that both polysaccharides can be classified as practically nontoxic based on their EC50 values, with ALG having a relatively higher toxicity compared to CMC. It was also observed that high doses of 1, 5 and 10 mg mL-1 of the two polysaccharides produced growth inhibitory effects against common duckweed. The toxicity of biopolymers against common duckweed, measured as EC50 values, seems to be correlated to the hydrophobicity of the monomers building the polymer. The EC50 values increase linearly with the increase of water solubility (log S) values and decrease linearly with the lipophilicity (log P) values.

scholarly journals Development of an Oxcarbazepine Solid Dispersion Using Skimmed Milk to Improve the Solubility and Dissolution Profile

2019 ◽  
Vol 11 (05) ◽  
Author(s):  
M. Shah ◽  
D. Patel
Keyword(s):  
Electron Microscopy ◽  
Solid Dispersion ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
X Ray ◽  
Infra Red ◽  
Crystalline Nature ◽  
Skimmed Milk ◽  
Scanning Electron

Oxcarbazepine has low solubility and low oral bioavailability, so it’s a challenge to formulate suitable dosage form. In this present investigation, to improve the dissolution rate and solubility, skimmed milk is used as a carrier. Physical mixers were prepared using various drugs to carrier ratio and spray drying technology was used to develop solid dispersion with the carrier. Various techniques were used to characterize the solid dispersion immediately after they were made which includes differential scanning calorimetry, scanning electron microscopy, fourier transform infra- red spectroscopy, X-ray diffraction and in-vitro dissolution profiles. The differential scanning calorimetry thermograms of raw drug indicated of its anhydrous crystalline nature. In thermograms of solid dispersion, the characteristic peak was absent suggesting the change from crystalline nature to amorphous form. X-ray diffraction confirmed those results. X-ray diffraction results of raw drug showed highly intense peak characteristic of its crystalline nature where solid dispersion showed less intense, more diffused peak indicating the change in crystalline form. Fourier transforms infra-red spectroscopy studies showed there was no interaction between drug and carrier. Scanning electron microscopy support the amorphous nature of mixer. The whole formulation showed distinct enhancement in the drug release behavior and solubility. The optimum oxcarbazepine to skimmed milk ratio 1:3 enhances the in-vitro drug release by 3.5 fold and also show distinct increase in solubility. It was concluded that for improvement of solubility of poorly water soluble oxcarbazepine, skimmed milk powder as a carrier can be utilize very well.

scholarly journals DESIGN, DEVELOPMENT, AND CHARACTERIZATION OF OCIMUM BASILICUM MUCILAGE-BASED, MODIFIED RELEASE MUCOADHESIVE GASTROSPHERES OF CARVEDILOL

2019 ◽  
pp. 218-225
Author(s):  
SAKHARE SS ◽  
SAYYAD FJ
Keyword(s):  
Controlled Release ◽  
Sodium Alginate ◽  
Entrapment Efficiency ◽  
Ocimum Basilicum ◽  
Differential Scanning Calorimetric ◽  
Design Development ◽  
X Ray Diffraction ◽  
Microscopy Technique ◽  
Zero Order Release

Objective: The present investigations aim to develop mucoadhesive gastrospheres of carvedilol using sodium alginate and Ocimum basilicum seed mucilage combination blend oral use. Methods: The gastrospheres were prepared by ionotropic gelation method using 32 factorial designs, the concentration of sodium alginate and O. basilicum mucilage was independent variables while % drug content (DC), % entrapment efficiency, and % drug release at 12 h were dependent variables. The gastrospheres were evaluated for other parameters such as Fourier-transform infrared (FTIR), powder X-ray diffraction, differential scanning calorimetric, and in vitro mucoadhesion studies. Results: In optimization studies from statistical second-order complete model equation among the polymers used O. basilicum mucilage had a more profound effect on DC and % encapsulation efficiency as compared to sodium alginate. The mean particle size of gastrospheres when measured by optical microscopy technique ranged from 774 to 882 μm. The percentage of gastrosphere adhering to goat intestinal mucosal tissue varied from 10% to 65% over 8 h in 0.1N HCl, whereas this was varied from 40% to 60% in phosphate buffer pH 6.8 with provided 12 h of controlled release following zero-order release pattern. Conclusion: Studies conclude that mucilage of O. basilicum can be used as controlled release mucoadhesive material in the formulation of gastrospheres.

scholarly journals Development and In-Vitro Evaluation of pH Responsive Polymeric Nano Hydrogel Carrier System for Gastro-Protective Delivery of Naproxen Sodium

2019 ◽  
Vol 2019 ◽  
pp. 1-13
Author(s):  
Rai Muhammad Sarfraz ◽  
Muhammad Rouf Akram ◽  
Muhammad Rizwan Ali ◽  
Asif Mahmood ◽  
Muhammad Usman Khan ◽  
...  
Keyword(s):  
Drug Release ◽  
Naproxen Sodium ◽  
Research Work ◽  
Entrapment Efficiency ◽  
Gravimetric Analysis ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Swelling Behaviour ◽  
X Ray

Current research work was carried out for gastro-protective delivery of naproxen sodium. Polyethylene glycol-g-poly (methacrylic acid) nanogels was developed through free radical polymerization technique. Formulation was characterized for swelling behaviour, entrapment efficiency, Fourier transform infrared (FTIR) spectroscopy, Differential scanning calorimetry (DSC), and Thermal Gravimetric Analysis (TGA), Powder X-ray diffraction (PXRD), Zeta size distribution, and Zeta potential measurements, and in-vitro drug release. pH dependent swelling was observed with maximum drug release at higher pH. PXRD studies confirmed the conversion of loaded drug from crystalline to amorphous form while Zeta size measurement showed size reduction. On the basis of these results it was concluded that prepared nanogels proved an effective tool for gastro-protective delivery of naproxen sodium.

The preparation, characterization, structure and dissolution analysis of apremilast solvatomorphs

2017 ◽  
Vol 73 (4) ◽  
pp. 305-313 ◽  
Author(s):  
Yun-Deng Wu ◽  
Xiao-Lei Zhang ◽  
Xiao-Hong Liu ◽  
Jian Xu ◽  
Mei Zhang ◽  
...  
Keyword(s):  
Differential Scanning Calorimetry ◽  
Hydrogen Bonding ◽  
Psoriatic Arthritis ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Dissolution Rates ◽  
X Ray ◽  
Similarity Factor ◽  
Hydrogen Bonding Interactions

Apremilast (AP) {systematic name: (S)-2-[1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl]-4-acetamidoisoindoline-1,3-dione} is an inhibitor of phosphodieasterase-4 (PDE4) and is indicated for the treatment of adult patients with active psoriatic arthritis. The ability of AP to form solvates has been investigated and three solvatomorphs of AP, namely, the AP ethyl acetate hemisolvate, C22H24N2O7S·0.5C4H8O2, the AP toluene hemisolvate, C22H24N2O7S·0.5C7H8, and the AP dichloromethane monosolvate, C22H24N2O7S·CH2Cl2, were obtained. The three AP solvatomorphs were characterized by X-ray powder diffraction, thermogravimetric analysis and differential scanning calorimetry. Single-crystal X-ray diffraction was used to analyze the structures, crystal symmetry, packing modes, stoichiometry and hydrogen-bonding interactions of the solvatomorphs. In addition, dissolution analyses were performed to study the dissolution rates of different AP solvatomorph tablets in vitro and to make comparisons with commercial apremilast tablets (produced by Celgene); all three solvatomorphs showed similar dissolution rates and similar values of the similarity factor f2 in a comparison of their dissolution profiles.

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