scholarly journals Nanoparticles and Colloidal Hydrogels of Chitosan–Caseinate Polyelectrolyte Complexes for Drug-Controlled Release Applications

2020 ◽  
Vol 21 (16) ◽  
pp. 5602
Author(s):  
Aastha Lall ◽  
Arnaud Kamdem Tamo ◽  
Ingo Doench ◽  
Laurent David ◽  
Paula Nunes de Oliveira ◽  
...  

Chitosan–caseinate nanoparticles were synthesized by polyelectrolyte complex (PEC) formation. Caseinate is an anionic micellar nanocolloid in aqueous solutions, which association with the polycationic chitosan yielded polyelectrolyte complexes with caseinate cores surrounded by a chitosan corona. The pre-structuration of caseinate micelles facilitates the formation of natural polyelectrolyte nanoparticles with good stability and sizes around 200 nm. Such natural nanoparticles can be loaded with molecules for applications in drug-controlled release. In the nanoparticles processing, parameters such as the chitosan degree of acetylation (DA) and molecular weight, order of addition of the polyelectrolytes chitosan (polycation) and caseinate (polyanion), and added weight ratio of polycation:polyanion were varied, which were shown to influence the structure of the polyelectrolyte association, the nanoparticle size and zeta potential. Attenuated total reflection-Fourier transform infrared (ATR-FTIR) analyses revealed the chemical structure of hydrogel colloidal systems consisting of nanoparticles that contain chitosan and caseinate. Transmission electron microscopy (TEM) allowed further characterization of the spherical morphology of the nanoparticles. Furtherly, insulin was chosen as a model drug to study the application of the nanoparticles as a safe biodegradable nanocarrier system for drug-controlled release. An insulin entrapment efficiency of 75% was achieved in the chitosan-caseinate nanoparticles.

Author(s):  
MUTHADI RADHIKA REDDY ◽  
SOUMYASTUTIPATNAIK

Objective: Flutrimazole is a topical antifungal agent which displays potent broad spectrum in vitro activity against dermatophytes, filamentous fungi, and yeasts. The purpose of the present study is to formulate and evaluate microspheres loaded topical gel containing flutrimazole as model drug microspheres were prepared using aqueous ionotropic gelation method. Methods: Different polymers, the different drug to polymer(s) ratio(s) and other parameters were screened to study their effects on the properties of microspheres and to optimize each parameter. The controlled release emulgel was formulated by changing the polymer ratio. Fourier transform infrared study confirmed the purity of the drug, concede no interaction between the drug and excipients and analyze the parameters affecting the morphology and other characteristics of the resultant products employing scanning electron microscopy. Results: Microspheres loaded topical gel has been shown that encapsulation and controlled release of flutrimazole could reduce the side effect while also reducing percutaneous absorption when administered to the skin. The microspheres obtained were subjected to the preformulation studies such as bulk density, tapped density, angle of repose, Carr’s index, and Hausner’s ratio the results obtained were within the limit. The microspheres were characterized by percentage yield, drug entrapment efficiency, and particle size analysis, then the optimized microspheres formulation were incorporated into the gel prepared with various polymer(s) ratio(s) and were evaluated by parameters such as visual inspection, pH measurement, spreadability studies, viscosity, and in vitro drug release using Franz diffusion cell. Conclusion: The result of studies revealed that the optimized batch shows 97.24% release in 12 h and stable for around there. The microsphere loaded gel has advantages such as efficient absorption and more drug retention time.


Nanomaterials ◽  
2021 ◽  
Vol 11 (9) ◽  
pp. 2438
Author(s):  
Hassan Mohamed El-Said Azzazy ◽  
Sherif Ashraf Fahmy ◽  
Noha Khalil Mahdy ◽  
Meselhy Ragab Meselhy ◽  
Udo Bakowsky

Wound healing is a major healthcare concern, and complicated wounds may lead to severe outcomes such as septicemia and amputations. To date, management choices are limited, which warrants the search for new potent wound healing agents. Natural products loaded in poly (lactic-co-glycolic acid) (PLGA) coated with chitosan (CS) constitute a promising antibacterial wound healing formulation. In this work, harmala alkaloid-rich fraction (HARF) loaded into PLGA nanoparticles coated with chitosan (H/CS/PLGA NPs) were designed using the emulsion-solvent evaporation method. Optimization of the formulation variables (HARF: PLGA and CS: PLGA weight ratios, sonication time) was performed using the 33 Box–Behnken design (BBD). The optimal NPs were characterized using transmission electron microscopy (TEM) and Attenuated Total Reflection Fourier-Transformed Infrared Spectroscopy (ATR-FTIR). The prepared NPs had an average particle size of 202.27 ± 2.44 nm, a PDI of 0.23 ± 0.01, a zeta potential of 9.22 ± 0.94 mV, and an entrapment efficiency of 86.77 ± 4.18%. In vitro drug release experiments showed a biphasic pattern where an initial burst of 82.50 ± 0.20% took place in the first 2 h, which increased to 87.50 ± 0.50% over 72 h. The designed optimal H/CS/PLGA NPs exerted high antibacterial activity against Staphylococcus aureus and Escherichia coli (MIC of 0.125 and 0.06 mg/mL, respectively) compared to unloaded HARF (MIC of 0.50 mg/mL). The prepared nanoparticles were found to be biocompatible when tested on human skin fibroblasts. Moreover, the wound closure percentage after 24 h of applying H/CS/PLGA NPs was found to be 94.4 ± 8.0%, compared to free HARF and blank NPs (68.20 ± 5.10 and 50.50 ± 9.40%, respectively). In conclusion, the three components of the developed nanoformulation (PLGA, chitosan, and HARF) have synergistic antibacterial and wound healing properties for the management of infected wounds.


2021 ◽  
Vol 11 (3) ◽  
pp. 462-473
Author(s):  
Gunjan P Malode ◽  
Sagar N Ande ◽  
Sarin A Chavhan ◽  
Shivam A Bartare ◽  
Lochana L Malode ◽  
...  

Nanoemulsions have small droplet size and are kinetically stable colloidal systems. These are the thermodynamically stable isotropic system in which two immiscible liquids are mixed to form a single phase by means of appropriate surfactant and co-surfactant. Nanoemulsion droplet sizes fall typically in the range of 20-200 nm and shows narrow size distribution. They have enhanced functional properties in comparison to conventional emulsions. The composition and structure of the nanoemulsions can be controlled for the encapsulation and effective delivery of bioactive lipophilic compounds. Nanoemulsions have potential application in the food industry for the delivery of nutraceuticals, coloring and flavoring agents, and antimicrobials. This review aims to provide consolidated information regarding various formulation and characterization techniques developed for nanoemulsions. Various characterization techniques for nanoemulsions include determination of entrapment efficiency, particle size, polydispersity index, zeta potential as well as characterization through differential scanning calorimetry, Fourier-transform infrared spectroscopy and transmission electron microscopy.


2019 ◽  
Vol 2019 ◽  
pp. 1-12 ◽  
Author(s):  
Nunthiya Deepuppha ◽  
Sudarat Khadsai ◽  
Boonjira Rutnakornpituk ◽  
Uthai Wichai ◽  
Metha Rutnakornpituk

pH- and thermoresponsive nanocomposite composed of poly(N-acryloyl glycine) (PNAG) matrix and magnetite nanoparticle (MNP) was synthesized and then used for drug controlled release application. The effects of crosslinkers, e.g., ethylenediamine and tris(2-aminoethyl)amine, and their concentrations (1 and 10 mol%) on the size, magnetic separation ability, and water dispersibility of the nanocomposite were investigated. The nanocomposite crosslinked with tris(2-aminoethyl)amine (size ranging between 50 and 150 nm in diameter) can be rapidly separated by a magnet while maintaining its good dispersibility in water. It can respond to the pH and temperature change as indicated by the changes in its zeta potential and hydrodynamic size. From the in vitro release study, theophylline as a model drug was rapidly released when the pH changed from neutral to acidic/basic conditions or when increasing the temperature from 10°C to 37°C. This novel nanocomposite showed a potential application as a magnetically guidable vehicle for drug controlled release with pH- and thermotriggered mechanism.


Author(s):  
D.M. Vanderwalker

Aluminum-lithium alloys have a low density and high strength to weight ratio. They are being developed for the aerospace industry.The high strength of Al-Li can be attributed to precipitation hardening. Unfortunately when aged, Al-Li aquires a low ductility and fracture toughness. The precipitate in Al-Li is part of a sequence SSSS → Al3Li → AlLi A description of the phases may be found in reference 1 . This paper is primarily concerned with the Al3Li phase. The addition of Zr to Al-Li is being explored to find the optimum in properties. Zirconium improves fracture toughness and inhibits recrystallization. This study is a comparision between two Al-Li-Zr alloys differing in Zr concentration.Al-2.99Li-0.17Zr(alloy A) and Al-2.99Li-0.67Zr (alloy B) were solutionized for one hour at 500oc followed by a water quench. The specimens were then aged at 150°C for 16 or 40 hours. The foils were punched into 3mm discs. The specimens were electropolished with a 1/3 nitric acid 2/3 methanol solution. The transmission electron microscopy was conducted on the JEM 200CX microscope.


Author(s):  
Mashkura Ashrafi ◽  
Jakir Ahmed Chowdhury ◽  
Md Selim Reza

Capsules of different formulations were prepared by using a hydrophilic polymer, xanthan gum and a filler Ludipress. Metformin hydrochloride, which is an anti-diabetic agent, was used as a model drug here with the aim to formulate sustained release capsules. In the first 6 formulations, metformin hydrochloride and xanthan gum were used in different ratio. Later, Ludipress was added to the formulations in a percentage of 8% to 41%. The total procedure was carried out by physical mixing of the ingredients and filling in capsule shells of size ‘1’. As metformin hydrochloride is a highly water soluble drug, the dissolution test was done in 250 ml distilled water in a thermal shaker (Memmert) with a shaking speed of 50 rpm at 370C &plusmn 0.50C for 6 hours. After the dissolution, the data were treated with different kinetic models. The results found from the graphs and data show that the formulations follow the Higuchian release pattern as they showed correlation coefficients greater than 0.99 and the sustaining effect of the formulations was very high when the xanthan gum was used in a very high ratio with the drug. It was also investigated that the Ludipress extended the sustaining effect of the formulation to some extent. But after a certain period, Ludipress did not show any significant effect as the pores made by the xanthan gum network were already blocked. It is found here that when the metformin hydrochloride and the xanthan gum ratio was 1:1, showed a high percentage of drug release, i.e. 91.80% of drug was released after 6 hours. But With a xanthan gum and metformin hydrochloride ratio of 6:1, a very slow release of the drug was obtained. Only 66.68% of the drug was released after 6 hours. The percent loading in this case was 14%. Again, when Ludipress was used in high ratio, it was found to retard the release rate more prominently. Key words: Metformin Hydrochloride, Xanthan Gum, Controlled release capsule Dhaka Univ. J. Pharm. Sci. Vol.4(1) 2005 The full text is of this article is available at the Dhaka Univ. J. Pharm. Sci. website


2018 ◽  
Vol 69 (2) ◽  
pp. 321-323
Author(s):  
Georgeta Zegan ◽  
Elena Mihaela Carausu ◽  
Loredana Golovcencu ◽  
Alina Sodor Botezatu ◽  
Eduard Radu Cernei ◽  
...  

Anionic clay matrix acting as drug controlled release system have shown in last years a great potential for delivery of bioactive molecules and chemical therapeutics. This organic-inorganic nanohybrid system is high efficient offering an excellent protection of intercalated compounds from degradation. Compared to other nanoparticles used in medical area, anionic clays type layered double hydroxides have found to be biocompatible according to toxicological studies. Ampicillin containing MgAlLDHs and ZnAlLDH samples have been prepared following two routes: anion-exchange procedure and reconstruction from calcined layered double hydroxides. Solid samples have been characterized by FTIR and SEM-EDX highlighting the alteration of pristine LDHs structure when the antibiotic is introduced in the interlayer gallery.


2020 ◽  
Vol 14 (3) ◽  
pp. 210-224
Author(s):  
Gayatri Patel ◽  
Bindu K.N. Yadav

Background: The purpose of this study was to formulate, characterize and in-vitro cytotoxicity of 5-Fluorouracil loaded controlled release nanoparticles for the treatment of skin cancer. The patents on nanoparticles (US8414926B1), (US61654404A), (WO2007150075A3) etc. helped in the selection polymers and method for the preparation of nanoparticles. Methods: In the present study nanoparticles were prepared by simple ionic gelation method using various concentrations of chitosan and sodium tripolyphosphate (TPP). Several process and formulation parameters were screened and optimized using 25-2 fractional factorial design. The prepared nanoparticles were evaluated for particle size, shape, charge, entrapment efficiency, crosslinking mechanism and drug release study. Results: The optimized 5-Fluorouracil loaded nanoparticle were found with particle size of of 320±2.1 nm, entrapment efficiency of 85.12%± 1.1% and Zeta potential of 29mv±1mv. Scanning electron microscopy and dynamic light scattering technique revealed spherical particles with uniform size. The invitro release profile showed controlled release up to 24 hr. Further study was carried using A375 basal cell carcinoma cell-line to elucidate the mechanism of its cytotoxicity by MTT assay. Conclusion: These results demonstrate that the possibility of delivering 5-Fluorouracil to skin with enhanced encapsulation efficiency indicating effectiveness of the formulation for treatment of basal cell carcinoma type of skin cancer.


2020 ◽  
Vol 6 (1) ◽  
Author(s):  
Chukwuebuka H. Ozoude ◽  
Chukwuemeka P. Azubuike ◽  
Modupe O. Ologunagba ◽  
Sejoro S. Tonuewa ◽  
Cecilia I. Igwilo

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.


2012 ◽  
Vol 730-732 ◽  
pp. 925-930
Author(s):  
Daniela Nunes ◽  
Vanessa Livramento ◽  
Horácio Fernandes ◽  
Carlos Silva ◽  
Nobumitsu Shohoji ◽  
...  

Nanostructured copper-diamond composites can be tailored for thermal management applications at high temperature. A novel approach based on multiscale diamond dispersions is proposed for the production of this type of materials: a Cu-nDiamond composite produced by high-energy milling is used as a nanostructured matrix for further dispersion of micrometer sized diamond. The former offers strength and microstructural thermal stability while the latter provides high thermal conductivity. A series of Cu-nDiamond mixtures have been milled to define the minimum nanodiamond fraction suitable for matrix refinement and thermal stabilization. A refined matrix with homogenously dispersed nanoparticles could be obtained with 4 at.% nanodiamond for posterior mixture with mDiamond and subsequent consolidation. In order to define optimal processing parameters, consolidation by hot extrusion has been carried out for a Cu-nDiamond composite and, in parallel, for a mixture of pure copper and mDiamond. The materials produced were characterized by X-ray diffraction, scanning and transmission electron microscopy and microhardness measurements.


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