scholarly journals Nanoliposomes as Vehicles for Astaxanthin: Characterization, In Vitro Release Evaluation and Structure

Molecules ◽  
2018 ◽  
Vol 23 (11) ◽  
pp. 2822 ◽  
Author(s):  
Li Pan ◽  
Hongyan Wang ◽  
Keren Gu

Astaxanthin was encapsulated in nanoliposomes by a film dispersion-ultrasonic technique using soybean phosphatidyl choline. The astaxanthin-loaded nanoliposomes displayed advantages in the aspects of high encapsulation efficiency and less particle size with a remarkably homodisperse size distribution. Based on X-ray diffraction and differential scanning calorimetry the analysis, it has been demonstrated that there could be interactions of astaxanthin with the lipid bilayer, resulting in the forming of astaxanthin-loaded nanoliposomes. The thermal gravimetric analysis revealed that the thermal stability of astaxanthin after encapsulation in nanoliposomes was remarkably enhanced as compared to astaxanthin alone. Furthermore, encapsulation could greatly enhance the water dispersibility of astaxanthin. This study also confirmed that encapsulation of astaxanthin in nanoliposomes could be an effective way to supply astaxanthin continuously in the body. The effects of astaxanthin incorporation on structural changes of the liposomal membrane were investigated through steady-state fluorescence measurements. This study revealed that the incorporation of astaxanthin into the lipid bilayer decreased membrane fluidity, but increased micropolarity in the membrane within a certain range of astaxanthin concentrations. Additionally, it indicated that the encapsulation of astaxanthin in the lipid bilayer could be applied to modulate the structural properties of membranes.

2019 ◽  
Vol 2019 ◽  
pp. 1-13
Author(s):  
Rai Muhammad Sarfraz ◽  
Muhammad Rouf Akram ◽  
Muhammad Rizwan Ali ◽  
Asif Mahmood ◽  
Muhammad Usman Khan ◽  
...  

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.


2022 ◽  
pp. 088532822110539
Author(s):  
Bi Wu ◽  
Yang Li ◽  
Yuan Y Li ◽  
Zhi H Shi ◽  
Xiao H Bian ◽  
...  

The aim of this study was to develop nanostructured-lipid carriers (NLC) encapsulated by Chitosan hydrogel beads for the efficient topical carrier. Dynamic light scattering (DLS), X-ray diffraction (XRD), Differential scanning calorimetry (DSC), and attenuated total reflectance-Fourier transform infrared spectroscopy (ATR-FTIR) were conducted to study the influence of the encapsulation on the characteristic of resveratrol-loaded NLC, and the results showed that there was no impact on resveratrol-loaded NLC. Chitosan hydrogel beads could significantly improve the physical stability of resveratrol-loaded NLC. In vitro release study revealed that resveratrol-loaded NLC-Chitosan hydrogel beads had a more significant sustained-release effect on resveratrol. In vitro transdermal studies suggested that the skin permeation of resveratrol was promoted by the effect of Chitosan hydrogel beads and increased resveratrol distribution in the skin. In vitro cytotoxicity showed that resveratrol-loaded NLC-Chitosan hydrogel beads did not exert a hazardous effect on L929 cells. Hence, NLC-Chitosan hydrogel beads might be a promising method for topical applications of resveratrol.


Polymers ◽  
2019 ◽  
Vol 11 (5) ◽  
pp. 917 ◽  
Author(s):  
Taieb Aouak ◽  
Wassem Sharaf Saeed ◽  
Nawaf M. Al-Hafi ◽  
Abdel-Basit Al-Odayni ◽  
Abdulaziz Ali Alghamdi ◽  
...  

2-hydroxyethyl methacrylate, methylmethacrylate, ethylene glycol dimethyl methacrylate, and lignocaine (drug) were mixed together and the monomers were copolymerized at 60 °C through a free radical polymerization in the presence of α,α′-Azoisobutyronitrile in tetrahydrofuran. A series of copolymer/drug composites with different monoacrylate monomer compositions were prepared by solvent evaporation and characterized by different methods such as nuclear magnetic resonance, differential scanning calorimetry, Fourier transform infrared, X-ray diffraction, and mechanical and optical testing. The water content in the copolymers and the cell viability test on the samples were also examined in this investigation. The results of the analyses of the properties of this drug-carrier system are promising, indicating that this material may be a potential candidate for contact lens applications. The release dynamic of this medication from the prepared drug-carrier systems was investigated in neutral pH media. The results obtained revealed that the diffusion of lignocaine through the copolymer matrix obeys the Fick model and the dynamic release can be easily controlled by the methyl methacrylate content in the copolymer.


Author(s):  
J P Raval ◽  
D R Naik

Designing and evaluating a multiparticulate controlled release dosage form, to increase the efficacy of acyclovir (a selective antiherpes agent). Spray drying technique for microsphere production is compared with novel solvent evaporation-matrix erosion technique for variable drug loading in different concentration of ethyl cellulose. The microspheres were characterized for physicochemical properties. The microspheres sizes were ranged from 7-25 μm. The spray dried microspheres had better encapsulation efficiency (up to 91%) compared to that of novel solvent evaporation-matrix erosion technique microspheres. Scanning electron microscopy confirmed spherical geometry due to high cross-linking density. Differential scanning calorimetry, Fourier-transform infrared spectroscopy and x-ray diffraction studies showed chemical stability and intactness of entrapped drug in the microspheres. In vitro release of acyclovir from spray dried microspheres continued for longer period compared to novel solvent evaporation-matrix erosion method. Overall, the release studies depended on the concentration of ethyl cellulose, extent of drug loading, and the technique used to prepare microspheres. Thus, marked retardation of drug release may provide a useful effective anti-retroviral drug therapy.  


2019 ◽  
Vol 10 (4) ◽  
pp. 2612-2621 ◽  
Author(s):  
Souvik chakraborty ◽  
Gowda D V ◽  
Vishal Gupta N

In this present research work, the development of biodegradable scaffolds loaded with Vancomycin micropartricles was carried out for the treatment of Osteomyelitis. Characterization Vancomycin Loaded microparticles and evaluation of the microparticles loaded scaffolds and also to carry out In-vitro release studies. Vancomycin hydrochloride microparticles were prepared with the help of double emulsion method. HPMC and Polaxomer 407 has been taken as the main polymers for the preparation of the microparticles. Chitosan was taken as the major polymer for the preparation of scaffolds for its greater biocompatibility and biodegradability. The preparation was done with the help of the solvent casting method. The formulation was taken for further characterization and evaluation studies. Fourier-Transform Infrared Spectroscopy and Differential scanning calorimetry were carried out for the pure vancomycin drug, and the chitosan polymer X-ray diffraction was carried out to check the crystallinity of the prepared scaffolds. The particle size, zeta potential and polydispersity index for vancomycin loaded microparticles were found to be 577.0±102.5 nm, 1624 mv and 0.254. The maximum and sustained release rate of the drug was found to be 95.6±0.478, at 16th Hr. By taking all the reports, a conclusion can be drawn that, the formulated VLM biodegradable scaffolds will show burst release at the initial time of administration, which is essential for the wound healing activity and will be sustained throughout the process of treatment of osteomyelitis.


Author(s):  
Mohammed Ibrahim ◽  
Alaa Zaky ◽  
Mohsen Afouna ◽  
Ahmed Samy

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.


Author(s):  
Venu Madhav K ◽  
Somnath De ◽  
Chandra Shekar Bonagiri ◽  
Sridhar Babu Gummadi

Fenofibrate (FN) is used in the treatment of hypercholesterolemia. It shows poor dissolution and poor oral bioavailability after oral administration due to high liphophilicity and low aqueous solubility. Hence, solid dispersions (SDs) of FN (FN-SDs) were develop that might enhance the dissolution and subsequently oral bioavailability. FN-SDs were prepared by solvent casting method using different carriers (PEG 4000, PEG 6000, β cyclodextrin and HP β cyclodextrin) in different proportions (0.25%, 0.5%, 0.75% and 1% w/v). FN-SDs were evaluated solubility, assay and in vitro release studies for the optimization of SD formulation. Differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and scanning electron microscopy (SEM) analysis was performed for crystalline and morphology analysis, respectively. Further, optimized FN-SD formulation evaluated for pharmacokinetic performance in Wistar rats, in vivo in comparison with FN suspension.  From the results, FN-SD3 and FN-SD6 have showed 102.9 ±1.3% and 105.5±3.1% drug release, respectively in 2 h. DSC and PXRD studies revealed that conversion of crystalline to amorphous nature of FN from FT-SD formulation. SEM studies revealed the change in the orientation of FN when incorporated in SDs. The oral bioavailability FN-SD3 and FN-SD6 formulations exhibited 2.5-folds and 3.1-folds improvement when compared to FN suspension as control. Overall, SD of FN could be considered as an alternative dosage form for the enhancement of oral delivery of poorly water-soluble FN.


Polymers ◽  
2021 ◽  
Vol 13 (15) ◽  
pp. 2575
Author(s):  
Smaher M. Elbayomi ◽  
Haili Wang ◽  
Tamer M. Tamer ◽  
Yezi You

The preparation of bioactive polymeric molecules requires the attention of scientists as it has a potential function in biomedical applications. In the current study, functional substitution of alginate with a benzoyl group was prepared via coupling its hydroxyl group with benzoyl chloride. Fourier transform infrared spectroscopy indicated the characteristic peaks of aromatic C=C in alginate derivative at 1431 cm−1. HNMR analysis demonstrated the aromatic protons at 7.5 ppm assigned to benzoyl groups attached to alginate hydroxyl groups. Wetting analysis showed a decrease in hydrophilicity in the new alginate derivative. Differential scanning calorimetry and thermal gravimetric analysis showed that the designed aromatic alginate derivative demonstrated higher thermo-stability than alginates. The aromatic alginate derivative displayed high anti-inflammatory properties compared to alginate. Finally, the in vitro antioxidant evaluation of the aromatic alginate derivative showed a significant increase in free radical scavenging activity compared to neat alginate against DPPH (2,2-diphenyll-picrylhydrazyl) and ABTS free radicals. The obtained results proposed that the new alginate derivative could be employed for gene and drug delivery applications.


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.


2021 ◽  
Vol 18 ◽  
Author(s):  
Sonia S. Pandey ◽  
Farhinbanu I. Shaikh ◽  
Arti R. Gupta ◽  
Rutvi J. Vaidya

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.


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