scholarly journals Optimization, Characterization and Pharmacokinetic Study of Meso-Tetraphenylporphyrin Metal Complex-Loaded PLGA Nanoparticles

2021 ◽  
Vol 22 (22) ◽  
pp. 12261
Author(s):  
Mariia R. Mollaeva ◽  
Nikita Yabbarov ◽  
Maria Sokol ◽  
Margarita Chirkina ◽  
Murad D. Mollaev ◽  
...  
Keyword(s):  
Spherical Shape ◽  
Physicochemical Characteristics ◽  
Plga Nanoparticles ◽  
Release Mechanism ◽  
X Ray Diffraction ◽  
Technological Parameters ◽  
Hemolysis Assay ◽  
Optimized Model ◽  
Nanoparticle Formulation

The selection of technological parameters for nanoparticle formulation represents a complicated development phase. Therefore, the statistical analysis based on Box–Behnken methodology is widely used to optimize technological processes, including poly(lactic-co-glycolic acid) nanoparticle formulation. In this study, we applied a two-level three-factor design to optimize the preparation of nanoparticles loaded with cobalt (CoTPP), manganese (MnClTPP), and nickel (NiTPP) metalloporphyrins (MeP). The resulting nanoparticles were examined by dynamic light scattering, X-ray diffraction, Fourier transform infrared spectroscopy, MTT test, and hemolytic activity assay. The optimized model of nanoparticle formulation was validated, and the obtained nanoparticles possessed a spherical shape and physicochemical characteristics enabling them to deliver MeP in cancer cells. In vitro hemolysis assay revealed high safety of the formulated MeP-loaded nanoparticles. The MeP release demonstrated a biphasic profile and release mechanism via Fick diffusion, according to release exponent values. Formulated MeP-loaded nanoparticles revealed significant antitumor activity and ability to generate reactive oxygen species. MnClTPP- and CoTPP-nanoparticles specifically accumulated in tissues, preventing wide tissue distribution caused by long-term circulation of the hydrophobic drug. Our results suggest that MnClTPP- and CoTPP-nanoparticles represent the greatest potential for utilization in in anticancer therapy due to their effectiveness and safety.

scholarly journals Magnetite Nanoparticles Coated with PEG 3350-Tween 80: In Vitro Characterization Using Primary Cell Cultures

Polymers ◽  
2020 ◽  
Vol 12 (2) ◽  
pp. 300 ◽  
Author(s):  
Jorge A Roacho-Pérez ◽  
Fernando G Ruiz-Hernandez ◽  
Christian Chapa-Gonzalez ◽  
Herminia G Martínez-Rodríguez ◽  
Israel A Flores-Urquizo ◽  
...  
Keyword(s):  
Stem Cells ◽  
Mesenchymal Stem Cells ◽  
Magnetic Nanoparticles ◽  
Magnetite Nanoparticles ◽  
Spherical Shape ◽  
Tween 80 ◽  
Hemolysis Assay ◽  
Adipose Mesenchymal Stem Cells ◽  
Average Size

Some medical applications of magnetic nanoparticles require direct contact with healthy tissues and blood. If nanoparticles are not designed properly, they can cause several problems, such as cytotoxicity or hemolysis. A strategy for improvement the biological proprieties of magnetic nanoparticles is their functionalization with biocompatible polymers and nonionic surfactants. In this study we compared bare magnetite nanoparticles against magnetite nanoparticles coated with a combination of polyethylene glycol 3350 (PEG 3350) and polysorbate 80 (Tween 80). Physical characteristics of nanoparticles were evaluated. A primary culture of sheep adipose mesenchymal stem cells was developed to measure nanoparticle cytotoxicity. A sample of erythrocytes from a healthy donor was used for the hemolysis assay. Results showed the successful obtention of magnetite nanoparticles coated with PEG 3350-Tween 80, with a spherical shape, average size of 119.2 nm and a zeta potential of +5.61 mV. Interaction with mesenchymal stem cells showed a non-cytotoxic propriety at doses lower than 1000 µg/mL. Interaction with erythrocytes showed a non-hemolytic propriety at doses lower than 100 µg/mL. In vitro information obtained from this work concludes that the use of magnetite nanoparticles coated with PEG 3350-Tween 80 is safe for a biological system at low doses.

scholarly journals A new strategy for the green synthesis of chondroitin sulfate-reduced gold nanoparticles; in vitro evaluation of synthesized nanoparticles

Bioimpacts ◽  
2020 ◽  
Vol 10 (4) ◽  
pp. 217-226
Author(s):  
Maryam Asariha ◽  
Azam Chahardoli ◽  
Farshad Qalekhani ◽  
Mahnaz Ghowsi ◽  
Mehdi Fouladi ◽  
...  
Keyword(s):  
Gold Nanoparticles ◽  
Antibacterial Activity ◽  
Green Synthesis ◽  
Chondroitin Sulfate ◽  
Blood Compatibility ◽  
Spherical Shape ◽  
Hemolysis Assay ◽  
Wide Range ◽  
New Strategy

introduction: The application of gold nanoparticles (GNPs) in medicine is expanding as an effective therapeutic and diagnostic compound. Different polysaccharides with high biocompatibility and hydrophilic properties have been used for synthesis and capping of GNPs. Chondroitin sulfate (CHS) as a polysaccharide possesses a wide range of biological functions e.g. anti-oxidant, anti-inflammation, anti-coagulation, anti-atherosclerosis, anti-thrombosis with insignificant immunogenicity and has not been used for the green synthesis of GNPs. Methods: GNPs were synthesized using CHS, and their physicochemical properties were evaluated. The antibacterial activity of CHS-GNPs was estimated against both gram-positive and gram-negative bacteria. The cytotoxicity of CHS and CHS-GNPs was obtained by MTT (3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide) test, and the electrocatalytic activity of CHS-GNPs was investigated. The blood compatibility was evaluated by the in vitro hemolysis assay. Results: The absorption band at 527 nm reveals the reduction of Au3+ into GNPs. The transmission electron microscopy (TEM) image displays the spherical shape of GNPs in the range of 5.8–31.4 nm. The CHS and CHS-GNPs at 300 µg/mL revealed a maximum DPPH (1, 1-diphenyl-2-picrylhydrazyl) scavenging activity of 73% and 65%, respectively. CHS-GNPs showed antibacterial activity against Bacillus subtilis, while CHS has no antibacterial activity. CHS-GNPs exhibited a cytotoxicity effect against MDA-MB-468 and βTC3 cancer cell lines, and the electrochemical study indicated a significant increase in electrocatalytic properties of CHS-GNPs coated electrode compared by the bare electrode. The hemolysis test proved the blood compatibility of CHS-GNPs. Conclusion: The results indicate the advantages of using CHS to produce blood-compatible GNPs with antioxidant, cytotoxic, and electrochemical properties.

Azacitidine Loaded PLGA Nanoparticles and their Dual Release Mechanism

2020 ◽  
Vol 10 (3) ◽  
pp. 280-289
Author(s):  
Kanchan Kashyap ◽  
Mayank Handa ◽  
Rahul Shukla
Keyword(s):  
Glioblastoma Multiforme ◽  
Drug Loading ◽  
Polymer Concentration ◽  
Plga Nanoparticles ◽  
Current Therapy ◽  
Release Mechanism ◽  
Burst Release ◽  
In Vivo Evaluation ◽  
Dual Release

Background: Glioblastoma multiforme (GBM) is a belligerent brain tumor constituting about 67% of primary brain tumours. The current therapy for glioblastoma multiforme is surgery, radiations and chemotherapy though the success rate is quite limited. Azacitidine is a hydrophilic anti-cancer agent which acts by demethylation and is used in the treatment of both acute and chronic myelomonocytic leukaemia along with GBM. Objective: Formulation of stable Azacitidine loaded poly-lactide-co-glycolide (PLGA) nanoparticles (NPs) with tailor-made release profiles. Methods: Preparation of Azacitidine loaded PLGA nanoparticles was done by double emulsion (w/o/w) solvent evaporation technique. PLGA was used in the formulation, as it is biocompatible and biodegradable. Polyvinyl alcohol worked as an emulsifier while Span 80 decreased the interfacial tension among two immiscible phases (aqueous and organic), resulting in increased stability of the formulation. Results: Polymer concentration was directly proportional to the entrapment and drug loading and inversely proportional to particle size. Azacitidine loaded PLGA NPs showed a biphasic release model. At the first stage, burst release was observed, followed by sustained release. About 43.93 ± 0.69% drug was released in 1 hour and the remaining drug was released in 48 hours. Conclusion: Dual release behavior first delivered an ample amount of dose which provided cytotoxic dose, followed by the maintenance dose for sustaining the cytotoxic drug levels. Future prospective requires In-vitro cell viability evaluation of tailor-made polymeric nanoparticles along with In-vivo evaluation for therapeutic intervention in a glioblastoma tumor model.

scholarly journals Effect of Temperature on Drug Release: Production of 5-FU-Encapsulated Hydroxyapatite-Gelatin Polymer Composites via Spray Drying and Analysis of In Vitro Kinetics

2020 ◽  
Vol 2020 ◽  
pp. 1-13
Author(s):  
Nalan Erdöl Aydin
Keyword(s):  
Drug Release ◽  
Polymer Composites ◽  
Drug Loading ◽  
Effect Of Temperature ◽  
Release Mechanism ◽  
Gravimetric Analysis ◽  
X Ray Diffraction ◽  
In Vitro Kinetics ◽  
Best Fit

In this study, 5-fluorouracil- (5-FU-) loaded hydroxyapatite-gelatin (HAp-GEL) polymer composites were produced in the presence of a simulated body fluid (SBF) to investigate the effects of temperature and cross-linking agents on drug release. The composites were produced by wet precipitation at pH 7.4 and temperature 37°C using glutaraldehyde (GA) as the cross-linker. The effects of different amounts of glutaraldehyde on drug release profiles were studied. Encapsulation (drug loading) was performed with 5-FU using a spray drier, and the drug release of 5-FU from the HAp-GEL composites was determined at temperatures of 32°C, 37°C, and 42°C. Different mathematical models were used to obtain the release mechanism of the drug. The morphologies and structures of the composites were analyzed by X-ray diffraction, thermal gravimetric analysis, Fourier transform infrared spectroscopy, and scanning electron microscopy. The results demonstrated that for the HAp-GEL composites, the initial burst decreased with increasing GA content at all three studied temperatures. Further, three kinetic models were investigated, and it was determined that all the composites best fit the Higuchi model. It was concluded that the drug-loaded HAp-GEL composites have the potential to be used in drug delivery applications.

scholarly journals Spherical crystals of celecoxib to improve solubility, dissolution rate and micromeritic properties

2007 ◽  
Vol 57 (2) ◽  
pp. 173-184 ◽  
Author(s):  
Venkadari Gupta ◽  
Srinivas Mutalik ◽  
Madhobhai Patel ◽  
Girish Jani
Keyword(s):  
Dissolution Rate ◽  
Spherical Shape ◽  
Aqueous Solubility ◽  
Spectroscopic Studies ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Acetone Water ◽  
Ir Spectroscopic ◽  
Spherical Crystals

Spherical crystals of celecoxib to improve solubility, dissolution rate and micromeritic propertiesCelecoxib spherical agglomerates were prepared with polyvinylpyrrolidone (PVP) using acetone, water and chloroform as solvent, non-solvent and bridging liquid, respectively. The agglomerates were characterized by differential scanning calorimetry (DSC), X-ray diffraction (XRD), IR spectroscopic studies and scanning electron microscopy (SEM). The IR spectroscopy and DSC results indicated the absence of any interactions between drug and additives. XRD studies showed a decrease in crystallinity in agglomerates. The crystals exhibited significantly improved micromeritic properties compared to pure drug. The loading efficiency (% or mg drug per 100 mg crystals) was in the range of 93.9 ± 2.3 and 97.3 ± 1.3% (n = 3) with all formulations. The aqueous solubility and dissolution rate of the drug from crystals was significantly (p < 0.05) increased (nearly two times). The solubility andin vitrodrug release rates increased with an increase in PVP concentration (from 2.5 to 10%). The SEM studies showed that the crystal posseses a good spherical shape with smooth and regular surface.

scholarly journals PCL/PHBV Microparticles as Innovative Carriers for Oral Controlled Release of Manidipine Dihydrochloride

2014 ◽  
Vol 2014 ◽  
pp. 1-10 ◽  
Author(s):  
Fernanda Malaquias Barboza ◽  
Willian Moreira Machado ◽  
Luiz Renato Olchanheski Junior ◽  
Josiane Padilha de Paula ◽  
Sônia Faria Zawadzki ◽  
...  
Keyword(s):  
Controlled Release ◽  
Animal Studies ◽  
Average Particle Size ◽  
Spherical Shape ◽  
Average Particle ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Chemically Modified ◽  
Diffraction Patterns

Microparticles of poly(ε-caprolactone) (PCL) and poly(3-hydroxybutyrate-co-3-hydroxyvalerate) (PHBV) containing manidipine dihydrochloride (MAN) were successfully prepared by the simple emulsion/solvent evaporation method. All formulations showed loading efficiency rates greater than 80% and average particle size less than 8 μm. Formulations had spherical shape with smooth and porous surface for PCL and PHBV, respectively. According to Fourier-transform infrared spectroscopy, initial components were not chemically modified during microencapsulation. X-ray diffraction patterns and differential scanning calorimetry demonstrated that this process led to drug amorphization.In vitrodissolution studies showed that all microparticles prolonged MAN release, mainly which one obtained using PCL that contained 5% of drug loaded (PCL-M5). Animal studies demonstrated that formulationPCL-M5was able to keep the variation of mean arterial pressure after phenylephrine administration up to 24 hours. These data confirmed the sustained antihypertensive effect of the investigated microparticles. Results provided an experimental basis for using formulationPCL-M5as a feasible carrier for oral controlled release of MAN intended for treating high blood pressure.

scholarly journals Glibenclamide-Loaded Polyvinylpyrrolidone (PVP) Nanoparticles and Glibenclamide-Loaded Soluplus® Nanomicelles Intended for Parenteral Administration: Effect of Solvents Mixtures on the Electrosprayed Nanoparticles and In vitro Characterization

2021 ◽  
pp. 241-260
Author(s):  
Maryam Al-Ghezi ◽  
Raghad F. Almilly ◽  
Wedad K. Ali
Keyword(s):  
Drug Release ◽  
Physicochemical Characteristics ◽  
Colloidal Dispersions ◽  
Parenteral Administration ◽  
Solvent Mixtures ◽  
X Ray Diffraction ◽  
Sustained Drug Release ◽  
Drug Molecules ◽  
In Vitro Characterization

Background and Objective: Glibenclamide (GB) is showing promising results in central nervous system (CNS) injuries treatment where intravenous administration of GB could overcome the oral limitations and assure maximum bioavailability. Dry powder of GB nanoparticles reconstituted for parenteral administration was prepared through electrospraying. Methods: The drug was incorporated with two polymers, polyvinylpyrrolidone (PVP) and Soluplus® (SP), at ratios 1:4 and 1:2 (GB/polymer). Different solvent mixtures were used to formulate the particles. Physicochemical characteristics were investigated. Results: The size of the GB-PVP nanoparticle ranged between (409-775) nm with a spherical, disk, fractured and, agglomerated morphology, while those of the GB-SP nanomicelles were of (447-785) nm with mostly irregular morphology, in consequence to the used solvents mixtures. The high encapsulation efficiency ≥ 98% reflects the well dispersed drug molecules within the polymer matrix, further confirmed by X-ray diffraction and infrared spectroscopy. GB-SP colloidal dispersions showed neutral zeta potentials with a cloud point of 36 ˚C, indicating prolonged circulation time and stability after parenteral administration. GB/SP nanomicelles at ratio 1:4 showed a sustained drug release reaching ≥ 94% in 36 hours. Conclusion: The GB-SP nanomicelles with extended drug release and regarding physicochemical properties represent a remarkable drug delivery system for parenteral administration.

scholarly journals Influence of Sodium Alginate Concentration on Microcapsules Properties Foreseeing the Protection and Controlled Release of Bioactive Substances

2021 ◽  
Vol 2021 ◽  
pp. 1-13
Author(s):  
Kamal Essifi ◽  
Mohamed Brahmi ◽  
Doha Berraaouan ◽  
Abderrahim Ed-Daoui ◽  
Ali El Bachiri ◽  
...  
Keyword(s):  
Uv Spectroscopy ◽  
Release Kinetics ◽  
Polymer Concentration ◽  
Physicochemical Characteristics ◽  
Release Mechanism ◽  
X Ray Diffraction ◽  
Bioactive Substances ◽  
Alginate Concentration ◽  
Bioactive Substance ◽  
Ca Alginate

To understand the abilities of Ca-alginate microcapsules and their specific applications in different fields, it is necessary to determine the physicochemical and structural properties of those formulated microcapsules. In this work, we aimed to study the effect of alginate concentration in the improvement of the encapsulation efficiency (EE) and on the release of phenolic and flavonoid substances. The relationship between the structure of the encapsulated bioactive substance and Ca-alginate network and their effect on the EE and release kinetics have been investigated. The incorporation, structure, morphology, and phase properties of all elaborated materials were characterized by UV-spectroscopy, Fourier transform infrared (ATR-FTIR), scanning electron microscope (SEM), and X-ray diffraction (DRX). The results indicate that increasing the polymer concentration increases the EE and decreases the loading capacity (LC), whereas the effect of alginate polymer concentration on the release was not observed. The release study of bioactive substances showed that the release kinetics is relatively dependent on the structure and the physicochemical characteristics of the bioactive substance, which became clear when the encapsulated compounds were released from the core of calcium alginate microcapsules. Thus, it could be concluded that the pores size of the Ca-alginate network is smaller than the volume of the crocin molecule (2794.926 Å3) and higher than the volume of the gallic acid molecule (527.659 Å3). For the same microcapsules system, the release mechanism is affected by the structure and physicochemical properties of the encapsulated molecules.

scholarly journals Ocular penetration of fluorometholone-loaded PEG-PLGA nanoparticles functionalized with cell-penetrating peptides

Nanomedicine ◽  
2019 ◽  
Vol 14 (23) ◽  
pp. 3089-3104 ◽  
Author(s):  
Roberto Gonzalez-Pizarro ◽  
Graziella Parrotta ◽  
Rodrigo Vera ◽  
Elena Sánchez-López ◽  
Ruth Galindo ◽  
...  
Keyword(s):  
Inflammatory Diseases ◽  
Physicochemical Characteristics ◽  
Plga Nanoparticles ◽  
Cell Penetrating Peptides ◽  
In Vivo Models ◽  
Corneal Epithelial ◽  
Cell Penetrating ◽  
Novel Strategy

Aim: Development of fluorometholone-loaded PEG-PLGA nanoparticles (NPs) functionalized with cell-penetrating peptides (CPPs) for the treatment of ocular inflammatory disorders. Materials & methods: Synthesized polymers and peptides were used for elaboration of functionalized NPs, which were characterized physicochemically. Cytotoxicity and ability to modulate the expression of proinflammatory cytokines were evaluated in vitro using human corneal epithelial cells (HCE-2). NPs uptake was assayed in both in vitro and in vivo models. Results: NPs showed physicochemical characteristics suitable for ocular administration without evidence of cytotoxicity. TAT-NPs and G2-NPs were internalized and displayed anti-inflammatory activity in both HCE-2 cells and mouse eye. Conclusion: TAT-NPs and G2-NPs could be considered a novel strategy for the treatment of ocular inflammatory diseases of the anterior and posterior segment.

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.

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