Microfluidic Synthesis of Rifampicin Loaded PLGA Nanoparticles and the Effect of Formulation on their Physical and Antibacterial Properties

2020 ◽  
Vol 73 (3) ◽  
pp. 151
Author(s):  
Thomas G. Meikle ◽  
Calum J. Drummond ◽  
Charlotte E. Conn
Keyword(s):  
Oleic Acid ◽  
Release Kinetics ◽  
Antibacterial Properties ◽  
Fold Increase ◽  
Plga Nanoparticles ◽  
Spectrophotometric Analysis ◽  
Poly Vinyl Alcohol ◽  
Synthesis Methods ◽  
Loading Efficiency ◽  
Model Drug

The encapsulation of drugs in nanoparticles serves as an effective way to modify pharmacokinetics and therapeutic efficacy. Nanoparticles comprised of poly(d,l-lactide-co-glycolide) (PLGA) are well suited for this purpose; they are accessible using multiple synthesis methods, are highly biocompatible and biodegradable, and possess desirable drug release properties. In the present study, we have explored the effects of various formulation parameters on the physical properties of PLGA nanoparticles synthesised using a microfluidic assisted nanoprecipitation method and loaded with a model drug. PLGA nanoparticles, with diameters ranging from 165–364nm, were produced using three alternate stabilisers; poly(vinyl alcohol) (PVA), d-α-tocopheryl polyethylene glycol 1000 succinate (TPGS), and didodecyldimethylammonium bromide (DMAB). Three additional formulations used PVA in addition to 20wt-% 1,2-dioleoyl-3-trimethylammonium-propane (DOTAP), 1,2-di-O-octadecenyl-3-trimethylammonium propane (DOTMA), and oleic acid. Spectrophotometric analysis demonstrated that the use of PVA increased the loading efficiency over that of TPGS and DMAB formulations, while the inclusion of oleic acid in the PVA formulation resulted in a further 3-fold increase in loading efficiency. Invitro release studies demonstrate that the inclusion of lipid additives significantly alters release kinetics; release was most rapid and complete in the formulation containing oleic acid, while the addition of DOTAP and DOTMA significantly reduced release rates. Finally, the antimicrobial activity of each formulation was tested against Staphylococcus aureus and Bacillus cereus, with minimum inhibitory concentrations nearing or exceeding that of free rifampicin.

scholarly journals Encapsulation of Large-Size Plasmids in PLGA Nanoparticles for Gene Editing: Comparison of Three Different Synthesis Methods

Nanomaterials ◽  
2021 ◽  
Vol 11 (10) ◽  
pp. 2723
Author(s):  
Tresa López-Royo ◽  
Víctor Sebastián ◽  
Laura Moreno-Martínez ◽  
Laura Uson ◽  
Cristina Yus ◽  
...  
Keyword(s):  
Electrostatic Interactions ◽  
Gene Editing ◽  
Structural Integrity ◽  
Viral Vector ◽  
Release Kinetics ◽  
Double Emulsion ◽  
Plga Nanoparticles ◽  
Synthesis Methods ◽  
Experimental Conditions ◽  
Large Size

The development of new gene-editing technologies has fostered the need for efficient and safe vectors capable of encapsulating large nucleic acids. In this work we evaluate the synthesis of large-size plasmid-loaded PLGA nanoparticles by double emulsion (considering batch ultrasound and microfluidics-assisted methodologies) and magnetic stirring-based nanoprecipitation synthesis methods. For this purpose, we characterized the nanoparticles and compared the results between the different synthesis processes in terms of encapsulation efficiency, morphology, particle size, polydispersity, zeta potential and structural integrity of loaded pDNA. Our results demonstrate particular sensibility of large pDNA for shear and mechanical stress degradation during double emulsion, the nanoprecipitation method being the only one that preserved plasmid integrity. However, plasmid-loaded PLGA nanoparticles synthesized by nanoprecipitation did not show cell expression in vitro, possibly due to the slow release profile observed in our experimental conditions. Strong electrostatic interactions between the large plasmid and the cationic PLGA used for this synthesis may underlie this release kinetics. Overall, none of the methods evaluated satisfied all the requirements for an efficient non-viral vector when applied to large-size plasmid encapsulation. Further optimization or alternative synthesis methods are thus in current need to adapt PLGA nanoparticles as delivery vectors for gene editing therapeutic technologies.

Incorporation, Release, and Effectiveness of Dexamethasone in Poly(Lactic-Co-Glycolic Acid) Nanoparticles for Inner Ear Drug Delivery

2011 ◽  
Vol 2 (1) ◽  
Author(s):  
Youdan Wang ◽  
Xinsheng Gao ◽  
Satish Kuriyavar ◽  
David Bourne ◽  
Brian Grady ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Inner Ear ◽  
Cell Damage ◽  
Release Kinetics ◽  
Drug Loading ◽  
Superparamagnetic Iron Oxide ◽  
Plga Nanoparticles ◽  
Submicron Particles ◽  
Loading Efficiency

Poly (D,L-lactide-co-glycolide) (PLGA) particles have been widely used as drug delivery carriers for a variety of payloads. Three forms of dexamethasone (DEX), namely, acetate, base, and phosphate, were incorporated into a PLGA matrix. First, we compared the drug loading efficiency and release kinetics of drug-loaded PLGA particles. Dexamethasone acetate (DEX-Ac) loaded particles exhibited a higher loading efficiency and a more linear release profile of drug as compared with the other forms of DEX particles. Also, we coincorporated oleic acid-coated superparamagnetic iron oxide nanoparticles (SPION) with DEX-Ac into PLGA submicron particles. No differences in size, zeta potential, drug loading, or release kinetics were found between particles prepared with and without SPION. Additionally, particles were applied to an in vitro cochlear, organotypic culture. DEX-Ac PLGA nanoparticles showed a protective effect against 4-hydroxynonenal induced hair cell damage. These results suggest a promising method for inner ear magnetic targeted treatment.

scholarly journals Novel Hydrogels of Chitosan and Poly (vinyl alcohol) Reinforced with Inorganic Particles of Bioactive Glass

Polymers ◽  
2021 ◽  
Vol 13 (5) ◽  
pp. 691
Author(s):  
O. Sánchez-Aguinagalde ◽  
Ainhoa Lejardi ◽  
Emilio Meaurio ◽  
Rebeca Hernández ◽  
Carmen Mijangos ◽  
...  
Keyword(s):  
Mechanical Properties ◽  
Drug Release ◽  
Bioactive Glass ◽  
Vinyl Alcohol ◽  
Release Kinetics ◽  
The Body ◽  
Poly Vinyl Alcohol ◽  
X Ray Diffraction ◽  
Inorganic Particles ◽  
Release Studies

Chitosan (CS) and poly (vinyl alcohol) (PVA) hydrogels, a polymeric system that shows a broad potential in biomedical applications, were developed. Despite the advantages they present, their mechanical properties are insufficient to support the loads that appear on the body. Thus, it was proposed to reinforce these gels with inorganic glass particles (BG) in order to improve mechanical properties and bioactivity and to see how this reinforcement affects levofloxacin drug release kinetics. Scanning electron microscopy (SEM), X-ray diffraction (XRD), swelling tests, rheology and drug release studies characterized the resulting hydrogels. The experimental results verified the bioactivity of these gels, showed an improvement of the mechanical properties and proved that the added bioactive glass does affect the release kinetics.

Formulation and Characterization of Oleic Acid Magnetic PEG PLGA Nanoparticles for Targeting Glioblastoma Multiforme

2021 ◽  
pp. 167970
Author(s):  
Khushboo Jani ◽  
Neeraj Kaushal ◽  
Mostafa Sadoqi ◽  
Gen Long ◽  
Zhe-Sheng Chen ◽  
...  
Keyword(s):  
Oleic Acid ◽  
Glioblastoma Multiforme ◽  
Plga Nanoparticles

Phthalocyanine functionalized poly(vinyl alcohol)s via CuAAC click chemistry and their antibacterial properties

2020 ◽  
Vol 17 (6) ◽  
pp. 1587-1596
Author(s):  
Ilke Gurol ◽  
Cagatay Altinkok ◽  
Esra Agel ◽  
Cihat Tasaltin ◽  
Mahmut Durmuş ◽  
...  
Keyword(s):  
Click Chemistry ◽  
Vinyl Alcohol ◽  
Antibacterial Properties ◽  
Poly Vinyl Alcohol

scholarly journals Development of a reservoir type prolonged release system with felodipine via simplex methodology

2015 ◽  
Vol 89 (1) ◽  
pp. 128-136
Author(s):  
Rareș Iuliu Iovanov ◽  
Ioan Tomuță ◽  
Sorin Emilian Leucuța
Keyword(s):  
Simplex Method ◽  
Release Kinetics ◽  
Prolonged Release ◽  
Lauryl Sulfate ◽  
Pore Former ◽  
Release System ◽  
Reservoir Type ◽  
Model Drug ◽  
Kinetics Of

Background and aims. Felodipine is a dihydropyridine calcium antagonist that presents good characteristics to be formulated as prolonged release preparations. The aim of the study was the formulation and in vitro characterization of a reservoir type prolonged release system with felodipine, over a 12 hours period using the Simplex method.Methods. The first step of the Simplex method was to study the influence of the granules coating method on the felodipine release. Furthermore the influence of the coating polymer type, the percent of the coating polymer and the percent of pore forming agent in the coating on the felodipine release were studied. Afterwards these two steps of the experimental design the percent of Surelease applied on the felodipine loaded granules and the percent of pore former in the polymeric coating formulation variables were studied. The in vitro dissolution of model drug was performed in phosphate buffer solution (pH 6.5) with 1% sodium lauryl sulfate. The released drug quantification was done using an HPLC method. The release kinetics of felodipine from the final granules was assessed using different mathematical models.Results. A 12 hours release was achieved using granules with the size between 315 – 500 µm coated with 45% Surelease with different pore former ratios in the coating via the top-spray method.Conclusion. We have prepared prolonged release coated granules with felodipine using a fluid bed system based on the Simplex method. The API from the studied final formulations was released over a 12 hours period and the release kinetics of the model drug substance from the optimized preparations fitted best the Higuchi and Peppas kinetic models. 

scholarly journals Morphology and Release Kinetics of Protein-Loaded Porous Poly(L-Lactic Acid) Spheres Prepared by Freeze-Drying Technique

2011 ◽  
Vol 2011 ◽  
pp. 1-8 ◽  
Author(s):  
Takashi Sasaki ◽  
Kazuki Tanaka ◽  
Daisuke Morino ◽  
Kensuke Sakurai
Keyword(s):  
Lactic Acid ◽  
Freeze Drying ◽  
Release Kinetics ◽  
Particle Surface ◽  
Spherical Particles ◽  
Freeze Dried ◽  
Model Drug ◽  
Drug Compound ◽  
Kinetics Of ◽  
Step Mechanism

Freeze-drying a biodegradable polymer, poly(L-lactic acid) (PLLA), from 1,4-dioxane solutions provided very porous spherical particles of ca. 3 mm in radius with specific surface area of 8–13 m2 g−1. The surface of the particle was found to be less porous compared with its interior. To apply the freeze-dried PLLA (FDPLLA) to drug delivery system, its morphology and drug releasing kinetics were investigated, bovine serum albumin (BSA) being used as a model drug compound. Immersion of FDPLLA into a BSA aqueous solution gave BSA-loaded FDPLLA, where mass fraction of the adsorbed BSA reached up to 79%. Time-dependent release profile of BSA in water suggested a two-step mechanism: (1) very rapid release of BSA deposited on and near the particle surface, which results in an initial burst, and (2) leaching of BSA from the interior of the particle by the diffusion process. It was suggested that the latter process is largely governed by the surface porosity. The porosity of both the interior and surface was found to decrease remarkably as the concentration of the original PLLA/1,4-dioxane solution increases, C0. Thus, C0 is a key parameter that controls the loading and releasing of BSA.

Synthesis, characterization and formulation of sodium calcium silicate bioceramic for drug delivery applications

2016 ◽  
Vol 23 (4) ◽  
pp. 375-380
Author(s):  
P. Manohar Reddy ◽  
Ravy Lakshmi ◽  
Febin Prabhu Dass ◽  
Swamiappan Sasikumar
Keyword(s):  
Drug Delivery ◽  
Calcium Silicate ◽  
Release Kinetics ◽  
Release Profile ◽  
Apatite Formation ◽  
X Ray Diffraction ◽  
Drug Release Profile ◽  
Sodium Calcium ◽  
Calcium Magnesium ◽  
Model Drug

AbstractSodium calcium silicate (Na2CaSiO4) is a bioactive silicate with Na2O, CaO and SiO2 as its basic components, which is similar to that of the composition of bioactive glasses. In the present study, pure sodium calcium silicate was synthesized by rapid combustion technique, and the synthesized sample was characterized by powder X-ray diffraction to check the phase purity. The scaffolds were prepared by varying the ratio of sodium calcium silicate and polyvinyl alcohol, and the apatite-formation ability of the scaffolds was examined by soaking them in a simulated body fluid. The results revealed the formation of hydroxyapatite on the surface of the scaffold after 5 days, which is found to be rapid when compared with the bioactivity of the calcium silicates and calcium magnesium silicates. The scaffolds were also loaded with ciprofloxacin as a model drug and analyzed for its drug release profile using UV spectrophotometer. The release profile did not vary with the change in bioceramic-to-biopolymer ratio, and 60% of the drug was released in 10 days, which is within the appreciable range for a targeted drug delivery system. Moreover, the experimental and simulated values of the release kinetics were compared by applying the existing mathematical model.

scholarly journals Sustained VEGF delivery via PLGA nanoparticles promotes vascular growth

2010 ◽  
Vol 298 (6) ◽  
pp. H1959-H1965 ◽  
Author(s):  
Justin S. Golub ◽  
Young-tae Kim ◽  
Craig L. Duvall ◽  
Ravi V. Bellamkonda ◽  
Divya Gupta ◽  
...  
Keyword(s):  
Tissue Engineering ◽  
Blood Vessel ◽  
Femoral Artery ◽  
Release Kinetics ◽  
Aortic Ring ◽  
Plga Nanoparticles ◽  
Cardiovascular Medicine ◽  
Vessel Growth ◽  
Vessel Volume

Technologies to increase tissue vascularity are critically important to the fields of tissue engineering and cardiovascular medicine. Currently, limited technologies exist to encourage angiogenesis and arteriogenesis in a controlled manner. In the present study, we describe an injectable controlled release system consisting of VEGF encapsulated in poly(lactic- co-glycolic acid) (PLGA) nanoparticles (NPs). The majority of VEGF was released gradually over 2–4 days from the NPs as determined by an ELISA release kinetics experiment. An in vitro aortic ring bioassay was used to verify the bioactivity of VEGF-NPs compared with empty NPs and no treatment. A mouse femoral artery ischemia model was then used to measure revascularization in VEGF-NP-treated limbs compared with limbs treated with naked VEGF and saline. 129/Sv mice were anesthetized with isoflurane, and a region of the common femoral artery and vein was ligated and excised. Mice were then injected with VEGF-NPs, naked VEGF, or saline. After 4 days, three-dimensional microcomputed tomography angiography was used to quantify vessel growth and morphology. Mice that received VEGF-NP treatment showed a significant increase in total vessel volume and vessel connectivity compared with 5 μg VEGF, 2.5 μg VEGF, and saline treatment (all P < 0.001). When the yield of the fabrication process was taken into account, VEGF-NPs were over an order of magnitude more potent than naked VEGF in increasing blood vessel volume. Differences between the VEGF-NP group and all other groups were even greater when only small-sized vessels under 300 μm diameter were analyzed. In conclusion, sustained VEGF delivery via PLGA NPs shows promise for encouraging blood vessel growth in tissue engineering and cardiovascular medicine applications.

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