A nanotechnological approach in the current therapy of COVID-19: model drug oseltamivir-phosphate loaded PLGA nanoparticles targeted with spike protein binder peptide of SARS-CoV-2

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.

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

Australian Journal of Chemistry ◽

10.1071/ch19359 ◽

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.

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Co-encapsulation of human serum albumin and superparamagnetic iron oxide in PLGA nanoparticles: Part II. Effect of process variables on protein model drug encapsulation efficiency

Journal of Microencapsulation ◽

10.3109/02652048.2013.814730 ◽

2013 ◽

Vol 31 (2) ◽

pp. 156-165 ◽

Cited By ~ 10

Author(s):

Quazi T. H. Shubhra ◽

Tivadar Feczkó ◽

Andrea F. Kardos ◽

Judit Tóth ◽

Hana Mackova ◽

...

Keyword(s):

Iron Oxide ◽

Human Serum Albumin ◽

Serum Albumin ◽

Encapsulation Efficiency ◽

Superparamagnetic Iron Oxide ◽

Plga Nanoparticles ◽

Process Variables ◽

Protein Model ◽

Model Drug ◽

Drug Encapsulation Efficiency

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Exploring the systemic delivery of a poorly water-soluble model drug to the retina using PLGA nanoparticles

European Journal of Pharmaceutical Sciences ◽

10.1016/j.ejps.2021.105905 ◽

2021 ◽

pp. 105905

Author(s):

Enqi Zhang ◽

Nadezhda Osipova ◽

Maxim Sokolov ◽

Olga Maksimenko ◽

Aleksey Semyonkin ◽

...

Keyword(s):

Plga Nanoparticles ◽

Water Soluble ◽

Systemic Delivery ◽

Soluble Model ◽

Poorly Water Soluble ◽

Model Drug

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Development of Drug Loaded Nanoparticles Binding to Hydroxyapatite Based on a Bisphosphonate Modified Nonionic Surfactant

Journal of Nanomaterials ◽

10.1155/2015/393968 ◽

2015 ◽

Vol 2015 ◽

pp. 1-12

Author(s):

Jiabin Zhang ◽

Xinrong Liu ◽

Tongming Deng ◽

Peng Yao ◽

Heliang Song ◽

...

Keyword(s):

Bone Graft ◽

Nonionic Surfactant ◽

Plga Nanoparticles ◽

Hydroxyl Group ◽

Binding Affinities ◽

Functionalized Nanoparticles ◽

Affinity Ligand ◽

Drug Eluting ◽

Bone Graft Substitutes ◽

Model Drug

This study aimed at development of drug loaded nanoparticles which could bind to hydroxyapatite (HA) to construct drug or growth factor releasing bone graft substitutes. To this end, the terminal hydroxyl group of a nonionic surfactant Brij 78 (polyoxyethylene (20) stearyl ether) was first modified with pamidronate (Pa). Using Pa-Brij 78 as both a surfactant and an affinity ligand to HA, three different Pa surface functionalized nanoparticles were prepared, named as solid lipid nanoparticles (Pa-SNPs), nanoemulsions (Pa-NEMs), and PLGA nanoparticles (Pa-PNPs). A model drug curcumin was successfully encapsulated in the three nanoparticles. The sizes of Pa-NEM and Pa-PNP were around 150 nm and the size of Pa-SNP was around 90 nm with polydispersity indexes (PDIs) less than 0.20. Drug encapsulation efficiencies of the three nanoparticles were all greater than 85%. Furthermore, the order of binding affinity of the nanoparticles to HA wasPa-PNP>Pa-NEM=Pa-SNP. After lyophilization, the sizes of the three nanoparticles were increased about 0.5–2.0-fold but their binding affinities to HA were almost the same as the fresh prepared nanoparticles. In conclusion, a Pa-modified Brij 78 was synthesized and used for fabrication of a series of drug loaded nanoparticles to construct drug-eluting HA-based bone graft substitutes.

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Preparation and Release Profiles of a Solid Oleoylchitosan Coated Poly(lactic-co-glycolic acid) Nanoparticles

Advanced Materials Research ◽

10.4028/www.scientific.net/amr.936.717 ◽

2014 ◽

Vol 936 ◽

pp. 717-722

Author(s):

Yan Yan Li ◽

Feng Song Liu

Keyword(s):

Drug Release ◽

Glycolic Acid ◽

Entrapment Efficiency ◽

Plga Nanoparticles ◽

Release Behavior ◽

Release Rates ◽

In Vitro Drug Release ◽

Drug Entrapment Efficiency ◽

Model Drug

A solid oleoylchitosan (OCS) coated Poly (lactic-co-glycolic acid) (PLGA) nanoparticles (OCS-coated PLGA NPs) were prepared using the emulsification–evaporation method. The nanoparticles in suspension (TEM) and solid state (SEM) were spherical and very regular and compact. The effects of OCS concentration, PLGA concentration, drug concentration, and release media on drug entrapment efficiency and in vitro drug release behavior were investigated for the release properties using rifampicin (RFP) as a model drug. Both the increase of PLGA concentration and the increase of OCS concentration could decrease the drug release rates. The RFP release rates decreased as the RFP concentration increased. The RFP release rate was sensitive to the pH of the release media.

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