Appraisal of amiodarone-loaded PLGA nanoparticles for prospective safety and toxicity in a rat model

Motawea, Amira; Ahmed, Dalia; Eladl, Amira; El-Mansy, Ahmed A; Saleh, Noha Mohamed

doi:10.1016/j.lfs.2021.119344

Cited by 9 publications

(14 citation statements)

References 58 publications

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“…Amira et al encapsulated AMD into PLGA nanoparticles prepared from polylactic acid-hydroxyacetic acid, which have good bioavailability. These nanocarriers can allow the AMD encapsulated in the carriers to be slowly released in vivo , avoiding toxicity to non-therapeutic organs ( 63 , 64 ).…”

Section: Practical Application Of Af Treatment Methods Based On Nano ...mentioning

confidence: 99%

“…For oral drugs to enter the blood, they must first be dissolved in the gastrointestinal fluid. The protective layer on the surface of the carrier can prevent the drug from being destroyed by the physical and chemical environment of the body's digestive system and the action of various enzymes or recognized and destroyed by the immune system before reaching the point of action, at the same time, it can also prevent the unstable drug from being converted into active ingredients prematurely in the body, and avoid toxic reactions due to excessive active drug doses ( 63 , 64 ). Taking advantage of this property can reconsider unstable and easily disrupted drugs for treatment, and can also enhance the bioavailability of those drugs that are greatly affected by presystemic metabolism in the gastrointestinal tract ( 65 ).…”

Section: Nano Drug Delivery Systemmentioning

confidence: 99%

“…It is released at a slow rather than constant rate over an extended period of time, prolonging the duration of action of the drug in the body ( 66 ). Reduce the frequency of medication, improve patient compliance, ensure that the drug stays at the effective concentration stably, avoid toxic and side effects caused by exceeding the therapeutic concentration, and improve the effectiveness and safety of the drug ( 63 , 64 ).…”

Section: Nano Drug Delivery Systemmentioning

confidence: 99%

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Nano drugs delivery system: A novel promise for the treatment of atrial fibrillation

Wang

Tong

et al. 2022

Front. Cardiovasc. Med.

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Atrial fibrillation (AF) is one of the most common sustained tachyarrhythmias worldwide, and its prevalence is positively correlated with aging. AF not only significantly reduces the quality of life of patients but also causes a series of complications, such as thromboembolism, stroke, and heart failure, increases the average number of hospitalizations of patients, and places a huge economic burden on patients and society. Traditional drug therapy and ablation have unsatisfactory success rates, high recurrence rates, and the risk of serious complications. Surgical treatment is highly traumatic. The nano drug delivery system has unique physical and chemical properties, and in the application of AF treatment, whether it is used to assist in enhancing the ablation effect or for targeted therapy, it provides a safer, more effective and more economical treatment strategy.

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Section: Practical Application Of Af Treatment Methods Based On Nano ...mentioning

confidence: 99%

Section: Nano Drug Delivery Systemmentioning

confidence: 99%

Section: Nano Drug Delivery Systemmentioning

confidence: 99%

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Nano drugs delivery system: A novel promise for the treatment of atrial fibrillation

Wang

Tong

et al. 2022

Front. Cardiovasc. Med.

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“…It has been reported in the literature that maximum uptake and contact with mucosal epithelial membranes were found for polymeric NPs of 50 to 500 nm [13]. Moreover, transcytosis of NPs for gastrointestinal (GI) absorption is more enhanced for NPs with a size < 500 nm [64,65].…”

Section: Entrapment Efficiency Percent (Ee%)mentioning

confidence: 99%

Surface-Decorated Nanocarrier as a Targeted Drug Delivery Cargo to Folate Receptor-Overexpressing Cells for Enhancing Anti-cancer and Anti-inflammatory Activity

Girgis

2023

J. Pharm. Res. Int.

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Aims: Folate receptor (FR) is overexpressed in most cancer cells and activated macrophages entailed in rheumatoid arthritis (RA). The aim of the current study was the fabrication of FR-targeted nanocarrier loaded with methotrexate (MTX) to magnify its therapeutic efficacy and limit its toxicity. Methodology: Folic acid-chitosan (FA-CS) conjugate was synthesized and characterized. MTX loaded poly(d,l-lactide-co-glycolide) (PLGA) nanoparticles (NPs) were prepared, optimized and coated with different concentrations of FA-CS conjugate. The selected FA-CS coated MTX NPs formulation (F10) was evaluated via in vitro and in vivo studies. Results: F10 had satisfactory encapsulation efficiency (76.2%), homogenous particle size (278.6 nm) and positive zeta potential (34.0 mV) and displayed biphasic drug release pattern in different pH media. Further characterization of F10 cinched MTX incorporation in the polymeric matrix of the targeted nanocarrier. In vitro cytotoxicity assay to FR-positive and FR-negative cancer cells revealed the improved anticancer effect of F10 to FR-positive cancer cells, which was absent in FR-negative cells, compared to free MTX or uncoated MTX NPs (F2). F10 showed appropriate storage stability at refrigerated temperature up to 3 months. Moreover, oral administration of F10 in the treatment of complete Freund’s adjuvant (CFA)-induced RA in BALB/c mice conferred prodigious therapeutic outcomes and declined systemic toxicity compared to oral treatment with conventional pure MTX or commercial MTX tablets. Conclusion: The fabricated targeted nanocarrier could enhance the anticancer activity of MTX to FR-overexpressing cancer cells and could be a promising novel approach for oral administration of MTX in the treatment of RA or other inflammatory conditions associated with FR-overexpressing activated macrophages.

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“…Its low aqueous solubility (0.2–0.5 mg/mL) and high lipophilic character (class II in the Biopharmaceutical Classification System) lead to problematic absorption [ 16 ]. Over time, multiple studies were performed in order to increase amiodarone’s bioavailability, these studies included: self-nano-emulsifying drug delivery systems [ 18 ], lipid nanocapsules [ 19 ], inclusion in cyclodextrins [ 20 , 21 , 22 ], nanoparticles [ 23 , 24 , 25 , 26 ], and liposomes [ 27 , 28 ]. By including amiodarone in all these new systems, a certain increase in its aqueous solubility was achieved.…”

Section: Introductionmentioning

confidence: 99%

The Influence of the Polymer Type on the Quality of Newly Developed Oral Immediate-Release Tablets Containing Amiodarone Solid Dispersions Obtained by Hot-Melt Extrusion

et al. 2022

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The present study aims to demonstrate the influence of the polymer-carrier type and proportion on the quality performance of newly developed oral immediate-release tablets containing amiodarone solid dispersions obtained by hot-melt extrusion. Twelve solid dispersions including amiodarone and different polymers (PEG 1500, PEG 4000; PEG 8000, Soluplus®, and Kolliphor® 188) were developed and prepared by hot-melt extrusion using a horizontal extruder realized by the authors in their own laboratory. Only eleven of the dispersions presented suitable physical characteristics and they were used as active ingredients in eleven tablet formulations that contain the same amounts of the same excipients, varying only in solid dispersion type. The solid dispersions’ properties were established by optical microscopy with reflected light, volumetric controls and particle size evaluation. In order to prove that the complex powders have appropriate physical characteristics for the direct compression process, they were subjected to different analyses regarding their flowability and compressibility behavior. Additionally, the Fourier transform infrared spectroscopy and X-ray diffraction analysis were performed on the obtained solid dispersions. After confirming the proper physical attributes for all blends, they were processed into the form of tablets by direct compression technology. The manufactured tablets were evaluated for pharmacotechnical (dimensions–diameter and thickness, mass uniformity, hardness and friability) and in vitro biopharmaceutical (disintegration time and drug release) performances. Furthermore, the influence of the polymer matrix on their quality was determined. The high differences in flow and compression performances of the solid dispersions prove the relevant influence of the polymer type and their concentration-dependent plasticizing properties. The increase in flowability and compressibility characteristics of the solid dispersions could be noticed after combining them with direct compression excipients owning superior mechanical qualities. The influence of the polymer type is best detected in the disintegration test, where the obtained values are quite different between the studied formulations. The use of PEG 1500 alone or combined in various proportions with Soluplus® leads to rapid disintegration. In contrast, the mixture of PEG 4000 and Poloxamer 188 in equal proportions determined the increase in disintegration time to 120 s. The use of Poloxamer 188 alone and a 3:1 combination of PEG 4000 and Soluplus® also generates a prolonged disintegration time for the tablets.

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Appraisal of amiodarone-loaded PLGA nanoparticles for prospective safety and toxicity in a rat model

Cited by 9 publications

References 58 publications

Nano drugs delivery system: A novel promise for the treatment of atrial fibrillation

Nano drugs delivery system: A novel promise for the treatment of atrial fibrillation

Surface-Decorated Nanocarrier as a Targeted Drug Delivery Cargo to Folate Receptor-Overexpressing Cells for Enhancing Anti-cancer and Anti-inflammatory Activity

The Influence of the Polymer Type on the Quality of Newly Developed Oral Immediate-Release Tablets Containing Amiodarone Solid Dispersions Obtained by Hot-Melt Extrusion

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