Isoniazid loaded core shell nanoparticles derived from PLGA–PEG–PLGA tri-block copolymers: In vitro and in vivo drug release

Gajendiran, Mani; Gopi, Venkatachalam; Vellaichamy, Elangovan; Murali, R.; Balasubramanian, S.

doi:10.1016/j.colsurfb.2012.12.008

Cited by 56 publications

(15 citation statements)

References 41 publications

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“…5 ). The optimized formulation showed an immediate release ( burst release) attributed to the non-loaded MEM fraction which is weakly bound to the NPs’ surface, because of the PEG coating [ 37 ]. After this initial phase, the drug displayed a sustained release diffusing slowly from the polymeric matrix into the release medium.…”

Section: Resultsmentioning

confidence: 99%

Memantine loaded PLGA PEGylated nanoparticles for Alzheimer’s disease: in vitro and in vivo characterization

et al. 2018

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BackgroundMemantine, drug approved for moderate to severe Alzheimer’s disease, has not shown to be fully effective. In order to solve this issue, polylactic-co-glycolic (PLGA) nanoparticles could be a suitable solution to increase drug’s action on the target site as well as decrease adverse effects. For these reason, Memantine was loaded in biodegradable PLGA nanoparticles, produced by double emulsion method and surface-coated with polyethylene glycol. MEM–PEG–PLGA nanoparticles (NPs) were aimed to target the blood–brain barrier (BBB) upon oral administration for the treatment of Alzheimer’s disease.ResultsThe production parameters were optimized by design of experiments. MEM–PEG–PLGA NPs showed a mean particle size below 200 nm (152.6 ± 0.5 nm), monomodal size distribution (polydispersity index, PI < 0.1) and negative surface charge (− 22.4 mV). Physicochemical characterization of NPs confirmed that the crystalline drug was dispersed inside the PLGA matrix. MEM–PEG–PLGA NPs were found to be non-cytotoxic on brain cell lines (bEnd.3 and astrocytes). Memantine followed a slower release profile from the NPs against the free drug solution, allowing to reduce drug administration frequency in vivo. Nanoparticles were able to cross BBB both in vitro and in vivo. Behavioral tests carried out on transgenic APPswe/PS1dE9 mice demonstrated to enhance the benefit of decreasing memory impairment when using MEM–PEG–PLGA NPs in comparison to the free drug solution. Histological studies confirmed that MEM–PEG–PLGA NPs reduced β-amyloid plaques and the associated inflammation characteristic of Alzheimer’s disease.ConclusionsMemantine NPs were suitable for Alzheimer’s disease and more effective than the free drug.Electronic supplementary materialThe online version of this article (10.1186/s12951-018-0356-z) contains supplementary material, which is available to authorized users.

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Section: Resultsmentioning

confidence: 99%

Memantine loaded PLGA PEGylated nanoparticles for Alzheimer’s disease: in vitro and in vivo characterization

et al. 2018

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“…This result is also confirmed by fitting the release data in the Korsmeyer–Peppas equation where n is an exponent coefficient that characterizes the release mechanism. For spherical matrix systems, as the n value is 0.43, the drug release mechanism is diffusion controlled, and when the n value is between 0.43 and 0.85, it means that the drug release is controlled by both the erosion and diffusion mechanisms (Siepmann and Siepmann, ; Gajendiran et al ., ). For both PLGA and PEG‐block‐PCL nanoparticle formulations, the values of exponent coefficient were 0.297 and 0.445, respectively.…”

Section: Resultsmentioning

confidence: 97%

Optimization of a validated stability‐indicating RP‐LC method for the determination of fulvestrant from polymeric based nanoparticle systems, drugs and biological samples

Gümüştaş

Sengel-Türk

Hasçicek

et al. 2014

Biomedical Chromatography

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Fulvestrant is used for the treatment of hormone receptor-positive metastatic breast cancer in postmenopausal women with disease progression following anti-estrogen therapy. Several reversed-phase columns with variable silica materials, diameters, lengths, etc., were tested for the optimization study. A good chromatographic separation was achieved using a Waters X-Terra RP(18) column (250 × 4.6 mm i.d. × 5 µm) and a mobile phase, consisting of a mixture of acetonitrile-water (65:35; v/v) containing phosphoric acid (0.1%). The separation was carried out 40 °C with detection at 215 nm.The calibration curves were linear over the concentration range between 1.0-300 and 1.0-200 µg/mL for standard solutions and biological media, respectively. The proposed method is accurate and reproducible. Forced degradation studies were also realized. This fully validated method allows the direct determination of fulvestrant in dosage form and biological samples. The average recovery of the added fulvestrant amount in the samples was between 98.22 and 104.03%. The proposed method was also applied for the determination of fulvestrant from the polymeric-based nanoparticle systems. No interference from using polymers and other excipients was observed in in vitro drug release studies. Therefore an incorporation efficiency of fulvestrant-loaded nanoparticle could be determined accurately and specifically.

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“…Compared with the non-encapsulated drug formulations, the drug release behavior of TAC-NPs showed a pronounced sustained property. For 0.1% TAC suspension, more than 85% of TAC was released during 12 h, but only 64% of TAC was released from the TAC-NPs after 48 h. This sustained release behavior might be attributed to the NPs with core/shell structure, where the drug was encapsulated in the hydrophobic core and consistently released via diffusion and the polymeric matrix degradation (Gajendiran et al., 2013; Panyam et al., 2003; Choudhury et al., 2015). On account of its release behavior, TAC-NPs could reduce the administration frequency.…”

Section: Resultsmentioning

confidence: 99%

Development and effects of tacrolimus-loaded nanoparticles on the inhibition of corneal allograft rejection

Liu

Zhang

et al. 2019

Drug Delivery

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Tacrolimus has been widely applied to prevent organ rejection after transplantation. However, the conventional pharmaceutical formulation of tacrolimus limits its applications in ocular therapy due to its hydrophobicity and low corneal penetrability. We optimized tacrolimus-loaded methoxy poly (ethylene glycol- block -poly ( d , l )-lactic- co -glycolic acid) nanoparticles (TAC-NPs) by simple and effective nanotechnology as a drug delivery system for corneal graft rejection to overcome these drawbacks. The prepared TAC-NPs were 82.9 ± 1.3 nm in size, and the drug loading and encapsulation efficiency were 8.01 ± 0.23% and 80.10 ± 2.33%. Furthermore, New Zealand rabbits were used to analyze the single-dose pharmacokinetics of the TAC-NPs using high-performance liquid chromatography tandem mass spectrometry (HPLC-MS/MS). In rats with allogenic penetrating keratoplasty, the administration of TAC-NPs dispersion drops improved the TAC concentrations in the aqueous humor and cornea, consistent with a significantly higher effective inhibition of IL-2, IL-17, and VEGF expression compared with conventional 0.1% tacrolimus drops. Meanwhile, we also compared two different topical administration methods (including eye drop and subconjunctival injection) of TAC-NPs to maximize the sustained release characteristic of NPs. In summary, the small-sized TAC-NPs enhanced transcorneal permeation and absorption of TAC and more effectively inhibited corneal allograft rejection, which indicated that biodegradable polymeric nanomaterials-based drug delivery system had great potential for improving the clinical therapy efficacy of hydrophobic drugs.

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Isoniazid loaded core shell nanoparticles derived from PLGA–PEG–PLGA tri-block copolymers: In vitro and in vivo drug release

Cited by 56 publications

References 41 publications

Memantine loaded PLGA PEGylated nanoparticles for Alzheimer’s disease: in vitro and in vivo characterization

Memantine loaded PLGA PEGylated nanoparticles for Alzheimer’s disease: in vitro and in vivo characterization

Optimization of a validated stability‐indicating RP‐LC method for the determination of fulvestrant from polymeric based nanoparticle systems, drugs and biological samples

Development and effects of tacrolimus-loaded nanoparticles on the inhibition of corneal allograft rejection

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