Rapamycin-loaded polysorbate 80-coated PLGA nanoparticles: Optimization of formulation variables and in vitro anti-glioma assessment

Escalona-Rayo, Oscar; Fuentes-Vázquez, Paulina; Jardon-Xicotencatl, Samantha; García-Tovar, Carlos; Mendoza-Elvira, Susana; Quintanar‐Guerrero, David

doi:10.1016/j.jddst.2019.05.026

Cited by 43 publications

(20 citation statements)

References 47 publications

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“…PLGA NP loaded with astaxanthin was synthesized at the optimal conditions three times to verify. The experimentally observed values for the three responses are close to the predicted values with low percentages of the relative error to ensure the validity and reproducibility of the model [33]. Figure 1 shows the linear relationship between the experimental value of the response and the predicted value.…”

Section: Resultsmentioning

confidence: 68%

Optimization and characterization of poly(lactic-co-glycolic acid) nanoparticles loaded with astaxanthin and evaluation of anti-photodamage effect in vitro

Liu

Yan

et al. 2019

R. Soc. open sci.

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Astaxanthin is a xanthophyll carotenoid with high beneficial biological activities, such as antioxidant function and scavenging oxygen free radicals, but its application is limited because of poor water solubility and low bioavailability. Here, we prepared and optimized poly(lactic-co-glycolic acid) (PLGA) nanoparticles loaded with astaxanthin using the emulsion solvent evaporation technique and investigated the anti-photodamage effect in HaCaT cells. The four-factor three-stage Box–Behnken design was used to optimize the nanoparticle formulation. The experimental determination of the optimal nanoparticle size was 154.4 ± 0.35 nm, the zeta potential was 22.07 ± 0.93 mV, encapsulation efficiency was 96.42 ± 0.73% and drug loading capacity was 7.19 ± 0.12%. The physico-chemical properties of the optimized nanoparticles were characterized by dynamic light scattering, scanning electron microscopy, transmission electron microscopy, Fourier-transform infrared spectroscopy, X-ray diffraction, differential scanning calorimetry and thermo-gravimetric analyser. In vitro study exhibited the excellent cell viability and cellular uptake of optimized nanoparticles on HaCaT cells. The anti-photodamage studies (cytotoxicity assay, reactive oxygen species content and JC-1 assessment) demonstrated that the optimized nanoparticles were more effective and safer than pure astaxanthin in HaCaT cells. These results suggest that our PLGA-coated astaxanthin nanoparticles synthesis method was highly feasible and can be used in cosmetics or the treatment of skin diseases.

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Section: Resultsmentioning

confidence: 68%

Optimization and characterization of poly(lactic-co-glycolic acid) nanoparticles loaded with astaxanthin and evaluation of anti-photodamage effect in vitro

Liu

Yan

et al. 2019

R. Soc. open sci.

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“…Examples of drugs/bioactive ingredients loaded in polymeric nanoparticles are depicted in Table 1. PCL, PLA, PLGA Coumarin-6 (C-6) nanospheres; C-6-loaded polymeric core-shell NPs (polymeric core-multilayer polyelectrolyte shell NPs), obtained by prepared by the spontaneous emulsification solvent drug delivery, theranostics, or bioimaging [9] PLGA Rapamycin nanospheres; Rapamycin-loaded polysorbate 80-coated PLGA NPs anti-glioma activity [10] AcDex Hyperforin nanospheres; Hyperforin-loaded AcDex-based NPs formulated via single emulsion/solvent evaporationusing ethyl acetate and water anti-inflammatory activity [11] PLGA Fenofibrate (Feno)…”

Section: Introductionmentioning

confidence: 99%

“…nanospheres; PLGA-Feno NPs diabetic retinopathy, neovascular age-related macular degeneration (ocular neovascularization) [12] biopolymer of PCL Amphotericin B nanocapsules; anti-leishmanial [13] PCL, PLA, PLGA Coumarin-6 (C-6) nanospheres; C-6-loaded polymeric core-shell NPs (polymeric core-multilayer polyelectrolyte shell NPs), obtained by prepared by the spontaneous emulsification solvent evaporation method drug delivery, theranostics, or bioimaging [9] PLGA Rapamycin nanospheres; Rapamycin-loaded polysorbate 80-coated PLGA NPs anti-glioma activity [10] AcDex Hyperforin nanospheres; Hyperforin-loaded AcDex-based NPs formulated via single emulsion/solvent evaporationusing ethyl acetate and water anti-inflammatory activity [11] PLGA Fenofibrate (Feno) nanospheres; PLGA-Feno NPs diabetic retinopathy, neovascular age-related macular degeneration (ocular neovascularization) [12] biopolymer of PCL Amphotericin B (Amp B) nanocapsules; PCL-NCs loaded with Amp B, obtained by nanoprecipitation method anti-leishmanial (Leishmania infections), anti-fungal [13] [22] Abbreviations: AcDex-acetalated dextran; F108-poly(ethylene oxide)-block-poly(propylene oxide)-block-poly(ethylene oxide); NCs-nanocapsules; NPs-nanoparticles; PCL-poly(ε-caprolactone); PEG-poly(ethylene glycol); PLA-poly(lactic acid); PLGA-poly(lactide-co-glycolide).…”

Section: Introductionmentioning

confidence: 99%

Polymeric Nanoparticles: Production, Characterization, Toxicology and Ecotoxicology

et al. 2020

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Polymeric nanoparticles (NPs) are particles within the size range from 1 to 1000 nm and can be loaded with active compounds entrapped within or surface-adsorbed onto the polymeric core. The term “nanoparticle” stands for both nanocapsules and nanospheres, which are distinguished by the morphological structure. Polymeric NPs have shown great potential for targeted delivery of drugs for the treatment of several diseases. In this review, we discuss the most commonly used methods for the production and characterization of polymeric NPs, the association efficiency of the active compound to the polymeric core, and the in vitro release mechanisms. As the safety of nanoparticles is a high priority, we also discuss the toxicology and ecotoxicology of nanoparticles to humans and to the environment.

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“…The desirability function technique was used to optimize the formulation using numerical and graphical analysis. A desirability value of 0 was considered not acceptable, while a value closer to 1 corresponded to the desired response [ 34 ].…”

Section: Methodsmentioning

confidence: 99%

Optimization and Evaluation of Poly(lactide-co-glycolide) Nanoparticles for Enhanced Cellular Uptake and Efficacy of Paclitaxel in the Treatment of Head and Neck Cancer

et al. 2020

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The particle size (PS) and encapsulation efficiency (EE%) of drug-loaded nanoparticles (NPs) may inhibit their cellular uptake and lead to possible leakage of the drug into the systemic circulation at the tumor site. In this work, ultra-high paclitaxel-loaded poly(lactide-co-glycolide) NPs (PTX-PLGA-NPs) with ultra-small sizes were prepared and optimized by adopting the principles of quality by design (QbD) approach. The optimized PTX-PLGA-NPs showed ultra-small spherical particles of about 53 nm with EE% exceeding 90%, a relatively low polydispersity index (PDI) of 0.221, an effective surface charge of −10.1 mV, and a 10-fold increase in the in vitro drug release over 72 h relative to free drug. The cellular viability of pharynx carcinoma cells decreased by almost 50% in 24 h following treatment with optimized PTX-PLGA-NPs, compared to only 20% from the free drug. The intracellular uptake of PTX-PLGA-NPs was highly favored, and the antitumor activity of PTX was remarkably improved with a reduction in its half maximal inhibitory concentration (IC50), by almost 50% relative to free drug solution. These results suggest that the optimal critical formulation parameters, guided by QbD principles, could produce PLGA-NPs with remarkably high EE% and ultra-small PS, resulting in enhanced cellular uptake and efficacy of PTX.

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Rapamycin-loaded polysorbate 80-coated PLGA nanoparticles: Optimization of formulation variables and in vitro anti-glioma assessment

Cited by 43 publications

References 47 publications

Optimization and characterization of poly(lactic-co-glycolic acid) nanoparticles loaded with astaxanthin and evaluation of anti-photodamage effect in vitro

Optimization and characterization of poly(lactic-co-glycolic acid) nanoparticles loaded with astaxanthin and evaluation of anti-photodamage effect in vitro

Polymeric Nanoparticles: Production, Characterization, Toxicology and Ecotoxicology

Optimization and Evaluation of Poly(lactide-co-glycolide) Nanoparticles for Enhanced Cellular Uptake and Efficacy of Paclitaxel in the Treatment of Head and Neck Cancer

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