Sterically Stabilized RIPL Peptide-Conjugated Nanostructured Lipid Carriers: Characterization, Cellular Uptake, Cytotoxicity, and Biodistribution

Kim, Chang‐Hyun; Sung, Si Woo; Lee, Eun Seok; Kang, Tae Heung; Yoon, Ho Yub; Goo, Yoon Tae; Cho, Ha Ra; Kim, Dong Yoon; Kang, Myung Joo; Choi, Yong Seok; Lee, Sang Kil; Choi, Young Wook

doi:10.3390/pharmaceutics10040199

Cited by 16 publications

(13 citation statements)

References 45 publications

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“…It clearly indicated that the protein adsorptions of BPNLC and PNLC are significantly lower than that of BNLC and TNLC, which may be due to its improved surface hydrophilicity. It was in accordance with the previous result [57,58]. Besides, the brush configuration of PEG chains in PNLC might effectively block the movement of protein to the vicinity of the NPs, which was mainly controlled by random Brownian motion, leading to the reduced BSA adsorption [59].…”

Section: Protein Adsorptionsupporting

confidence: 91%

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Development of tamoxifen‐loaded surface‐modified nanostructured lipid carrier using experimental design: in vitro and ex vivo characterisation

Ganesan

Damodharan

2020

IET nanobiotechnol.

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The present study aimed to develop a surface-modified biocompatible nanostructured lipid carrier (NLCs) system using polyoxyethylene (40) stearate (POE-40-S) to improve the oral bioavailability of poorly water-soluble Biopharmaceutics Classification System class-II drug like tamoxifen (TMX). Also aimed to screen the most influential factors affecting the particle size (PS) using Taguchi (L 12 (2 11)) orthogonal array design (TgL 12 OA). Then, to optimize the TMX loaded POE-40-S (P) surface-modified NLCs (TMX-loaded-PEG-40-S coated NLC (PNLCs) or PNLCs) by central composite design (CCD) using a four-factor, five-level model. The most influential factors affecting the PS was screened and optimized. The in-vitro study showed that increased drug-loading (DL) and encapsulation efficiency (EE), decreased PS and charge, sustained drug release for the prolonged period of the time with good stability and suppressed protein adsorption. The Ex-vivo study showed that decreased mucous binding with five-fold enhanced permeability of PNLC formulation after surface modification with POE-40-S. The in-vitro cytotoxicity study showed that the blank carrier is biocompatible and cytotoxicity of the formulation was dependent on the concentration of the drug. Finally, it can be concluded that the surface-modified PNLCs formulation was an effective, biocompatible, stable formulation in the enhancement of dissolution rate, solubility, stability with reduced mucus adhesion and increased permeability thereby which indicates its enhanced oral bioavailability.

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Section: Protein Adsorptionsupporting

confidence: 91%

“…The protein adsorption of BNLCs, BPNLCs, TNLCs and PNLCs formulation was evaluated using BSA, the most abundant protein in serum, as a model plasma protein [57]. Since, protein adsorption occurred when the NPs came in contact with the plasma, which induced the recognition of macrophages and reduction of the tumour accumulation of the NPs [46].…”

Section: Resultsmentioning

confidence: 99%

Development of tamoxifen‐loaded surface‐modified nanostructured lipid carrier using experimental design: in vitro and ex vivo characterisation

Ganesan

Damodharan

2020

IET nanobiotechnol.

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“…2c), indicating that the presence of LNCs in the filtrate would significantly interfere with the quantification of free peptide or protein using this quantification method (p = 0.005). The presence of LNCs in the filtrate has never been reported in previous publications (12,13,20,(23)(24)(25)(26)(27)(28).…”

Section: The Limitations Of Centrifugal-filtration Devicesmentioning

confidence: 64%

“…to quantify their adsorption or encapsulation rates. This is particularly true for LNCs (12,(23)(24)(25)(26)(27)(28), and the studies of LNC/NFL peptide association (13,20,24). Generally, after separation using the devices, the BCA assay or liquid chromatography is used to quantify the proportion of free NFL peptide in the filtrate and the proportion of adsorbed NFL peptide at the LNC surface is then evaluated.…”

Section: Results and Discussion A Size-exclusion Chromatography Systementioning

confidence: 99%

Characterization of Biological Material Adsorption to the Surface of Nanoparticles without a Prior Separation Step: a Case Study of Glioblastoma-Targeting Peptide and Lipid Nanocapsules

et al. 2021

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Purpose Current preclinical therapeutic strategies involving nanomedicine require increasingly sophisticated nanosystems and the characterization of the complexity of such nanoassemblies is becoming a major issue. Accurate characterization is often the factor that can accelerate the translational approaches of nanomedicines and their pharmaceutical development to reach the clinic faster. We conducted a case study involving the adsorption of the NFL-TBS.40-63 (NFL) peptide (derived from neurofilaments) to the surface of lipid nanocapsules (LNCs) (a combined nanosystem used to target glioblastoma cells) to develop an analytical approach combining the separation and the quantification in a single step, leading to the characterization of the proportion of free peptide and thus the proportion of peptide adsorbed to the lipid nanocapsule surface. Methods LNC suspensions, NFL peptide solution and LNC/ NFL peptide mixtures were characterized using a Size-Exclusion Chromatography method (with a chromatographic apparatus). In addition, this method was compared to centrifugal-filtration devices, currently used in literature for this case study. Results Combining the steps for separation and characterization in one single sequence improved the accuracy and robustness of the data and led to reproducible results. Moreover the data deviation observed for the centrifugal-filtration devices demonstrated the limits for this increasingly used characterization approach, explained by the poor separation quality and highlighting the importance for the method optimization.The high potential of the technique was shown, proving that H-bond and/or electrostatic interactions mediate adsorption of the NFL peptide to the surface of LNCs. Conclusions Used only as a characterization tool, the process using chromatographic apparatus is less time and solvent consuming than classical Size-Exclusion Chromatography columns only used for separation. It could be a promising tool for the scientific community for characterizing the interactions of other combinations of nanosystems and active biological agents.

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“…53 When it enters the cytoplasm, it will be hydrolyzed into Calcein by esterase and remain in the cell, emitting strong green fluorescence. 54 Calcein-AM is the most suitable fluorescent probe to stain living cells because of its low cytotoxicity. The excitation and emission wavelengths of Calcein are 490 nm and 515 nm, respectively.…”

Section: Live/dead Double Staining Methodsmentioning

confidence: 99%

<p>Primary Studies on Construction and Evaluation of Ion-Sensitive in situ Gel Loaded with Paeonol-Solid Lipid Nanoparticles for Intranasal Drug Delivery</p>

Sun¹,

Xie²,

Wang³

et al. 2020

IJN

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Background: Paeonol (PAE) is a potential central neuroprotective agent with poor water solubility and rapid metabolism in vivo. The key to improve the clinical application of PAE in the treatment of neurodegenerative diseases is to improve the brain delivery of it. The purpose of this study was to construct a paeonol-solid lipid nanoparticles-in situ gel (PAE-SLNs-ISG) drug delivery system based on nose-brain transport pathway. Materials and Methods: In this study, the stability of PAE in simulated biological samples was studied firstly in order to clarify the reasons for low oral bioavailability. Paeonol-solid lipid nanoparticles (PAE-SLNs) were prepared by high-temperature emulsification-low-temperature curing combined with ultrasound. The PAE-SLNs-ISG drug delivery system was constructed, and related formulation optimization, preparation characterization, cell evaluation and in vivo evaluation were performed. Results: The metabolic mechanism of PAE incubated in the liver microsomes metabolic system was in accordance with the first-order kinetics, and the half-life was 0.23 h. PAE-SLNs were polyhedral or spherical particles with good dispersion and the particle size was 166.79 nm ± 2.92 nm. PAE-SLNs-ISG solution was a Newtonian fluid with a viscosity of 44.36 mPa • S ± 2.89 mPa • S. The viscosity of PAE-SLNs-ISG gel was 1542.19 mPa • S ± 19.30 mPa • S, and the rheological evaluation showed that the gel was a non-Newtonian pseudoplastic fluid with shear thinning, thixotropy and yield value. The release mechanism of PAE from PAE-SLNs was drug diffusion; the release mechanism of PAE from PAE-SLNs-ISG was a synergistic effect of skeleton erosion and drug diffusion. The cell viabilities of PAE-SLNs and PAE-SLNs-ISG in the concentration range of 0.001 µg/mL to 10 µg/mL were higher than 90%, showing a low level of cytotoxicity. The geometric mean fluorescent intensities of RPMI 2650 cells incubated with fluorescein isothiocyanate-solid lipid nanoparticles (FITC-SLNs) for 1 h, 4 h and 6 h were 1841 ± 24, 2261 ± 27 and 2757 ± 22, respectively. Cyanine7 NHS ester-solid lipid nanoparticles-in situ gel (Cy7-SLNs-ISG) accumulated effectively in the brain area after administration through the olfactory area, and the fluorescence response was observed in olfactory bulb, cerebellum and striatum. Conclusion: SLNs-ISG nose-brain drug delivery system can effectively deliver SLNs to brain regions, and it is a potentially effective strategy to realize the brain region delivery of PAE.

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Sterically Stabilized RIPL Peptide-Conjugated Nanostructured Lipid Carriers: Characterization, Cellular Uptake, Cytotoxicity, and Biodistribution

Cited by 16 publications

References 45 publications

Development of tamoxifen‐loaded surface‐modified nanostructured lipid carrier using experimental design: in vitro and ex vivo characterisation

Development of tamoxifen‐loaded surface‐modified nanostructured lipid carrier using experimental design: in vitro and ex vivo characterisation

Characterization of Biological Material Adsorption to the Surface of Nanoparticles without a Prior Separation Step: a Case Study of Glioblastoma-Targeting Peptide and Lipid Nanocapsules

<p>Primary Studies on Construction and Evaluation of Ion-Sensitive in situ Gel Loaded with Paeonol-Solid Lipid Nanoparticles for Intranasal Drug Delivery</p>

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