Surface modification of pralidoxime chloride-loaded solid lipid nanoparticles for enhanced brain reactivation of organophosphorus-inhibited AChE: Pharmacokinetics in rat

Toxicology ◽  
2020 ◽  
Vol 444 ◽  
pp. 152578
Author(s):  
Daina N. Buzyurova ◽  
Tatiana N. Pashirova ◽  
Irina V. Zueva ◽  
Evgenia A. Burilova ◽  
Zukhra M. Shaihutdinova ◽  
...  
Keyword(s):  
Surface Modification ◽  
Solid Lipid Nanoparticles ◽  
Lipid Nanoparticles ◽  
Solid Lipid ◽  
Pralidoxime Chloride

scholarly journals Optimization of Redispersible Spray Dried Powder of Chitosan Coated Solid Lipid-Based Nanosystems

2018 ◽  
Vol 8 (01) ◽  
Author(s):  
Munawiroh S. Z. ◽  
Lipipun V. ◽  
Ritthidej G. C.
Keyword(s):  
Surface Modification ◽  
Spray Drying ◽  
Solid Lipid Nanoparticles ◽  
Drug Stability ◽  
Lipid Nanoparticles ◽  
Inlet Temperature ◽  
Linear Quadratic ◽  
Feed Concentration ◽  
Solid Lipid ◽  
Spray Dried

The present work describes the optimization of spray dried powder of solid lipid-based nanosystems to improve drug stability, surface modification and to obtain nanosystems after redispersion. Chitosan coated solid lipid nanoparticles containing bromocriptine mesylate (cBMSLN) were prepared by high pressure homogenization technique following by chitosan addition. For spray drying, response surface methodology with central composite rotatable design was to optimize 3 parameters: inlet temperature, pump rate and feed concentration. From regression analysis, powder yield, moisture content and size of redispersed nanoaggregates as responses were fitted well with linear, quadratic and quadratic equation models, respectively. Spherical powders with size of 4-5 µm and 70% yield were obtained at optimum parameters which were also used to prepare powder of chitosan coated nanostructured lipid carriers containing BM (cBMNLC). Amorphous characteristics were confirmed from powder XRD patterns and DSC chromatograms in all prepared powders. Redispersion of powders yielded nanosystems of some original nanosize and a greater portion of larger size. Smoother surface of NLC systems was observed, so was with chitosan coating. Drug entrapment was >85% but significantly decreased in chitosan coated formulations while drug retention after spray drying showed opposite results. After storage, spray dried powder could retain higher drug content than the original nanosystems. Obviously, NLC systems had better drug stability results than SLN systems. It could be concluded that redispersible spray dried powders of chitosan coated lipid-based nanosystems especially NLC systems were successfully obtained with surface modification, nanoaggregate size range and improved drug stability.Keywords: Solid lipid nanoparticles, nanostructure lipid carriers, chitosan, spray drying, optimization, redispersion, bromocriptine mesylate

scholarly journals Solid Lipid Nanoparticles Surface Modification Modulates Cell Internalization and Improves Chemotoxic Treatment in an Oral Carcinoma Cell Line

Nanomaterials ◽  
2019 ◽  
Vol 9 (3) ◽  
pp. 464 ◽  
Author(s):  
Lide Arana ◽  
Laura Bayón-Cordero ◽  
Laura Sarasola ◽  
Miren Berasategi ◽  
Sandra Ruiz ◽  
...  
Keyword(s):  
Surface Modification ◽  
Cell Line ◽  
Solid Lipid Nanoparticles ◽  
Scale Up ◽  
Controlled Drug Release ◽  
Lipid Nanoparticles ◽  
Hydrophilic Drugs ◽  
Solid Lipid ◽  
Cell Internalization ◽  
Model Drug

Solid lipid nanoparticles (SLN) present low toxicity, versatility to incorporate both lipophilic and hydrophilic drugs, controlled drug release and they are easy to scale-up. It is well known that the endocytosis pathway by which SLN are taken up and the subsequent subcellular distribution are crucial for the biological effect of the incorporated drug. In addition, interactions between SLN and cells depend on many factors, such as, the composition of nanoparticle surface. In this work different amounts of phosphatidylethanolamine polyethylene glycol (PE–PEG) were added to SLN composed of stearic acid, Epikuron 200 and sodium taurodeoxycholate. Characterization of obtained nanoparticle suspensions were performed by the analysis of particle size, polydispersity index, ζ-potential, cell toxicity and cell internalization pathway. We have observed that the presence of PE–PEG improves active cell internalization of the nanoparticles in an oral adenocarcinoma cell line, reducing non-specific internalization mechanisms. Finally, we have tested the effect of surface coating on the efficiency of incorporated drugs using all-trans retinoic acid as a model drug. We have observed that delivery of this drug into PE–PEG coated SLN increases its chemotoxic effect compared to non-coated SLN. Therefore, it can be concluded that surface modification with PE–PEG improves the efficiency and the specificity of the SLN-loaded drug.

scholarly journals Surface Modification of Optimized Asenapine Maleate Loaded Solid Lipid Nanoparticles Using Box-Behnken Design

2021 ◽  
pp. 176-193
Author(s):  
A. Rekha Devi ◽  
M. Vidyavathi ◽  
S. P. Suryateja
Keyword(s):  
Surface Modification ◽  
Drug Release ◽  
Solid Lipid Nanoparticles ◽  
Oral Bioavailability ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Brain Targeting ◽  
Average Particle ◽  
Box Behnken Design ◽  
Solid Lipid

Aim: The aim of the present study was to design and evaluate solid lipid nanoparticles of Asenapine maleate (<2% bioavailability) to enhance its oral bioavailability and surface modification for brain targeting. Methods: A modified solvent injection method was used to produce Asenapine maleate loaded solid lipid nanoparticles. A RSM 3-factor, 3-level Box-Behnken design was applied to study the effect of three independent variables, concentrations of lipid (A), drug (B) and surfactant (C) on three dependent variables, particles size (Y1), entrapment efficiency (Y2), and drug release (Y3). 3-D surface response plots were drawn and optimized formulation was selected based on desirability factor. Then it was coated with tween 80 for ease of permeability through blood brain barrier due to intact absorption of solid lipid nanoparticles. Results: The results of coated optimized formulation showed average particle size of 108.9 nm, entrapment efficiency of 78.62%, and in vitro drug release of 98.88±0.102% at 36 hr at pH 7.4. Morphologically, particles were almost spherical in shape with uniform size distribution. Targeting of coated optimized formulation to brain after oral administration was confirmed by fluorescence microscopy studies on male albino wistar strain rats. This research also envisaged that there is a >85% cell viability up to 125µg/ ml concentration of coated solid lipid nanoparticles by MTT assay. Conclusion: Thus, the current study successfully designed, developed an optimized SLN formulation of Asenapine maleate using a 3-factor, 3-level Box-Behnken design for brain targeting to treat Schizophrenia by bypassing the first pass metabolism with enhanced oral bioavailability.

Enhancement of oral bioavailability of pentoxifylline by solid lipid nanoparticles

2009 ◽  
Vol 00 (00) ◽  
pp. 090820062440031-9 ◽  
Author(s):  
Jaleh Varshosaz ◽  
Mohsen Minayian ◽  
Elaheh Moazen
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Oral Bioavailability ◽  
Lipid Nanoparticles ◽  
Solid Lipid
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