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 ◽  
...  

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.

2005 ◽  
Vol 11 (S03) ◽  
pp. 52-55 ◽  
Author(s):  
F. S. Peixoto ◽  
P. M. Dias ◽  
G. A. Ramaldes ◽  
J. M. C. Vilela ◽  
M. S. Andrade ◽  
...  

Solid lipid nanoparticles (SLN) have generated increasing attention as an alternative carrier system, particularly for lipophilic drugs [1-2]. The system consists of lipid nanoparticles, which are solid at room temperature. The solid matrix offers the possibility to improve the stability against coalescence and the reduced mobility of incorporated drug molecules is a pre requisite for controlled drug release [3]. Dexamethasone acetate was used as a model drug because of its wide application in the pharmaceutical field and lipophilic properties.


Author(s):  
S. Pragati ◽  
S. Kuldeep ◽  
S. Ashok ◽  
M. Satheesh

One of the situations in the treatment of disease is the delivery of efficacious medication of appropriate concentration to the site of action in a controlled and continual manner. Nanoparticle represents an important particulate carrier system, developed accordingly. Nanoparticles are solid colloidal particles ranging in size from 1 to 1000 nm and composed of macromolecular material. Nanoparticles could be polymeric or lipidic (SLNs). Industry estimates suggest that approximately 40% of lipophilic drug candidates fail due to solubility and formulation stability issues, prompting significant research activity in advanced lipophile delivery technologies. Solid lipid nanoparticle technology represents a promising new approach to lipophile drug delivery. Solid lipid nanoparticles (SLNs) are important advancement in this area. The bioacceptable and biodegradable nature of SLNs makes them less toxic as compared to polymeric nanoparticles. Supplemented with small size which prolongs the circulation time in blood, feasible scale up for large scale production and absence of burst effect makes them interesting candidates for study. In this present review this new approach is discussed in terms of their preparation, advantages, characterization and special features.


2012 ◽  
Vol 2 (1) ◽  
pp. 8 ◽  
Author(s):  
Vandita Kakkar ◽  
Indu Pal Kaur

Sesamol loaded solid lipid nanoparticles (SSLNs) were prepared with the aim of minimizing its distribution to tissues and achieving its targeting to the brain. Three scale-up batches (100x1 L) of S-SLNs were prepared using a microemulsification technique and all parameters were statistically compared with the small batch (1x;10 mL). S-SLNs with a particle size of less than 106 nm with a spherical shape (transmission electron microscopy) were successfully prepared with a total drug content and entrapment efficiency of 94.26±2.71% and 72.57±5.20%, respectively. Differential scanning calorimetry and infrared spectroscopy confirmed the formation of lipidic nanoparticles while powder X-ray diffraction revealed their amorphous profile. S-SLNs were found to be stable for three months at 5±3°C in accordance with International Conference on Harmonisation guidelines. The SLN preparation process was successfully scaled-up to a 100x batch on a laboratory scale. The procedure was easy to perform and allowed reproducible SLN dispersions to be obtained.


2011 ◽  
Vol 364 ◽  
pp. 313-316 ◽  
Author(s):  
Karn Orachai Kullavadee ◽  
Ruktanonchai Uracha ◽  
Siwaporn Meejoo Smith

SLN have shown a great promise as an alternative drug carrier for intravenous and dermal applications. This work focuses on the basic properties of drug-free Compritol® ATO 888 based SLN systems by using cationic surfactant (CPC) and nonionic surfactant (Tween 80). Effects of surfactant on the physical properties of SLNs were investigated in the absence of model drug to avoid the interaction between drug and surfactant. These SLN samples have different particle size, zeta potential and morphology. DSC was used to quantify the crystallinity of SLN systems. It was found that %RI of both SLNs was similar, indicating that types of surfactant did not affect on crystallization of solid lipid. Spherical-like particle was observed with SLN-C, while rod-like particle was found with SLN-T. The results demonstrated that surfactant plays an important role on SLN physical characteristics.


Author(s):  
Munawiroh S. Z. ◽  
Lipipun V. ◽  
Ritthidej G. C.

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


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