Determining the Enhancement of Oral Bioavailability VIA Solid Lipid Nanoparticles of Anticancer Drug Dasatinib - An In-vitro Cytotoxicity and Pharmacokinetic Study

2021 ◽  
pp. 161-168
Author(s):  
A. A. Mohamed Yasir Arafath ◽  
B. Jaykar
Keyword(s):  
Anticancer Drug ◽  
Pharmacokinetic Study ◽  
Solid Lipid Nanoparticles ◽  
Oral Bioavailability ◽  
Lipid Nanoparticles ◽  
In Vitro Cytotoxicity ◽  
Solid Lipid

Preparation, Characterization and Optimization of Irbesartan Loaded Solid Lipid Nanoparticles for Oral Delivery

2021 ◽  
pp. 97-104
Author(s):  
Kumara Swamy S ◽  
Ramesh Alli
Keyword(s):  
Drug Release ◽  
Solid Lipid Nanoparticles ◽  
Oral Bioavailability ◽  
Oral Delivery ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Sustained Drug Release ◽  
Bioavailability Enhancement ◽  
Solid Lipid

The purpose of this study was to develop and evaluate irbesartan (IS) loaded solid lipid nanoparticles (SLNs; IS-SLNs) that might enhance the oral bioavailability of IS. IS, an angiotensin-receptor antagonist, used to treat hypertension. However, poor aqueous solubility and poor oral bioavailability has limited therapeutic applications of IS. Components of the SLNs include either of trimyristin/tripalmitin/tristearin/trilaurate/stearic acid/beeswax, and surfactants (Poloxamer 188 and soylecithin). The IS-SLNs were prepared by hot homogenization followed by ultrasonication method and evaluated for particle size, poly dispersity index (PDI), zeta potential (ZP), entrapment efficiency (EE), drug content and in vitro drug release. The physical stability of optimized formulation was studied at refrigerated and room temperature for two months. The optimized IS-SLN formulation (F4) had a mean diameter of about 217.6±3.62 nm, PDI of 0.163±0.032, ZP of -28.5±4.12, assay of 99.8±0.51 and EE of 93.68±2.47%. The formulation showed sustained drug release compared with control formulation over 24 h. Optimized formulation was found to be stable over two months. IS-SLN showed nearly spherical in shape using and converted to amorphous form by DSC. Thus, the results conclusively demonstrated SLNs could be considered as an alternative delivery system for the oral bioavailability enhancement of IS.

Capsaicin-loaded solid lipid nanoparticles: design, biodistribution, in silico modeling and in vitro cytotoxicity evaluation

2020 ◽  
Vol 32 (9) ◽  
pp. 095101
Author(s):  
Selvaraj Kunjiappan ◽  
Murugesan Sankaranarayanan ◽  
Banoth Karan Kumar ◽  
Parasuraman Pavadai ◽  
Ewa Babkiewicz ◽  
...  
Keyword(s):  
Solid Lipid Nanoparticles ◽  
In Silico ◽  
Lipid Nanoparticles ◽  
In Vitro Cytotoxicity ◽  
Solid Lipid ◽  
In Silico Modeling

scholarly journals In vitro cytotoxicity assays of solid lipid nanoparticles in epithelial and dermal cells

2011 ◽  
Vol 304 ◽  
pp. 012032 ◽  
Author(s):  
D M Ridolfi ◽  
P D Marcato ◽  
D Machado ◽  
R A Silva ◽  
G Z Justo ◽  
...  
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Lipid Nanoparticles ◽  
In Vitro Cytotoxicity ◽  
Cytotoxicity Assays ◽  
Solid Lipid ◽  
Dermal Cells

scholarly journals Solid Lipid Nanoparticles for Dibucaine Sustained Release

Pharmaceutics ◽  
2018 ◽  
Vol 10 (4) ◽  
pp. 231 ◽  
Author(s):  
Raquel de M. Barbosa ◽  
Ligia Ribeiro ◽  
Bruna Casadei ◽  
Camila da Silva ◽  
Viviane Queiróz ◽  
...  
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Encapsulation Efficiency ◽  
Colloidal Stability ◽  
Lipid Nanoparticles ◽  
In Vitro Cytotoxicity ◽  
Tail Flick ◽  
Release Kinetic ◽  
Solid Lipid

Dibucaine (DBC) is among the more potent long-acting local anesthetics (LA), and it is also one of the most toxic. Over the last decades, solid lipid nanoparticles (SLN) have been developed as promising carriers for drug delivery. In this study, SLN formulations were prepared with the aim of prolonging DBC release and reducing its toxicity. To this end, SLN composed of two different lipid matrices and prepared by two different hot-emulsion techniques (high-pressure procedure and sonication) were compared. The colloidal stability of the SLN formulations was tracked in terms of particle size (nm), polydispersity index (PDI), and zeta potential (mV) for 240 days at 4 °C; the DBC encapsulation efficiency was determined by the ultrafiltration/centrifugation method. The formulations were characterized by differential scanning calorimetry (DSC), electron paramagnetic resonance (EPR), and release kinetic experiments. Finally, the in vitro cytotoxicity against 3T3 fibroblast and HaCaT cells was determined, and the in vivo analgesic action was assessed using the tail flick test in rats. Both of the homogenization procedures were found suitable to produce particles in the 200 nm range, with good shelf stability (240 days) and high DBC encapsulation efficiency (~72–89%). DSC results disclosed structural information on the nanoparticles, such as the lower crystallinity of the lipid core vs. the bulk lipid. EPR measurements provided evidence of DBC partitioning in both SLNs. In vitro (cytotoxicity) and in vivo (tail flick) experiments revealed that the encapsulation of DBC into nanoparticles reduces its intrinsic cytotoxicity and prolongs the anesthetic effect, respectively. These results show that the SLNs produced are safe and have great potential to extend the applications of dibucaine by enhancing its bioavailability.

Lacidipine Loaded Solid Lipid Nanoparticles for Oral Delivery: Preparation, Characterization and In vivo Evaluation

2016 ◽  
Vol 9 (6) ◽  
pp. 3524-3530 ◽  
Author(s):  
Kishan V. ◽  
Sandeep V ◽  
Narendar D ◽  
Arjun N
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Oral Bioavailability ◽  
Oral Delivery ◽  
Lipid Nanoparticles ◽  
Pharmacokinetic Studies ◽  
Electron Microscopic ◽  
In Vivo Evaluation ◽  
Solid Lipid

The objective of this study was to develop and evaluate lacidipine (LD) loaded solid lipid nanoparticles (LD-SLNs) for improving the oral bioavailability. LD-SLNs were prepared in two steps. First step was hot homogenization and next by ultrasonication method, using triglycerides (tripalmitin and tristearin), monoglyceride and surfactants (Poloxamer 188 and egg lecithin E80). The prepared LD-SLNs were characterized for particle size, PDI, zeta potential, drug content, entrapment efficiency (EE %).         In vitro drug release studies using a dialysis bag method in 0.1N HCl and pH 6.8 phosphate buffer were conducted. In addition, long-term physical stability of the optimized SLNs was investigated at refrigerated and room temperature for 60 days. FTIR and DSC studies revealed that no interaction between the drug and lipids. LD-SLNs prepared with Dynasan-116 (F3), having the size of 141.86nm, PDI of 0.293, ZP of -22.3 m with 94.75% of EE was optimized and was stable for 60days. Scanning electron microscopic studies showed nearly spherical shaped particles. Further, pharmacokinetic studies were conducted in wistar rats. The relative bioavailability of LD in SLNs was 2.03 times when compared with that of the LD suspension. The results are indicative of SLNs as suitable lipid based carrier system for improving the oral bioavailability of LD. 

In vitro cytotoxicity of co-exposure to superparamagnetic iron oxide and solid lipid nanoparticles

2020 ◽  
pp. 074823372097738
Author(s):  
Okunola A Alabi ◽  
Adny H Silva ◽  
Michele P Rode ◽  
Carine dal Pizzol ◽  
Angela Machado de Campos ◽  
...  
Keyword(s):  
Iron Oxide ◽  
Solid Lipid Nanoparticles ◽  
Superparamagnetic Iron Oxide ◽  
Lipid Nanoparticles ◽  
In Vitro Cytotoxicity ◽  
Ros Generation ◽  
Solid Lipid ◽  
Viability Assay ◽  
Low Cytotoxicity

Increased production and use of different types of nanoparticles (NPs) in the last decades has led to increased environmental release of these NPs with potential detrimental effects on both the environment and public health. Information is scarce in the literature on the cytotoxic effect of co-exposure to many NPs as this concern is relatively recent. Thus, in this study, we hypothesized scenarios of cell’s co-exposure to two kinds of NPs, solid lipid nanoparticles (SLNs) and superparamagnetic iron oxide nanoparticles (SPIONs), to assess the potential cytotoxicity of exposure to NPs combination. Cytotoxicity of SPIONs, SLNs, and their 1:1 mixture (MIX) in six tumor and six non-tumor cell lines was investigated. The mechanisms underlining the induced cytotoxicity were studied through cell cycle analysis, detection of reactive oxygen species (ROS), and alterations in mitochondrial membrane potential (ΔΨM). Double staining with acridine orange and ethidium bromide was also used to confirm cell morphology alterations. The results showed that SPIONs induced low cytotoxicity compared to SLNs. However, the mixture of SPIONs and SLNs showed synergistic, antagonistic, and additive effects based on distinct tests such as viability assay, ROS generation, ΔΨM, and DNA damage, depending on the cell line. Apoptosis triggered by ROS and disturbances in ΔΨM are the most probable related mechanisms of action. As was postulated, there is possible cytotoxic interaction between the two kinds of NPs.

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