Production of Ibuprofen-Loaded Solid Lipid Nanoparticles Using Rapid Expansion of Supercritical Solution

2015 ◽  
Vol 31 ◽  
pp. 15-29 ◽  
Author(s):  
Zahra Akbari ◽  
Massoud Amanlou ◽  
Javad Karimi-Sabet ◽  
Abolfazl Golestani ◽  
Mojtaba Shariaty Niassar

The purpose of this study was to prepare ibuprofen loaded solid lipid nanoparticles (IBU-SLNs) that is, effective in oral drug delivery. IBU-SLNs were synthesized by co-precipitation of rapid expansion of supercritical solution (CO-RESS). The produced SLNs consisted of stearic acid as lipid matrix. The unprocessed stearic acid, ibuprofen and IBU-SLNs were characterized by means of scanning electron microscopy (SEM), X-ray diffraction (XRD), differential scanning calorimetry (DSC), fourier transform infrared spectrophotometry (FTIR) and high performance liquid chromatography (HPLC). XRD patterns along with DSC showed that ibuprofen was present in both amorphous and crystalline form within lipid matrix. FTIR showed that molecular interactions that could alter the chemical structure of the IBU did not occur. The RESS process could produce ultrafine spherical particles of SLNs with high drug loading capacity. The IBU dissolution profile showed that the formulated SLNs have effectively increased the IBU solubility

2020 ◽  
Vol 10 (4) ◽  
pp. 404-418
Author(s):  
Kruti Borderwala ◽  
Ganesh Swain ◽  
Namrata Mange ◽  
Jaimini Gandhi ◽  
Manisha Lalan ◽  
...  

Background: The objective of this study was to develop solid lipid nanoparticles (SLNs) of poorly water soluble anti-hyperlipidemic drugs-Ezetimibe in combination with Simvastatin. Methods: This study describes a 32 full factorial experimental design to optimize the formulation of drug loaded lipid nanoparticles (SLN) by the high speed homogenization technique. The independent variables amount of lipid (GMS) and amount of surfactant (Poloxamer 188) were studied at three levels and arranged in a 32 factorial design to study the influence on the response variables- particle size, % entrapment efficiency (%EE) and cumulative drug release (% CDR) at 24 h. Results: The particle size, % EE and % CDR at 24 h for the 9 batches (B1 to B9) showed a wide variation of 104.6-496.6 nm, 47.80-82.05% (Simvastatin); 48.60-84.23% (Ezetimibe) and 54.64-92.27% (Simvastatin); 43.8-97.1% (Ezetimibe), respectively. The responses of the design were analysed using Design Expert 10.0.2. (Stat-Ease, Inc, USA), and the analytical tools of software were used to draw response surface plots. From the statistical analysis of data, polynomial equations were generated. Optimized formulation showed particle size of 169.5 nm, % EE of 75.43% (Simvastatin); 79.10% (Ezetimibe) and 74.13% (Simvastatin); 77.11% (Ezetimibe) %CDR after 24 h. Thermal analysis of prepared solid lipid nanoparticles gave indication of solubilisation of drugs within lipid matrix. Conclusion: Fourier Transformation Infrared Spectroscopy (FTIR) showed the absence of new bands for loaded solid lipid nanoparticles indicating no interaction between drugs and lipid matrix and being only dissolved in it. Electron microscope of transmission techniques indicated sphere form of prepared solid lipid nanoparticles with smooth surface with size approximately around 100 nm.


RSC Advances ◽  
2015 ◽  
Vol 5 (84) ◽  
pp. 68743-68750 ◽  
Author(s):  
Sacheen Kumar ◽  
Jaspreet Kaur Randhawa

Paliperidone is an antipsychotic drug having poor water solubility and bioavailability. Solid lipid nanoparticles of stearic acid loaded with paliperidone were prepared to enhance the bioavailability.


2021 ◽  
Author(s):  
Bárbara Fernandes Pinto ◽  
Lorena Natasha Brito Ribeiro ◽  
Gisela Bevilacqua Rolfsen Ferreira da Silva ◽  
Camila Simões Freitas ◽  
Lucas Kraemer ◽  
...  

Rationale: The FDA approved Dimethyl Fumarate (DMF) as an oral drug for Multiple Sclerosis treatment based on its immunomodulatory activities. However, it also caused severe adverse effects mainly related to the gastrointestinal system. Objective: Investigated the potential effects of solid lipid nanoparticles (SLN) containing DMF, administered by inhalation on the clinical signs, central nervous system (CNS) inflammatory response, and lung function changes in mice with experimental autoimmune encephalomyelitis (EAE). Materials and Methods: EAE was induced using MOG35-55 peptide in female C57BL/6J mice and were treated via inhalation with DMF-encapsulated SLN (CTRL/SLN/DMF and EAE/SLN/DMF), empty SLN (CTRL/SLN and EAE/SLN), or saline solution (CTRL/saline and EAE/saline), every 72 hours during 21 days. Results: After 21 days post-induction, EAE mice treated with DMF-loaded SLN, when compared to EAE/saline and EAE/SLN, showed decreased clinical score and weight loss, reduction in brain and spinal cord injury and inflammation, also related to the increased influx of Foxp3+ cells into the spinal cord and lung tissues. Moreover, our data revealed that EAE mice showed signs of respiratory disease, marked by increased vascular permeability, leukocyte influx, production of TNF-α and IL-17, perivascular and peribronchial inflammation, with pulmonary mechanical dysfunction associated with loss of respiratory volumes and elasticity, which DMF-encapsulated reverted in SLN nebulization. Conclusion: Our study suggests that inhalation of DMF-encapsulated SLN is an effective therapeutic protocol that reduces not only the CNS inflammatory process and disability progression, characteristic of EAE disease, but also protects mice from lung inflammation and pulmonary dysfunction.


Author(s):  
S. Khaleel Basha ◽  
R. Dhandayuthabani ◽  
M. Syed Muzammil ◽  
V. Sugantha Kumari

2006 ◽  
Vol 6 (9) ◽  
pp. 2991-2995 ◽  
Author(s):  
K. Ruckmani ◽  
M. Sivakumar ◽  
P. A. Ganeshkumar

Solid Lipid Nanoparticles (SLN) containing Methotrexate (MTX), an anticancer drug for intravenous administration was formulated and characterized. The SLN dispersions with MTX, stearic acid, and soya lecithin in the ratio of 1:4:1, 1:4:1.5, and 1:4:2, sodium taurodeoxycholate and distilled water were prepared by micro emulsification solidification method. The results show that the prepared MTX-SLN particles (with MTX–Stearic acid–Soya lecithin—1:4:2) have an average size of 270 nm with 51.3% drug entrapment. The in vitro-release was attained up to 15th h. The pharmacokinetic studyreveals that the half-life and MRT of SLNs were higher than MTX solution. The life span of EAC (Ehrlich Ascite Carcinoma) bearing mice was increased when treated with MTX-SLNs (Methotrexate nanoparticles). These results clearly indicate that SLNs are a promising sustained release drug targeting system for lipophilic antitumour drugs.


RSC Advances ◽  
2014 ◽  
Vol 4 (57) ◽  
pp. 30186-30192 ◽  
Author(s):  
Sacheen Kumar ◽  
Jaspreet K. Randhawa

Gelucire® 50/13, a macrogol glyceride, was used as a surfactant for the preparation and stabilization of paliperidone-loaded Capmul® GMS-50K matrix-based solid lipid nanoparticles (SLNs). The homogeneously distributed paliperidone did not affect the crystal structure of the lipid matrix in the SLNs.


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