Correlation between long-term stability of solid lipid nanoparticles (SLN™) and crystallinity of the lipid phase

1999 ◽  
Vol 47 (2) ◽  
pp. 125-132 ◽  
Author(s):  
C. Freitas ◽  
R.H. Müller
Molecules ◽  
2020 ◽  
Vol 25 (13) ◽  
pp. 2991 ◽  
Author(s):  
Debora Santonocito ◽  
Maria Grazia Sarpietro ◽  
Claudia Carbone ◽  
Annamaria Panico ◽  
Agata Campisi ◽  
...  

Curcumin (CUR) has a wide range of pharmacological properties, including anti-inflammatory and antioxidant activities, and it can be considered a good candidate for the potential treatment of central nervous system (CNS) pathologies, although its use in clinical practice is compromised due to its high lipophilicity. Solid lipid nanoparticles (SLNs) are well-known nanocarriers representing a consolidated approach for the delivery of lipophilic compounds, but their systemic use is limited due their short half-life. The formulation of stealth SLNs (pSLNs) could be a valid strategy to overcome this limit. Curcumin-loaded-pSLNs were prepared by the solvent evaporation method. Formulation was characterized for their mean size, zeta potential, size distribution, and morphology. Drug antioxidant activity was evaluated by Oxygen Radical Absorbance Capacity (ORAC) assay. Finally, the obtained formulations were analyzed in terms of long-term stability. Curcumin-loaded-pSLNs showed good technological parameters with a mean particle size below 200 nm, as confirmed by TEM images, and a zeta potential value around −30 mV, predicting good long-term stability. Differential Scanning Calorimetry (DSC) analysis confirmed that PEG micelles interacted with the SLN surface; this suggests the location of the PEG on the pSLN surface. Therefore, these preliminary studies suggest that the produced formulation could be regarded as a promising carrier for the systemic administration.


2013 ◽  
Vol 14 (2) ◽  
pp. 847-853 ◽  
Author(s):  
Felice Cerreto ◽  
Patrizia Paolicelli ◽  
Stefania Cesa ◽  
Hend M. Abu Amara ◽  
Felicia Diodata D’Auria ◽  
...  

2012 ◽  
Vol 15 (3) ◽  
pp. 467 ◽  
Author(s):  
Su-Eon Jin ◽  
Chong-Kook Kim

Purpose: Long-term stable cationic solid lipid nanoparticles (cSLNs) were formulated to transfer SMAD3 antisense oligonucleotides (ASOs) into the cells to enhance the intracellular activity of the ASOs. The SMAD3 ASOs were designed to block the inflammatory processes linked to TGFβ/SMAD3 pathway. Methods: The cSLN formulation was prepared by high-pressure homogenization method composed of 1,2-dioleoyl-3-trimethylammonium propane (DOTAP), dioleoylphosphoethanolamine (DOPE), Tween 20, and tricaprin as a solid lipid core (1:1:1:1.67, w/w). The size and the zeta potential of the prepared cSLNs were measured by light scattering. The cSLN/ASO complexes were generated and introduced into the murine macrophage cells. After the treatment of the complexes, the cellular uptake of the complexes was determined by flow cytometry and the intracellular activity of SMAD3 ASOs from the complexes was evaluated by western blotting of SMAD3. In addition, TGFβ1, an upstream molecule of TGFβ/SMAD3 pathway, was monitored by ELISA. Results: The nano-scale sized cSLNs were positively charged and physically stable at 4oC during the storage up to 24 months. The uptake efficiency of the cSLN/ASO complexes into macrophage cells was enhanced up to 80% without cytotoxicity. After the treatment of the cSLN/ASO complexes, SMAD3 as well as TGFβ1 was significantly suppressed based on the SMAD3 ASO activity in the macrophage cells. In addition, the cSLN/ASO complexes prevented the morphological change to dendritic shape in the activated macrophage cells. Conclusion: These results suggest that the cSLNs have a potential to deliver the SMAD3 ASOs to intracellular compartments for the anti-inflammatory effect. The development of this strategy might lead to anti-inflammatory and anti-fibrotic therapies in immunological disorders. This article is open to POST-PUBLICATION REVIEW. Registered readers (see “For Readers”) may comment by clicking on ABSTRACT on the issue’s contents page.


2017 ◽  
Vol 4 (1) ◽  
pp. 17-29 ◽  
Author(s):  
Sukhwinder Singh ◽  
Sukhmeet Singh Kamal ◽  
Amit Sharma ◽  
Daljit Kaur ◽  
Manoj Kumar Katual ◽  
...  

Objectives: The present study aims on preparing Levosulpiride loaded solid lipid nanoparticles (SLNs) to reduce the dose, frequency of dosing, reduce side effects and to increase the bioavailable fraction of drug (<30% orally in general). Methods: Levosulpiride was characterized by preformulation studies like physical appearance, melting point, assay, calibration curve, FTIR analysis and DSC analysis. The calibration curve of the drug was prepared in pH 6.8 phosphate buffer. Two lipids (Stearic acid and Palmitic acid) were used as lipid phase to prepare SLNs. Factorial design (23) was applied to formulate 16 formulations (8 for each lipid i.e. SF1-SF8 and PF1-PF8). Levosulpiride SLNs were prepared by solvent evaporation method followed by homogenization. Results: The optimized formulations were characterized by particle size analysis, zeta potential analysis, in vitro drug release and drug release kinetics. Drug-excipient interaction in optimized formulation was characterized by FTIR, DSC and TEM analysis. Conclusion: On the basis of evaluation parameters, the formulation SF1 (containing Stearic acid) and PF1 (containing Palimitic acid) found to be better formulations amongst their groups with a controlled drug release after a period of 24 hrs.


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