Optimization of the lyophilization process for long-term stability of solid–lipid nanoparticles

2012 ◽  
Vol 38 (10) ◽  
pp. 1270-1279 ◽  
Author(s):  
Melissa D. Howard ◽  
Xiuling Lu ◽  
Michael Jay ◽  
Thomas D. Dziubla
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Lipid Nanoparticles ◽  
Term Stability ◽  
Long Term Stability ◽  
Solid Lipid

scholarly journals Curcumin Containing PEGylated Solid Lipid Nanoparticles for Systemic Administration: A Preliminary Study

Molecules ◽  
2020 ◽  
Vol 25 (13) ◽  
pp. 2991 ◽  
Author(s):  
Debora Santonocito ◽  
Maria Grazia Sarpietro ◽  
Claudia Carbone ◽  
Annamaria Panico ◽  
Agata Campisi ◽  
...  
Keyword(s):  
Zeta Potential ◽  
Solid Lipid Nanoparticles ◽  
Antioxidant Activities ◽  
Lipid Nanoparticles ◽  
Systemic Administration ◽  
Term Stability ◽  
Long Term Stability ◽  
Solid Lipid ◽  
Wide Range

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.

scholarly journals Solid Lipid Nanoparticles as Effective Reservoir Systems for Long-Term Preservation of Multidose Formulations

2013 ◽  
Vol 14 (2) ◽  
pp. 847-853 ◽  
Author(s):  
Felice Cerreto ◽  
Patrizia Paolicelli ◽  
Stefania Cesa ◽  
Hend M. Abu Amara ◽  
Felicia Diodata D’Auria ◽  
...  
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Lipid Nanoparticles ◽  
Solid Lipid ◽  
Reservoir Systems ◽  
Long Term Preservation

scholarly journals Long-term Stable Cationic Solid Lipid Nanoparticles for the Enhanced Intracellular Delivery of SMAD3 Antisense Oligonucleotides in Activated Murine Macrophages

2012 ◽  
Vol 15 (3) ◽  
pp. 467 ◽  
Author(s):  
Su-Eon Jin ◽  
Chong-Kook Kim
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Antisense Oligonucleotides ◽  
Lipid Nanoparticles ◽  
Homogenization Method ◽  
Tween 20 ◽  
Solid Lipid ◽  
Intracellular Activity ◽  
Macrophage Cells ◽  
Anti Inflammatory

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.

scholarly journals Short Term Stability Testing of Efavirenz-Loaded Solid Lipid Nanoparticle (SLN) and Nanostructured Lipid Carrier (NLC) Dispersions

Pharmaceutics ◽  
2019 ◽  
Vol 11 (8) ◽  
pp. 397 ◽  
Author(s):  
Pedzisai A. Makoni ◽  
Kasongo Wa Kasongo ◽  
Roderick B. Walker
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Encapsulation Efficiency ◽  
Lipid Nanoparticles ◽  
Nanostructured Lipid Carriers ◽  
Nanostructured Lipid Carrier ◽  
Solid Lipid Nanoparticle ◽  
Short Term ◽  
Term Stability ◽  
Solid Lipid ◽  
Lipid Nanoparticle

The short term stability of efavirenz-loaded solid lipid nanoparticle and nanostructured lipid carrier dispersions was investigated. Hot High Pressure Homogenization with the capability for scale up production was successfully used to manufacture the nanocarriers without the use of toxic organic solvents for the first time. Glyceryl monostearate and Transcutol® HP were used as the solid and liquid lipids. Tween® 80 was used to stabilize the lipid nanocarriers. A Box-Behnken Design was used to identify the optimum operating and production conditions viz., 1100 bar for 3 cycles for the solid lipid nanoparticles and 1500 bar for 5 cycles for nanostructured lipid carriers. The optimized nanocarriers were predicted to exhibit 10% efavirenz loading with 3% and 4% Tween® 80 for solid lipid nanoparticles and nanostructured lipid carriers, respectively. Characterization of the optimized solid lipid nanoparticle and nanostructured lipid carrier formulations in relation to shape, surface morphology, polymorphism, crystallinity and compatibility revealed stable formulations with particle sizes in the nanometer range had been produced. The nanocarriers had excellent efavirenz loading with the encapsulation efficiency >90%. The optimized nanocarriers exhibited biphasic in vitro release patterns with an initial burst release during the initial 0–3 h followed by sustained release over a 24 h period The colloidal systems showed excellent stability in terms of Zeta potential, particle size, polydispersity index and encapsulation efficiency when stored for 8 weeks at 25 °C/60% RH in comparison to when stored at 40 °C/75% RH. The formulations manufactured using the optimized conditions and composition proved to be physically stable as aqueous dispersions.

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