Design and characterization of a new drug nanocarrier made from solid–liquid lipid mixtures

García-Fuentes, Marcos; Alonso, Marı́a José; Torres, Dolores

doi:10.1016/j.jcis.2004.10.012

Cited by 74 publications

(34 citation statements)

References 32 publications

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“…NE showed the smallest particle size as well as lowest PI value. These findings are in agreement with that reported by Garcia-Fuentes et al (2005) and Ali et al (2010). Our results are in contrast to the work of Lin et al (2007) who found that particle size of NLC prepared using monocaprate (solid lipid), and medium chain triglyceride (liquid lipid) depended on the content of liquid lipid loading.…”

Section: Physicochemical Characterisation Of Sln Nlc and Nesupporting

confidence: 92%

“…It was reported that the prerequisite to obtain high drug loading is the creation of less ordered solid matrix in lipid nanoparticles. For a number of drugs, the solubility in oils is higher than their solubility in solid lipids and the incorporation of liquid lipid to solid lipid can lead to massive crystal order disturbances in the matrix of lipid nanoparticles leading to improved drug encapsulation efficiency and a reduced drug leakage during storage (Muller et al, 2002b;Garcia-Fuentes et al, 2005). In our study, it was clear that the E.E of NLC were enhanced with increasing the content of CA.…”

Section: Drug Eementioning

confidence: 61%

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Development of nanostructured lipid carriers for controlled delivery of mefenamic acid

Khurana

Bedi

Jain

2012

IJBNN

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This study was aimed to develop nanostructured lipid carriers (NLC) for the possible delivery of mefenamic acid. This study describes the effect of liquid lipid concentration on the characteristics of NLC such as particle size, polydispersity index, zeta potential, drug entrapment efficiency, and occlusivity index. Transmission electron microscopy revealed nearly spherical shape NLC with negligible effect of liquid lipid content on the particle morphology. The differential scanning calorimetry demonstrated a depression in the melting point and crystallinity index of the NLC with an increase in the amount of liquid lipid. The in vitro drug release studies demonstrated that solid lipid nanoparticle (0% oil), and NLC possessed a biphasic release pattern characterised by a rapid initial release followed by a sustained release, in comparison to nanoemulsions (100% oil) of which a nearly constant release was observed. Compared to NE and SLN, the excellent physical stability of NLC against drug leakage was seen.

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Section: Physicochemical Characterisation Of Sln Nlc and Nesupporting

confidence: 92%

Section: Drug Eementioning

confidence: 61%

Development of nanostructured lipid carriers for controlled delivery of mefenamic acid

Khurana

Bedi

Jain

2012

IJBNN

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“…13 , 14 Bioactive TGFβ3 released from PLA microgrooved surfaces inhibits the proliferation of lung epithelial cells for up to 24 hours. 15 Previous attempts at controlled release of cytokines include lipid nanoparticles, 16 chitosan or gelatinbased particles, 17 , 18 collagen, 19 , 20 ceramics, 21 , 22 and porous glass. 23 Although the shortterm bioactivity of TGFβ3 has been investigated, exploration of prolonged release via microencapsulation is necessary for widespread needs to regulate cellular activities in the long term during wound healing and tissue regeneration.…”

Section: Introductionmentioning

confidence: 99%

Sustained Release of TGFβ3 from PLGA Microspheres and Its Effect on Early Osteogenic Differentiation of Human Mesenchymal Stem Cells

et al. 2006

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Despite the widespread role of transforming growth factor-β3 (TGFβ3) in wound healing and tissue regeneration, its long-term controlled release has not been demonstrated. Here, we report microencapsulation of TGFβ3 in poly-d-l-lactic-co-glycolic acid (PLGA) microspheres and determine its bioactivity. The release profiles of PLGA-encapsulated TGFβ3 with 50:50 and 75:25 PLA:PGA ratios differed throughout the experimental period. To compare sterilization modalities of microspheres, bFGF was encapsulated in 50:50 PLGA microspheres and subjected to ethylene oxide (EO) gas, radiofrequency glow discharge (RFGD), or ultraviolet (UV) light. The release of bFGF was significantly attenuated by UV light, but not significantly altered by either EO or RFGD. To verify its bioactivity, TGFβ3 (1.35 ng/mL) was control-released to the culture of human mesenchymal stem cells (hMSC) under induced osteogenic differentiation. Alkaline phosphatase staining intensity was markedly reduced 1 week after exposing hMSC-derived osteogenic cells to TGFβ3. This was confirmed by lower alkaline phosphatase activity (2.25 ± 0.57 mU/mL/ng DNA) than controls (TGFβ3-free) at 5.8 ± 0.9 mU/mL/ng DNA (p < 0.05). Control-released TGFβ3 bioactivity was further confirmed by lack of significant differences in alkaline phosphatase upon direct addition of 1.35 ng/mL TGFβ3 to cell culture (p > 0.05). These findings provide baseline data for potential uses of microencapsulated TGFβ3 in wound healing and tissue-engineering applications.

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“…We have previously described several modifications that can be applied to the core and the shell of lipid nanocarriers [16,19,26]. Based on this structural flexibility of lipid nanocarriers, we proposed the potential interest of PEG-NC as delivery systems for drugs with poor solubility both in water and in oils.…”

Section: Encapsulation Of F10320d1 In Peg-ncmentioning

confidence: 99%

“…Moreover, PEG-STE may form phase-separated solid lipid layers on the surface of the nanocapsules, which could act as a diffusional barrier to prevent drug leakage. Indeed,we have previously measured the diffusion coefficients of PEG-STE coated nanoparticles by NMR and we have found that while the diffusion coefficient of the particles was 9,9x10 -13 m 2 s -1 (corresponding to the Brownian motion of a sphere of 200nm, the size of the nanoparticle), the observed diffusion coefficient for the oil inside the particle was 35 times higher and similar to the pure oil (3x10 -11 m 2 s -1 ), indicating the confinement of the oil inside the protective PEG-STE monolayer [19]. We hypothesized that the presence of a solid surfactant shell on the surface could be useful to impart controlled release to PEG-NC loaded with drugs with modest solubility in water and oils, providing we were able to integrate the drug in the lipid core of the nanocarrier.…”

mentioning

confidence: 91%

PEGylated Lipid Nanocapsules with Improved Drug Encapsulation and Controlled Release Properties

Hervella¹,

Alonso-Sande²,

Lédo³

et al. 2014

CTMC

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Drugs with poor lipid and water solubility are some of the most challenging to formulate in nanocarriers, typically resulting in low encapsulation efficiencies and uncontrolled release profiles. PEGylated nanocapsules (PEG-NC) are known for their amenability to diverse modifications that allow the formation of domains with different physicochemical properties, an interesting feature to address a drug encapsulation problem. We explored this problem by encapsulating in PEG-NC the promising anticancer drug candidate F10320GD1, used herein as a model for compounds with such characteristics. The nanocarriers were prepared from Miglyol®, lecithin and PEG-sterate through a solvent displacement technique. The resulting system was a homogeneous suspension of particles with size around 200 nm. F10320GD1 encapsulation was found to be very poor (<15%) if PEG-NC were prepared using water as continuous phase; but we were able to improve this value to 85% by fixing the pH of the continuous phase to 9. Interestingly, this modification also improved the controlled release properties and the chemical stability of the formulation during storage. These differences in pharmaceutical properties together with physicochemical data suggest that the pH of the continuous phase used for PEG-NC preparation can modify drug allocation, from the external shell towards the inner lipid core of the nanocapsules. Finally, we tested the bioactivity of the drug-loaded PEG-NC in several tumor cell lines, and also in endothelial cells. The results indicated that drug encapsulation led to an improvement on drug cytotoxicity in tumor cells, but not in non-tumor endothelial cells. Altogether, the data confirms that PEG-NC show adequate delivery properties for F10320GD1, and underlines its possible utility as an anticancer therapy. Graphical Abstract:!

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Design and characterization of a new drug nanocarrier made from solid–liquid lipid mixtures

Cited by 74 publications

References 32 publications

Development of nanostructured lipid carriers for controlled delivery of mefenamic acid

Development of nanostructured lipid carriers for controlled delivery of mefenamic acid

Sustained Release of TGFβ3 from PLGA Microspheres and Its Effect on Early Osteogenic Differentiation of Human Mesenchymal Stem Cells

PEGylated Lipid Nanocapsules with Improved Drug Encapsulation and Controlled Release Properties

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