Solid lipid nanoparticles

Mehnert, W.; Mäder, Karsten

doi:10.1016/j.addr.2012.09.021

Cited by 663 publications

(139 citation statements)

References 105 publications

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“…The main advantages of these systems include protection of labile substances from chemical degradation, control of release of substances due to the solid state of the lipid matrix, low toxicity and formation of films over the skin showing occlusive properties [7][8][9].…”

Section: Introductionmentioning

confidence: 99%

Effect of Ouratea sp. butter in the crystallinity of solid lipids used in nanostructured lipid carriers (NLCs)

Galvão

Trindade

Santos

et al. 2015

J Therm Anal Calorim

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The aim of this work was to evaluate the effect of Ouratea sp. butter (OB) on crystallinity of solid lipids used in nanostructured lipid carriers systems. Firstly, the composition of fatty acids in OB was evaluated by transesterification reaction for gas chromatography fatty acid methyl ester analysis. The solid lipids such as stearic acid (SA), beeswax (BW) and carnauba wax (CW) were submitted to recrystallization process (heating-cooling). Moreover, binary mixtures between solid lipids and OB were prepared in ratio 1:1 (w/w) by heating of the components above the melting point followed by cooling at room temperature. Thus, the samples were characterized by differential scanning calorimetry (DSC), thermogravimetry (TG), X ray diffraction (XRD) and hot-stage polarized optical microscopy (HSPOM). DSC curves showed a shift of the melting point to lower temperatures in the lipid mixtures with OB. TG data suggested a thermal stability reduction in the lipid mixtures containing SA and CW and an increase thermal stability in the mixture containing BW. XRD data confirmed DSC results, showing a reduction in intensity of main diffraction peaks of the lipid mixtures and a presence of the amorphous portion in angle 2h: 22°. Finally, HSPOM demonstrated that the microstructures of solid lipids decreased in size and thickness in the mixtures containing OB at room temperature and slightly before the melting point, confirming previous characterizations. These results suggest that lipid mixtures with OB present a lower crystallinity, and it is expected that amorphous portion facilitates drug incorporation, for example.

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Section: Introductionmentioning

confidence: 99%

Effect of Ouratea sp. butter in the crystallinity of solid lipids used in nanostructured lipid carriers (NLCs)

Galvão

Trindade

Santos

et al. 2015

J Therm Anal Calorim

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“…To enhance the solubility of such poorly water-soluble APIs, the use of nanoparticle formulations with particle sizes less than 100 nm has recently attracted considerable attention in the field of pharmaceutical research. [1][2][3] Recently, we successfully prepared lipid nanoparticles (LNs), which had a mean particle size of approximately 50 nm with a narrow particle size distribution, using wet milling, roll mixing, and high pressure homogenization to form small particles. 4) The LNs improved the solubility of nifedipine (NI), a poorly water-soluble drug, and improved its oral absorption of NI when NI-LNs were administrated to rats.…”

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confidence: 99%

Effect of Alkyl Chain Length and Unsaturation of the Phospholipid on the Physicochemical Properties of Lipid Nanoparticles

Funakoshi

Iwao

Noguchi

et al. 2015

CHEMICAL & PHARMACEUTICAL BULLETIN

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Previously, we developed lipid nanoparticles (LNs) containing poorly water-soluble drugs using two types of phospholipids, a neutral phospholipid (hydrogenated soybean phosphatidylcholine) and a negativelycharged phospholipid (dipalmitoylphosphatidylglycerol), with mean particle sizes of less than 100 nm. Here, we studied the effects of alkyl chain length and unsaturation of neutral and negatively-charged phospholipids on the physicochemical properties of LNs. Three neutral phospholipids, dimyristoylphosphatidylcholine, dipalmitoylphosphatidylcholine and distearoylphosphatidylcholine, having different alkyl chain lengths, were compared. The mean particle size of the LNs increased with the alkyl chain length, while the concentration of the drug entrapped in the LNs decreased. The particle size of all of the LNs could be maintained at less than 100 nm for 1 month in cool and dark conditions, with the LNs with longer alkyl chain lipids showing greater stability. In the unsaturated phospholipids, the double bond in the alkyl chain of dioleoylphosphatidylcholine and dierucoylphosphatidylcholine did not affect the physicochemical properties of the LNs. The negatively-charged phospholipids dipalmitoylphosphatidylglycerol and distearoylphosphatidylglycerol were also compared; LNs with longer alkyl chain lipids had larger particle sizes and lower drug concentrations, similar to the results for neutral phospholipids. We concluded that although some changes in physicochemical properties were observed among LNs with different phospholipid alkyl chain lengths, this methodology was general. LNs with suitable physicochemical properties could be prepared irrespective of the type of phospholipids used.Key words lipid nanoparticle; poorly water-soluble drug; phospholipid; alkyl chain Many candidate active pharmaceutical ingredients (APIs) in formulations show poor solubility in water. To enhance the solubility of such poorly water-soluble APIs, the use of nanoparticle formulations with particle sizes less than 100 nm has recently attracted considerable attention in the field of pharmaceutical research.1-3) Recently, we successfully prepared lipid nanoparticles (LNs), which had a mean particle size of approximately 50 nm with a narrow particle size distribution, using wet milling, roll mixing, and high pressure homogenization to form small particles.4) The LNs improved the solubility of nifedipine (NI), a poorly water-soluble drug, and improved its oral absorption of NI when NI-LNs were administrated to rats. 5) NI-LNs showed excellent long-term stability in suspension for approximately 4 months in cool and dark conditions, and freeze-drying techniques combined with sugar as a cryoprotectant allowed the preparation of LNs with a good aqueous re-dispersibility.6,7) NI-LNs lyophilized with trehalose exhibited suitable pharmacokinetic properties and good biocompatibility. 8) Generally, two types of phospholipids, neutral phosphatidylcholine (PC) and negatively-charged phosphatidylglycerol (PG) are used to prepare LNs. PG was added to...

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“…For the production of LSNs and NLC, HPH is a reliable and powerful technique, and easily scalable for large quantities [17]. In addition, HPL leads to homogeneous products, with low tendency to aggregation and therefore more stable [18].…”

Section: Resultsmentioning

confidence: 99%

Natural lipids in nanostructured lipid carriers and its cytotoxicity

Lima

Rampazo

Costa

et al. 2017

J. Phys.: Conf. Ser.

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Abstract. Nanostructured lipid carriers (NLCs) are active carrier systems which modulate the sustained release of actives and protect unstable compounds against degradation. NLCs can also protect skin from sun light, due to its particulates nature, which gives them intrinsic scattering properties. In this work, we present the preparation of NLCs using natural lipids and its cytotoxicity profile. It was used a vegetal butter with melting point (m. o C). NLCs were prepared by hot high pressure homogenization method and particles were characterized by average size (Z ave ), polydispersity index (PDI) and zeta potential (PZ) (Fig.1). The thermal behavior of the NLCs was studied using Differential Scanning Calorimetry (DSC). All the formulations were followed up for 60 days in order to evaluate their stability. NLCs exhibited a Z ave around 150-200 nm, PDI less than 0.2 and PZ varying from -25 to -40 mV. The m.p. for the lyophilized NLCs was about 40-56°C. Cytotoxicity of the formulations were evaluated for human keratinocytes (HaCaT) and melanocytes (Melan-A) in the exponential growth phase. Cell viability was used as indicator of cytotoxicity and determined after 4 days of culture by MTT assay. It was found that the NLC formulations were not toxic against HaCaT and Melan-A cells. Results showed that the NLCs produced are potential carriers for nanocosmetics and sunscreen products.

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Solid lipid nanoparticles

Cited by 663 publications

References 105 publications

Effect of Ouratea sp. butter in the crystallinity of solid lipids used in nanostructured lipid carriers (NLCs)

Effect of Ouratea sp. butter in the crystallinity of solid lipids used in nanostructured lipid carriers (NLCs)

Effect of Alkyl Chain Length and Unsaturation of the Phospholipid on the Physicochemical Properties of Lipid Nanoparticles

Natural lipids in nanostructured lipid carriers and its cytotoxicity

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