Nanostructured lipid carriers: Promising drug delivery systems for future clinics

Beloqui, Ana; Solinís, Maria Ángelés; Rodríguez-Gascón, Alicia; Almeida, António J.; Préat, Véronique

doi:10.1016/j.nano.2015.09.004

Cited by 524 publications

(278 citation statements)

References 166 publications

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“…Nanostructured lipid carriers (NLCs), consisting of solid and liquid lipids, have the advantages of improved drug entrapment efficiency (EE%) and drug loading (DL%) capacity for drugs with poor pharmacokinetic properties. 20,21 The lipophilic characteristic of NLCs makes it easy to be captured by the reticuloendothelial system in vivo. 22 Various solutions have been attempted to overcome these obstacles in recent years.…”

Section: Introductionmentioning

confidence: 99%

Effect of A-317491 delivered by glycolipid-like polymer micelles on endometriosis pain

Yuan

Ding

Meng

et al. 2017

IJN

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Endometriosis is a common gynecological disease with a lack of effective clinical treatment. Current therapy often results in endometriosis pain recurrence and serious side effects. P2X 3 receptor, an adenosine triphosphate (ATP)-gated ion channel, might be implicated in endometriosis pain. In this study, chitosan oligosaccharide-g-stearic acid (CSOSA) polymer micelles-coated nanostructured lipid carriers (NLCs) were developed as a novel delivery system for A-317491, a selective P2X 3 receptor antagonist for endometriosis pain therapy. A-317491-loaded NLC (NLC/A-317491) could be coated by CSOSA micelles to form CSOSA/NLC/A-317491 nanoparticles. Pheochromocytoma PC12 cells, which highly expressed P2X 3 receptors, were used as a cell model, and the CSOSA/NLC/A-317491 partly blocked the Ca 2+ influx induced by ATP stimulation. In nude mouse and rat endometriotic models, CSOSA/NLC could accumulate into endometriotic lesions after vein injection. In endometriotic rats, CSOSA/NLC/A-317491 reversed mechanical and heat hyperalgesia with long-term efficacy, which might be attributed to the massive CSOSA/NLC/A-317491 distribution in the endometriotic lesions. In conclusion, A-317491 delivered by CSOSA/NLC nanoparticles attenuated endometriosis pain in rats, and CSOSA/NLC/A-317491 could be used as an effective treatment strategy for P2X 3 -targeted therapy in endometriosis pain.

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Section: Introductionmentioning

confidence: 99%

Effect of A-317491 delivered by glycolipid-like polymer micelles on endometriosis pain

Yuan

Ding

Meng

et al. 2017

IJN

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“…For the selective transduction in cancers, various improved AAVs have been reported by targeting tumorspecific antigens [68]. Additionally, non-viral delivery mediated by lipid nanoparticles is also a promising technique [69]. Nevertheless, epigenome editing tools should ideally be introduced into all the cancer cells; thus, there is still a hurdle to translate this technology into clinics.…”

Section: Discussionmentioning

confidence: 99%

Cancer induction and suppression with transcriptional control and epigenome editing technologies

2017

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Cancer epigenetics is one of the most important research subjects in dissecting cancer mechanisms and therapeutic targets because the emergence and malignant transformation of various cancers are caused by unnatural expression of cancer-related genes attributed to their epigenetic errors. The original concept of cancer epigenetics basically stands on the analysis of the epigenetic status in naturally occurring cancer cells; however, the rapidly emerging technology called epigenome editing would change this situation drastically. Epigenome editing, the most promising derivative technology of genome editing, can modify the epigenetic states at the pre-defined genomic locus using the programmable effectors, consisting of various epigenetic factors combined with site-specific DNA-binding domains. This technology can be utilized in a reversible manner; i.e., cancer modeling can be achieved by introducing aberrant epigenetic marks in normal cells, and cancer suppression can be achieved by correcting the epigenetic errors in cancer cells. In this review, we summarize the basics of epigenome editing and cancer epigenetics, followed by the current examples of cancer induction and suppression with the transcriptional control and epigenome editing technologies.

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“…Possible reasons for increased oral absorption of Cur NLCs are increased drug solubility in nanoparticle form, obviated degradation of drugs by gastric acid and digestive enzymes, and NLCs' property of eluding drug efflux of through the Pgp pump. 49 As shown in Figure 4C, oral administration of Cur-TCA NLCs and Cur NLCs produced quite different plasma profiles of Cur. TCA-NLC formulations of Cur exhibited superior oral bioavailability.…”

Section: Pharmacokinetic Studiesmentioning

confidence: 94%

“…Near-neutral NLC surface charge has been reported to enhance permeability by averting mucus entrapment of the carrier, owing to the mucus-carrier electrostatic interaction. 49 The ζ-potential of TCA NLCs was about -7 to -3 mV, and might have assisted in the penetration of NLCs across the mucus layer. Cur-TCA 20 NLCs were selected for further studies on identifying sitespecific absorption through the small intestine.…”

mentioning

confidence: 99%

Improving intestinal absorption and oral bioavailability of curcumin via taurocholic acid-modified nanostructured lipid carriers

Tian¹,

Asghar²,

Wu³

et al. 2017

IJN

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The expression of multiple receptors on intestinal epithelial cells enables an actively targeted carrier to significantly enhance the oral delivery of payloads. Conjugating the receptors’ ligands on the surfaces of a particulate-delivery system allows site-specific targeting. Here, we used taurocholic acid (TCA) as a ligand for uptake of nanostructured lipid carriers (NLCs) mediated by a bile-acid transporter to improve oral bioavailability of curcumin (Cur). First, synthesis of TCA–polyethylene glycol 100–monostearate (S100-TCA) was carried out. Then, the physical and chemical properties of S100-TCA-modified Cur-loaded NLCs (Cur-TCA NLCs) with varying levels of S100-TCA modifications were investigated. Small particle size (<150 nm), high drug encapsulation (>90%), drug loading (about 3%), negative ζ-potential (−7 to −3 mV), and sustained release were obtained. In situ intestinal perfusion studies demonstrated improved absorption rate and permeability coefficient of Cur-TCA NLCs. Depending on the degree of modification, Cur-TCA NLCs displayed about a five- to 15-fold higher area under the curve in rats after oral administration than unmodified Cur NLCs, which established that the addition of S100-TCA to the NLCs boosted absorption of Cur. Further investigations of TCA NLCs might reveal a bright future for effective oral delivery of poorly bioavailable drugs.

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Nanostructured lipid carriers: Promising drug delivery systems for future clinics

Cited by 524 publications

References 166 publications

Effect of A-317491 delivered by glycolipid-like polymer micelles on endometriosis pain

Effect of A-317491 delivered by glycolipid-like polymer micelles on endometriosis pain

Cancer induction and suppression with transcriptional control and epigenome editing technologies

Improving intestinal absorption and oral bioavailability of curcumin via taurocholic acid-modified nanostructured lipid carriers

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