Novel PEG-grafted nanostructured lipid carrier for systematic delivery of a poorly soluble anti-leukemia agent Tamibarotene: characterization and evaluation

Liu, Xin; Zhang, Zhihua; Jiang, Yuqi; Hu, Yue; Wang, Zhonglan; Feng, Ruihua; Zhang, Jie; Huang, Guihua

doi:10.3109/10717544.2014.885614

Cited by 21 publications

(16 citation statements)

References 32 publications

(31 reference statements)

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“…Apparently, the release rate of BN-PEG-NLC was faster than that of BN-NLC. It could be explained by the fact that amphiphilic PEG chains on the NLC acting as a hydrophilic shield may reduce the surface tension of the NLC, and make the NLC surface to be wet easily (Yuan et al, 2007;Liu X et al, 2015).…”

Section: Discussionmentioning

confidence: 99%

Baicalin-loaded PEGylated lipid nanoparticles: characterization, pharmacokinetics, and protective effects on acute myocardial ischemia in rats

2016

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Section: Discussionmentioning

confidence: 99%

Baicalin-loaded PEGylated lipid nanoparticles: characterization, pharmacokinetics, and protective effects on acute myocardial ischemia in rats

2016

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“…It is known that Am580, an isomer of Am80, crosses the blood-brain barrier in mice [17]. Am80 has been reported to attain some extent of access into the brain: cerebral tissue content of Am80 in normal male rats reaches around 100 pmol/g tissue at 2 h after subcutaneous administration of the drug at 1 mg/kg, then decreased at 6 h, and returned to the control levels at 24-120 h [76,77]. Rarβ is a target gene of RAR/RXR, and Rarβ mRNA was not increased by Am80/HX630 treatment in vivo (Supplementary Figure 13A), in contrast to the in vitro study (Fig.…”

Section: Discussionmentioning

confidence: 99%

Cooperative Therapeutic Action of Retinoic Acid Receptor and Retinoid X Receptor Agonists in a Mouse Model of Alzheimer's Disease

Kawahara

Suenobu

Ohtsuka

et al. 2014

JAD

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Abstract. Alzheimer's disease (AD) is a neurodegenerative process involving amyloid-␤ (A␤) peptide deposition, neuroinflammation, and progressive memory loss. Here, we evaluated whether oral administration of retinoic acid receptor (RAR)␣,␤ agonist Am80 (tamibarotene) or specific retinoid X receptor (RXR) pan agonist HX630 or their combination could improve deficits in an AD model, 8.5-month-old amyloid-␤ protein precursor 23 (A␤PP23) mice. Co-administration of Am80 (0.5 mg/kg) and HX630 (5 mg/kg) for 17 days significantly improved memory deficits (Morris water maze) in A␤PP23 mice, whereas administration of either agent alone produced no effect. Only co-administration significantly reduced the level of insoluble A␤ peptide in the brain. These results thus indicate that effective memory improvement via reduction of insoluble A␤ peptide in 8.5-month-old A␤PP23 mice requires co-activation of RAR␣,␤ and RXRs. RAR␣-positive microglia accumulated A␤ plaques in the A␤PP23 mice. Rat primary microglia co-treated with Am80/HX630 showed increased degradation activity towards 125 I-labeled oligomeric A␤ 1-42 peptide in an insulin-degrading enzyme (IDE)-dependent manner. The co-administration increased mRNA for IDE and membrane-associated IDE protein in vivo, suggesting that IDE contributes to A␤ clearance in Am80/HX630-treated A␤PP23 mice. Am80/HX630 also increased IL-4R␣ expression in microglial MG5 cells. The improvement in memory of Am80/HX630-treated A␤PP23 mice was correlated with the levels and signaling of hippocampal interleukin-4 (IL-4). Therefore, Am80/HX630 may promote differentiation of IL-4-responsive M2-like microglia and increase their activity for clearance of oligomeric A␤ peptides by restoring impaired IL-4 signaling in A␤PP23 mice. Combination treatment with RAR and RXR agonists may be an effective approach for AD therapy.

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“…[34][35][36] Various strategies such as emulsion solvent evaporation, solvent dispersion, and nano-crystallization have been used to improve the bioavailability of poorly soluble drugs. Lipids, including phospholipids, can serve as drug carriers in eye drops owing to their excellent capacity for encapsulation, safety, and biocompatibility.…”

Section: Preparation and Characterization Of L/npsmentioning

confidence: 99%

Corneal permeation properties of a charged lipid nanoparticle carrier containing dexamethasone

Ban¹,

Zhang²,

Huang³

et al. 2017

IJN

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Drug delivery carriers can maintain effective therapeutic concentrations in the eye. To this end, we developed lipid nanoparticles (L/NPs) in which the surface was modified with positively charged chitosan, which engaged in hydrogen bonding with the phospholipid membrane. We evaluated in vitro corneal permeability and release characteristics, ocular irritation, and drug dynamics of modified and unmodified L/NPs in aqueous humor. The size of L/NPs was uniform and showed a narrow distribution. Corneal permeation was altered by the presence of chitosan and was dependent on particle size; the apparent permeability coefficient of dexamethasone increased by 2.7 and 1.8 times for chitosan-modified and unmodified L/NPs, respectively. In conclusion, a chitosan-modified system could be a promising method for increasing the ocular bioavailability of unmodified L/NPs by enhancing their retention time and permeation into the cornea. These findings provide a theoretical basis for the development of effective drug delivery systems in the treatment of ocular disease.

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Novel PEG-grafted nanostructured lipid carrier for systematic delivery of a poorly soluble anti-leukemia agent Tamibarotene: characterization and evaluation

Cited by 21 publications

References 32 publications

Baicalin-loaded PEGylated lipid nanoparticles: characterization, pharmacokinetics, and protective effects on acute myocardial ischemia in rats

Baicalin-loaded PEGylated lipid nanoparticles: characterization, pharmacokinetics, and protective effects on acute myocardial ischemia in rats

Cooperative Therapeutic Action of Retinoic Acid Receptor and Retinoid X Receptor Agonists in a Mouse Model of Alzheimer's Disease

Corneal permeation properties of a charged lipid nanoparticle carrier containing dexamethasone

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