DSPE-PEG: A Distinctive Component in Drug Delivery System

Che, Jianfei; Okeke, Chukwunweike Ikechukwu; Hu, Zhongbo; Xu, Jing

doi:10.2174/1381612821666150115144003

Cited by 104 publications

(76 citation statements)

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“…It is a PEGylated phospholipid that has been widely used for the preparation of various nano-carrier formulations, such as micelles, long-circulating liposomes or lipid-protected particles, where the PEG layer often acts as a steric barrier that protects the molecular assemblies against uptake by the mononuclear phagocytic system (MPS) to produce a prolonged blood circulation time, improved stability and increased encapsulation efficiency24.…”

Section: Resultsmentioning

confidence: 99%

A self-assembling nanomedicine of conjugated linoleic acid-paclitaxel conjugate (CLA-PTX) with higher drug loading and carrier-free characteristic

Zhong

Yao

Zhang

et al. 2016

Sci Rep

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The main objective of this study was to demonstrate the proof-of-principle for the hypothesis that conjugated linoleic acid-paclitaxel conjugate (CLA-PTX), a novel fatty acid modified anti-cancer drug conjugate, could self-assemble forming nanoparticles. The results indicated that a novel self-assembling nanomedicine, CLA-PTX@PEG NPs (about 105 nm), with Cremophor EL (CrEL)-free and organic solvent-free characteristics, was prepared by a simple precipitation method. Being the ratio of CLA-PTX:DSPE-PEG was only 1:0.1 (w/w), the higher drug loading CLA-PTX@PEG NPs (about 90%) possessed carrier-free characteristic. The stability results indicated that CLA-PTX@PEG NPs could be stored for at least 9 months. The safety of CLA-PTX@PEG NPs was demonstrated by the MTD results. The anti-tumor activity and cellular uptake were also confirmed in the in vitro experiments. The lower crystallinity, polarity and solubility of CLA-PTX compared with that of paclitaxel (PTX) might be the possible reason for CLA-PTX self-assembling forming nanoparticles, indicating a relationship between PTX modification and nanoparticles self-assembly. Overall, the data presented here confirm that this drug self-delivery strategy based on self-assembly of a CLA-PTX conjugate may offer a new way to prepare nanomedicine products for cancer therapy involving the relationship between anticancer drug modification and self-assembly into nanoparticles.

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Section: Resultsmentioning

confidence: 99%

A self-assembling nanomedicine of conjugated linoleic acid-paclitaxel conjugate (CLA-PTX) with higher drug loading and carrier-free characteristic

Zhong

Yao

Zhang

et al. 2016

Sci Rep

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“…PEG-conjugated lipids are used extensively in the field of drug delivery as excipients30. DSPE-PEGs are biocompatible, biodegradable and have been a component of several nanoparticle platforms for drug or nucleic acid delivery that are undergoing clinical trials30313233.…”

Section: Discussionmentioning

confidence: 99%

“…DSPE-PEGs are biocompatible, biodegradable and have been a component of several nanoparticle platforms for drug or nucleic acid delivery that are undergoing clinical trials30313233. The liposomal formulation Doxil contains DSPE-PEG as one of its constituents and has been clinically approved for use against ovarian cancer and AIDS related Kaposi sarcoma34.…”

Section: Discussionmentioning

confidence: 99%

PEG-lipid micelles enable cholesterol efflux in Niemann-Pick Type C1 disease-based lysosomal storage disorder

Brown

Patel

Ward

et al. 2016

Sci Rep

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2-Hydroxy-propyl-β-cyclodextrin (HPβCD), a cholesterol scavenger, is currently undergoing Phase 2b/3 clinical trial for treatment of Niemann Pick Type C-1 (NPC1), a fatal neurodegenerative disorder that stems from abnormal cholesterol accumulation in the endo/lysosomes. Unfortunately, the extremely high doses of HPβCD required to prevent progressive neurodegeneration exacerbates ototoxicity, pulmonary toxicity and autophagy-based cellular defects. We present unexpected evidence that a poly (ethylene glycol) (PEG)-lipid conjugate enables cholesterol clearance from endo/lysosomes of Npc1 mutant (Npc1−/−) cells. Herein, we show that distearyl-phosphatidylethanolamine-PEG (DSPE-PEG), which forms 12-nm micelles above the critical micelle concentration, accumulates heavily inside cholesterol-rich late endosomes in Npc1−/− cells. This potentially results in cholesterol solubilization and leakage from lysosomes. High-throughput screening revealed that DSPE-PEG, in combination with HPβCD, acts synergistically to efflux cholesterol without significantly aggravating autophagy defects. These well-known excipients can be used as admixtures to treat NPC1 disorder. Increasing PEG chain lengths from 350 Da-30 kDa in DSPE-PEG micelles, or increasing DSPE-PEG content in an array of liposomes packaged with HPβCD, improved cholesterol egress, while Pluronic block copolymers capable of micelle formation showed slight effects at high concentrations. We postulate that PEG-lipid based nanocarriers can serve as bioactive drug delivery systems for effective treatment of lysosomal storage disorders.

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“…Although specific bacteriophages for C. parapsilosis have been not yet identified, the disadvantage of phage therapy includes the potential ability of bacteriophages to transfer the DNA from a microbe to another. This DNA transfer could be in charge of the transfer of pathogenicity determinants and virulence factors, resulting in the generation of even more resistant microbial strains [45–47]. Although the toxicity of mPEG-PCL to the skin has not been evaluated, the mPEG-PCL, a highly biocompatible and biodegradable copolymer, has been widely used as a component of nanoparticles for transdermal delivery [48].…”

Section: Discussionmentioning

confidence: 99%

The mPEG-PCL Copolymer for Selective Fermentation of Staphylococcus lugdunensis Against Candida parapsilosis in the Human Microbiome

Kao

Wang

Marito

et al. 2016

J Microb Biochem Technol

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Many human skin diseases, such as seborrheic dermatitis, potentially occur due to the over-growth of fungi. It remains a challenge to develop fungicides with a lower risk of generating resistant fungi and non-specifically killing commensal microbes. Our probiotic approaches using a selective fermentation initiator of skin commensal bacteria, fermentation metabolites or their derivatives provide novel therapeutics to rein in the over-growth of fungi. Staphylococcus lugdunensis (S. lugdunensis) bacteria and Candida parapsilosis (C. parapsilosis) fungi coexist in the scalp microbiome. S. lugdunensis interfered with the growth of C. parapsilosis via fermentation. A methoxy poly(ethylene glycol)-b-poly(ε-caprolactone) (mPEG-PCL) copolymer functioned as a selective fermentation initiator of S. lugdunensis, selectively triggering the S. lugdunensis fermentation to produce acetic and isovaleric acids. The acetic acid and its pro-drug diethyleneglycol diacetate (Ac-DEG-Ac) effectively suppressed the growth of C. parapsilosis in vitro and impeded the fungal expansion in the human dandruff. We demonstrate for the first time that S. lugdunensis is a skin probiotic bacterium that can exploit mPEG-PCL to yield fungicidal short-chain fatty acids (SCFAs). The concept of bacterial fermentation as a part of skin immunity to re-balance the dysbiotic microbiome warrants a novel avenue for studying the probiotic function of the skin microbiome in promoting health.

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DSPE-PEG: A Distinctive Component in Drug Delivery System

Cited by 104 publications

References 0 publications

A self-assembling nanomedicine of conjugated linoleic acid-paclitaxel conjugate (CLA-PTX) with higher drug loading and carrier-free characteristic

A self-assembling nanomedicine of conjugated linoleic acid-paclitaxel conjugate (CLA-PTX) with higher drug loading and carrier-free characteristic

PEG-lipid micelles enable cholesterol efflux in Niemann-Pick Type C1 disease-based lysosomal storage disorder

The mPEG-PCL Copolymer for Selective Fermentation of Staphylococcus lugdunensis Against Candida parapsilosis in the Human Microbiome

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