Self-assembled biodegradable amphiphilic PEG–PCL–lPEI triblock copolymers at the borderline between micelles and nanoparticles designed for drug and gene delivery

Endres, Thomas; Beck-Broichsitter, Moritz; Samsonova, Olga; Renette, Thomas; Kissel, Thomas

doi:10.1016/j.biomaterials.2011.06.064

Cited by 162 publications

(131 citation statements)

References 44 publications

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“…35 The polymeric micelles used in this study had a relatively small average hydrodynamic diameter of 27.74 nm, a narrow size distribution with a PDI of 0.212, and a moderate positive charge of 12.12 mV, all of which are consistent with previous reports (Table 1). 23 Based on the SEM findings, all of the particles exhibited a spherical shape and were uniform in size ( Figure 5A). Control groups were established to evaluate the effects of particle size (FDA microparticles group) and zeta potential (FDA nanoparticles group and PEG-PCL micelle group) on the corneal penetration of drugs.…”

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confidence: 94%

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Positively charged micelles based on a triblock copolymer demonstrate enhanced corneal penetration

Li¹,

Li²,

Zhou³

et al. 2015

IJN

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Purpose The cornea is a main barrier to drug penetration after topical application. The aim of this study was to evaluate the abilities of micelles generated from a positively charged triblock copolymer to penetrate the cornea after topical application. Methods The triblock copolymer poly(ethylene glycol)-poly(ε-caprolactone)- g -polyethyleneimine was synthesized, and the physicochemical properties of the self-assembled polymeric micelles were investigated, including hydrodynamic size, zeta potential, morphology, drug-loading content, drug-loading efficiency, and in vitro drug release. Using fluorescein diacetate as a model drug, the penetration capabilities of the polymeric micelles were monitored in vivo using a two-photon scanning fluorescence microscopy on murine corneas after topical application. Results The polymer was successfully synthesized and confirmed using nuclear magnetic resonance and Fourier transform infrared. The polymeric micelles had an average particle size of 28 nm, a zeta potential of approximately +12 mV, and a spherical morphology. The drug-loading efficiency and drug-loading content were 75.37% and 3.47%, respectively, which indicates that the polymeric micelles possess a high drug-loading capacity. The polymeric micelles also exhibited controlled-release behavior in vitro. Compared to the control, the positively charged polymeric micelles significantly penetrated through the cornea. Conclusion Positively charged micelles generated from a triblock copolymer are a promising vehicle for the topical delivery of hydrophobic agents in ocular applications.

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“…23 Briefly, mPEG and ε-CL (at an amount calculated to result in the designated PCL block length) were placed into a reaction flask and dried at reduced pressure at a temperature of 70°C for 2 hours. Subsequently, the flask was purged with dry argon and Sn(Oct) 2 (0.1 mol% corresponding to ε-CL), sealed under dry argon, and immersed in an oil bath.…”

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confidence: 99%

Positively charged micelles based on a triblock copolymer demonstrate enhanced corneal penetration

Li¹,

Li²,

Zhou³

et al. 2015

IJN

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“…Methoxy poly(ethylene glycol) (MPEG)-based modification has attracted increasing attention in the field of drug delivery due to its relatively low melting point that enables it to be fabricated by existing melt processing techniques and the ability to stabilize the delivery vehicle against undesirable aggregation and non-specific electrostatic www.nature.com/aps Peng W et al Acta Pharmacologica Sinica npg interactions with its surroundings [7] . Furthermore, PEG segments also counteract protein absorption, which increase the circulatory half-life in the body [8][9][10] due to its chain flexibility, high surface density and the absence of functional groups. Thus, in the present work, the amphiphilic matrix of methoxy poly(ethylene glycol)-poly(ε-caprolactone) (MPEG-PCL) containing a high percentage of PEG segments was synthesized via ring opening polymerization [11] and used for the delivery of CAP for the first time.…”

Section: Introductionmentioning

confidence: 99%

Oral delivery of capsaicin using MPEG-PCL nanoparticles

et al. 2014

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Aim: To prepare a biodegradable polymeric carrier for oral delivery of a water-insoluble drug capsaicin (CAP) and evaluate its quality. Methods: CAP-loaded methoxy poly (ethylene glycol)-poly(ε-caprolactone) nanoparticles (CAP/NPs) were prepared using a modified emulsification solvent diffusion technique. The quality of CAP/NPs were evaluated using transmission electron microscopy, powder X-ray diffraction, differential scanning calorimetry and Fourier transform infrared techniques. A dialysis method was used to analyze the in vitro release profile of CAP from the CAP/NPs. Adult male rats were orally administered CAP/NPs (35 mg/kg), and the plasma concentrations of CAP were measured with a validated HPLC method. The morphology of rat gastric mucosa was studied with HE staining. Results: CAP/NPs had an average diameter of 82.54±0.51 nm, high drug-loading capacity of 14.0%±0.13% and high stability. CAP/NPs showed a biphasic release profile in vitro: the burst release was less than 25% of the loaded drug within 12 h followed by a more sustained release for 60 h. The pharmacokinetics study showed that the mean maximum plasma concentration was observed 4 h after oral administered of CAP/NPs, and approximately 90 ng/mL of CAP was detected in serum after 36 h. The area under the curve for the CAP/NPs group was approximately 6-fold higher than that for raw CAP suspension. Histological studies showed that CAP/NPs markedly reduced CAP-caused gastric mucosa irritation. Conclusion: CAP/NPs significantly enhance the bioavailability of CAP and markedly reduce gastric mucosa irritation in rats.

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“…It can shield PEI to decrease its cytotoxicity and increase the circulation time and stability in the shell of gene delivery micelles. 50 The pEGFP-ZNF580 could be condensed and loaded by these MPs to form complexes. In the present study, to testify whether the different mPEG/PEI ratios of complexes influence the transfection efficiency of complexes dramatically or not, a series of MPs consisting of different mass ratios of mPEG-b-P(MMDco-LA) to P(MMD-co-LA)-g-PEI were prepared.…”

Section: Discussionmentioning

confidence: 99%

Co-self-assembly of cationic microparticles to deliver pEGFP-ZNF580 for promoting the transfection and migration of endothelial cells

Feng¹,

Guo²,

Li³

et al. 2016

IJN

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Self-assembled biodegradable amphiphilic PEG–PCL–lPEI triblock copolymers at the borderline between micelles and nanoparticles designed for drug and gene delivery

Cited by 162 publications

References 44 publications

Positively charged micelles based on a triblock copolymer demonstrate enhanced corneal penetration

Positively charged micelles based on a triblock copolymer demonstrate enhanced corneal penetration

Oral delivery of capsaicin using MPEG-PCL nanoparticles

Co-self-assembly of cationic microparticles to deliver pEGFP-ZNF580 for promoting the transfection and migration of endothelial cells

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