Biodistribution properties of nanoparticles based on mixtures of PLGA with PLGA–PEG diblock copolymers

Beletsi, A.; Panagi, Z.; Avgoustakis, Konstantinos

doi:10.1016/j.ijpharm.2005.03.024

Cited by 117 publications

(72 citation statements)

References 19 publications

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“…2A). Increasing the percentage of PEG in the polymer and using a lower molecular weight (compared to the PLGA polymer) caused a decrease in diameter, a finding explained by copolymeric PEG decreasing polymer association during NP formation (Beletsi et al, 2005). F1 exhibited negative zeta potential values of -20.9 mV, which was significantly higher (P value < 0.001) than that of the PEGylated PLGA (F4 and F7) types (Fig.…”

Section: Effect Of Polymer Typementioning

confidence: 92%

Preparation and in vivo evaluation of insulin-loaded biodegradable nanoparticles prepared from diblock copolymers of PLGA and PEG

Haggag

Abdel-Wahab

Ojo

et al. 2016

International Journal of Pharmaceutics

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A B S T R A C TThe aim of this study was to design a controlled release vehicle for insulin to preserve its stability and biological activity during fabrication and release. A modified, double emulsion, solvent evaporation, technique using homogenisation force optimised entrapment efficiency of insulin into biodegradable nanoparticles (NP) prepared from poly (DL-lactic-co-glycolic acid) (PLGA) and its PEGylated diblock copolymers. Formulation parameters (type of polymer and its concentration, stabiliser concentration and volume of internal aqueous phase) and physicochemical characteristics (size, zeta potential, encapsulation efficiency, in vitro release profiles and in vitro stability) were investigated. In vivo insulin sensitivity was tested by diet-induced type II diabetic mice. Bioactivity of insulin was studied using Swiss TO mice with streptozotocin-induced type I diabetic profile. Insulin-loaded NP were spherical and negatively charged with an average diameter of 200-400 nm. Insulin encapsulation efficiency increased significantly with increasing ratio of co-polymeric PEG. The internal aqueous phase volume had a significant impact on encapsulation efficiency, initial burst release and NP size. Optimised insulin NP formulated from 10% PEG-PLGA retained insulin integrity in vitro, insulin sensitivity in vivo and induced a sustained hypoglycaemic effect from 3 h to 6 days in type I diabetic mice..

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Section: Effect Of Polymer Typementioning

confidence: 92%

Preparation and in vivo evaluation of insulin-loaded biodegradable nanoparticles prepared from diblock copolymers of PLGA and PEG

Haggag

Abdel-Wahab

Ojo

et al. 2016

International Journal of Pharmaceutics

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“…Recent observations indicate that very small particles can pass through the sinusoidal fenestrations in the liver and gain access to the parenchymal cells of the liver. 43, 44 Sonavane et al prepared gold nanoparticles of different particle sizes (15, 50, 100, and 200 nm) and distribution in organs like the liver, lung, and spleen and showed that tissue distribution of gold nanoparticles is size-dependent. 45 The smallest gold nanoparticles (15 nm) show the most widespread organ distribution.…”

Section: In Vivo Studiesmentioning

confidence: 99%

Pegylation of poly(γ-benzyl-L-glutamate) nanoparticles is efficient for avoiding mononuclear phagocyte system capture in rats

Özcan¹,

Segura‐Sánchez²,

Bouchemal³

et al. 2010

IJN

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Poly(γ-benzyl-L-glutamate) (PBLG) derivatives are synthetic polypeptides for preparing nanoparticles with well controlled surface properties. The aim of this paper was to investigate the biodistribution of pegylated PBLG in rats. For this purpose, nanoparticles were prepared by a nanoprecipitation method using mixtures of different PBLG derivates, including a pegylated derivate to avoid mononuclear phagocyte system uptake. The morphology, size distribution, and surface charge of the nanoparticles were investigated as a function of the amount of polymer employed for the preparation. Moderately polydispersed nanoparticles (polydispersity index less than 0.2) were obtained. Their size increased with polymer concentration. The zeta potential values were negative whatever the formulations. The availability of polyethylene glycol chains on the nanoparticles' surface was confirmed by measuring the decrease in bovine serum albumin adsorption. For in vivo distribution studies, pegylated and nonpegylated nanoparticles were prepared with polymer mixtures containing PBLG-fluorescein isothiocyanate and imaged by fluorescence microscopy to measure their accumulation in liver and spleen tissues of rats after intravenous administration. Injection of stealth formulations resulted in negligible fluorescence in liver and spleen compared with nonpegylated formulations, which suggests that these nanoparticles are promising candidates as a stealth-type long-circulating drug carrier system and could be useful for active targeting of drugs while reducing systemic side effects.

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“…PEG chains scattered on the surface of nanoparticles were reported to dramatically reduce the uptake of nanoparticles via i.v. injection into the RES cells and subsequently reduced the drug accumulation in liver and spleen (Beletsi et al, 2005). Previously, we have reported that Am80-NLC had a much lower drug concentration in liver than Am80 solution (Liu et al, 2013).…”

Section: Biodistribution Studymentioning

confidence: 90%

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

et al. 2014

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The School of Pharmaceutical Science, Shandong University, Ji'nan, Shandong Province, PR China Abstract Tamibarotene (Am80), a poorly water-soluble drug for the treatment of acute promyelocytic leukemia (APL), loaded nanostructured lipid carrier (Am80-NLC) was developed and characterized previously. The purpose of the present work was to develop PEGylated nanostructured lipid carrier (PEG-NLC) for intravenous delivery of Am80, with the aim to further extend the circulation in blood and decrease the adverse events. Am80-loaded PEG-NLC (Am80-PEG-NLC) modified with PEG-40 stearate (PEG40-SA, molecular weight 2000 Da) was formulated by the method of melt-emulsification and low temperature-solidification technique. Am80-NLC was developed as well as control. Based on the optimized results of single-factor screening experiment, the average drug entrapment efficiency, the mean particle size, and zeta potential of Am80-NLC and Am80-PEG-NLC were found to be 89.8-94.3%, 178.9-201.6 nm, and À37.74 to À20.1 mV, respectively. In vitro drug release of Am80-NLC and Am80-PEG-NLC possessed a sustained release characteristic and their release behavior was in accordance with the Ritger-Peppas equation. In vivo, after intravenous (i.v.) injection to rats, the mean residence time (MRT) of Am80-PEG-NLC group was significantly prolonged and the AUC value was improved as well compared with the Am80-NLC group. Furthermore, the biodistribution in mice showed that Am80-PEG-NLC preferentially decreased the accumulation of Am80 in kidney and increased the drug concentration in brain after i.v. injection. In conclusion, Am80-PEG-NLC may be a potential delivery system for Am80 in the treatment of APL.

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Biodistribution properties of nanoparticles based on mixtures of PLGA with PLGA–PEG diblock copolymers

Cited by 117 publications

References 19 publications

Preparation and in vivo evaluation of insulin-loaded biodegradable nanoparticles prepared from diblock copolymers of PLGA and PEG

Preparation and in vivo evaluation of insulin-loaded biodegradable nanoparticles prepared from diblock copolymers of PLGA and PEG

Pegylation of poly(γ-benzyl-L-glutamate) nanoparticles is efficient for avoiding mononuclear phagocyte system capture in rats

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

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Biodistribution properties of nanoparticles based on mixtures of PLGA with PLGA–PEG diblock copolymers

Cited by 117 publications

References 19 publications

Preparation and in vivo evaluation of insulin-loaded biodegradable nanoparticles prepared from diblock copolymers of PLGA and PEG

Preparation and in vivo evaluation of insulin-loaded biodegradable nanoparticles prepared from diblock copolymers of PLGA and PEG

Pegylation of poly(&gamma;-benzyl-L-glutamate) nanoparticles is efficient for avoiding mononuclear phagocyte system capture in rats

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

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Pegylation of poly(γ-benzyl-L-glutamate) nanoparticles is efficient for avoiding mononuclear phagocyte system capture in rats