Preparation, characterization, and drug release behaviors of drug nimodipine‐loaded poly(ε‐caprolactone)‐poly(ethylene oxide)‐poly(ε‐caprolactone) amphiphilic triblock copolymer micelles

Ge, Haixiong; Hu, Yong; Jiang, Xiqun; Cheng, Daming; Yuan, Yuyan; Hong, Bo; Yang, Changzheng

doi:10.1002/jps.10143

Cited by 195 publications

(96 citation statements)

References 29 publications

(36 reference statements)

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“…Size of particles decreased with decreasing the CL/PEG molar ratio of copolymer. A similar observation has been reported previously, where particle size of polymeric nanoparticles obtained through nanoprecipitation method was decreased by decreasing the molecular weight or concentration of copolymers in acetone and also by increasing the surfactant concentration (Molpeceres et al, 1996;Ge et al, 2000;Ge et al, 2002). In nanoprecipitation method, formation of smaller nanodroplets during emulsification leads to increased specific surface area.…”

Section: Discussionsupporting

confidence: 86%

“…As can be shown in Figure 5, amount of drug released from all formulations were in the range of 49-82% after 30 hours. Thus drug release rate could not be mainly controlled by polymer degradation because PCL degrades very slowly in the solution medium (Ryu et al, 2001;Ge et al, 2002). Therefore drug diffusion from polymeric nanospheres might be the main mechanism of release.…”

Section: Discussionmentioning

confidence: 99%

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Synthesis, Characterization and in vitro Anti-Tumoral Evaluation of Erlotinib-PCEC Nanoparticles

Barghi¹,

Asgari²,

Barar³

et al. 2015

Asian Pacific Journal of Cancer Prevention

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Background: Development of a nanosized polymeric delivery system for erlotinib was the main objective of this research. Materials and Methods: Poly caprolactone-polyethylene glycol-polycaprolactone (PCEC) copolymers with different compositions were synthesized via ring opening polymerization. Formation of triblock copolymers was confirmed by HNMR as well as FT-IR. Erlotinib loaded nanoparticles were prepared by means of synthesized copolymers with solvent displacement method. Results: Physicochemical properties of obtained polymeric nanoparticles were dependent on composition of used copolymers. Size of particles was decreased with decreasing the PCL/PEG molar ratio in used copolymers. Encapsulation efficiency of prepared formulations was declined by decreasing their particle size. Drug release behavior from the prepared nanoparticles exhibited a sustained pattern without a burst release. From the release profiles, it can be found that erlotinib release rate from polymeric nanoparticles is decreased by increase of CL/PEG molar ratio of prepared block copolymers. Based on MTT assay results, cell growth inhibition of erlotinib has a dose and time dependent pattern. After 72 hours of exposure, the 50% inhibitory concentration (IC50) of erlotinib hydrochloride was appeared to be 14.8 μM. Conclusions: From the obtained results, it can be concluded that the prepared PCEC nanoparticles in this study might have the potential to be considered as delivery system for erlotinib.

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Section: Discussionsupporting

confidence: 86%

Section: Discussionmentioning

confidence: 99%

Synthesis, Characterization and in vitro Anti-Tumoral Evaluation of Erlotinib-PCEC Nanoparticles

Barghi¹,

Asgari²,

Barar³

et al. 2015

Asian Pacific Journal of Cancer Prevention

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“…Burst release phenomenon according to the literature does not have a clear mechanism however can be controlled by the manufacturing procedure [37]. The initial fast release from the nanoparticles could be attributed to the rapid dissolution of drug located on/close to nanoparticles' surface [38,39]. The higher dissolution rate of encapsulated IXA compared to free (crystalline) IXA can be attributed to the mainly amorphous state of IXA entrapped into the polymeric matrix, as indicated by XRD studies (See Fig.…”

Section: In Vitro Drug Releasementioning

confidence: 98%

Synthesis of folate- pegylated polyester nanoparticles encapsulating ixabepilone for targeting folate receptor overexpressing breast cancer cells

Sıafaka

Betsiou

Tsolou

et al. 2015

J Mater Sci: Mater Med

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The aim of this study was the preparation of novel polyester nanoparticles based on folic acid (FA)-functionalized poly(ethylene glycol)-poly(propylene succinate) (PEG-PPSu) copolymer and loaded with the new anticancer drug ixabepilone (IXA). These nanoparticles may serve as a more selective (targeted) treatment of breast cancer tumors overexpressing the folate receptor. The synthesized materials were characterized by 1 H-NMR, FTIR, XRD and DSC. The nanoparticles were prepared by a double emulsification and solvent evaporation method and characterized with regard to their morphology by scanning electron microscopy, drug loading with HPLC-UV and size by dynamic light scattering. An average size of 195 nm and satisfactory drug loading efficiency (3.5 %) were observed. XRD data indicated that IXA was incorporated into nanoparticles in amorphous form. The nanoparticles exhibited sustained drug release properties in vitro. Based on in vitro cytotoxicity studies, the blank FA-PEG-PPSu nanoparticles were found to be non-toxic to the cells. Fluorescent nanoparticles were prepared by conjugating Rhodanine B to PEG-PPSu, and live cell, fluorescence, confocal microscopy was applied in order to demonstrate the ability of FA-PEG-PPSu nanoparticles to enter into human breast cancer cells expressing the folate receptor. Graphical Abstract 1 Introduction

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“…For these reasons, the use of a carrier that would improve the solubility of NM in body fluids and enhance drug delivery, seems much promising. In the recent decades, nanospheres [8-12, 15, 16, 18] or microspheres [11,13,14,17] were widely used as drug carriers. A few reports have been published on the use of liquid and solid microemulsions [19,20], solid dispersions [21][22][23] or drug-loaded type systems based on cyclodextrins [24][25][26] and lipid [27][28][29] or phospholipid micelles [30,31].…”

Section: Introductionmentioning

confidence: 99%

Mesoporous drug carrier systems for enhanced delivery rate of poorly water-soluble drug: nimodipine

et al. 2015

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Two mesoporous silica materials: MCM-41 and SBA-15 were applied as potential nanocarriers for poorly soluble drug-nimodipine. Drug incorporation was performed using modified adsorption from the solution method and loaded samples before and after washing procedure were studied. The physical properties were verified by: differential scanning calorimetry, X-ray powder diffraction, electron microscopies (SEM/TEM) and Fourier-transform infrared spectroscopy (FT-IR). FT-IR results for bulk nimodipine were interpreted on the basis of first principles calculations (DFT). As a result of encapsulation process, in both matrices nimodipine appeared simultaneously in two forms: crystalline and amorphous, but the first one turned out to be easily removable during washing procedure. The in vitro dissolution and release tests were performed with ultra pure water under supersaturating conditions. The release rate of the amorphous nimodipine from mesoporous silica materials was at least 70 times higher than dissolution rate of bulk drug, thus revealed a potential usefulness of such carrier in future pharmaceutical applications in terms of delivery of poorly soluble drugs.

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Preparation, characterization, and drug release behaviors of drug nimodipine‐loaded poly(ε‐caprolactone)‐poly(ethylene oxide)‐poly(ε‐caprolactone) amphiphilic triblock copolymer micelles

Cited by 195 publications

References 29 publications

Synthesis, Characterization and in vitro Anti-Tumoral Evaluation of Erlotinib-PCEC Nanoparticles

Synthesis, Characterization and in vitro Anti-Tumoral Evaluation of Erlotinib-PCEC Nanoparticles

Synthesis of folate- pegylated polyester nanoparticles encapsulating ixabepilone for targeting folate receptor overexpressing breast cancer cells

Mesoporous drug carrier systems for enhanced delivery rate of poorly water-soluble drug: nimodipine

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