• Bulletin of the Korean Chemical Society
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• v.33 no.10
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• pp.3225-3232
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• 2012

The purposes of this research were to synthesize amoxicillin-carrying magnetic nanoparticles. Magnetic nanoparticles were prepared by a chemical precipitation of ferric and ferrous chloride salts in the presence of a strong basic solution. PLGA and PLGA-PEG copolymers were prepared by ring opening polymerization of lactide (LA) and glycolide (GA) (mole ratio of LA: GA 3:1) with or without polyethylene glycol (PEG). Amoxicillin loaded magnetic PLGA and PLGA-PEG nanoparticles were prepared by an emulsion-evaporation process (o/w). Transmission electron microscopy (TEM) and scanning electron microscopy (SEM) photomicrographs showed that the magnetic nanoparticles have the mean diameter within the range of 65-260 nm also they were almost spherical in shape. Magnetic nanoparticles prepared with PLGA showed more efficient entrapment (90%) as compared with PLGA-PEG (48-52%) nanoparticles. In-vitro release of amoxicillin from magnetic PLGA nanoparticles showed that 78% of drug was released over 24 hours. The amount of amoxicillin released from PLGA-PEG s was higher than PLGA.

• Polymer(Korea)
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• v.32 no.2
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• pp.143-149
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• 2008

We synthesized PEG-PLA (or PLGA) amphiphilic di-block copolymers, which consist of PEG as biocompatible and hydrophilic block and PLA (or PLGA) as biodegradable and hydrophobic block, by ring opening polymerization of LA in the presence of methoxy PEG as a macroinitiator. The compositions and the molecular weights of the copolymers were controlled by changing the feed ratio of LA (and GA) to PEG initiator. The di-block copolymers could self-assemble in aqueous media to form micellar structure. A hydrophobic model drug, pioglitazone, was loaded into the polymer micelle using solid dispersion and dialysis methods, and the drug-loaded micelles were characterized by AFM, DLS and HPLC measurements. The drug loading capacity and in vitro release studies were performed and evaluated under various conditions. These results indicated that the amphiphilic di-block copolymers of PEG-PLA (or PLGA) could solubilize pioglitazone by solid dispersion method and the drug release was modulated according to micellar chemical compositions.

• Asian Pacific Journal of Cancer Prevention
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• v.16 no.18
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• pp.8259-8263
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• 2016

Background: Nano-therapy has the potential to revolutionize cancer therapy. Chrysin, a natural flavonoid, was recently recognized as having important biological roles in chemical defenses and nitrogen fixation, with anti-inflammatory and anti-oxidant effects but the poor water solubility of flavonoids limitstheir bioavailability and biomedical applications. Objective: Chrysin loaded PLGA-PEG-PLGA was assessed for improvement of solubility, drug tolerance and adverse effects and accumulation in a gastric cancer cell line (AGS). Materials and Methods: Chrysin loaded PLGA-PEG copolymers were prepared using the double emulsion method (W/O/W). The morphology and size distributions of the prepared PLGA-PEG nanospheres were investigated by 1H NMR, FT-IR and SEM. The in vitro cytotoxicity of pure and nano-chrysin was tested by MTT assay and miR-34a was measured by real-time PCR. Results: 1H NMR, FT-IR and SEM confirmed the PLGA-PEG structure and chrysin loaded on nanoparticles. The MTT results for different concentrations of chrysin at different times for the treatment of AGS cell line showed IC50 values of 68.2, 56.2 and $42.3{\mu}M$ and 58.2, 44.2, $36.8{\mu}M$ after 24, 48, and 72 hours of treatment, respectively for chrysin itslef and chrysin-loaded nanoparticles. The results of real time PCR showed that expression of miR-34a was upregulated to a greater extent via nano chrysin rather than free chrysin. Conclusions: Our study demonstrates chrysin loaded PLGA-PEG promises a natural and efficient system for anticancer drug delivery to fight gastric cancer.

• Polymer(Korea)
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• v.34 no.3
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• pp.253-260
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• 2010

In this study, we prepared and evaluated a series of biocompatible and biodegradable block copolymer hydrogels with a delayed swelling property for tissue expander application. The hydrogels were synthesized via a radical crosslinking reaction of poly(ethylene glycol) (PEG) diacrylate and poly(D,L-lactide-co-glycolide)-poly(ethylene glycol)-poly(D,L-lactide-co-glycolide)(PLGA-PEG-PLGA) triblock copolymer diacrylate as a swelling/degradation controller (SDC). For the synthesis of various SDCs that can lead to different degradation and swelling properties, various PLGA-PEG-PLGA triblock copolymers with different LA/GA ratios and different PLGA block lengths were synthesized and modified to have terminal acrylate groups. The resultant hydrogels were flexible and elastic even in the dry state. The in vitro degradation tests showed that the delayed swelling properties of the hydrogels could be modulated by varying the chemical composition of the biodegradable crosslinker (SDC) and the block ratio of SDC/PEG. The histopathologic observation after implantation of hydrogels in mice was performed and evaluated by macrography and microscopy. Any significant inflammation or necrosis was not observed in the implanted tissues. Due to their biocompatibility, elasticity, sufficient swelling pressure, delayed swelling and controllable degradability, the hydrogels could be useful for tissue expansion and other biomedical applications.

• Biomolecules & Therapeutics
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• v.16 no.4
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• pp.425-430
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• 2008

The objectives of this study were to prepare PLGA film onto the surface of the capsular tension ring (CTR) for controlled drug release and investigate the influence of plasticizers, the test drug and measurement conditions on flexibility of the film. Film solutions were prepared by dissolving PLGA, plasticizer (triethyl citrate, TEC or polyethylene glycol, PEG), test drug (dexamethasone) in ethyl acetate then films were prepared by spray coating and evaporation method. Then, the flexibility of PLGA film was determined by elongation test. The addition of plasticizer, PEG or TEC to PLGA copolymer caused a depression of glass transition temperature ($T_g$) and the elasticity of PLGA films increased. The addition of dexamethasone to the PLGA/TEC matrix decreased the flexibility of film. Dimensional factors of the PLGA films such as width and thickness were significantly influenced on flexibility of films and film length and elongation speed had no considerable influence on elongation of films. In this study, sufficiently flexible and stable PLGA films capable of being coated onto CTR could be prepared. This PLGA films can be used as a platform for local drug delivery.

• Asian Pacific Journal of Cancer Prevention
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• v.17 no.5
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• pp.2453-2457
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• 2016

Background: Dysregulation of HSP90 gene expression is known to take place in breast cancer. Here we used D,L-lactic-co-glycolic acid-polyethylene glycol-17-dimethylaminoethylamino-17-demethoxy geldanamycin (PLGA-PEG-17DMAG) complexes and free 17-DMAG to inhibit the expression of HSP90 gene in the T47D breast cancer cell line. The purpose was to determine whether nanoencapsulating 17DMAG improves the anti-cancer effects as compared to free 17DMAG. Materials and Methods: The T47D breast cancer cell line was grown in RPMI 1640 supplemented with 10% FBS. Encapsulation of 17DMAG was conducted through a double emulsion method and properties of copolymers were characterized by Fourier transform infrared spectroscopy and H nuclear magnetic resonance spectroscopy. Assessment of drug cytotoxicity was by MTT assay. After treatment of T47D cells with a given amount of drug, RNA was extracted and cDNA was synthesized. In order to assess HSP90 gene expression, real-time PCR was performed. Results: Taking into account drug load, IC50 was significant decreased in nanocapsulated 17DMAG in comparison with free 17DMAG. This finding was associated with decrease of HSP90 gene expression. Conclusions: PLGA-PEG-17DMAG complexes can be more effective than free 17DMAG in down-regulating of HSP90 expression, at the saesm time exerting more potent cytotoxic effects. Therefore, PLGA-PEG could be a superior carrier for this type of hydrophobic agent.

• Asian Pacific Journal of Cancer Prevention
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• v.16 no.9
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• pp.3753-3758
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• 2015

Background: Polymeric nanoparticles are attractive materials that have been widely used in medicine for drug delivery, with therapeutic applications. In our study, polymeric nanoparticles and the anticancer drug, chrysin, were encapsulated into poly (D, L-lactic-co-glycolic acid) poly (ethylene glycol) (PLGA-PEG) nanoparticles for local treatment. Materials and Methods: PLGA: PEG triblock copolymers were synthesized by ring-opening polymerization of D, L-lactide and glycolide as an initiator. The bulk properties of these copolymers were characterized using 1H nuclear magnetic resonance spectroscopy and Fourier transform infrared spectroscopy. In addition, the resulting particles were characterized by scanning electron microscopy. Results: The chrysin encapsulation efficiency achieved for polymeric nanoparticles was 70% control of release kinetics. The cytotoxicity of different concentration of pure chrysin and chrysin loaded in PLGA-PEG ($5-640{\mu}M$) on T47-D breast cancer cell line was analyzed by MTT-assay. Conclusions: There is potential for use of these nanoparticles for biomedical applications. Future work should include in vivo investigation of the targeting capability and effectiveness of these nanoparticles in the treatment of breast cancer.

• KSBB Journal
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• v.17 no.1
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• pp.33-37
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• 2002

To improve in vitro release kinetic of G-CSF in PLGA microsphere, G-CSF was PEGylated with methoxy polyethylene glycol-aldehyde (mPEG-aldehyde, MW 5000). The majority of G-CSF was mono-PEGylated and it was characterized using SDS-PAGE, HPLC, and peptide mapping. The PLGA microencapsulation with the native, or PEGylated G-CSF was performed using W/O/w method, where the encapsulation efficiency was high. For the high loading of G-CSF to microsphere, G-CSF and PEGylated G-CSF were concentrated and then verified the protein stability using native gel and gel filtration chromatography. In comparison with native G-CSF, PEGylated G-CSF was released during the extended period and its maximum amount of released G-CSF was also increased.

• Polymer(Korea)
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• v.34 no.3
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• pp.274-281
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• 2010

In this study, PEG-PLA(or PLGA) amphiphilic di-block copolymers were synthesized by ring opening polymerization of D,L-lactide(or glycolide) and applied to polymeric micelle system for solubilization of a rosiglitazone as diabetes drug. The drug could be efficiently loaded into the polymer micelle by solid dispersion technique, and the drug-loaded micelles were characterized and evaluated as a drug delivery carrier by fluorescence spectrometer, DSC, and DLS measurements. The colloidal stability of drug loaded micelles in aqueous media could be enhanced by addition of 2-hydroxy-N-picolylnitinamide as a hydrotropic agent. The polymer micelles also showed biocompatible and nontoxic properties in vitro cell viability using MTT assay, and the drug loaded micelles were observed to be more effective than free drug for decreasing glucose in blood of rats.

• Asian Pacific Journal of Cancer Prevention
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• v.15 no.20
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• pp.8693-8698
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• 2014

Background: Up-regulation of hsp90 gene expression occurs in numerous cancers such as lung cancer. D,L-lactic-co-glycolic acid-poly ethylene glycol-17-dimethylaminoethylamino-17-demethoxy geldanamycin (PLGA-PEG-17DMAG) complexes and free 17-DMAG may inhibit the expression. The purpose of this study was to examine whether nanocapsulating 17DMAG improves the anti cancer effect over free 17DMAG in the A549 lung cancer cell line. Materials and Methods: Cells were grown in RPMI 1640 supplemented with 10% FBS. Capsulation of 17DMAG is conducted through double emulsion, then the amount of loaded drug was calculated. Other properties of this copolymer were characterized by Fourier transform infrared spectroscopy and H nuclear magnetic resonance spectroscopy. Assessment of drug cytotoxicity on the grown of lung cancer cell line was carried out through MTT assay. After treatment, RNA was extracted and cDNA was synthesized. In order to assess the amount of hsp90 gene expression, real-time PCR was performed. Results: In regard to the amount of the drug load, IC50 was significant decreased in nanocapsulated(NC) 17DMAG in comparison with free 17DMAG. This was confirmed through decrease of HSP90 gene expression by real-time PCR. Conclusions: The results demonstrated that PLGA-PEG-17DMAG complexes can be more effective than free 17DMAG in down-regulating of hsp90 expression by enhancing uptake by cells. Therefore, PLGA-PEG could be a superior carrier for this kind of hydrophobic agent.