• Journal of Pharmaceutical Investigation
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• v.34 no.2
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• pp.101-106
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• 2004

This work aims at examining the cellular uptake behavior of poly(D,L-lactide-co-glycolide) (PLGA) nanoparticles derivatized with a protein transduction domain (PTD) using HeLa cells. For this purpose, $Tat_{49-57}$ peptide derived from transcriptional activation (Tat) protein of HIV type-1 was covalently conjugated to the terminal end of PLGA. Nanoparticles were ten prepared with the $Tat_{49-57}-PLGA$ conjugates by a spontaneous phase inversion method. The prepared particles had a mean diameter of ca. 84 nm, as measured by dynamic light scattering. The interaction of the Tat-PLGA nanoparticles with cells was examined by using confocal laser scanning microscopy. It was found tat Tat-PLGA nanoparticles incubated with HeLa cells could efficiently translocate into cytoplasm, while plain PLGA nanoparticles showed negligible cellular uptake. In addition, even at $4^{\circ}C$ or in the presence of sodium azide significant cellular internalization of Tat-PLGA nanoparticles was still observed. These results indicate that a non-endocytotic translocation mechanism might be involved in the cellular uptake of Tat-PLGA nanoparticles.

• Polymer(Korea)
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• v.36 no.6
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• pp.789-794
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• 2012

Poly(lactic-co-glycolic acid) (PLGA) has been most widely used due to its advantages such as good biodegradability, controllable rate of degradation and metabolizable degradation products. We manufactured composite scaffolds of PLGA scaffold penetrated DBP gel (PLGA/DBP gel) by a simple method, solvent casting/salt leaching prep of PLGA scaffolds and subsequent soaking in DBP gel. Chondrocytes were seeded on the PLGA/DBP gel. The mechanical strength of scaffold, histology (H&E, Safranin-O, Alcian-blue) and immunohistochemistry (collagen type I, collagen type II) were performed to elucidate in vitro and in vivo cartilage-specific extracellular matrices. It was better to keep the characteristic of chondrocytes in the PLGA/DBP gel scaffolds than that PLGA scaffolds. This study suggests that PLGA/DBP gel scaffold may serve as a potential cell delivery vehicle and a structural basis for in vivo tissue engineered cartilage.

• Polymer(Korea)
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• v.33 no.1
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• pp.7-12
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• 2009

PLGA microspheres have been known as an injectable system for tissue engineering. The purpose of this study was to investigate the condition of emulsion formation and cell adhesion on the microsphere surface. BSA-loaded PLGA microsphere was fabricated by oil-in-water (O/W) and water-in-oil-in-water (W/O/W) solvent evaporation method. Sodium alginate was dissolved in water phase to control initial burst release and to improve lag time by PLGA bulk degradation. In addition, the morphology of cells attached on the micro spheres was studied using a scanning electron microscopy (SEM). Cellular proliferation behavior of human disc cells cultivated on PLGA micro spheres was analyzed using a MTT assay. MTT assay revealed that the cells can attach and proliferate on PLGA microspheres. According to these results, we concluded that BSA -loaded alginate/PLGA microspheres can be used as an injectable system for tissue engineering application.

• Polymer(Korea)
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• v.34 no.4
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• pp.333-340
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• 2010

Zaltoprofen, a propionic acid derivative non-steroidal anti-inflammatory drug (NSAID), is known to have powerful inhibitory effects on acute, subacute and chronic inflammation. We developed poly(lactide-co-glycolide)(PLGA) microspheres loaded with zaltoprofen for sustained controlled delivery using an oil-water solvent evaporation methods by varying PLGA molecular weight and cosurfactant contents. Physicochemical properties and morphology of zaltoprofen-loaded PLGA microspheres were investigated by scanning electron microscope, X-ray diffraction and differential scanning calorimeter. The size of microspheres increased with the molecular weight of PLGA and the content of cosurfactants. The increase of PLGA molecular weight and cosurfactant content decreased the porosity of microspheres, subsequently resulting in the slow drug release. The results demonstrated that the adjustment of PLGA molecular weight and the cosurfactant content allowed us to control the drug release profiles of drug-loaded microspheres.

• Archives of Pharmacal Research
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• v.12 no.2
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• pp.88-93
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• 1989

In order to obtain some informations about the effect of molecular weight on the release rate of drug from drug carrier, two types of poly-L-glutamic acid (PLGA)-cytarabine (ara-C) conjugates, PLGA-ara-C:I and PLGA-ara-C:II, were synthesized using two types of PLGA having different average molecular weight, 43,000 and 77,800, respectively. The PLGA-ara-C conjugates were synthesized by mixed anhydride method and found to be covalently linked. Both types of conjugates charged negatively at biological pH. The pH-dependent release rate of ara-C was observed in both cases, and the release rate was accelerated in basic, acidic conditions (the k values were 0.015 $day^{-1}$ at pH 7.0, 0.024 $day^{-1}$ at pH 5.0, and 0.059 $day^{-1}$ at pH 9.0 in the case of PLGA-ara-C:I) and in the presence of pretense. The time required for the release of 16.5% of ara-C from PLGA-ara-C:I were 8 hr and 144 hr in the presence and absence of protease, respectively. Although both types of conjugates showed similar drug substitution ratio, they showed different release rates. Between the two types of conjugates, PLGA-ara-C:II showed the faster release rate (0.030 vs 0.042 $day^{-1}$ in pH 7.4 phosphate buffer solution at $37^{\circ}C$) and the smaller activation energy for the release of drug (12.5 vs 7.7 Kcal/mol) than PLGA-ara-C:I. The characteristic effect of molecular weight on the release rates of PLGA-ara-C conjugates suggests that the drug release rate might be effectively controlled over a prolonged period of time by the combined use of the different types of PLGA-ara-C conjugates having different molecular weights.

• 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.

• Polymer(Korea)
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• v.24 no.5
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• pp.728-735
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• 2000

Fentanyl-loaded biodegradable poly(L-lactide-co-glycolide) (75 : 25 by mole ratio of lactide to glycolide, PLGA) microspheres (MSs) were prepared to study the possibility for long-acting local anesthesia. We developed the fentanyl base (FB, slightly water-soluble)-loaded PLGA MSs by means of conventional O/W solvent evaporation method. The size of MSs was in the range of 10~150 ${\mu}{\textrm}{m}$. The morphology of MSs was characterized by SEM, and the in vitro release amounts of FB were analyzed by HPLC. The lowest porous cross-sectional morphology and the highest encapsulation efficiency were obtained by using gelatin as an emulsifier. The influences of several preparation parameters, such as emulsifier types, molecular weights and concentrations of PLGA, and initial drug loading amount, etc., have been observed in the release patterns of FB. The release of FB in vitro was more prolonged over 25 days, with close to zero-order pattern by controlling the preparation parameters. We also investigated the physicochemical properties of FB-loaded PLGA MSs by X-ray diffraction and differential scanning calorimeter.

• KSBB Journal
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• v.18 no.2
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• pp.107-110
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• 2003

Biodegradable polymers, poly(lactic-co-glycolic acid) (PLGA), poly(3-hydroxybutyrate) (PHB), and medium chain length polyhydroxyalkanoates (MCL-PHA) containing rose bengal (model drug) were coated onto the surface of stainless steel (stent materials) and their in vitro release characteristics were investigated. Drug release increased with; decreasing PLGA concentration, increasing rose bengal concentration, and Increasing dip-coating duration. The order of drug release from the polymer coating was: PHB > PLGA > MCL-PHA. These results suggest that drug release can be controlled by: changing the concentration and type of polymer, the drug concentration, and the dip-coating duration.

• Journal of the Korean Society for Precision Engineering
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• v.33 no.1
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• pp.63-67
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• 2016

We present a method of fabricating poly (lactic-co-glycolic acid) (PLGA) porous microfibers using a pore template. PLGA microfibers were synthesized using a glass capillary tube in a poly-(dimethylsiloxane) (PDMS) microfluidic chip. Gelatin solution was used as a porous template to prepare pores in microfibers. Two phases of PLGA solutions in different solvents-DMSO (dimethyl sulfoxide) and DCM (dichloromethane)-were used to control the porosity and strength of the porous microfibers. The porosity of the PLGA microfibers differed depending on the ratio of flow rates in the two phases. The porous structure was formed in a spiral shape on the microfiber. The porous structure of the microfiber is expected to improve transfer of oxygen and nutrients, which is important for cell viability in tissue engineering.

• Journal of Pharmaceutical Investigation
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• v.40 no.4
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• pp.251-254
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• 2010

The formation of acylated peptide impurities in poly(lactide-co-glycolide) (PLGA) formulations is one of the major challenges to the development of successful sustained-release product. Octreotide, synthetic analogue of somatostatin, has been identified to be acylated in PLGA microsphere formulations. The purpose of this study was to investigate the pH effect on the formation of acylated octreotides by PLGA. In the incubation with PLGA in 0.1 M phosphate buffer at pH 7.4, approximately 98% of octreotide adsorbed to PLGA through 14 days and 66.3% of acylated octreotides were produced after 42 days, whereas the interaction of octreotide with PLGA was significantly inhibited in the incubation at pH 4, in which the acylated octreotides were observed to be 9.2% after 42 days. In the interaction study at pH 4.1-7.4, the production of acylated octreotides was demonstrated to be dependent on environmental pH. Below pH 5.0, the acylation of octreotide was significantly inhibited. This study indicates that the pH is the major factor for the formation of acylated octreotide in PLGA formulations.