• Archives of Pharmacal Research
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• v.21 no.4
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• pp.418-422
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• 1998

Aim of this work is to prepare poly(DL-lactide-co-glycolide) (PLGA) nanoparticles by dialysis method without surfactant and to investigate drug loading capacity and drug release. The size of PLGA nanoparticles was 269.9 $\pm$118.7 nm in intensity average and the morphology of PLGA nanoparticies was spherical shape from the observation of SEM and TEM. In the effect of drug loading contents on the particle size distribution, PLGA nanoparticles were monomodal pattern with narrow size distribution in the empty and lower drug loading nanoparticles whereas bi- or trimodal pattern was showed in the higher drug loading ones. Release of clonazepam from PLGA nanoparticles with higher drug loading contents was slower than that with lower loading contents.

• Clean Technology
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• v.12 no.2
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• pp.53-61
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• 2006

A PGSS (Particles from Gas Saturated Solutions) process designed to generate nano-particles using supercritical fluids has been conducted for the fabrication of Poly(lactide-co-glycolide) (PLGA) microparticles that encapsulate a protein drug. It is demonstrated that the polymer and the dry powder of a protein can be mixed under supercritical carbon dioxide conditions and that the protein component retains its biological activity. In this experiment, the mixture of polymer which is plasticized and dry powder protein was sprayed to form solid polymer that encapsulate the protein. It is found that supercritical fluid process give fine tuning of particle size and particle size distribution by simple manipulations of the process parameters. Porous particles were formed with irregular shape. Protein encapsulated in the polymer was found to have enzymatic activity without significant loss of its initial value.

• Polymer(Korea)
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• v.24 no.4
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• pp.505-512
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• 2000

The mixture density data for poly(lactide-co-glycolide) [PLGA] with supercritical $CO_2$, CHF$_3$ and CHClF$_2$ were obtained in the temperature range of 27 to 10$0^{\circ}C$ and at pressures as high as 3000 bar (PLGA$_{x}$, Where the molar concentration of glycolide in the backbone, x, range from 0 to 50 mol%). The PLA-$CO_2$, PLA-CHF$_3$, and PLA-CHClF$_2$ systems dissolve in the pressure less than 1430 below 700, and below 100 bar, respectively. The mixture density shows from 1.084 to 1.334 g/cm$^3$ at temperatures from 27 to 93$^{\circ}C$. The PLGA$_{15}$ -$CO_2$ mixture dissolves at pressures of below 1900 bar and the mixture density is in the range of 1.158 to 1.247 g/cm$^3$ at temperatures between 37 and 92$^{\circ}C$. The solubilities of the PLGA$_{25}$ for $CO_2$, CHF$_3$, and CHClF$_2$ are shown to pressure as high as 2390, 1470, and 118 bar, respectively, and the mixture density exhibits iron 1.154 to 1.535 g/cm$^3$ at temperatures from 29 to 81$^{\circ}C$. The PLGA$_{50}$-$CO_2$ system does not dissolve at 24$0^{\circ}C$ and 3000 bar while the PLGA$_{50}$-CHCIF$_2$ does easily at 5$0^{\circ}C$ and 100 bar. The mixture density for the PLGA-CHClF$_2$ system increases even at low pressures as the glycolide molar concentration increases.es.es.

• Polymer(Korea)
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• v.25 no.6
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• pp.884-892
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• 2001

Biodegradable wafers were prepared with poly (L-lactide-co-glycolide) (50 : 50 mole ratio of lactide to glycolide, molecular weight:5000 g/mole) by direct compression method for the sustained release of nifedipine to investigate the possibility of the treatment of hypertension. PLGA wafers were prepared by altering initial drug/polymer loading ratio, wafer thickness, and hydroxypropyl methylcellulose (HPMC) content. These wafers showed new zero-order release patterns for 11 days, and various biphasic release patterns could be obtained by altering the composition of wafers such as addition of matrix binder as HPMC to the PLGA wafer to reduce release rate of initial phase. The onset of polymer mass loss only occured after 4 days and about 40% of mass loss was observed after 11 days nifedipine release. This system had advantages in terms of simplicity in design and obviousness of drug release rate and may be useful as an implantable dosage form.

• 한국당과학회:학술대회논문집
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• 2006.11a
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• pp.57-57
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• 2006

• YAKHAK HOEJI
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• v.44 no.4
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• pp.293-299
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• 2000

Biodegradable microspheres made from poly-lactide-co-glycolide polymers have been considered as a new delivery system for single-dose vaccine. Purified tetanus toxoid (TT) was encapsulated in poly-lactide(PLA) and poly-lactide-co-glycolide (PLGA) microparticles using a solvent evaporation method in a multiple emulsion system (water-in oil-in water). The morphology of 77-loaded microparticles was spherical and the suface of them was smooth. The particle size was in a range of 2-10. Protein loading efficiency was 68-97.8%. PLGA (85:15) microparticle showed the highest efficiency. Protein release pattern was influenced by polymer molecular weight and composition. The release rate of PLA(Mw 100,000) microsphere was higher than any other microspheres. In consequence of the hydrolysis of PLGA(50:50) microspheres, environmental pH decreased from 7.4 to 5.0. The PLA, PLGA (75:25) and PLGA (85:15) microshperes showed no significant pH change. The antigenicity or n in microshperes was assayed by indirect sandwich ELISA using equine polyclonal tetanus antitoxin for capture antibody and human polyclonal tetanus antitoxin for primary antibody. The antigenicity of TT in PLA (Mw 100,000), PLGA(50:50, Mw 100,000) and PLGA (75:25, Mw 73,300) after 30 days incubation showed 54, 40.9 and 76.7%, respectively.

• Archives of Pharmacal Research
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• v.23 no.4
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• pp.385-390
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• 2000

To demonstrate the effect of formulation conditions on the controlled release of protein from poly(lactide-co-glycolide) (PLGA) microspheres for use as a parenteral drug carrier, ovalbumin (OVA) microspheres were prepared using the W/O/W multiple emulsion solvent evaporation and extraction method. Methylene chloride or ethyl acetate was applied as an organic phase and poly(vinyl alcohol) as a secondary emulsion stabilizer. Low loading efficiencies of less than 20％ were observed and the in vitro release of OVA showed a burst effect in all batches of different microspheres, followed by a gradual release over the next 6 weeks. Formulation processes affected the size and morphology, drug content, and the controlled release of OVA from PLGA microspheres.

• Archives of Pharmacal Research
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• v.16 no.4
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• pp.312-317
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• 1993

To confirm a new evaluation tedhnique for biodegradability of biopolymer microsphers in vivo condition, magnetic microsphere sytem was adopted for tracing the microspheres injected and lodged in micr. Microsphers of poly(DL-lactic acid), poly(L-alctic acid) and poly(DL-lactide-coglycolide)(PLGA) were prepared by solvent-extraction method and their organ distribution and biodegradation in mice was examined. Magnetic microspheres lodged in mice organs were recollected from the homogenates of mice organs with a constant flow magnetic separation apparatus. Recollected microspheres were observed by scanning electron microscopy and also were assayed for their magnetite ocntent by atomic absorption spectrophotometry to evaluate the biodegradability of polymeric microspheres. This method seems to be practical and simple to estimate the biodegradability of biopolymers over the conventional methods.

• Polymer(Korea)
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• v.28 no.4
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• pp.328-334
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• 2004

A series of methoxy poly(ethylene glycol) (MPEG)-poly(L-lactide-co-glycolide) (PLGA) diblock copolymers were synthesized by ring-opening polymerization of L-lactide and glycolide with carbitol (134 g/mole) or different molecular weights of MPEG (550, 2000, and 5000 g/mole) as an initiator in presence of Sn(Oct)$_2$. The properties of diblock copolymers were characterized by using $^1$H-NMR, GPC, and XRD. After uniform mixing of block copolymers and 1% albumin bovine-fluorescein isothiocyanate(FITC-BSA) with a freeze miller, the wafers loaded FITC-BSA were fabricated by using a mold with a dimensions of 3 mm${\times}$1mm diameter. The release profiles of FITC-BSA and the pH changes of wafer were examined using pH 7.4 PBS for 30 days at 37$^{\circ}C$. The release profiles of albumin showed fast initial burst as the molecular weights of MPEG increased. As a result of this study, the release behavior of BSA was controlled with introducing MPEG in the block copolymers.

• Journal of Biomedical Engineering Research
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• v.13 no.2
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• pp.147-154
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• 1992

Poly (glycolic aclu-co-glycine-L-lactic aclu) has been prepared by rlng opening polymerlzation. The monomer 6-methyl morpholine-2, 5-dlone was synthe-slzed by bromoproplonylation of 2 bromopropionyl bromide with glycine. Glycolide and 6-methyl morpholine-2, 5-dione have been used as starling materials for polydepsipeptides. The synthesized copolymers have been Identlrled by NMR and FT-lR spectrophotometer. The Tg value of poly(glycollc aclu-co glycine-L-tactic acld ) Is In creased with increasing mole fraction of 6-methylmorpholine-2, 5-dlone(60-$84^{\circ}C$). The glass trasltion temperature of poly(glycolic acid-co-glycine-L-lactic-acid) (62-$86^{\circ}C$) is lower than that of poly (L-lactic acrid-co-glycine-L-lactic acid ). The thermal degradation of poly( L-lactic acid-co- glycine-L-lactic acid ) Is decreased with increasing mole fraction of L-lactide. The thermal degrada pion of poly(glycolic acrid-co-91ycine-L-lactic aclu ) is increased with increasing mole Fraction of glycolide.