• Korean Chemical Engineering Research
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• v.56 no.4
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• pp.461-468
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• 2018

Microspheres were prepared by solvent-evaporation method with Poly-L-lactic acid (PLLA) as a starting material, and the effects of preparation variables on microsphere shape and average particle size were investigated. As the concentration of PVA solution increased from 1 to 5 wt%, the average particle size decreased from $370{\mu}m$ to $160{\mu}m$ and then increased to $240{\mu}m$ at 7 wt%. On the other hand, As the addition volume of PVA solution increased from 10 mL to 50 mL, the average particle size decreased from $370{\mu}m$ to $220{\mu}m$. Also, as the stirring speed increased from 500 rpm to 1,500 rpm, the average particle size decreased from $370{\mu}m$ to $110{\mu}m$. When dichloromethane and chloroform were used as organic solvents, respectively, the average particle size did not show any significant difference. However, when dichloromethane was used, voids were observed on the particle surface, but when chloroform was used, smooth spherical particles were obtained.

• Journal of Pharmaceutical Investigation
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• v.35 no.2
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• pp.95-99
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• 2005

Mucoadhesive microspheres were prepared by interpolymer complexation of chitosan with poly(acrylic acid) (PAA) and solvent evaporation method to increase gastric residence time. The chitosan-PAA complex formation was confirmed by differential scanning calorimetry and swelling study. The DSC thermogram of chitosan-PAA microspheres showed two exothermic peaks for the decomposition of chitosan and PAA. The swelling ratio of the chitosan-PAA microspheres was dependent on the pH of the medium. The swelling ratio was higher at pH 2.0 than at neutral pH. The results indicated that the microspheres were formed by electrostatic interaction between the carboxyl groups of PAA and the amine groups of chitosan. The effect of various process parameters on the formation and morphology of microspheres was investigated. The best microspheres were obtained when 1.5% of the high molecular weight chitosan and 0.3% of PAA were used as an internal phase. The optimum internal phase volume was 7%. The com oil was used as the external phase of emulsion, and span 80 was used as the surfactant. The prepared microspheres had spherical shape.

• Macromolecular Research
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• v.10 no.5
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• pp.246-252
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• 2002

In order to the development of the delivery device of long-acting local anesthetics for postoperative analgesia and control of chronic pain of cancer patient, fentnyl-loaded poly (L-lactide-co-glycolido) (PLGA, molecular weight, 5,000 g/mole; 50 : 50 mole ratio by lactide to glycolide) microspheres (FMS) were studied. FMS were prepared by an emulsion solvent-evaporation method. The influence of several preparation parameters such as initial drug loading, PLGA concentration, emulsifier concentration, oil phase volume, and fabrication temperature has been investigated on the fentanyl release profiles. Generally, the drug showed the biphasic release patterns, with an initial diffusion followed by a lag period before the onset of the degradation phase, but there was no lag time in our system. Fentanyl was slowly released from FMS over 10 days in vitro with a quasi-zero order property. The release rate increased with increasing drug loading as well as decreasing polymer concentration with relatively small initial burst effect. From the results, FMS may be a good formulation to deliver the anesthetic for the treatment of chronic pain.

• Archives of Pharmacal Research
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• v.27 no.1
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• pp.1-12
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• 2004

Initial burst is one of the major challenges in protein-encapsulated microparticle systems. Since protein release during the initial stage depends mostly on the diffusional escape of the protein, major approaches to prevent the initial burst have focused on efficient encapsulation of the protein within the microparticles. For this reason, control of encapsulation efficiency and the extent of initial burst are based on common formulation parameters. The present article provides a literature review of the formulation parameters that are known to influence the two properties in the emulsion-solvent evaporation/extraction method. Physical and chemical properties of encapsulating polymers, solvent systems, polymer-drug interactions, and properties of the continuous phase are some of the influential variables. Most parameters affect encapsulation efficiency and initial burst by modifying solidification rate of the dispersed phase. In order to prevent many unfavorable events such as pore formation, drug loss, and drug migration that occur while the dispersed phase is in the semi-solid state, it is important to understand and optimize these variables.

• Journal of Pharmaceutical Investigation
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• v.26 no.1
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• pp.13-22
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• 1996

Poly(D,L-lactic acid) (PLA) microspheres containing alprazolam(APZ) were prepared by a solvent-emulsion evaporation method and their release patterns were investigated in vitro. Various batches of microspheres with different size and drug content were obtained by changing the ratio of APZ to PLA, PLA concentration in the dispersed phase and stirring rate. Rod-like APZ crystals on microsphere surface, which were released rapidly and could act as a loading dose, were observed with increasing drug content. The release rate was increased with increase in drug contents and decrease in the molecular weight of PLA. The release rate of APZ for long-acting injectable delivery system in vitro, which would aid in predicting in vitro release profile, could be controlled by properly optimizing various factors affecting characteristics of microspheres.

• Polymer(Korea)
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• v.37 no.6
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• pp.702-710
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• 2013

Zaltoprofen loaded polyoxalate (POX) microspheres were prepared by an emulsion solvent-evaporation/extraction method like oil-in-water (O/W) for sustained release of zaltoprofen. The influence of several preparation parameters such as fabrication temperature, stirring speed, intensity of the sonication, initial drug ratio, molecular weight ($M_w$) of POX, concentration of POX and concentration of emulsifier has been investigated on the zaltoprofen release profiles. Physicochemical properties and morphology of zaltoprofen loaded POX microspheres were investigated by scanning electron microscopy (SEM), X-ray diffraction (XRD), differential scanning calorimeter (DSC) and Fourier transform infrared (FTIR). Through the analyzed results, it was demonstrated that the characteristics of the microspheres greatly affected by the prepared condition. The releases behavior of zaltoprofen was investigated for 10 days in vitro. It was confirmed that the release behavior of zaltoprofen can be controlled by the manufacturing factor of solvent-evaporation/extraction method.

• Polymer(Korea)
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• v.37 no.1
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• pp.28-33
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• 2013

Zaltoprofen, a propionic acid derivative non-steroidal anti-inflammatory drug, was known to have powerful inhibitory effects on acute, subacute and chronic inflammation. For initial release and sustained release, the microspheres were prepared using an emulsion-solvent evaporation method like an O/W emulsion method with varying the ratio of zaltoprofen-loaded polyoxalate (POX)/PLGA micropheres. The morphology of the microspheres was confirmed by scanning electron microscopy. The crystallinity of microspheres was analyzed by X-ray diffraction and differential scanning calorimeter. Fourier transform infrared spectroscopy was used to analyze the chemical structure of microspheres. The increased ratio of POX microspheres affected the initial drug release, and the sustained release of drug was influenced by ratio of PLGA microspheres. In this study, the initial release behavior of zaltoprofen can be controlled by the ratio of POX/PLGA microspheres.

• Journal of Pharmaceutical Investigation
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• v.38 no.2
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• pp.99-104
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• 2008

PLGA micro/nano particles encapsulating ranitidine as a hydrophilic model drug were prepared by the double-emulsion solvent evaporation method. Surface morphology investigation by scanning electron microscope (SEM) showed that the emulsification by sonication could produce nanoparticles, whereas microparticles were prepared using high speed homogenizer. Moreover, while nanohalf-shell structure instead of spherical nanoparticle could be produced by adding poloxamer into oil phase (MC) with PLGA 504H, the addition of poloxamer didn't change particle shape in case of PLGA 502H. On the other hand, microparticle with poloxamer had more surface pores than those without poloxamer. The size and polydispersity (PDI) of particles were determined by particle size analyzer. Effective diameters of particles were in the range of $400{\sim}800\;nm$ and $1200{\sim}3300\;nm$ in case of nanoparticles and microparticles, respectively. Encapsulation efficiencies were in the range of $1.2{\sim}2.9%$. The addition of poloxamer produced the particles with higher encapsulation efficiency. In vitro release study in phosphate buffer (pH 7.4) at $37^{\circ}C$ showed common large initial burst release. However, the relative slower release profile could be observed in case of microparticles. Poloxamer addition increased the release rate, which was thought to be related to the increased surface area of particles.

• Bulletin of the Korean Chemical Society
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• v.32 no.5
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• pp.1465-1470
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• 2011

In this study, a poly(lactic-co-glycolic acid) (PLGA) microspheres was fabricated using emulsion solvent evaporation technique. During the procedure fabrication, some parameters process have effected on the formation of micro-carriers. The structure and morphology of micro-carriers were evaluated by SEM observation. Beside, heparin incorporated into microspheres was determined using toluidine blue method. Specifically, the effects of some parameters process such as ultrasonic levels, PLGA concentrations and freeze-dry times on the size, structure, porous formation and heparin entrapment of micro-carriers were studied carefully. We found that, the morphology and structure of carriers were influenced by the all above parameters. The diameter of the carriers varied from 20 to 400 ${\mu}M$ depending on experimental conditions. At suitable freeze-dry time, the pores were automatically formation on surface of microspheres with a significantly in the numbers of pore. After heparin incorporated porous PLGA microspheres, it was suggested that the highly heparin incorporated into porous PLGA microspheres could enhance of angiogenesis for tissue regeneration easily.

• Proceedings of the Materials Research Society of Korea Conference
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• 2009.11a
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• pp.38.2-38.2
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• 2009

Regeration of natural tissuesor to create biological substitutes for defective or lost tissues and organs through the use of cells. In addition to cells and their porous, drugs are required to promote tissue regeneration. Therefore, the present studies were prepared using simvastatim loaded porous poly(lactide-co-glycolide) (PLGA) by double emulsion solvent evaporation water-in-oil-in-water technique (W/O/W) as drug delivery system strategies for injuring tissue. The resulting microspheres were evaluated for morphology, particle size, encapsulation efficiency, degradation of PLGA microspheres in vitro drug release and in vitro cell viability. Scanning electronic microscopic (SEM) showed that the porosities of the particles was changed by experimental conditions and cultured cells were attached well on porous microspheres surface. The X-ray diffraction (XRD) and differential scanning calometry (DSC) analysis indicate thatsimvastatim was highly dipersed in the microsphere at amorphousstate.