• 제목/요약/키워드: Polymeric microparticles

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Development of SS-AG20-loaded Polymeric Microparticles by Oil-in-Water (o/w) Emulsion Solvent Evaporation and Spray Drying Methods for Sustained Drug Delivery

  • Choi, Eun-Jung;Bai, Cheng-Zhe;Hong, A-Reum;Park, Jong-Sang
    • Bulletin of the Korean Chemical Society
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    • 제33권10호
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    • pp.3208-3212
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    • 2012
  • Controlled drug delivery systems employing microparticles offer lots of advantages over conventional drug dosage formulations. Microencapsulation technique have been conducted with biodegradable polymers such as poly(lactic-co-glycolic acid) (PLGA) and poly(lactic acid) (PLA) for its adjustable biodegradability and biocompatibility. In this study, we evaluated two techniques, oil-in-water (o/w) emulsion solvent evaporation and spray drying, for preparation of polymeric microparticles encapsulating a newly synthesized drug, SS-AG20, for the long-term drug delivery of this low-molecular-weight drug with a very short half-life. Drug-loaded microparticles prepared by the solvent evaporation method showed a smoother morphology; however, relatively poor encapsulation efficiency and drastic initial burst were discovered as drawbacks. Spray-dried drug-loaded microparticles had an imperfect surface with pores and distorted portions so that its initial burst was critical (70.05-87.16%) when the preparation was carried out with a 5% polymeric solution. By increasing the concentration of the polymer, the morphology was refined and undesirable initial burst was circumvented (burst was reduced to 35.93-74.85%) while retaining high encapsulation efficiency. Moreover, by encapsulating the drug with various biodegradable polymers using the spray drying method, gradual and sustained drug release, for up to 2 weeks, was achieved.

고분자 박막 내에 담지 된 실리카 마이크로입자의 광산란 효과에 의한 광에너지 상향전환 효율 향상 (Light Scattering-enhanced Upconversion Efficiency in Silica Microparticles-embedded Polymeric Thin Film)

  • 최현석;이학래;이명수;박정민;김재혁
    • 공업화학
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    • 제30권1호
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    • pp.88-94
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    • 2019
  • 삼중항-삼중항 소멸에 의한 광에너지 상향전환 기술(triplet-triplet annihilation upconversion, TTA-UC)은 특정 조건을 만족시키는 유기물들의 에너지 전달 및 융합 과정에 의해 저에너지의 광자를 고에너지의 광자로 변환시키는 신개념 에너지 전환기술이다. 본 연구에서는 실리카 마이크로입자(silica microparticle, SM)를 UC가 구현되는 폴리우레탄 박막 내에 담지 시켜 입사되는 광원의 광산란 효과를 도모함으로써 TTA-UC 효율을 향상시키고, 그 기작에 대해 탐구하였다. Seeded growth method를 통하여 약 950 nm의 균일한 크기를 갖는 SM을 합성하였으며, UC 박막 내에 담지 된 SM의 농도를 증가시킴에 따라 635 nm 광원 조사 시 430-570 nm 영역에서의 UC 세기가 최대 1.64배 증가함을 확인하였다. 삼중항 lifetime 측정을 통하여 광감응제 PdTPBP와 전자수용체 perylene 간의 triplet-triplet energy transfer(TTET) 효율을 분석한 결과, 박막 내에 담지 된 SM이 chromophore 간의 TTET에 미치는 영향은 미미한 것으로 나타났다. 또한, 입사 강도-UC 세기의 상관관계를 분석하여 TTA-UC 효율을 분석한 결과, SM이 박막 내에 존재할 경우 UC 양자효율이 최대 1.5배 향상됨을 확인하였다.

Preparation of 5-Fluorouracil-Loaded Poly(L-lactide-co-glycolide) Wafer and Evaluation of In Vitro Release Behavior

  • Lee, Jin-Soo;Chae, Gang-Soo;An, Tae-Kun;Gilson Khang;Cho, Sun-Hang;Lee, Hai-Bang
    • Macromolecular Research
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    • 제11권3호
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    • pp.183-188
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    • 2003
  • The controlled delivery of anticancer agents using biodegradable polymeric implant has been developed to solve the problem of penetration of blood brain barrier and severe systemic toxicity. This study was performed to prepare 5-FU-loaded poly (L-lactide-co-glycolide) (PLGA) wafer fabricated microparticles prepared by two different method and to evaluate their release profile for the application of the treatment of brain tumor. 5-FU-loaded PLGA microparticles were characterized by scanning electron microscopy (SEM), powder X-ray diffraction (XRD), and differential scanning calorimetry (DSC). SEM observation of the 5-FU-loaded PLGA microparticles prepared by rotary solvent evaporation method showed that 5-FU was almost surrounded by PLGA and significant reduction of crystallinity of 5-FU was confirmed by XRD. In case of release profile of 5-FU from 5-FU-loaded PLGA wafer fabricated microparticles prepared by mechanical mixing, the release profile of 5-FU followed near first order release kinetics. In contrast to the above result, release profile of 5-FU from 5-FU-loaded PLGA wafer fabricated microparticles prepared by rotary solvent evaporation method followed near zero order release kinetics. These results indicate that preparation method of the 5-FU-loaded PLGA microparticles to fabricate into wafers was contributed to drug release profile.

고분자 미세입자의 전기분사와 다공성 박막 제작에의 응용 (Electrospraying of Polymeric Microparticles and its Application to Fabrication of Porous Membrane)

  • 정영훈;오하나
    • 한국기계가공학회지
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    • 제14권5호
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    • pp.126-133
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    • 2015
  • Recently, there has been demand for polymeric porous membranes in various fields, such as environmental engineering, pharmaceutics, tissue engineering, drug delivery, biology, and fuel cells. In this study, it is proposed that a polymer particle-based porous membrane can be fabricated using electrospraying and sintering processes. Electrospraying can fabricate polymeric particles with diameters ranging from several micrometers to tens of nanometers without the cumbersome particle aggregation problem. Additionally, the particles can be sintered through thermo-compression under the glass transition temperature. In this study, a polymethyl methacrylate particle-based porous membrane with an average pore size of less than 500 nm is fabricated using the proposed method.

균열 진전에 대한 미세 입자의 영향 (The effects of microparticles on the crack propagation)

  • 정보영;박성도;윤영기;윤희석
    • 한국정밀공학회:학술대회논문집
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    • 한국정밀공학회 2003년도 춘계학술대회 논문집
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    • pp.1495-1498
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    • 2003
  • Recently, self-healing methods of a cracked matrix, especially polymeric composite materials, became the center of engineering researchers. In this paper, we summarized the self-healing concept for polymeric composite materials and investigated the effect of microparticle on the crack growth behavior in colorless and transparent matrix by experimental observation to describe the crack propagation around the microparticle inside epoxy matrix composite. Compression splitting test for the specimen involving microparticle was conducted. In addition, FE analysis was pursued to present the stress contour around microparticle in the matrix. Through the experiments and FE analysis, we found that the size. relative position, bonding condition and relative stiffness of microparticle are important parameters to decide the direction of crack propagation, which is related to the rupture of microparticle for self-healing

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단백질 캡슐화를 위한 동축 이중 노즐을 사용한 전기분무건조법 (Electrohydrodynamic Spray Drying Using Co-axial Nozzles for Protein Encapsulation)

  • 호환기;박세현;박철호;이종휘
    • 폴리머
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    • 제33권4호
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    • pp.353-357
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    • 2009
  • 분무건조는 약물의 입자 제조에 널리 사용되고 있는 효과적이고 안정적인 공정 중 하나이다. 과거 분무건조의 방법에서는 입자의 응집을 조절하기 쉽지 않았으며, 크기 조절에도 많은 어려움을 겪어 왔다. 특히 고분자 입자의 제조는 저분자 유기물질인 식품, 의약원료 등과 비교하여 상대적으로 제조하기 어려운 면이 있었다. 본 연구에서는 기존의 분무건조기를 개조하여 노즐에 전기장을 외부에서 가해 줌과 동시에 동축 이중 노즐을 사용하여 고분자 입자의 제조를 시도하였다. 내부 고분자 물질로는 폴리에틸렌글리콜과 폴리락타이드코글리코라이드를, 외부 물질로는 락토오스를 사용하였다. 그 결과 전기장을 사용하지 않는 분무건조에 비해 비교적 일정한 크기와 모양을 제조할 수 있었으며, 입자 간의 응집을 줄일 수 있음을 확인하였다. 전기분무건조된 PLGA 분말은 주로 $2{\sim}5{\mu}m$ 기인 둥근 모양의 입자로 구성되었다.

Control of Encapsulation Efficiency and Initial Burst in Polymeric Microparticle Systems

  • Yeo, Yeon;Park, Ki-Nam
    • Archives of Pharmacal Research
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    • 제27권1호
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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.

전기방사법을 이용한 유용성 생리활성성분을 포함한 고분자 마이크로입자 제조 (Electrospray-assisted Preparation of Polymer Microparticles Containing Water-insoluble Bioactive Compounds)

  • 황윤균;정민국;조성연;박성일;조은철
    • 대한화장품학회지
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    • 제43권1호
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    • pp.11-18
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    • 2017
  • Ethyl (4-(2,3-dihydro- 1H-indene-5-carboxyamido) benzoate)는 노화방지 효과가 있으나 난용성 및 결정화 특성을 가지고 있어 제형화 및 2차 가공을 통해 입자내 활성성분을 담지시키는데 어려움이 있으며, 3,5,7-trihydroxy-4'-methoxy-8-prenylflavone는 플라보노이드(flavonoid)류의 일종으로 미백기능을 가지고 있으나 복합제형에 사용할 경우 제형의 착색을 일으키는 물질 중 하나이다. 본 연구에서는 전기방사법을 이용하여 유용성/난용성 생리활성성분인 ethyl (4-(2,3-dihydro-1H-indene-5-carboxyamido) benzoate)와 3,5,7-trihydroxy-4'-methoxy-8-prenylflavone 성분을 각각 poly (methyl methacrylate)와 polycaprolactone 고분자 입자 내에 담지 시키고 이를 화장품 제형에 적용했을 때 나타나는 효과에 대해서 기술하였다. 입자내 활성성분을 담지시킨 고분자 입자를 제조하는 과정에는 고분자의 농도, 노즐의 구조, 그리고 고분자와 생리활성 성분의 상용성이 중요한 역할을 하였다. 아울러 3,5,7-trihydroxy-4'-methoxy-8-prenylflavone가 캡슐화된 polycaprolactone 고분자 입자를 금속산화물이 포함된 화장품 제형과 혼합하였을 경우, 고분자 입자는 캡슐화 되지 않은 flavonoid가 제형에 포함되었을 경우 나타나는 착색현상을 방지하는 데 효과적일 수 있다는 결과를 확인하였다.

리포익산 나노 입자의 식욕 억제에 대한 고분자의 영향 (Polymer Effects on Appetite Suppression by Lipoic Acid Nanoparticles)

  • 최혜민;박철호;이기업;박중열;고은희;김현식;이종휘
    • Journal of Pharmaceutical Investigation
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    • 제37권6호
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    • pp.349-354
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    • 2007
  • For decades, the various virtues of ${\alpha}-lipoic$ acid (ALA), a natural material synthesized in most cells, have been intensively studied and proved. Recently it was reported that ALA caused significant bodyweight reduction via appetite suppression. Unfortunately, the efficacy requires an administration over 50 mg/kg. The low bioavailability and the short plasma half life of ALA lead us to explore novel pharmaceutical dosage forms using nanoparticles. In this study, the effect of polymeric stabilizers on the bioavailability improvement of ALA nanoparticles was investigated. The reduction of particle size via nano-comminution technology was successful resulting in volume average particle sizes of 320 - 340 nm. The in vitro release rate of ALA did not reflect the decrease of particle size, possibly because of the self polymerization of ALA during nano-comminution. The type of polymeric stabilizers could not affect the release rate either. However, the in vivo food intake results of ALA showed that nano-suspensions were more effective than microparticles or a salt form. The nano-suspension containing polyvinyl pyrrolidone as the primary stabilizer and polyacrylic acid as the secondary stabilizer showed more improved efficacy for 2 hours.