Polymer(Korea), Vol.34, No.4, 333-340, July, 2010
보조계면활성제 첨가에 따른 잘토프로펜을 함유한 PLGA 미립구의 생체외 방출 거동: 제조 및 특성
Effect of Cosurfactants on the Release Behavior of Zaltoprofen-loaded PLGA Microspheres in In Vitro : Preparation and Characterization
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초록
잘토프로펜은 프로피온산 유도체인 비스테로이드성 소염진통제로서 아급성 및 만성염증에 큰 억제 효과를 가지고 있다. 지속적인 약물의 방출을 위해서 PLGA의 분자량과 보조계면활성제의 농도를 달리하여 O/W 용매증발법에 의해 잘토프로펜이 함유된 PLGA 미립구를 제조하였다. 잘토프로펜이 함유된 PLGA 미립구의 물리화학적 성질 및 표면형태를 조사하기 위해 주사현미경, X선 회절 분석법 그리고 시차 주사 열량계를 이용하였다. PLGA 분자량과 보조계면활성제의 농도가 증가할수록 미립구의 크기도 증가한다. PLGA 분자량과 보조계면활성제의 농도가 증가할수록 미립구의 다공성이 줄어들고, 느린 약물의 방출을 보인다. 본 연구에서는 PLGA의 분자량과 보조계 면활성제의 농도를 조절하여 약물이 함유된 미립구의 방출 계수를 제어할 수 있을 것으로 사료된다.
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.
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