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Journal of the Korean Industrial and Engineering Chemistry, Vol.9, No.3, 457-461, June, 1998
불소화지방산염 첨가에 의한 디팔미토일포스파티딜콜린/콜레스테롤/불소화계면활성제 베지클의 제조와 물성 측정
The Preparation and Physicochemical Properties of Dipalmitoylphosphatidylcholine/Cholesterol/Fluorinated Surfactant Vesicle Incorporated Fatty Acid Salt
초록
본 연구에서는 베지클의 응용성을 확장하기 위한 기초연구로서, DPPC(dipalmitoylphosphaticylcholine)/Chol(Cholesterol)계에 불소화계면활성제(C8F17(CH2)2OCO-CH2CH(SO3Na)COO(CH2)2C8F17, FS)/불소화지방산염 ((C7F15COONH4, FFS)을 여러 가지 비율로 변화시켜 첨가함으로써 베지클을 변형 제조하고, 그 물리화학적 성질을 비교측정하였다. 제조된 베지클계에 대한 제타-전위 측정(Zetamaster Particle Electrophoresis Analyzer) 결과, 균일한 전하의 베지클이 형성되는 것으로 확인되었고, 이는 FFS 분자가 FS와 DPPC 사이에서 보조계면활성제로 기능하여 DPPC와 FS의 각 성분이 동일 베지클내에 공존하도록 작용했기 때문으로 풀이된다. 베지클의 입자크기 결정에서는 FFS의 농도가 증가할수록 그 크기가 감소하고, 제타-전위도 음의 값으로 더욱 작아지는 것으로 나타났다. 베지클의 분산도 변화에서도 DPPC/Chol/FS/FFS계의 경우가 DPPC/Chol/FS계에 비해 안정성이 훨씬 큰 것으로 조사되었다. 베지클의 서방유출 실험에서도 막내에 포집된 MB(Methylene Blue)의 유출속도가 DPPC/Chol/FS/FFS계에서 감소된다는 결과를 얻었고, 이는 FFS의 첨가로 인해 막의 유동성이 감소되기 때문으로 풀이된다. 이 결과는 형광방출 측정의 IExcimer/IMonomer 값에서도 확인되는 것으로 막의 미세점도가 FFS 첨가 베지클에서 증가되는 것으로 나타났다. 단백질로서 알부민에 대한 친화도를 비교한 결과에서는 DPPC/Chol/FS/FFS계의 친화도가 다소 낮아지는 것으로 나타났다. 이들 실험결과에 바탕하여 FFS의 첨가에 의해 DPPC/Chol/FS 베지클계는 더욱 안정하고 균일한 막의 구조를 갖는 리포솜을 형성한다는 결론을 얻었다.
The vesicle system of DPPC(dipalmitoylphosphaticylcholine)/Chol(Cholesterol) has been modified by incorporating various mole fractions of flourinated surfactant(C8F17(CH2)2OCO-CH2CH(SO3Na)COO(CH2)2C8F17. Sodium bis(1H,1H,2H,2H-heptadecaflurododecyl)-2-sulfosuccinate, FS)/fluorinated fatty acid salt (C7F15COONH4, ammoniumpentadecaflurooctyrate, FFS), and their physicochemical properties have been investigated in an attempt to enhance the stability of phospholipid vesicle system. The ζ-potential measurement by use of Zetamaster sub-micron Particle Electrophoresis Analyzer (Malvern Co.) showed that a charged homogeneous DPPC/Chol/FS vesicle has been formed owing to the incorporated FFS effect on the membrane, playing a role as a cosurfactant in the bilayer between DPPC and FS components. With increase in the concentration of FFS, it was found that the particle size and also surface charge of the DPPC/Chol/FS vesicle decreased. The stability of DPPC/Chol/FS/FFS liposome was found to be enhanced significantly compared to that of DPPC/Chol/FS according to the dispersity change as a function of time. The release rate of dye molecule of Methylene Blue from the DPPC/Chol/FS/FFS vesicle was determined to be slower than that of DPPC/Chol/FS system, and it may be attributed to the increase in microviscosity of the hydrophobic region in the bilayer. The affinfinity of DPPC/Chol/FS/FFS vesicles to albumin was found to be slightly lowered compared to that of DPPC/Chol/FS. Based on these findings, it was confirmed that a more stable and homogeneous vesicle system of DPPC/Chol/FS could be prepared by addition of FFS, acting as a cosurfactant in the aggregate formation.
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