5-FLUOROURACIL - VARIOUS KINDS OF LOADED LIPOSOMES - ENCAPSULATION EFFICIENCY, STORAGE STABILITY AND FUSOGENIC PROPERTIES

被引:45
作者
FRESTA, M
VILLARI, A
PUGLISI, G
CAVALLARO, G
机构
[1] UNIV CATANIA,FAC FARM,IST CHIM FARMACEUT & TOSSICOL,VIALE A DORIA 6,I-95125 CATANIA,ITALY
[2] UNIV MESSINA,DIPARTIMENTO FARMACOCHIM,I-98010 MESSINA,ITALY
[3] UNIV PALERMO,DIPARTIMENTO CHIM & TECNOL FARMACEUT,I-90125 PALERMO,ITALY
关键词
5-FLUOROURACIL; MULTILAMELLAR VESICLE; STABLE PLURILAMELLAR VESICLE; LARGE UNILAMELLAR VESICLE; STORAGE STABILITY; PARTICLE SIZE; DRUG LEAKAGE;
D O I
10.1016/0378-5173(93)90356-K
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
This paper describes the optimization of 5-fluorouracil (5-FU) loaded liposome formulations. Four different preparation procedures were carried out, obtaining two types of multilamellar vesicles (MLVs), stable plurilamellar vesicles (SPLVs) and large unilamellar vesicles (LUVs). In this study various phospholipids were used to prepare liposomes. The lipid mixtures containing dipalmitoylphosphatidylserine seemed the best for biological 5-FU delivery by presenting better encapsulation efficiency parameters, serum and storage stability, and fusogenic properties, which are an important prerequisite for in vivo liposome-cell interaction. The presence of cholesterol in the liposome composition was an important factor thereby ensuring serum and storage stability of the various vesicular systems. The most suitable liposome preparation was the SPLVs, that showed both good drug loading and stability parameters, compared to LUVs which had the highest loading capacity but low serum and storage stability.
引用
收藏
页码:145 / 156
页数:12
相关论文
共 45 条
[1]  
ACKERMAN NB, 1986, CANCER, V58, P1653, DOI 10.1002/1097-0142(19861015)58:8<1653::AID-CNCR2820580813>3.0.CO
[2]  
2-P
[3]   OPTIMIZATION AND UPSCALING OF DOXORUBICIN-CONTAINING LIPOSOMES FOR CLINICAL USE [J].
AMSELEM, S ;
GABIZON, A ;
BARENHOLZ, Y .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1990, 79 (12) :1045-1052
[4]   DIFFUSION OF UNIVALENT IONS ACROSS LAMELLAE OF SWOLLEN PHOSPHOLIPIDS [J].
BANGHAM, AD ;
STANDISH, MM ;
WATKINS, JC .
JOURNAL OF MOLECULAR BIOLOGY, 1965, 13 (01) :238-+
[5]   RADIOPAQUE LIPOSOMES - EFFECT OF FORMULATION CONDITIONS ON ENCAPSULATION EFFICIENCY [J].
BENITA, S ;
POLY, PA ;
PUISIEUX, F ;
DELATTRE, J .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1984, 73 (12) :1751-1755
[6]   INTERACTIONS OF LIPOSOMES WITH SERUM-PROTEINS [J].
BONTE, F ;
JULIANO, RL .
CHEMISTRY AND PHYSICS OF LIPIDS, 1986, 40 (2-4) :359-372
[7]   PRODRUGS OF 5-FLUOROURACIL .1. HYDROLYSIS KINETICS AND PHYSICOCHEMICAL PROPERTIES OF VARIOUS N-ACYL DERIVATIVES OF 5-FLUOROURACIL [J].
BUUR, A ;
BUNDGAARD, H .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1984, 21 (03) :349-364
[8]   CALORIMETRIC STUDIES OF THE INTERACTION OF 4-BIPHENYLACETIC ACID AND ITS BETA-CYCLODEXTRIN INCLUSION COMPOUND WITH LIPID MODEL MEMBRANE [J].
CASTELLI, F ;
PUGLISI, G ;
PIGNATELLO, R ;
GURRIERI, S .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1989, 52 (02) :115-121
[9]  
CHABNER BA, 1982, PHARM PRINCIPLES CAN, P132