Liposomes incorporating sodium deoxycholate for hexamethylmelamine (HMM) oral delivery: Development, characterization, and in vivo evaluation

被引:52
作者
Sun, Jukui [1 ]
Deng, Yingjie [1 ]
Wang, Siling [1 ]
Cao, Jinna [1 ]
Gao, Xiaofei [2 ]
Dong, Xiaodong [1 ]
机构
[1] Shenyang Pharmaceut Univ, Dept Pharmaceut, Shenyang 110016, Liaoning Prov, Peoples R China
[2] China Med Univ, Affiliated Hosp 4, Dept Pharmaceut, Shenyang, Peoples R China
关键词
Liposome; bile salts; oral route; entrapment efficiency; stability; PHOSPHOLIPID-VESICLES; MEMBRANES; BIOAVAILABILITY; STABILITY; MECHANISM; CHOLATE; BINDING; SALTS;
D O I
10.3109/10717541003667764
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Liposomes incorporating sodium deoxycholate (NaDC) were prepared by the method of reverse phase evaporation and used for drug delivery by the oral route. Hexamethylmelamine (HMM), an anti-tumor agent, was chosen as a model drug and encapsulated into liposomes incorporating NaDC (NaDC-Lip). Several properties of NaDC-Lip containing HMM (HMM NaDC-Lip), such as particle size, entrapment efficiency, pinacyanol chloride (PIN) spectral characteristics with various molar ratio of NaDC/PC, as well as the vesicle stability measurements with calcein were evaluated. In vivo, the area under the plasma concentration-time curve obtained from the pharmacokinetics study of HMM NaDC-Lip was found to be similar to 9.76- and 1.21-fold higher than that of HMM solution and HMM Lip, respectively, indicating that NaDC-Lip can be used as a potential carrier for oral drug administration.</.
引用
收藏
页码:164 / 170
页数:7
相关论文
共 28 条
[1]   HEXAMETHYLMELAMINE - PHARMACOLOGY AND MECHANISM OF ACTION [J].
AMES, MM .
CANCER TREATMENT REVIEWS, 1991, 18 :3-14
[2]  
[曹金娜 CAO Jin-na], 2009, [中国药学杂志, Chinese Pharmaceutical Journal], V44, P120
[3]   Oral immunisation with peptide and protein antigens by formulation in lipid vesicles incorporating bile salts (bilosomes) [J].
Conacher, M ;
Alexander, J ;
Brewer, JM .
VACCINE, 2001, 19 (20-22) :2965-2974
[4]   Vesicle to micelle phase transitions involved in the interaction of sodium cholate with phosphatidylcholine liposomes [J].
delaMaza, A ;
Parra, JL .
COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS, 1997, 127 (1-3) :125-134
[5]   Stability of liposomal formulations: action of amphiphilic molecules [J].
Elorza, MA ;
Elorza, B ;
Chantres, JR .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1997, 158 (02) :173-183
[6]   Transfer of lipophilic drugs between liposomal membranes and biological interfaces: Consequences for drug delivery [J].
Fahr, A ;
van Hoogevest, P ;
May, S ;
Bergstrand, N ;
Leigh, MLS .
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, 2005, 26 (3-4) :251-265
[7]   RAPID SEPARATION OF LOW-MOLECULAR WEIGHT SOLUTES FROM LIPOSOMES WITHOUT DILUTION [J].
FRY, DW ;
WHITE, JC ;
GOLDMAN, ID .
ANALYTICAL BIOCHEMISTRY, 1978, 90 (02) :809-815
[8]  
[高晓非 GAO Xiao-fei], 2009, [药物分析杂志, Chinese Journal of Pharmaceutical Analysis], V29, P247
[9]  
[高晓非 GAO Xiaofei], 2008, [中国新药杂志, Chinese Journal New Drugs], V17, P1326
[10]  
GARATTINI E, 1983, CANCER CHEMOTH PHARM, V11, P51