Freeze-Dried Targeted Mannosylated Selenium-Loaded Nanoliposomes: Development and Evaluation

被引:18
|
作者
Youngren, Susanne R. [1 ]
Mulik, Rohit [1 ]
Jun, Byoung [1 ]
Hoffmann, Peter R. [2 ]
Morris, Kenneth R. [1 ]
Chougule, Mahavir B. [1 ]
机构
[1] Univ Hawaii, Coll Pharm, Dept Pharmaceut Sci, Hilo, HI 96720 USA
[2] Univ Hawaii, John A Burns Sch Med, Dept Cell & Mol Biol, Honolulu, HI 96822 USA
来源
AAPS PHARMSCITECH | 2013年 / 14卷 / 03期
关键词
mannosylation; nanoliposome; selenium; thermal properties; DIFFERENTIAL SCANNING CALORIMETRY; GLUTATHIONE-PEROXIDASE ACTIVITY; ORAL-DRUG DELIVERY; INTESTINAL M-CELLS; CHILDHOOD ASTHMA; LIPID NANOPARTICLES; UNILAMELLAR VESICLES; ELEMENTAL SELENIUM; INTRINSIC ASTHMA; ALLERGIC DISEASE;
D O I
10.1208/s12249-013-9988-3
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The aim of this investigation was to develop and evaluate freeze-dried mannosylated liposomes for the targeted delivery of selenium. Dipalmitoylphosphatidylcholine, distearoylphosphatidylglycerol, and cholesterol were dissolved in a chloroform and methanol mixture and allowed to form a thin film within a rotatory evaporator. This thin film was hydrated with a sodium selenite (5.8 mu M) solution to form multilamellar vesicles and homogenized under high pressure to yield unilamellar nanoliposomes. Se-loaded nanoliposomes were mannosylated by 0.1% w/v mannosamine (Man-Lip-Se) prior to being lyophilized. Mannosamine concentration was optimized with cellular uptake studies in M receptor expressing cells. Non-lyophilized and lyophilized Man-Lip-Se were characterized for size, zeta potential, and entrapment efficiency. The influence of liposomal composition on the characteristics of Man-Lip-Se were evaluated using acidic and basic medium for 24 h. Thermal analysis and powder X-ray diffraction were used to determine the interaction of components within the Man-Lip-Se. The size, zeta potential and entrapment efficiency of the optimum Man-Lip-Se were observed to be 158 +/- 28.9 nm, 33.21 +/- 0.89 mV, and 77.27 +/- 2.34%, respectively. An in vitro Se release of 70-75% up to 24 h in PBS pH 6.8 and <8% Se release in acidic media (0.1 N HCl) in 1 h was observed. The Man-Lip-Se were found to withstand gastric-like environments and showed sustained release. Stable freeze-dried Man-Lip-Se were successfully formulated with a size of <200 nm, similar to 75% entrapment, and achieved controlled release of Se with stability under acidic media, which may be of importance in the targeted delivery of Se to the immune system.
引用
收藏
页码:1012 / 1024
页数:13
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