Formulation and in vitro evaluation of a PEGylated microscopic lipospheres delivery system for ceftriaxone sodium
Formulation and in vitro evaluation of a PEGylated microscopic lipospheres delivery system for ceftriaxone sodium
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DOI：
10.3109/10717540903334959
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发表时间：
2009-11-01
期刊：
影响因子：
6
通讯作者：
Okorie, O.
中科院分区：
文献类型：
--
作者：
Attama, A. A.;Okafor, C. E.;Okorie, O.
本研究的目的是制备头孢曲松钠脂球分散体并对其进行体外评价。以Softisan (R) 154中30%w/w的磷脂(R) 90H为脂质基质，添加PEG 4000(10、20、30和40%w/w)，采用熔融乳化法制备头孢曲松钠脂球。通过颗粒大小、颗粒形态、包封效率、负载能力和pH对脂球进行表征。以大肠杆菌为模式生物，对头孢曲松钠负载脂球进行了微生物学研究。采用Franz细胞和模拟肠液（SIF）作为受体介质，研究了头孢曲松钠从脂球通过孔径为0.22 μ m的人工膜的体外渗透。显微照片显示球形颗粒在微米范围内，1个月后最小生长（最大尺寸=64.76 +/- 3.81 μ m）。微生物学研究表明，以20%w/w的PEG 4000和2%w/w或3%w/w的头孢曲松钠配制的脂球具有显著的抗氧化活性(P
The aim of this study was to formulate and evaluate in vitro, ceftriaxone sodium lipospheres dispersions for oral administration. Ceftriaxone sodium lipospheres were prepared by melt-emulsification using 30%w/w Phospholipon (R) 90H in Softisan (R) 154 as the lipid matrix containing increasing quantities of PEG 4000 (10, 20, 30, and 40%w/w). Characterization based on particle size, particle morphology, encapsulation efficiency, loading capacity and pH were carried out on the lipospheres. Microbiological studies of the ceftriaxone sodium-loaded lipospheres were performed using Escherichia coli as the model organism. In vitro permeation of ceftriaxone sodium from the lipospheres through artificial membrane (0.22 mu m pore size) was carried out using Franz cell and simulated intestinal fluid (SIF) without pancreatin as acceptor medium. Photomicrographs revealed spherical particles within a micrometer range with minimal growth after I month (Maximum size=64.76 +/- 3.81 mu m). Microbiological studies indicated that lipospheres formulated with 20%w/w of PEG 4000 containing 2%w/w or 3%w/w of ceftriaxone sodium gave significantly (P