Investigations on 5-fluorouracil solid lipid nanoparticles (SLN) prepared by hot homogenization.
Investigations on 5-fluorouracil solid lipid nanoparticles (SLN) prepared by hot homogenization.
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发表时间：
2005-04
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通讯作者：
Shirui Mao;Pu Wang;D. Bi
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作者：
Shirui Mao;Pu Wang;D. Bi
采用热均质法制备固体脂质纳米粒，考察不同处方因素对固体脂质纳米粒性能的影响。以粒径、物理稳定常数(K(E))和Zeta电位为标准，考察了磷脂和泊洛沙姆含量对SLNS稳定性的影响。结果表明，磷脂含量对Zeta-电位有显著影响，且随着磷脂含量的增加，Zeta-电位显著增加。然而，当磷脂含量高达1.5%时，由于粘度的增加，颗粒尺寸显著增大。泊洛沙姆188在浓度低至1.0%时对粒径无明显影响。以5-氟尿嘧啶(5-FU)为模型药物，进一步考察了磷脂和泊洛沙姆含量对药物包封率的影响。结果表明，5-FU包封率随磷脂含量的增加而显著增加，与泊洛沙姆含量无关，说明5-FU已进入磷脂双层膜。
The purpose of this study was to investigate the effect of different formulation factors on the properties of solid lipid nanoparticles (SLN) prepared by a hot homogenization method. Using the particle size, physical stability constant (K(e)) and zeta-potential as standards, the stability of SLNs was investigated as a function of phospholipid and poloxamer contents. It was demonstrated that the content of phospholipid had a significant influence on the zeta-potential, which increased considerably with increasing phospholipid content. However, the particle size increased remarkably when the phospholipid content was as high as 1.5% due to the increased viscosity. Poloxamer 188 exhibited no remarkable influence on particle size when the concentration was as low as 1.0%. The influence of the phospholipid and poloxamer content on the embedding ratios of drug substances was further studied using 5-fluorouracil (5-Fu) as a model drug. It was shown that the embedding ratio increased considerably with phospholipid content and independent of poloxamer content, implying that 5-Fu was incorporated into the phospholipid bilayer membrane.