Casadei Maria Antonietta, Cerreto Felice, Cesa Stefania, Giannuzzo Maria, Feeney Michelle, Marianecci Carlotta, Paolicelli Patrizia
Dipartimento di Studi di Chimica e Tecnologia delle Sostanze Biologicamente Attive, Università La Sapienza, 00185 Rome, Italy.
Int J Pharm. 2006 Nov 15;325(1-2):140-6. doi: 10.1016/j.ijpharm.2006.06.012. Epub 2006 Jun 10.
Solid lipid nanoparticles (SLN) containing or not (S)-(+)-2-(4-isobutylphenyl)propionic acid (ibuprofen) were prepared with Preciol ATO 5 as lipid phase by the hot homogenization technique and characterized through particle size analyses and zeta potential measurements. DSC experiments carried out on the freeze-dried samples of loaded SLN showed a shift of the melting endotherm of the lipid phase, with the maximum at a temperature value higher then that of the "empty" SLN. (1)H NMR of the nanosuspension allowed to calculate the encapsulation efficiency of the particles that was 52+/-3%. By adding dextran methacrylate (DEX-MA) to the aqueous phase and submitting the mixture to UV irradiation, systems of SLN (drug-loaded and unloaded) incorporated into a dextran hydrogel were prepared. Finally, dissolution studies of ibuprofen from the freeze-dried samples were performed. The comparison among the release profiles of ibuprofen from SLN, DEX-MA hydrogel and SLN/DEX-MA-hydrogel allows to affirm that this last system, retaining about 60% of the drug after 2h in acid medium and releasing it slowly in neutral solution, is suitable for modified delivery oral formulations.
采用热均质技术，以Preciol ATO 5为脂质相，制备了含有或不含（S）-（+）-2-（4-异丁基苯基）丙酸（布洛芬）的固体脂质纳米粒（SLN），并通过粒度分析和ζ电位测量对其进行了表征。对负载型SLN的冻干样品进行差示扫描量热法（DSC）实验，结果显示脂质相的熔融吸热峰发生了偏移，其最大值出现在比“空白”SLN更高的温度值处。纳米悬浮液的核磁共振氢谱（1H NMR）可用于计算颗粒的包封率，其值为52±3%。通过向水相中加入甲基丙烯酸葡聚糖（DEX-MA）并对混合物进行紫外线照射，制备了包封于葡聚糖水凝胶中的SLN（载药和未载药）体系。最后，对冻干样品中的布洛芬进行了溶出度研究。比较布洛芬在SLN、DEX-MA水凝胶和SLN/DEX-MA水凝胶中的释放曲线可知，最后一种体系在酸性介质中2小时后保留约60%的药物，并在中性溶液中缓慢释放，适用于改良型口服给药制剂。
