Ochiuz Lacramioara, Grigoras Cristian, Popa Marcel, Stoleriu Iulian, Munteanu Corneliu, Timofte Daniel, Profire Lenuta, Grigoras Anca Giorgiana
Department of Pharmaceutical Technology, Faculty of Pharmacy, Grigore T. Popa University of Medicine and Pharmacy of Iasi, Universitatii Street, 16, Iasi 700115, Romania.
Petru Poni Institute of Macromolecular Chemistry, Aleea, Grigore Ghica Voda, 41A, Iasi 700487, Romania.
Molecules. 2016 Jun 29;21(7):858. doi: 10.3390/molecules21070858.
The present paper focuses on solid lipid particles (SLPs), described in the literature as the most effective lipid drug delivery systems that have been introduced in the last decades, as they actually combine the advantages of polymeric particles, hydrophilic/lipophilic emulsions and liposomes. In the current study, we present our most recent advances in the preparation of alendronate (AL)-loaded SLPs prepared by hot homogenization and ultrasonication using various ratios of a self-emulsifying lipidic mixture of Compritol 888, Gelucire 44/14, and Cremophor A 25. The prepared AL-loaded SLPs were investigated for their physicochemical, morphological and structural characteristics by dynamic light scattering, differential scanning calorimetry, thermogravimetric and powder X-ray diffraction analysis, infrared spectroscopy, optical and scanning electron microscopy. Entrapment efficacy and actual drug content were assessed by a validated HPLC method. In vitro dissolution tests performed in simulated gastro-intestinal fluids and phosphate buffer solution pH 7.4 revealed a prolonged release of AL of 70 h. Additionally, release kinetics analysis showed that both in simulated gastrointestinal fluids and in phosphate buffer solution, AL is released from SLPs based on equal ratios of lipid excipients following zero-order kinetics, which characterizes prolonged-release drug systems.
本文聚焦于固体脂质颗粒（SLPs），文献中将其描述为过去几十年中引入的最有效的脂质药物递送系统，因为它们实际上结合了聚合物颗粒、亲水/亲脂性乳液和脂质体的优点。在当前研究中，我们展示了通过热均质化和超声处理，使用Compritol 888、Gelucire 44/14和Cremophor A 25的自乳化脂质混合物的各种比例制备载阿仑膦酸盐（AL）的SLPs的最新进展。通过动态光散射、差示扫描量热法、热重分析和粉末X射线衍射分析、红外光谱、光学和扫描电子显微镜对制备的载AL的SLPs的物理化学、形态和结构特征进行了研究。通过经过验证的高效液相色谱法评估包封率和实际药物含量。在模拟胃肠液和pH 7.4的磷酸盐缓冲溶液中进行的体外溶出试验显示，AL的释放延长至70小时。此外，释放动力学分析表明，在模拟胃肠液和磷酸盐缓冲溶液中，AL均基于脂质辅料的等比例从SLPs中以零级动力学释放，这是长效释放药物系统的特征。
