Department of Pharmaceutical Sciences, University of Ferrara, via Fossato di Mortara 17, 44121 Ferrara, Italy.
Pharm Dev Technol. 2013 Feb;18(1):266-73. doi: 10.3109/10837450.2012.717947. Epub 2012 Sep 24.
Salbutamol sulphate is widely used as bronchodilator for the treatment of asthma. Its use is limited by the relatively short duration of action and hence sustained delivery of salbutamol sulphate offers potential benefits to patients.
This study explores the preparation of lipid microparticles (LMs) as biocompatible carrier for the prolonged release of salbutamol sulphate.
The LMs were produced using different lipidic materials and surfactants, by classical melt emulsification-based methods (oil-in-water and water-in-oil-in-water emulsions) and the spray congealing technique.
For the LMs obtained by melt emulsification a lack of release modulation was observed. On the other hand, the sustained release of salbutamol sulphate was achieved with glyceryl behenate microparticles prepared by spray congealing. These LMs were characterized by scanning electron microscopy, X-ray diffractometry and differential scanning calorimetry. The drug loading was 4.72% (w/w). The particle size distribution measured by laser diffraction and electrical zone sensing was represented by a volume median diameter (Dv(50)) of 51.7-71.4 µm. Increasing the atomization air pressure from 4 to 8 bar produced a decrease of the Dv(50) to 12.7-17.5 µm.
Incorporation of the hydrophilic salbutamol sulphate into LMs with sustained release characteristics was achieved by spray congealing.
硫酸沙丁胺醇被广泛用作支气管扩张剂来治疗哮喘。但由于其作用持续时间相对较短，因此硫酸沙丁胺醇的持续释放为患者带来了潜在的益处。
本研究旨在探索脂质微球（LMs）作为硫酸沙丁胺醇长效释放的生物相容性载体的制备方法。
采用不同的脂质材料和表面活性剂，通过经典的熔融乳化法（油包水和水包油包水乳液）和喷雾冷凝技术制备 LMs。
对于熔融乳化法得到的 LMs，观察到缺乏释放调节。另一方面，通过喷雾冷凝法制备的氢化蓖麻油酸甘油酯微球实现了硫酸沙丁胺醇的持续释放。这些 LMs 通过扫描电子显微镜、X 射线衍射和差示扫描量热法进行了表征。药物载量为 4.72%（w/w）。通过激光衍射和电区感应测量的粒径分布用体积中值直径（Dv(50)）表示为 51.7-71.4 µm。将雾化空气压力从 4 巴增加到 8 巴会使 Dv(50)降低至 12.7-17.5 µm。
通过喷雾冷凝成功地将亲水性硫酸沙丁胺醇包封于具有持续释放特性的 LMs 中。
