Diego-Taboada Alberto, Maillet Laurent, Banoub Joseph H, Lorch Mark, Rigby Alan S, Boa Andrew N, Atkin Stephen L, Mackenzie Grahame
Hull York Medical School, University of Hull, Hull HU6 7RX, UK.
J Mater Chem B. 2013 Feb 7;1(5):707-713. doi: 10.1039/c2tb00228k. Epub 2012 Nov 27.
Sporopollenin exine capsules (SEC) extracted from Lycopodium clavatum spores were shown to encapsulate ibuprofen as a drug model, with 97 ± 1% efficiency as measured by recovery of the loaded drug and absence of the drug on the SEC surface by scanning electron microscopy (SEM). The encapsulated ibuprofen was shown to be unchanged from its bulk crystalline form by solid state NMR, FTIR and XRD. Essential for drug delivery applications, SEC were shown to be non-toxic to human endothelial cells and free of allergenic protein epitopes by MALDI-TOF-MS and ESI-QqToF-MS. Potential application for targeted release into the intestinal region of the gastrointestinal tract (GIT) was demonstrated by 88 ± 1% of the drug being retained in simulated gastric fluid (SGF) after 45 minutes and 85 ± 2% being released after 5 min in buffer (PBS; pH 7.4). The SEC were shown to provide significant taste masking of encapsulated ibuprofen in a double blind trial with 10 human volunteers.
从石松孢子中提取的孢粉素外壁胶囊（SEC）被证明可以将布洛芬作为药物模型进行包封，通过负载药物的回收率以及扫描电子显微镜（SEM）检测SEC表面无药物，测得包封效率为97±1%。通过固态核磁共振、傅里叶变换红外光谱和X射线衍射表明，包封的布洛芬与其块状晶体形式相比没有变化。对于药物递送应用至关重要的是，通过基质辅助激光解吸电离飞行时间质谱（MALDI-TOF-MS）和电喷雾串联四极杆飞行时间质谱（ESI-QqToF-MS）表明，SEC对人内皮细胞无毒且无致敏蛋白表位。45分钟后，88±1%的药物保留在模拟胃液（SGF）中，5分钟后在缓冲液（PBS；pH 7.4）中85±2%的药物释放，证明了其在胃肠道（GIT）肠道区域靶向释放的潜在应用。在一项针对10名人类志愿者的双盲试验中，SEC被证明对包封的布洛芬具有显著的掩味效果。
