Department of Clinical Medicine, University of Bologna, Bologna, Italy.
Nanomedicine. 2013 Jul;9(5):675-85. doi: 10.1016/j.nano.2012.11.007. Epub 2012 Dec 6.
Colitis is the term used for chronic inflammatory bowel diseases at substantially increased risk of developing a form of colorectal cancer (CRC) known as colitis-associated cancer. In our study we synthesized core-shell polymeric micelles obtained by self-assembly of block copolymers for high efficiency delivery of anti-inflammatory and anti-cancer compounds to colonocytes and colon mucosa. We achieved an efficient intracellular delivery of these hydrophobic compounds (prednisone, retinoic acid and doxorubicin) to cultured colonocytes without cellular toxicity. The efficacy of retinoic acid and doxorubicin administration was significantly increased using these nanosized carriers. Moreover, these polymeric micelles have been shown to overcome the multidrug resistance efflux mechanism effectively delivering doxorubicin to multidrug-resistant colon cancer cells. These nanocarriers are also suitable for selective in vivo delivery of lipophilic drugs by enema administration to the inflamed colon tissue, specifically targeting the inflamed mucosa.
This team of investigators studied polymeric micelles as highly efficient drug delivery systems enabling intracellular delivery of hydrophobic compounds (prednisone, retinoic acid, and doxorubicin) to cultured colonocytes without cellular toxicity, also demonstrating beneficial in vivo effects.
结肠炎是用于慢性炎症性肠病的术语，这些疾病有发展为结直肠癌（CRC）的风险，这种 CRC 被称为结肠炎相关癌症。在我们的研究中，我们合成了由嵌段共聚物自组装而成的核壳聚合物胶束，以实现将抗炎和抗癌化合物高效递送至结肠细胞和结肠黏膜。我们实现了这些疏水性化合物（泼尼松、维甲酸和阿霉素）向培养的结肠细胞的有效细胞内递药，而没有细胞毒性。使用这些纳米载体显著提高了维甲酸和阿霉素的给药效果。此外，这些聚合物胶束已被证明能够有效克服多药耐药外排机制，将阿霉素递送至多药耐药的结肠癌细胞。这些纳米载体也适合通过灌肠将亲脂性药物选择性递送至发炎的结肠组织，特别针对发炎的黏膜。
本研究小组研究了聚合物胶束作为高效药物递送系统，能够将疏水性化合物（泼尼松、维甲酸和阿霉素）递送至培养的结肠细胞内，而没有细胞毒性，同时也显示出有益的体内效果。
