Rao Sripriya Venkata Ramana, Agarwal Payal, Shao Jun
Biotechnology and Drug Delivery Laboratory, Department of Pharmacy and Administrative Sciences, College of Pharmacy and Allied Health Professions, St. John's University, 8000 Utopia Parkway, Queens, NY 11439, USA.
Int J Pharm. 2008 Oct 1;362(1-2):10-5. doi: 10.1016/j.ijpharm.2008.05.016. Epub 2008 May 23.
To develop a self-nanoemulsifying drug delivery system (SNEDDS) for protein drugs, and particularly, to test the in vitro transport of beta-lactamase (BLM) by SNEDDS across the cell monolayer. Fluorescently labeled BLM (FITC-BLM), a model protein, formulated into 16 SNEDDS preparations through a solid dispersion technique were studied for transport across MDCK monolayer. All the SNEDDS nanoemulsions resulted in higher transport rate than the free solution. The transport rate by SNEDDS depends on the SNEDDS composition. SNEDDS NE-12-7 (oil: Lauroglycol FCC, surfactant: Cremophor EL and a cosurfactant: Transcutol HP) at the ratio of 5:4:3, rendered the highest transportation rate, 33% as compared to negligible transport by the free solution. FITC-BLM solution mixed with the surfactant and the cosurfactant of SNEDDS NE-12-7 or with blank SNEDDS NE-12-7 increased the transport only by 3.3 and 1.5 folds, respectively, compared to free solution alone. It was found that the monolayer integrity was not compromised in the presence of SNEDDS NE-12-7 or its surfactant/cosurfactant. The SNEDDS significantly increased the transport of FITC-BLM across MDCK monolayer in vitro. SNEDDS may be a potential effective delivery system for non-invasive protein drug delivery.
开发一种用于蛋白质药物的自纳米乳化药物递送系统（SNEDDS），特别是测试SNEDDS介导的β-内酰胺酶（BLM）在细胞单层上的体外转运。通过固体分散技术将荧光标记的BLM（FITC-BLM），一种模型蛋白，制成16种SNEDDS制剂，研究其在MDCK单层上的转运。所有SNEDDS纳米乳剂的转运速率均高于游离溶液。SNEDDS的转运速率取决于其组成。比例为5:4:3的SNEDDS NE-12-7（油相：月桂二醇FCC，表面活性剂：聚氧乙烯蓖麻油EL，助表面活性剂：二乙二醇单乙基醚HP）具有最高的转运速率，与游离溶液可忽略不计的转运相比为33%。与单独的游离溶液相比，FITC-BLM溶液与SNEDDS NE-12-7的表面活性剂和助表面活性剂混合或与空白SNEDDS NE-12-7混合后，转运仅分别增加了3.3倍和1.5倍。发现在存在SNEDDS NE-12-7或其表面活性剂/助表面活性剂的情况下，单层完整性未受到损害。SNEDDS显著增加了FITC-BLM在体外跨MDCK单层的转运。SNEDDS可能是一种用于非侵入性蛋白质药物递送的潜在有效递送系统。
