Ocular diseases are usually treated with a topical application of drug solutions (i.e. eye drops). These traditional dosage forms account for nearly 90% of currently available marketed formulations. However, ocular physiological barriers and the poor water solubility of drug candidates present a number of problems for the development of ocular drug delivery systems.

Recently, various ophthalmic drug delivery strategies aim at improving the bioavailability of poor soluble ocular drugs have emerged. Among them, lipid-based nanocarriers exhibit a variety of potential advantages as delivery systems for ocular administration. New technological advances and unmet clinical needs provide a key driving force for the research and development of lipid-based nanocarriers for ocular drug delivery (GAN Li, et al, Drug Discovery Today, in press) .

A novel ocular gene drug delivery system by utilizing cationic core-shell liponanoparticles (DLCS-NP) has been published on Biomaterials (JIANG Min, GAN Li, et al, 2012, 33: 7621-7630). Researchers from Dr. GAN Yong’s group, Shanghai Institute of Materia Medica, designed the DLCS-NP by hydration of thin lipid film with chitosan nanoparticle (CS-NP) suspension, followed by post-insertion of the cationic phospholipid DOTAP (1,2-dioleoyl-3- trimethylammonium-propane). This specific delivery strategy has multiple functions, including better DNA protecting effect, good cellular uptake efficiency, utilization of multiple endocytic pathways, and endolysosome escaping ability.

This study was supported by the Natural Sciences Foundation of Shanghai China(No.11ZR1444700) and the National Natural Sciences Foundation of China(No.81102387) and partially supported by National Science & Technology Major Project “Key New Drug Creation and Manufacturing Program” (No.2009ZX09301-01) and the National Basic Research Program of China(No.2009CB930300).

Full text: http://dx.doi.org/10.1016/j.drudis.2012.10.005

http://dx.doi.org/10.1016/j.biomaterials.2012.06.079

Figure. The schematic diagram, preparation procedure, and intracellular pathways of DLCS-NP