| | Category | ME | L11 | Dendrimer-Dexamethasone Conjugates/Nanodevices for Targeted |
| | Delivery |
| | Abstract | Since the discovery and development of drugs is an expensive and |
| | tedious process, drug delivery systems are becoming increasingly |
| | popular. Dendrimers are repeatedly branched synthetic polymers with |
| | well-defined spherical structure, tailored surface properties, nanometer |
| | scale size (~5-10 nm), high degree of molecular uniformity, and ability to |
| | deliver drugs intracellularly. Since these surface functional groups can be |
| | used to covalently attach imaging agents, drugs, or targeting ligands for |
| | targeted delivery or controlled release, dendrimer nanodevices can be |
| | effective delivery vehicles. |
| | |
| | The novel idea behind this study was to develop and characterize a small |
| | dendrimer-dexamethasone conjugate for delivery of dexamethasone in |
| | order to minimize systemic effects and increase efficacy at the targeted |
| | site. Dexamethasone, a synthetic member of the glucocorticoid class of |
| | steroid hormones and an anti-inflammatory and immunosuppressant drug, |
| | was conjugated to Generation 4 polyamidoamine (PAMAM) dendrimers |
| | using a coupling reaction with PyBOP as the coupling reagent. The |
| | synthesized conjugate was characterized using Nuclear Magnetic |
| | Resonance Spectroscopy (NMR), High Performance Liquid |
| | Chromatography (HPLC), and Matrix-assisted Laser Desorption Time-of- |
| | Flight mass spectroscopy (MALDI-TOF). Since it is often challenging to |
| | prepare delivery systems that can release the drugs within the target |
| | tissue in a predetermined manner, drug release mechanisms and profiles in |
| | conditions that these conjugates observe were understood to allow for a |
| | more accurate prediction of their in vivo efficacy. |
| | |
| | Such an unique conjugate would serve as an optimal transport vehicle for |
| | delivering dexamethasone to specific tissues, thus providing treatments to |
| | the body in a predetermined fashion. This vehicle could eventually be |
| | utilized in patients with ocular diseases, such as macular degeneration or |
| | diabetic retinopathy, as well as potentially any other disease (including |
| | cancer and inflammation) in order that patients’ lives would be significantly |
| | improved. |
| | Bibliography | http://www.nlm.nih.gov/medlineplus/eyediseases.html |