I am planning to immobilize anti-oxidants like Gallic acid in a nanocarrier with targeting moiety decorated on the surface of the nanocarrier. If i link the anti-oxidant with a covalent bond is it still possible for the nanocarrier to exert free radical scavenging properties once it reaches the target site or is it essential to release the anti-oxidant cargo to exert free radical scavenging properties at the target site.
Antioxidant properties is depends on the several factors like structure of compounds, presence of functional groups (electron donating) and side chains of the compounds. these all properties will consider while u attach any antioxidant compound with your nanocarrier. Some times these antioxidants were not directly involved in the scavenging activity, while they activate some metabolic enzymatic system which are involved in the scavenging of ROS. The one more factor was also take in the mind that the nature and molecular mass of the scavenging compound which also affect the ROS scavenging property.
Gallic acid would retain its anti-oxidant property, but, depending on how it is fixed on the carrier, it could change its activity. Hydroxyl groups are the active sites for radical scavenging in polyphenols, so when you change the strength of the concrete O-H bond, which is responsible for scavenging the radical (in GA it should be the middle one), you would affect the AO activity, too. My advice: Try it!
It depends how gallic acid (or other antioxidant ) works. If it inhibits or activates a pathway (see for instance Chem Biol Interact. 2015 Oct 5;240:292-303. doi: 10.1016/j.cbi.2015.08.026.), then it has probably to be free to exert such actions. For free radical scavenging, if the phenol groups are available, it should work but the rate constants would certainly be modified. Thus my advice is the same as that of Magdalena: try it!
Dear Yaswanth,
If you immobilize antioxidant ensuring that its active groups are free and unaffected, you will certainly achieve your goal. However, to the best of my knowledge each antioxidant molecule can perform its job only one time and targeting several nanocarriers with immobilized antioxidants will not only be expensive, but also could have negative impacts. Therefore, I advise you to use liposome technology and target liposomes (with nanocarrier in its phospholipid bilayer) containing several antioxidant molecules to target site.
Dear Yaswanth
Antioxidants usually reacts themselves when exerting their function and they are consumed in the process. As such, I can not see the application of inmobilizing in the surface. In such case, the drug will be probably consumed before it reaches its target. In the interlayer they will be protected, but they will have to be released in order to perform its job.
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