A mesoporous silica nanoparticles (MSNs) were prepared to develop a drug delivery system by loading them with hydralazine, and functionalizing them with polyethylene glycol (PEG). The particles were subsequently characterized by TEM, N2 adsorption/desorption, XRD, and UV-vis spectroscopy to observe the morphology, chemical structure, and drug release profile. In addition, we tested functionalized MSNs using PC 12 in culture. LDH, MTT, ATP, and glutathione assays were employed to examine the physiological functioning of the samples, and the loss of LDH from the cytoplasm assayed the integrity of the membranes. First, in this work, we demonstrated the effectiveness of MSNs to seal / restore the integrity of nerve fiber membrane of damaged spinal cord with a preferential targeting ability. Second, to retard the secondary damage associated with acrolein which is significantly increased after spinal cord injury resulting in oxidative stress, mitochondrial dysfunction, increased membrane permeability, impaired axonal conductivity, and eventually cell death, we investigated the ability of MSNs as a drug carrier to transport hydralazine. Hydralazine is a commercially available anti-hypertension drug that is capable of binding to and neutralizing acrolein and its protein adducts. MSNs incorporated with hydralazine exhibited site-selective delivery with a tunable release rate and reduction of toxicity to peripheral environments. Such a formulation shows a promising potential by not only increasing the efficacy of the “experimental therapy” treatment through controlled and concentrated release of drug / polymer - but also producing an enhanced cellular internalization with a prolonged duration. The use of multifunctional nanocarriers will open the opportunity to enhance therapeutic effects to central nervous system (CNS) by providing a better understand the physiology and developing the treatment of spinal and brain injury.