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Full-Text Articles in Medicine and Health Sciences
Development Of Glucocorticoid Prodrug For The Treatment Of Lupus Nephritis, Xiaobei Wang
Development Of Glucocorticoid Prodrug For The Treatment Of Lupus Nephritis, Xiaobei Wang
Theses & Dissertations
Nephritis is one of the major complications of systemic lupus erythematosus (SLE). While glucocorticoids (GC) are frequently used as the first line treatment for lupus nephritis, long-term GC usage is often complicated by severe adverse effects. To address this challenge, we have developed a polyethylene glycol (PEG)-based macromolecular prodrug (ZSJ-0228) of dexamethasone, which self-assembles into micelles in aqueous media. When compared to the dose equivalent daily dexamethasone 21-phosphate disodium (Dex) treatment, monthly intravenous administration of ZSJ-0228 for two months significantly improved the survival of lupus-prone NZB/W F1 mice and was much more effective in normalizing proteinuria, with clear histological evidence …
Next Generation Of Translational Long-Acting Cabotegravir, Tian Zhou
Next Generation Of Translational Long-Acting Cabotegravir, Tian Zhou
Theses & Dissertations
Recent development of long-acting antiretroviral therapeutic regimens has opened a new chapter for HIV/AIDS management. Cabotegravir (CAB), as one of the very first long-acting antiretroviral regimens, has drawn tremendous attention. However, the remaining challenges include suboptimal dosing intervals, large injection volume, injection site reactions, lack of tissue penetration, etc. As one of the pioneers in this field, our lab was successful in harnessing mononuclear phagocytes as “Trojan horses” for antiretroviral drug delivery and transportation to viral reservoirs. We proposed this targeted delivery strategy could address the limitations of current CAB formulation. To this end, we developed folic acid decorated CAB …
Synthesis And Characterization Of Redox-Sensitive Polymer And Prodrug For Targeted Drug Delivery, Chang-Hee Whang
Synthesis And Characterization Of Redox-Sensitive Polymer And Prodrug For Targeted Drug Delivery, Chang-Hee Whang
Electronic Theses and Dissertations
Systemic administration of chemotherapeutics is associated with various side effects deriving from accumulation in off-target sites and acute toxicity of the drugs. In the past decade, engineering targeted drug delivery platforms arose as a novel paradigm to overcome such obstacles and ultimately achieve advanced forms of chemotherapy. This thesis reports successful syntheses of l-RSP, a redox-sensitive self-immolative polymer, and DNS-SN38, thiol-sensitive SN-38 prodrug, as potential candidates for targeted drug delivery platforms. By covalently conjugating a redox-trigger (p-nitrobenzyl alcohol) and self-immolative linker (p-hydroxybenzyl alcohol) to the cyclization spacer (n-2-(hydroxyethyl)ethylene diamine), a novel self-immolative monomer was obtained. Polymerization of the respective monomer …