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Full-Text Articles in Medicine and Health Sciences
Development Of Long-Acting Antiviral Drug Nanoformulations, Denise Cobb
Development Of Long-Acting Antiviral Drug Nanoformulations, Denise Cobb
Theses & Dissertations
Antiretroviral therapy (ART) has improved the quality and duration of life for people living with human immunodeficiency virus (HIV) infection. However, opportunities to improve its profile abound. ART is limited by putative viral reservoir penetrance, emergence of viral mutations, inherent toxicities, and regimen non-adherence. These highlight the need improved drug delivery schemes. Previously, our lab has demonstrated that targeting mononuclear phagocytes for antiretroviral drug delivery extends drug half-life and improves penetrance into viral reservoirs, addressing these limitations of ART. Herein, we developed synthetic and biologic antiretroviral (ARV) drug nanocarriers improve the pharmacokinetic (PK) and pharmacodynamic (PD) profiles of ARVs through …
Macromolecular Prodrug For The Treatment Of Ulcerative Colitis, Yuanyuan Sun
Macromolecular Prodrug For The Treatment Of Ulcerative Colitis, Yuanyuan Sun
Theses & Dissertations
Ulcerative colitis is a chronic inflammatory bowel disease affecting the colon. More than 1 million Americans are affected, with the annual economic burden up to 14.9 billion in the United States. By far, ulcerative colitis still lacks the cure and the current treatment strategies are limited due to severe side effects and in-sufficient efficacy. The tofacitinib (Xeljanz) is the only approved oral medication by for adults with moderately-to-severely-active ulcerative colitis. But the related side effects and serious infections still have to be resolved. In the previous study in our lab, the researchers have successfully developed and characterized multiple hy-drophilic prodrug …
Development Of A Long-Acting Nanoformulation Of Dolutegravir For Prevention And Treatment Of Hiv-1 Infection, Brady Sillman
Development Of A Long-Acting Nanoformulation Of Dolutegravir For Prevention And Treatment Of Hiv-1 Infection, Brady Sillman
Theses & Dissertations
Dolutegravir (DTG) is a potent human immunodeficiency virus type 1 (HIV-1) integrase strand-transfer inhibitor (INSTI) with a high barrier to viral drug resistance. However, opportunities to improve its profile abound. These include extending the drug’s apparent half-life, increasing penetrance to “putative” viral reservoirs, and reducing inherent toxicities. These highlight, in part, the need for long-acting, slow effective release antiretroviral therapy (LASER ART) delivery schemes. A long-acting (LA) DTG was made by synthesizing a hydrophobic and lipophilic prodrug encased with poloxamer (P407) surfactant. This modified DTG (MDTG) reduced systemic metabolism and polarity, increased lipophilicity and membrane permeability, improved encapsulation, and formed …
Synthesis And Development Of Long-Acting Abacavir Prodrug Nanoformulations, Dhirender Singh
Synthesis And Development Of Long-Acting Abacavir Prodrug Nanoformulations, Dhirender Singh
Theses & Dissertations
Over the past decade, work from our laboratory has demonstrated the potential of targeted nanoformulated antiretroviral therapy (nanoART) to produce sustained high plasma and tissue drug concentrations for weeks following a single intramuscular (IM) administration that can suppress ongoing viral replication and mitigate dose associated viral resistance. While progress has occurred towards developing long-acting nanoformulations for protease and nonnucleoside reverse transcriptase (RT) inhibitors, development of nanoformulations of hydrophilic nucleoside RT inhibitor drugs have remained elusive. Abacavir (ABC); a hydrophilic molecule exhibited limited utilities to develop into long-acting nanoformulation platform. Furthermore, inefficient conversion of ABC to its biological active metabolites; carbovir …