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Nanomedicine Reformulation of Chloroquine and Hydroxychloroquine

Nanotechnology Characterization Laboratory, Cancer Research Technology Program, Leidos Biomedical Research, Inc., Frederick National Laboratory for Cancer Research sponsored by the National Cancer Institute, Frederick, MD 21702, USA
Author to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Molecules 2021, 26(1), 175;
Received: 8 December 2020 / Revised: 28 December 2020 / Accepted: 29 December 2020 / Published: 31 December 2020
The chloroquine family of antimalarials has a long history of use, spanning many decades. Despite this extensive clinical experience, novel applications, including use in autoimmune disorders, infectious disease, and cancer, have only recently been identified. While short term use of chloroquine or hydroxychloroquine is safe at traditional therapeutic doses in patients without predisposing conditions, administration of higher doses and for longer durations are associated with toxicity, including retinotoxicity. Additional liabilities of these medications include pharmacokinetic profiles that require extended dosing to achieve therapeutic tissue concentrations. To improve chloroquine therapy, researchers have turned toward nanomedicine reformulation of chloroquine and hydroxychloroquine to increase exposure of target tissues relative to off-target tissues, thereby improving the therapeutic index. This review highlights these reformulation efforts to date, identifying issues in experimental designs leading to ambiguity regarding the nanoformulation improvements and lack of thorough pharmacokinetics and safety evaluation. Gaps in our current understanding of these formulations, as well as recommendations for future formulation efforts, are presented. View Full-Text
Keywords: chloroquine; hydroxychloroquine; nanomedicine; nanoformulation chloroquine; hydroxychloroquine; nanomedicine; nanoformulation
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MDPI and ACS Style

Stevens, D.M.; Crist, R.M.; Stern, S.T. Nanomedicine Reformulation of Chloroquine and Hydroxychloroquine. Molecules 2021, 26, 175.

AMA Style

Stevens DM, Crist RM, Stern ST. Nanomedicine Reformulation of Chloroquine and Hydroxychloroquine. Molecules. 2021; 26(1):175.

Chicago/Turabian Style

Stevens, David M., Rachael M. Crist, and Stephan T. Stern 2021. "Nanomedicine Reformulation of Chloroquine and Hydroxychloroquine" Molecules 26, no. 1: 175.

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