Hydroxychloroquine: Pharmacological, physicochemical aspects and activity enhancement through experimental formulations

Copolymer Involving 2-Hydroxyethyl Methacrylate and 2-Chloroquinyl Methacrylate: Synthesis, Characterization and In Vitro 2-Hydroxychloroquine Delivery Application

“…The profile of each thermal curve shows a sharp endothermic peak characterizing the absorption enthalpy during the melting process. The melting temperature of each sample was taken from the top of the peak, which was 90 °C for HCQ, which agreed with the literature [15], and 167 °C for CQMA. The slight change in the heat capacity of the CQMA sample observed at 117 °C seemed to indicate a glass transition temperature, revealing the presence of a polymer resulting from a thermal polymerization of a fraction of the monomer during the DSC heating process in a nitrogen gas atmosphere.…”

“…The solubility of any drug in an aqueous medium is a key factor in any drug delivery process, because it governs its rate and kinetics of absorption by target organs. The solubility of pure HCQ in water reported in the literature was estimated at 26.1 mg·L −1 at 25 °C [ 15 ]. It is well known that the solubility of a poorly water-soluble drug increases with a decrease in the size of its dispersed particles [ 41 , 42 , 43 ].…”

“…The World Health Organization (WHO) is currently conducting clinical tests (SOLIDARITY) to assess the effectiveness of 2-hydroxychloroquine as a treatment for COVID-19, while some countries have already included treatment with 2-hydroxychloroquine in their clinical advice for patients with COVID-19 [ 13 , 14 ]. In addition, the HCQ base has a partition coefficient ranged between 2.89 and 3.87 and a water solubility of 26.1 mg·L −1 [ 15 ]. These two properties place this drug in the Biopharmaceutical Classification System-II (BCS-II); in other words; this medication is highly permeable but poorly soluble.…”