Experimental Data of Fabricated Co-crystals of Doxorubicin HCl with Flavonoids

Abstract

Objectives: This current research work aimed for improvement of the solubility and permeability of poorly permeable Doxorubicin HCl through generating co-crystals. The main goal for the preparation of oral drugs is to decrease the overall cost of healthcare and route of administration is made easy. Methodology: In this study co-crystals of Doxorubicin HCl with Quercetin hydrate and Naringin has been prepared based on ease of hydrogen bond formation. The co-crystal batches of Doxorubicin HCl-Quercetin hydrate in ratio 1:1, 1:2, 2:1 and Doxorubicin HCl-Naringin in ratio 1:1 are prepared by slow solvent evaporation technique. Results and Discussion: The formation of co-crystal was confirmed by PXRD, DSC and FTIR. Doxorubicin HCl with Naringen crystal batch show improved solubility. The dynamic solubility of Doxorubicin HCl-Naringin co-crystal in the ratios 1:1 increased by approximately 9.2-fold as compared to pure drug and Doxorubicin HCl-Quercetin hydrate cocrystal batches.

Pharmaceutical Hydrates Analysis—Overview of Methods and Recent Advances

“…A separate group of hydrates form hydrated co-crystals, which are quite common among obtained forms of APIs. Despite being more complex than simple hydrates, their analysis unfolds with application of the same methods [ 62 , 110 , 111 , 112 , 113 , 114 , 115 ].…”

Cocrystallization of Amantadine Hydrochloride with Resveratrol: The First Drug–Nutraceutical Cocrystal Displaying Synergistic Antiviral Activity

“…To achieve this target, the polyphenol nutraceutical resveratrol (RVA) was selected as the cocrystal former by virtue of considerations for its structure and bioactivity. Structurally, there are three phenolic hydroxyl groups in an RVA molecule, which provides the possibility to form noncovalent interactions with their hydrogen-donating and/or -accepting capabilities, especially for the chloride ions of pharmaceutical hydrochlorides, as detailed in similar reports, through charge-assisted hydrogen-bonding interactions between phenolic hydroxyl groups and chloride ions. − More importantly, there have been antiviral activities, some of which are even superior to those of existing antiviral drugs against respiratory and herpes viruses, discovered for RVA, − and its excellent natural bioactivity makes it a better adjuvant with the antiviral drug ATHC. On this basis of the above background, the first case of an antiviral drug–nutraceutical cocrystal, ATHC-RVA, has been designed and prepared by a bidirectional coupling optimization cocrystallization strategy in the present work.…”

pH-Responsive Nano-transferosomes of Purpurin-18 Sodium Salt and Doxorubicin for Enhanced Anticancer Efficiency by Photodynamic and Chemo Combination Therapy

“…Despite the worthy combined therapy of PDT and/or chemotherapy to treat cancer, there are concerns regarding instability of light, side effects, and significant hepatic first-pass metabolism. , Liposome systems are biocompatible lipid-based pH-responsive carriers that are largely applied to anti-cancer treatment. , The amphiphilic properties that are phospholipid properties effectively load hydrophilic drugs into the core of the liposome. , Transferosome, a liposome-class carrier system, is fabricated by employing an edge activator (EA) as a surfactant to provide a tight bilayer structure of liposome flexibility. , The flexibility of transferosomes is advantageous in passive targeting strategies for cancer treatment. According to the enhanced permeability and retention (EPR) effects of passive targeting, nanoparticles up to a size of 400 nm are passively retained at the tumor site. ,, As a result, transferosomes effectively permeate the leaky vasculature at the tumor site …”

“… 8 Although DOX is hydrophilic and is used to treat various cancers, its dangerous side effects, such as cardiac toxicity and photosensitivity, hinder its extensive use. 9 …”

“…Despite the worthy combined therapy of PDT and/or chemotherapy to treat cancer, there are concerns regarding instability of light, side effects, and significant hepatic first-pass metabolism. 9 , 15 Liposome systems are biocompatible lipid-based pH-responsive carriers that are largely applied to anti-cancer treatment. 6 , 16 The amphiphilic properties that are phospholipid properties effectively load hydrophilic drugs into the core of the liposome.…”