TY - JOUR
T1 - Designing of Stable Cocrystals of Cytarabine and Doxorubicin HCl Using Suitable Coformers
AU - Dheeraj, H. M.
AU - Awasthi, Ankit
AU - Pai, Aravind
AU - Birangal, Sumith
AU - Vasanthraju, S. G.
AU - Pai, Girish
AU - Sathyanarayana, Muddukrishna Badamane
N1 - Funding Information:
The authors are grateful to Manipal Academy of Higher Education for letting us conduct the research activity.
Publisher Copyright:
© 2021, Colegio de Farmaceuticos de la Provincia de Buenos Aires. All rights reserved.
PY - 2021
Y1 - 2021
N2 - In the present study cocrystal of cytarabine with L-tartaric acid and nicotinamide and cocrystal of Doxorubicin HCl with maraviroc has been prepared. The cytarabine and doxorubicin HCl are potential anticancer drugs used in the treatment of various types of cancer. Though they have certain advantages, they also have issues like low oral bioavailability, metabolic stability, toxicity and show major side effects during the treatment. In order to enhance their therapeutic potential, an attempt has been made to develop the cocrystals of both the drugs using crystal engineering. The prepared cocrystals will exhibit enhanced improved oral bioavailability, metabolic stability, and therapeutic potential. A cocrystal is a structurally homogenous crystalline material containing an API and the conformer in definite stochiometric amounts. In this study the coformers selected were L-tartaric acid and nicotinamide for cytarabine and maraviroc for doxorubicin HCl based on the ease of hydrogen bond formation. The cocrystals of Cytarabine with L-Tartaric acid and doxorubicin HCl with maraviroc were prepared in ratio 1:1,1:2,2:1. The cocrystals of Cytarabine with nicotinamide was prepared in ratio 1:1. Both the drugs formed stable cocrystals with the selected coformers. The formation of cocrystal was confirmed by FTIR, DSC, and PXRD. The saturation solubility of cytarabine with L-tartaric acid did not show higher solubility when compared to pure cytarabine. The solubility of cytarabine with nicotinamide cocrystal 1:1 ratio was increased by 1.47 fold as compared to pure drug. And cocrystals of doxorubicin HCl-maraviroc showed higher solubility when compared to pure doxorubicin HCl. The cocrystals of ratio 1:1, 1:2 and 2:1 showed an increased solubility with an increase by 1.72, 1.68, and 2.46 folds, respectively as compared to pure drug.
AB - In the present study cocrystal of cytarabine with L-tartaric acid and nicotinamide and cocrystal of Doxorubicin HCl with maraviroc has been prepared. The cytarabine and doxorubicin HCl are potential anticancer drugs used in the treatment of various types of cancer. Though they have certain advantages, they also have issues like low oral bioavailability, metabolic stability, toxicity and show major side effects during the treatment. In order to enhance their therapeutic potential, an attempt has been made to develop the cocrystals of both the drugs using crystal engineering. The prepared cocrystals will exhibit enhanced improved oral bioavailability, metabolic stability, and therapeutic potential. A cocrystal is a structurally homogenous crystalline material containing an API and the conformer in definite stochiometric amounts. In this study the coformers selected were L-tartaric acid and nicotinamide for cytarabine and maraviroc for doxorubicin HCl based on the ease of hydrogen bond formation. The cocrystals of Cytarabine with L-Tartaric acid and doxorubicin HCl with maraviroc were prepared in ratio 1:1,1:2,2:1. The cocrystals of Cytarabine with nicotinamide was prepared in ratio 1:1. Both the drugs formed stable cocrystals with the selected coformers. The formation of cocrystal was confirmed by FTIR, DSC, and PXRD. The saturation solubility of cytarabine with L-tartaric acid did not show higher solubility when compared to pure cytarabine. The solubility of cytarabine with nicotinamide cocrystal 1:1 ratio was increased by 1.47 fold as compared to pure drug. And cocrystals of doxorubicin HCl-maraviroc showed higher solubility when compared to pure doxorubicin HCl. The cocrystals of ratio 1:1, 1:2 and 2:1 showed an increased solubility with an increase by 1.72, 1.68, and 2.46 folds, respectively as compared to pure drug.
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M3 - Article
AN - SCOPUS:85123438171
SN - 0326-2383
VL - 40
SP - 39
EP - 48
JO - Latin American Journal of Pharmacy
JF - Latin American Journal of Pharmacy
IS - 1
ER -