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Pharmaceutics 2018, 10(1), 7;

Curcumin-Artemisinin Coamorphous Solid: Xenograft Model Preclinical Study

School of Chemistry, University of Hyderabad, Hyderabad 500 046, India
Technology Business Incubator, University of Hyderabad, Hyderabad 500 046, India
Virchow Biotech Pvt. Ltd., Animal House Facility, Hyderabad 500 055, India
Council of Scientific and Industrial Research National Chemical Laboratory, Pune 411 008, India
Author to whom correspondence should be addressed.
Received: 29 November 2017 / Revised: 27 December 2017 / Accepted: 4 January 2018 / Published: 9 January 2018
(This article belongs to the Special Issue Dissolution Enhancement of Poorly Soluble Drugs)
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Curcumin is a natural compound present in Indian spice turmeric. It has diverse pharmacological action but low oral solubility and bioavailability continue to limit its use as a drug. With the aim of improving the bioavailability of Curcumin (CUR), we evaluated Curcumin-Pyrogallol (CUR-PYR) cocrystal and Curcumin-Artemisinin (CUR-ART) coamorphous solid. Both of these solid forms exhibited superior dissolution and pharmacokinetic behavior compared to pure CUR, which is practically insoluble in water. CUR-ART coamorphous solid showed two fold higher bioavailability than CUR-PYR cocrystal (at 200 mg/kg oral dose). Moreover, in simulated gastric and intestinal fluids (SGF and SIF), CUR-ART is stable up to 3 and 12 h, respectively. In addition, CUR-PYR and CUR-ART showed no adverse effects in toxicology studies (10 times higher dose at 2000 mg/kg). CUR-ART showed higher therapeutic effect and inhibited approximately 62% of tumor growth at 100 mg/kg oral dosage of CUR in xenograft models, which is equal to the positive control drug, doxorubicin (2 mg/kg) by i.v. administration. View Full-Text
Keywords: curcumin; artemisinin; coamorphous; cocrystal; stability; bioavailability; xenograft curcumin; artemisinin; coamorphous; cocrystal; stability; bioavailability; xenograft

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Mannava, M.K.C.; Suresh, K.; Kumar Bommaka, M.; Bhavani Konga, D.; Nangia, A. Curcumin-Artemisinin Coamorphous Solid: Xenograft Model Preclinical Study. Pharmaceutics 2018, 10, 7.

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