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Open AccessArticle

Curcumin-Artemisinin Coamorphous Solid: Xenograft Model Preclinical Study

1
School of Chemistry, University of Hyderabad, Hyderabad 500 046, India
2
Technology Business Incubator, University of Hyderabad, Hyderabad 500 046, India
3
Virchow Biotech Pvt. Ltd., Animal House Facility, Hyderabad 500 055, India
4
Council of Scientific and Industrial Research National Chemical Laboratory, Pune 411 008, India
*
Author to whom correspondence should be addressed.
Pharmaceutics 2018, 10(1), 7; https://doi.org/10.3390/pharmaceutics10010007
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)
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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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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