Abstract
Abstract Curcumin, a potent natural chemopreventive agent, has shown significant anti-oxidant, anti-inflammatory, anti-proliferative, anti-metastatic, anti-angiogenic properties and is found to be effective against many ailments of inflammatory origin. However, it has elicited only limited success in various pre-clinical and clinical studies presumably due to its poor oral bioavailability. To increase the bioavailability of curcumin, we have developed novel polymeric implants using polycaprolactone (Mol. Wt. 65,000) (P-65) to achieve continuous (“24/7”) controlled delivery of curcumin directly into the systemic circulation. In this study, we investigated rate of curcumin release from the polymeric implants and tissue levels of curcumin in vivo by subcutaneously grafting 2-cm implants containing 20% (w/w) curcumin in female rats. Animals were euthanized at different intervals, and blood, different tissues and implants were collected. Measurement of the residual curcumin in the implants showed a burst release of 4.66 (11.7%) and 7.34 mg (18.4%) after 7 and 14 days, respectively, followed by a more controlled release. After 70 weeks nearly 76% curcumin was released. In another study, implants containing 10% curcumin showed similar rate of release from the implants. The in vivo release patterns mimicked the rate of release observed in vitro under ‘sink’ conditions. A solvent extraction and HPLC methodology was developed to measure tissue levels of curcumin. After 4 days, curcumin was detected at a level of 60 ± 20 ng/g liver and declined to almost constant levels of 12-14 ng/g tissue after 22 days. Analysis of CYP1A1 and GSTM levels as the biomarkers of curcumin efficacy showed a 13- and 16-fold induction in CYP1A1 levels after 4 and 7 days, respectively. GSTM levels were also found to be increased by 3- and 4-fold after 4 and 7 days, respectively. These studies showed that polymeric implants can deliver controlled amounts of curcumin systemically over an extended period of time increasing its bioavailability and elicit modulation of phase I and phase II enzymes (Supported from the USPHS grant CA-118114 and Agnes Brown Duggan Endowment.). Citation Format: {Authors}. {Abstract title} [abstract]. In: Proceedings of the 101st Annual Meeting of the American Association for Cancer Research; 2010 Apr 17-21; Washington, DC. Philadelphia (PA): AACR; Cancer Res 2010;70(8 Suppl):Abstract nr 1880.
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