کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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2083885 | 1545362 | 2012 | 7 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Controlled systemic delivery by polymeric implants enhances tissue and plasma curcumin levels compared with oral administration Controlled systemic delivery by polymeric implants enhances tissue and plasma curcumin levels compared with oral administration](/preview/png/2083885.png)
Curcumin possesses potent anti-inflammatory and anti-proliferative activities but with poor biopharmaceutical attributes. To overcome these limitations, curcumin implants were developed and tissue (plasma, brain and liver) curcumin concentrations were measured in female ACI rats for 3 months. Biological efficacy of tissue levels achieved was analyzed by modulation of hepatic cytochromes. Curcumin implants exhibited diffusion-mediated biphasic release pattern with ∼2-fold higher in vivo release as compared to in vitro. Plasma curcumin concentration from implants was ∼3.3 ng/ml on day 1, which dropped to ∼0.2 ng/ml after 3 months, whereas only 0.2–0.3 ng/ml concentration was observed from 4–12 days with diet and was undetected subsequently. Almost 10-fold higher curcumin levels were observed in brain on day 1 from implants compared with diet (30.1 ± 7.3 vs 2.7 ± 0.8 ng/g) and were still significant even after 90 days (7.7 ± 3.8 vs 2.2 ± 0.8 ng/g). Although curcumin levels were similar in liver from both the routes (∼25–30 ng/g from day 1–4 and ∼10–15 ng/g at 90 days), implants were more efficacious in altering hepatic CYP1A1 levels and CYP3A4 activity at ∼28-fold lower doses at 90 days. Curcumin implants provided much higher plasma and tissue concentrations and are a viable alternative for delivery of curcumin to various organs like brain.
Schematic of observed curcumin distribution to various tissues from polymeric implants as compared to dietary administration.Figure optionsDownload high-quality image (106 K)Download as PowerPoint slide
Journal: European Journal of Pharmaceutics and Biopharmaceutics - Volume 80, Issue 3, April 2012, Pages 571–577