Oral colon‑specific drug delivery system reduces the nephrotoxicity of rhubarb anthraquinones when they produce purgative efficacy
Affiliations: Hebei Key Laboratory of Research and Development for Chinese Medicine, Chengde Medical College, Chengde, Hebei 067000, P.R. China, Department of Natural Medicinal Chemistry, School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang, Liaoning 110016, P.R. China
- Published online on: August 17, 2017 https://doi.org/10.3892/etm.2017.4959
- Pages: 3589-3601
Copyright: © Liu et al. This is an open access article distributed under the terms of Creative Commons Attribution License.
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Rhubarb is commonly used to treat constipation in China and anthraquinones (AQs) are the active components present in rhubarb. However, an increasing number of studies have reported that AQs induce nephrotoxicity. In the present study, rhubarb total free anthraquinones (RTFA) oral colon‑specific drug delivery granules (RTFA‑OCDD‑GN) were prepared to determine whether RTFA‑OCDD‑GN could reduce the nephrotoxicity that occurs when AQs produce purgative efficacy. RTFA‑OCDD‑GN were prepared using pH‑enzyme double‑layer coating technology and the cumulative release rate of RTFA in RTFA‑OCDD‑GN was assessed. The first black stool time, the number and state of feces over 8 h were observed to measure the purgative efficacy. In the nephrotoxicity test, biochemical and histopathological examinations were performed following 20 and 40 days administration, and 20 days convalescence. The cumulative release rate of RTFA in RTFA‑OCDD‑GN was >80% in simulated colonic fluid. RTFA‑OCDD‑GN produced considerable purgative efficacy compared with rhubarb medical material samples (RMMS). Following 40 days RMMS administration, blood urea nitrogen, creatinine and urine β2‑microglobulin levels in the high‑dosage group were significantly increased compared with the control and RTFA‑OCDD‑GN groups (P<0.05). All specimens from the high‑dosage RMMS group exhibited swelling/degeneration of renal proximal convoluted tubule epithelial cells. No difference in pathological conditions and biochemical indicators was detected between the RTFA‑OCDD‑GN groups and the control group. The nephrotoxicity of AQs was significantly reduced following RTFA‑OCDD‑GN administration, which produced considerable purgative efficacy compared with RMMS.