Similar articles

Abstract: Both geniposide (Ge) and natural borneol (NB) are bioactive substances derived from traditional Chinese herbs. The effect of NB on the pharmacokinetics of Ge in rat via intranasal administration was investigated. The concentrations of Ge in plasma were determined by reversed-phase high-performance liquid chromatography (HPLC) after intranasal administration of Ge (4 mg/kg) alone and combined with different doses (0.08, 0.8, and 8 mg/kg) of NB. The intravenous administration was given as a reference (4 mg/kg of Ge and 8 mg/kg of NB). Compared with the intravenous administration, the absolute bioavailability of Ge was 76.14% through intranasal administration combined with NB. Compared with the intranasal administration of Ge alone, Ge could be absorbed rapidly in the nasal cavity combined with NB; the peak time of Ge in the plasma became shorter (3–5 min vs. 40 min); the peak concentration became higher (1.32–4.25 μg/ml vs. 0.67 μg/ml); and, the relative bioavailability of Ge combined with NB was 90.3%–237.8%. The enhancing effect was attenuated as the dose of NB decreased. The results indicated that NB can accelerate the absorption of Ge dose-dependently in the nasal cavity.

[1]Albrecht, J., Kopietz, R., Frasnelli, J., Wiesmann, M., Hummel, T., Lundstrom, J.N., 2010. The neuronal correlates of intranasal trigeminal function—an ALE meta-analysis of human functional brain imaging data. Brain Res. Rev., 62(2):183-196.

[2]Cai, Z., Hou, S., Li, Y., Zhao, B., Yang, Z., Xu, S., Pu, J., 2008. Effect of borneol on the distribution of gastrodin to the brain in mice via oral administration. J. Drug Target., 16(2):178-184.

[3]Chen, X.M., Zhu, J.B., Sun, W.D., Zhang, L.J., 2006. Effect of absorption enhancers on nasal ginsenoside Rg₁ delivery and its nasal ciliotoxicity. Acta Pharm. Sin., 41(2):149-155 (in Chinese).

[4]Dai, J.P., Chen, J., Bei, Y.F., Han, B.X., Wang, S., 2009. Influence of borneol on primary mice oral fibroblasts: a penetration enhancer may be used in oral submucous fibrosis. J. Oral Pathol. Med., 38(3):276-281.

[5]Hou, Y.C., Tsai, S.Y., Lai, P.Y., Chen, Y.S., Chao, P.D., 2008. Metabolism and pharmacokinetics of genipin and geniposide in rats. Food Chem. Toxicol., 46(8):2764-2769.

[6]Hu, L.M., Fan, G.W., Gao, X.M., Zhang, B.L., 2005. Comparison of influence of natural borneol and synthetic borneol on gastric mucosal barrier in rats. J. Tianjin Univ. Tradition. Chin. Med., 24(3):123-125 (in Chinese).

[7]Illum, L., 2003. Nasal drug delivery—possibilities, problems and solutions. J. Control. Release, 87(1-3):187-198.

[8]Koo, H.J., Lim, K.H., Jung, H.J., Park, E.H., 2006. Anti-inflammatory evaluation of gardenia extract, geniposide and genipin. J. Ethnopharmacol., 103(3):496-500.

[9]Li, F., Feng, J., Cheng, Q., Zhu, W., Jin, Y., 2007. Delivery of ¹²⁵I-cobrotoxin after intranasal administration to the brain: a microdialysis study in freely moving rats. Int. J. Pharm., 328(2):161-167.

[10]Lu, Y., Chen, X., Du, S., Wu, Q., Yao, Z., Zhai, Y., 2010. The in situ and in vivo study on enhancing effect of borneol in nasal absorption of geniposide in rats. Arch. Pharm. Res., 33(5):691-696.

[11]Lv, H., Sun, H., Sun, W., Liu, L., Wang, P., Wang, X., Cao, H., 2008. Pharmacokinetic studies of a Chinese triple herbal drug formula. Phytomedicine, 15(11):993-1001.

[12]Merkus, F.W.H.M., Schipper, N.G.M., Verhoef, J.C., 1996. The influence of absorption enhancers on intranasal insulin absorption in normal and diabetic subjects. J. Control. Release, 41(1-2):69-75.

[13]Suzuki, Y., Kondo, K., Ikeda, Y., Umemura, K., 2001. Antithrombotic effect of geniposide and genipin in the mouse thrombosis model. Planta Med., 67(9):807-810.

[14]Ueno, K., Takeda, Y., Iwasaki, Y., Yoshizaki, F., 2001. Simultaneous estimation of geniposide and genipin in mouse plasma using high-performance liquid chromatography. Anal. Sci., 17(10):1237-1239.

[15]Xiao, Y.Y., Ping, Q.N., Chen, Z.P., 2007. The enhancing effect of synthetical borneol on the absorption of tetramethyl-pyrazine phosphate in mouse. Int. J. Pharm., 337(1-2):74-79.

[16]Ye, G., Zhu, H.Y., Zhao, H.L., Xu, B., Huang, C.G., 2006. HPLC method for the determination and pharmacokinetic studies on geniposide in rat serum after oral administration of traditional Chinese medicinal preparation Yin-Zhi-Ku decoction. Biomed. Chromatogr., 20(8):743-747.

[17]Yu, Y., Wang, W., Li, S.M., 2006. Simultaneous determination of borneol and nimodipine in mice plasma by GC-MSⁿ. Chin. Pharm. J., 41(16):1259-1262 (in Chinese).

[18]Zhang, Q., Du, S., Lu, Y., Rao, X., 2009. Studies on O/W partition coefficient and absorption kinetics of geniposide in fructus gardeniae extract in rat intestine. China J. Chin. Mat. Med., 34(14):1840-1844 (in Chinese).

[19]Zhou, S., Kawakami, S., Yamashita, F., Hashida, M., 2010. Intranasal administration of CpG DNA lipoplex prevents pulmonary metastasis in mice. Cancer Lett., 287(1):75-81.