Preparation, Characterization, and In Vitro and In Vivo Evaluation of Tanshinone IIA Lipid Microspere

Abstract:

Prepared Tanshinone IIA lipid microspere and evaluated its physicochemical properties in vitro and pharmacodynamics properties in vivo. Particle size, zeta potential, entrapment efficiency, quantitative determination and stability of Tan-IIA-LM with different dilution medium were investigated respectively by Dynamic Light Scattering, HPLC and Sephadex G-50 Microcolumn, and osmotic pressure and solution pH of Tan-IIA-LM were measured to evaluate the preparation comprehensively. Further more, comparative study of protection on focal cerebral ischemia/reperfusion injury in rats between Tan-IIA-LM and STS was studied.The results showed that average particle size was 203nm, zeta potential was-36.10 mV, content was 0.8mg·mL^-1, entrapment efficiency was 93% and the Tan-IIA-LM which was diluted by 0.9% sodium chloride injection and 5.0% glucose injection were stable within 6 hours. Tan-IIA-LM had obvious protection on focal cerebral ischemia/reperfusion injury in rats.

• Periodical: Advanced Materials Research (Volume 988)
• Pages: 93-100
• DOI: https://doi.org/10.4028/www.scientific.net/AMR.988.93
• Online since: July 2014
• Authors: Xin Li Liang, Jun Xia Zhao, Xiu Qiang Shi, Guo Wei Zhao, Zheng Gen Liao*, Jing Zhang, Zhe Li
• Keywords: Focal Cerebral Ischemia/Reperfusion, Lipid Microsphere, Tanshinone IIA

References

[1] Nasirideen S, Kas HS, Oner F, et al. Naproxen incorporated lipid emulsions. I. Fomulation and stability studies[J]. J Clin Pharm Ther, 1998, 23: 57-65.

DOI: 10.1046/j.1365-2710.1998.00139.x

[2] DAVIS S S, HADGRAFT J, PALIN K J. Medical and pharmaceutical applications of emulsion. Encylopedia of Emulsion Eechnology[M]. New York: Marcel Dekker Inc. (1985).

[3] PRANKERD R J, STELLA V J. The use of oil-in-water emulsions as a vehicle for parenteral drug administration [J]. J Parenter Sci Technol, 1990, 44(3): 139-149.

[4] CHEN T, LAUSIER J M, RHODES C T. Possible strategies for the formulation of antineoplastic drugs[J]. Drug Ind Pharm. 1986, 12(7): 1084-1089.

[5] Chen Y, Wu X, Yu S, et al. Neurprotective capabilities of tanshinone ⅡA against cerebral ischemia/reperfusion injury via anti-apoptotic pathway in rats[J]. Biol Pharm Bull, 2012, 35(2): 164-170.

DOI: 10.1248/bpb.35.164

[6] Herbal Intelligence Center of State Pharmaceutical Administration. Herbal medicine effective components manual[M]. People's Medical Publishing House, 1986: 1019-1020.

[7] Wang J J, Yuan H N, Qian X Y, et al. Research Status of main pharmacological effects and clinical application of Tanshinone IIA[J]. Journal of Hangzhou Teachers College，2007, 27(6): 408-411.

[8] Li R H, Wang L. Pharmacology research progress of Tan-IIA[J]. Modern Journal of Integrated Chinese Traditional and Western Medicine, 2006, 15(23) : 3303-3305.

[9] Ye L B, Xi T, Chen F, et al. Protection on Tan-IIA on focal cerebral ischemia-reperfusion injury in rats[J]. Journal of China Pharmaceutical University, 2004, 35(3): 267-270.

[10] Wu C Q, Wang C Y, Shao X, et al. Protection and mechanism of effective fraction from Buyang Huanwu Decoction on focal cerebral ischemia-reperfusion injury in rats[J]. Chinese Traditional and Herbal Drugs. 2011, 42(1): 115.

[11] Wang L X, He H B, Tang X, et al. In vitro and vivo assesement of sodium norcantharidin lipid microsphere[J]. Acta Pharmaceutica Sinica. 2006, 41(8): 784-788.

[12] Liu L P, Jin Y, Li Y . Determination of entrapment efficiency of clotrimazole liposome with Sephadex G-50 gel minicolumn centrifugation-HPLC[J]. Chin J Pharm Anal, 2007, 27(11): 1814.

[13] Wei R P, Wang Q Y, Zhu W C, et al. Determination of entrapment efficiency of Amphotericin B with minicolumn centrifugation-HPLC [J]. Chin J Pharm Anal, 2009, 29(3): 429.

[14] Gao X F, Deng Y J, Cao J N, et al. Minicolumn centrifugation-HPLC determination of entrapment efficiency for liposomal formulation of altretamine[J]. Chin J Pharm Anal, 2009 29(2): 248-249.

[15] Yu Y Y, Zhao J H, Feng N P, et al. Minicolumn centrifugation-HPLC determination of entrapment efficiency for liposomal formulation of Podophyllotoxin[J]. Chin J Pharm Anal, 2010, 41(10): 1635-1636.

[16] Liang Y, Yang Y M, Yuan S L. Research progress of pharmacological effects and clinical application of Tanshinone IIA [J]. Chinese Traditional and Herbal Drugs, 2000, 31(4) : 304-306.

[17] Chen W Y, Sun C M, Wang H M, et al. Effect of tanshinone II A pretreatment on IL-1β and RelA Mrna expression in rats with focal cerebral ischemia[J]. Nan Fang Yi Ke Da Xue Xue Bao, 2010, 30(9): 215-218.

[18] Xu H J, Su T W, Zhao C L, et al. Protection of tanshinone IIA on focal cerebral ischemia/reper- fusion injury in rats[J]. Chin Hosp Pharm, 2013, 33(16): 1334-1337.

[19] Xinli Liang, Mengliang Zhu, Yunchao Cao, et al. Preparation, characterization evaluation of Tanshinone IIA lipid microspere and comparative study of pharmacokinetics with Sodium Tanshinone IIA Sulfonate injection. Advanced Materials Research Vols. 781-784 (2013).

DOI: 10.4028/www.scientific.net/amr.781-784.1044

[20] Cao Y C, Liao Z G, Liang X L, et al. Comparative study of pharmacokinetics and tissue distribution between Tanshinone IIA lipid microspere with Sodium Tanshinone IIA Sulfonate injection[J]. Chinese Traditional and Herbal Drugs. 2013, 44(15): 2105-2111.

DOI: 10.4028/www.scientific.net/amr.781-784.1044