Preparation and characterization of Biochanin A loaded solid lipid nanoparticles

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Chunlei Tao1,2,3
Hailin Cheng4
Kai Zhou1
Qing Luo1
Weidong Chen1,2,3


Biochanin A, the predominant isoflavones found in plants, had proved its human health benefits. The purpose of this research was to study whether Biochanin A (BCA) loaded solid lipid nanoparticles (SLN) could improve solution and prolong the halfâ€life of BCA. BCAâ€SLN was prepared by emulsion evaporation and low temperature solidification technique, and freezeâ€dried powders were developed to improve stability.The mean particle sizes, zeta potential, entrapment
efficiency (EE), and drug loading capacity (DL) of BCA was 176.0 nm, −18.7 ± 0.26, 97.15 ± 0.28%, and 6.38 ± 0.04%, respectively. The results of differential scanning calorimetry (DSC) and Xâ€ray diffraction analysis (XRD) indicated that the BCA was wrapped and absorbed in the nanoparticles. The solution of preparation is much higher than the untreated BCA.Results of stability of SLN showed a relatively shortâ€term stability after storage at 4°C and 25°C for 15 days. Drug release of untreated BCA and BCAâ€SLN was fit into the Biexponential equations and Weibull equations, respectively, and SLN showed sustained release properties. But after freezeâ€dried, stability was improved, and the EE and DL had a slightly decrease. The mean particle size was slightly increased, but the structure was not changed. In conclusion, SLN systems can represent an
effective strategy to change the poor aqueous solubility and prolong the halfâ€time of BCA.


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Tao1,2,3, C., Cheng4, H., Zhou1, K., Luo1, Q., & Chen1,2,3, W. (2014). Preparation and characterization of Biochanin A loaded solid lipid nanoparticles. Asian Journal of Pharmaceutics (AJP), 6(4).


Chen HQ, Zheng YJ, Li GH. Biochanin A protects dopaminergic neurons

against lipopolysaccharideâ€induced damage through inhibition of

microglia activation and proinflammatory factors generation. Neurosci

Lett 2007;417:112â€7.

Lapcík O, Vítková M, Klejdus B, Alâ€Maharik N, Adlercreutz H.

Immunoassay for biochanin A. J Immunol Methods 2004;294:155â€63.

Küçükboyacı N, Güvenç A, Dinç E, Adıgüzel N, Bani B. New

HPLC†chemometric approaches to the analysis of isoflavones in

Trifolium lucanicum Gasp. J Sep Sci 2010;33:2558â€67.

Dornstauder E, Jisa E, Unterrieder I, Krenn L, Kubelka W, Jungbauer A.

Estrogenic activity of two standardized red clover extracts (menoflavon)

intended for large scale use in hormone replacement therapy. J Steroid

Biochem Mol Biol 2001;78:65â€75.

Kole L, Giri B, Manna SK. Biochaninâ€A, an isoflavon, showed

antiâ€proliferative and antiâ€inflammatory activities through the inhibition

of iNOS expression, p38â€MAPK and ATFâ€2 phosphorylation and blocking

NFκB nuclear translocation. Eur J Pharmacol 2011;653:8â€15.

Lee KH, Choi EM. Biochanin A Stimulates Osteoblastic Differentiation

and Inhibits Hydrogen Peroxideâ€Induced Production of Inflammatory

Mediators in MC3T3â€E1 Cells. Biol Pharm Bull 2005;28:1948â€53.

Lin VC, Ding HY, Tsai PC, Wu JY, Lu YH, Chang TS. In vitro and in vivo

Melanogenesis Inhibition by Biochanin A from Trifolium pratense. Biosci

Biotechnol Biochem 2011;75:914â€8.

Szliszka E, Czuba ZP, Mertas A, Paradysz A, Krol W. The dietary

isoflavone biochaninâ€A sensitizes prostate cancer cells to TRAILâ€induced

apoptosis. Urol Oncol 2011. [Epub ahead of print]

Hsu JT, Hung HC, Chen CJ, Hsu WL, Ying C. Effects of the dietary

phytoestrogen biochanin A on cell growth in the mammary carcinoma

cell line MCFâ€7. J Nutr Biochem 1999;10:510â€7.

Moon YJ, Shin BS, An G, Morris ME. Biochanin A Inhibits Breast

Cancer Tumor Growth in A Murine Xenograft Model. Pharm Res


Han EH, Kim JY, Jeong HG. Effect of Biochanin A on the aryl hydrocarbon receptor and cytochrome P450 1A1 in MCFâ€7 human breast carcinomacells. Arch Pharm Res 2006;29:570â€6.

Lee YS, Seo JS, Chung HT, Jang JJ. Inhibitory effects of Biochanin A

on mouse lung tumor induced benzo(a)pyrene. J Korean Med Sci


Mansoor TA, Ramalho RM, Luo X, Ramalhete C, Rodrigues CM,

Ferreira MJ. Isoflavones as Apoptosis Inducers in Human Hepatoma

HuHâ€7 Cells. Phytother Res 2011;25:1819â€24.

Yanagihara K, Ito A, Toge T, Numoto M. Antiproliferative effects

of isoflavones on human cancer cell lines established from the

gastrointestinal tract. Cancer Res 1993;53:5815â€21.

Fung MC, Szeto YY, Leung KN, Wongâ€Leung YL, Mak NK. Effects of

biochanin A on the growth and differentiation of myeloid leukemia

wehiâ€3B (JCS) cells. Life Sci 1997;61:105â€15.

Zhang S, Morris ME. Effects of the flavonoids biochanin A, morin,

phloretin, and silymarin on Pâ€glycoproteinâ€mediated transport.

J Pharmacol Exp Ther 2003;304:1258â€67.

Ambudkar SV, Dey S, Hrycyna CA, Ramachandra M, Pastan I,

Gottesman MM. Biochemical, cellular, and pharmacological aspects of

the multidrug transporter. Annu Rev Pharmacol Toxicol 1999;39:361â€98.

Han HK, Lee HK. Enhanced dissolution and bioavailability of biochanin A via the preparation of solid dispersion: In vitro and in vivo evaluation. Int J Pharm 2011;415:89â€94.

Moon YJ, Sagawa K, Frederick K, Zhang S, Morris ME. Pharmacokinetics and bioavailability of the isoflavone biochanin A in rats. The AAPS Journal 2006;8:E433â€42.

Müller RH, Mäder K, Gohla S. Solid lipid nanoparticles (SLN) for

controlled drug deliveryâ€a review of the state of the art. Eur J Pharm

Biopharm 2000;50:161â€77.

Jores K, Mehnert W, Drechsler M, Bunjes H, Johann C, Mäder K.

Investigations on the structure of solid lipid nanoparticles (SLN) and

oilâ€loaded solid lipid nanoparticles by photon correlation spectroscopy,

fieldâ€flow fractionation and transmission electron microscopy. J Control

Release 2004;95:217â€27.

Bummer PM. Physical chemical considerations of lipidâ€based oral drug

delivery - solid lipid nanoparticles. Crit Rev Ther Drug Carrier Syst


Manjunath K, Reddy JS, Venkateswarlu V. Solid lipid nanoparticles

as drug delivery systems. Methods Find Exp Clin Pharmacol


Aji Alex MR, Chacko AJ, Jose S, Souto EB. Lopinavir loaded solid lipid

nanoparticles (SLN) for intestinal lymphatic targeting. Eur J Pharm Sci


Harde H, Das M, Jain S. Solid lipid nanoparticles: An oral bioavailability

enhancer vehicle. Expert Opin Drug Deliv 2011;8:1407â€24.

Hu L, Xing Q, Meng J, Shang C. Preparation and enhanced oral

bioavailability of Cryptotanshinoneâ€loaded Solid lipid nanoparticles.

AAPA PharmSci Tech 2010;11:582â€7.

Dodiya S, Chavhan S, Korde A, Sawant KK. Solid lipid nanoparticles

and nanosuspension of adefovir dipivoxil for bioavailability

improvement: Formulation, characterization, pharmacokinetic and

biodistribution studies. Drug Dev Ind Pharm 2012 Jun 12 [Epub ahead

of print].Dai W, Zhang D, Duan C, Jia L, Wang Y, Feng F, et al. Preparation and characteristics of oridoninâ€loaded nanostructured lipid carriers as a

controlledâ€release delivery system. J Microencapsul 2010;27:234â€41.

Yang CR, Zhao XL, Hu HY, Li KX, Sun X, Li L, et al. Preparation,

optimization and characteristic of huperzine A loaded nanostrured

lipid carriers. Chem Pharm Bull 2010;58:656â€61.

Attama AA, Schicke BC, Paepenmüller T, Müllerâ€Goymann CC. Solid lipid nanodispersions containing mixed lipid core and a polar heterolipid:

Characterization. Eur J Pharm Biopharm 2007;67:48â€57.

Venkateswarlu V, Manjunath K. Preparation, characterization and in vitro release kinetics of clozapine solid lipid nanoparticles. J Control Release 2004;95:627â€38.

Kuo YC, Chung JF. Physicochemical properties of nevirapineâ€loaded

solid lipid nanoparticles and nanostructured lipid carriers. Colloids

Surf B Biointerfaces 2011;83:299â€306.

Bayindir ZS, Yuksel N. Characterization of niosomes prepared with

various nonionic surfactants for paclitaxel oral delivery. J Pharm Sci


Lin XH, Li XW, Zheng LQ, Yu L, Zhang QQ, Liu WC. Preparation and

characterization of monocaprate nanostructured lipid carriers. Colloids

Surf A Physicochem Eng Aspects 2007;311:106â€11.

Han F, Li SM, Yin R, Liu HZ, Xu L. Effect of surfactants on the formation

and characterization of a new type of colloidal drug delivery system:

Nanostructured lipid carriers. Colloids Surf A: Physicochem Eng Aspects


Jenning V, Thünemann AF, Gohla SH. Characterisation of a novel solid

lipid nanoparticle carrier system based on binary mixtures of liquid

and solid lipids. Int J Pharm 2000;199:167â€77.