Preparation and characterization of docetaxel self-nanoemulsifying powders (SNEPs):A strategy for improved oral delivery

Sharath Sunkavalli; Basanth Babu Eedara; Karthik Yadav Janga; Ashok Velpula; Raju Jukanti; Suresh Bandari

Korean Journal of Chemical Engineering, Vol.33, No.3, 1115-1124, March, 2016

DOI10.1007/s11814-015-0205-9 Export Citation

Preparation and characterization of docetaxel self-nanoemulsifying powders (SNEPs):A strategy for improved oral delivery

Sharath Sunkavalli, Basanth Babu Eedara, Karthik Yadav Janga, Ashok Velpula, Raju Jukanti, and Suresh Bandari^†

Department of Pharmaceutics, St. Peter’s Institute of Pharmaceutical Sciences, Vidyanagar, Hanamkonda, Warangal-506001, Telangana State, India

E-mail:

Liquid self-nanoemulsifying drug delivery systems (L-SNEDDS) of docetaxel were prepared using varying ratios of Capmul PG 8 NF (oil), Cremophor EL (surfactant) and Transcutol-P (co-surfactant). The optimized L-SNEDDS (L11) was transformed into self-nanoemulsifying powder (SNEP) by physical adsorption on to Neusilin US2 and evaluated for dissolution behavior, in vitro cytotoxicity and in vivo oral bioavailability. Optimized L-SNEDDS (L11) composed of 50% of oil, 41.7% of surfactant and 8.3% co-surfactant produced stable emulsion with smaller globules (43±3nm). In vitro dissolution studies showed the rapid drug release within 5min (95.42±1%) from SNEPN. In vitro cytotoxicity assessed by the MTT assay using MCF-7 human breast cancer cell lines revealed that L-SNEDDS significantly reduced the IC50 value and was 2.3 times lower than the pure docetaxel. Further, the oral bioavailability studies in male Wistar rats showed higher Cmax values following treatment with SNEPN (0.98±0.13 μg/mL) and L-SNEDDS (1.09±0.06 μg/mL) compared to pure docetaxel (0.37±0.04 μg/mL).

Keywords:Docetaxel;Liquid Self-nanoemulsifying Drug Delivery Systems;Self-nanoemulsifying Powders;Oral Bioavailability;Cytotoxicity

[References]

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[Referenced By]

[1] Mei L, Zhang Z, Zhao L, Huang L, Yang XL, Tang J, Feng SS, Adv. Drug Deliv. Rev., 65, 880 (2013)

[2] Feng SS, Zhao L, Tang J, Nanomedicine (Lond), 6, 407 (2011)

[3] Fossella FV, Lee JS, Shin DM, Calayag M, Huber M, Perez-Soler R, Murphy WK, Lippman S, Benner S, Glisson B, Chasen M, Hong WK, Raber M, J. Clin. Oncol., 13, 645 (1995)

[4] Kaye SB, Piccart M, Aapro M, Francis P, Kavanagh J, Eur. J. Cancer, 33, 2167 (1997)

[5] Clarke SJ, Rivory LP, Clin. Pharmacokinet., 36, 99 (1999)

[6] Campora E, Colloca G, Ratti R, Addamo G, Coccorullo Z, Venturino A, Guarneri D, Anticancer Res., 28, 3993 (2008)

[7] Wils P, Phung-Ba V, Warnery A, Lechardeur D, Raeissi S, Hidalgo IJ, Scherman D, Biochem. Pharmacol., 48, 1528 (1994)

[8] Engels FK, Sparreboom A, Mathot RA, Verweij J, Br. J. Cancer, 93, 173 (2005)

[9] Kuppens IE, van Maanen MJ, Rosing H, Schellens JH, Beijnen JH, Biomed. Chromatogr., 19, 355 (2005)

[10] van Herwaarden AE, Wagenaar E, van der Kruijssen CM, van Waterschoot RA, Smit JW, Song JY, van der Valk MA, van Tellingen O, van der Hoorn JW, Rosing H, Beijnen JH, Schinkel AH, J. Clin. Invest., 117, 3583 (2007)

[11] Gao L, Zhang D, Chen M, Duan C, Dai W, Jia L, Zhao W, Int. J. Pharm., 355, 321 (2008)

[12] Chakraborty S, Shukla D, Mishra B, Singh S, Eur. J. Pharm. Biopharm., 73, 1 (2009)

[13] Lawrence MJ, Rees GD, Adv. Drug Deliv. Rev., 45, 89 (2000)

[14] Pouton CW, Eur. J. Pharm. Sci., 11, S93 (2000)

[15] Kim CK, Cho YJ, Gao ZG, J. Control. Release, 70, 149 (2001)

[16] Holm R, Porter CJ, Edwards GA, Mullertz A, Kristensen HG, Charman WN, Eur. J. Pharm. Sci., 20, 91 (2003)

[17] Kallakunta VR, Bandari S, Jukanti R, Veerareddy PR, Powder Technol., 221, 375 (2012)

[18] Kallakunta VR, Eedara BB, Jukanti R, Ajmeera RK, Bandari S, J. Pharm. Invest., 43, 185 (2013)

[19] Inugala S, Eedara BB, Sunkavalli S, Dhurke R, Kandadi P, Jukanti R, Bandari S, Eur. J. Pharm. Sci., 74, 1 (2015)

[20] Ramasahayam B, Eedara BB, Kandadi P, Jukanti R, Bandari S, Drug Dev. Ind. Pharm., 41, 753 (2015)

[21] Tuleu C, Newton M, Rose J, Euler D, Saklatvala R, Clarke A, Booth S, J. Pharm. Sci., 93, 1495 (2004)

[22] Franceschinis E, Voinovich D, Grassi M, Perissutti B, Filipovic-Grcic J, Martinac A, Meriani-Merlo F, Int. J. Pharm., 291, 87 (2005)

[23] Wilson CG, Mahony BO, Bulletin Technique, 90, 13 (1997)

[24] Qi X, Qin J, Ma N, Chou X, Wu Z, Int. J. Pharm., 472, 40 (2014)

[25] Craig DQM, Barker SA, Banning D, Booth SW, Int. J. Pharm., 114, 103 (1995)

[26] Shafiq S, Shakeel F, Talegaonkar S, Ahmad FJ, Khar RK, Ali M, Eur. J. Pharm. Biopharm., 66, 227 (2007)

[27] Zhang P, Liu Y, Feng N, Xu J, Int. J. Pharm., 355, 269 (2008)

[28] Kang BK, Lee JS, Chon SK, Jeong SY, Yuk SH, Khang G, Lee HB, Cho SH, Int. J. Pharm., 274, 65 (2004)

[29] Elkordy AA, Essa EA, Dhuppad S, Jammigumpula P, Int. J. Pharm., 434, 122 (2012)

[30] Carr RL, Chem. Eng., 72, 163 (1965)

[31] Moes JJ, Koolen SL, Huitema AD, Schellens JH, Beijnen JH, Nuijen B, Int. J. Pharm., 420, 244 (2011)

[32] Eedara BB, Veerareddy PR, Jukanti R, Bandari S, Drug Dev. Ind. Pharm., 40, 1030 (2014)

[33] Bandari S, Jadav S, Eedara BB, Jukanti R, Veerareddy PR, Korean J. Chem. Eng., 30(1), 238 (2013)

[34] Mosmann T, J. Immunol. Methods, 65, 55 (1983)

[35] Danhier F, Lecouturier N, Vroman B, Jerome C, Marchand-Brynaert J, Feron O, Preat V, J. Control. Release, 133, 11 (2009)

[36] Wang F, Shen Y, Xu X, Lv L, Li Y, Liu J, Li M, Guo A, Guo S, Jin F, Int. J. Pharm., 456, 101 (2013)

[37] Prasad YV, Puthli SP, Eaimtrakarn S, Ishida M, Yoshikawa Y, Shibata N, Takada K, Int. J. Pharm., 250, 181 (2003)

[38] Chambin O, Jannin V, Champion D, Chevalier C, Rochat-Gonthier MH, Pourcelot Y, Int. J. Pharm., 278, 79 (2004)

[39] El Maghraby GM, Int. J. Pharm., 355, 285 (2008)

[40] Itoh K, Tozuka Y, Oguchi T, Yamamoto K, Int. J. Pharm., 238, 153 (2002)

[41] Shah NH, Patel CI, Infeld MH, Malick AW, Int. J. Pharm., 106, 15 (1994)

[42] Takeuchi T, Nagira S, Yamamoto H, Kawashima Y, Int. J. Pharm., 293, 155 (2005)

[43] Wong HL, Bendayan R, Rauth AM, Xue HY, Babakhanian K, Wu XY, J. Pharmacol. Exp. Ther., 317, 1372 (2006)

[44] Caliph SM, Charman WN, Porter CJ, J. Pharm. Sci., 89, 1073 (2000)