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http://dx.doi.org/10.4333/KPS.2004.34.2.125

Preparation of Phospholipid Nanoemulsions Loaded with Paclitaxel  

Seo, Dong-Hoan (College of pharmacy, Sung Kyun Kwan University)
Han, Hee-Dong (Nanobiomaterials Laboratory, Korea Research Institute of Chemical Technology)
Chi, Sang-Cheol (College of pharmacy, Sung Kyun Kwan University)
Shin, Byung-Cheol (Nanobiomaterials Laboratory, Korea Research Institute of Chemical Technology)
Publication Information
Journal of Pharmaceutical Investigation / v.34, no.2, 2004 , pp. 125-130 More about this Journal
Abstract
Paclitaxel is an effective antineoplastic drug for various cancers especially ovarian and breast cancer. This study is to find the optimum condition for the preparation of nanoemulsions and to improve the stability and loading amount of paclitaxel in nanoemulsions. Nanoemulsions were prepared by modified spontaneous emulsification solvent diffusion method. It was composed of phosphatidylcholine:cholesterol:1,2-Distearoyl-sn-Glycero-3-Phosphoethanolamine-N-[Metoxy (Polyethylene glycol)-2000]:paclitaxel at a weight ratio of 5:3:1:1 and the Tween 80 as a surfactant. The particle size and the shape of nanoemulsions were measured by particle analyzer and SEM, respectively. The loading amount of paclitaxel in nanoemulsion was measured by UV-visible spectroscopy at 227 nm. The particle sizes were $80{\sim}120\;nm$ and the loading efficiency of paclitaxel was $8{\sim}39%$. The optimum conditions for the preparation of nanoemulsions were 8% w/w phospholipid, 16% w/v Tween 80 and 2% w/w paclitaxel, respectively.
Keywords
Paclitaxel; Nanoemulsions; Phospholipid; Tween 80;
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1 S.S. Feng and G. Huang, Effects of emulsifiers on the controlled release of paclitaxel(Taxol$^{\circledR}$) from nanospheres of biodegradable polymers, J. Control. Release, 71, 53-69 (2001)   DOI   ScienceOn
2 M.F. Shieh, I.M. Chu, CJ. Lee, P. Kan, D.M. Hau and J.J. Shieh, Liposomal delivery system for Taxol, J. Fermentation. Bioeng., 83, 87-90 (1997)   DOI   ScienceOn
3 M. Schmitt-Sody, S. Strieth, S. Krasnici, B. Sauer, B. Schulze, M. Teifel, U. Michaelis, K. Naujoks and M. Dellian, Neovascular targeting therapy: paclitaxel encapsulated in cationic liposome improves antitumoral efficacy, Clin. Cancer Res., 6, 2335-2341 (2003)
4 R. Kunstfeld, G. Wickenhauser, U. Michaelis, M. Teifel, W. Umek, K. Naujoks, K Wolff and P. Petzelbauer, Paclitaxel encapsulated in cationic liposomes diminishes tumor angiogenesis and melanoma growth in a 'Humanizes' SCIM mouse model, J. Invest. Dermatol., 120, 476-482 (2003)   DOI   ScienceOn
5 S.C. Kim, D.W. Kim, Y.H. Shim, J.S. Bang, H.S. Oh, S.W. Kim and M.H. Seo, In vivo evaluation of polymeric micellar paclitaxel formulation: toxicity and efficacy, J. Control. Release, 72, 191-202 (2001)   DOI   ScienceOn
6 B.B. Lundberg, V. Risovic, M. Ramaswamy and K.M. Wasan, A lipophilic paclitaxel derivative incorporated in a lipid emulsion for parenteral administration, J. Control. Release, 86, 93-100 (2003)   DOI   ScienceOn
7 L. He, G.L. Wang and Q. Zhang, An alternative paclitaxel microemulsion formulation: hypersensitivity evaluation and pharmacokinetic profile, Int. J. Pharm., 250, 45-50 (2003)
8 S. Alcaro, C.A. Ventura, D. Paolino, D. Battaglia, F. Ortuso, L. Cattel, G. Puglisi and M. Fresta, Preparation, characterization, molecular modeling and in vitro activity of paclitaxel-cyclodextrin complexes, Bioorg. Med. Chem. Lett., 12, 1637-1641 (2002)   DOI   ScienceOn
9 D.G. Rodrigues, C.C. Covolan, S.T. Cora야:, R. Barboza and R.C. Maranhao, Use of a cholesterol-rich emulsion that binds to low-density lipoprotein receptors as a vesicle for paclitaxel, J. Pharma. Pharmacol., 54, 765-772 (2002)   DOI   ScienceOn
10 H. Murakami, M. Kobayashi, H. Takeuchi and Y. Kawashima, Preparation of poly(DL-lactide-co-glycolide) nanoparticles by modified spontaneous emulsification solvent diffusion method Int. J. Pharm., 187, 143-152 (1999)
11 L.Z. Wang, P.C. Ho, H.S. Lee, H.K Vaddi, Y.W. Chan and C.S. Yung, Quantitation of paclitaxel in macro-sample rat plasma by a sensitive reversed-phase HPLC assay, J. Pharmaceut. Biomed., 31, 283-289 (2003)   DOI   ScienceOn
12 G. Theodoridis, G. Laskaris, C.F. de Jong, A.J.P Hofte and R. Verpoorte, Determination of paclitaxel and related diterpenoids in plant extracts by high-performance liquid chromatography with UV detection in high-performance liquid chromato-graphy-mass spectrometry, J. Chromatogr. A, 802, 297-305 (1998)   DOI   ScienceOn
13 H.Y. Kwon, J.Y. Lee, S.W. Chio, Y.S. Jang and J.H. Kim, Preparation of PLGA nanoparticles containing estrogen by emulsification-diffusion method, Colloids and surfaces, 182, 123-130 (2001)   DOI   ScienceOn
14 S.J. Park, S.H. Kim, J.R. Lee, H.B.. Lee and S.K. Hong, Preparation and characterization of biodegradable Poly( $\varepsilon$ - caprolactone) microcapsules containing erythromycin by emulsion solvent evaporation technique, Polymer(Korea), 26, 326-334 (2002)
15 P. Kan, Z.B. Chen, R.Y. Kung, C.J. Lee and I.M. Chu, Study on the formulation of o/w emulsion as carriers for lipopholic drugs, Colloids and Surface. B. -Biointerfaces, 15, 117-125 (1999)   DOI   ScienceOn
16 J.D. Ng, B. Lober, J. Witz, A.T. Dietrich D. Kern and R Giege, The crystallization of biological macromolecules from precipitates: evidence for Ostwald ripening, J. Cryst. Growth, 168, 50-62 (1996)   DOI   ScienceOn
17 K.M. Park, M.K. Lee, K.J. Hwang and C.K. Kim, Phospholipid-based microemulsions of flubiprofen by the spontaneous emulsification process, Int. J. Pharm., 183, 145-154 (1999)
18 T. Suzuki, H. Komatsu and K. Miyajima, Effects of glucose and its oligomers on the stability of freeze-dried liposomes, Bioch. Biophy. Acta, 1278, 176-182 (1996)   DOI   ScienceOn
19 P. Kan, Z.B. Chen, C.J. Lee and I.M. Chu, Development of nonionic surfactant/phospholipid o/w emulsion as a paclitaxel delivery system, J. Control. Res., 58, 271-278 (1999)   DOI   ScienceOn
20 M. Jumaa and B.W. Muller, Parenteral emulsions stabilized with of phospholipids and PEG-660-12-hydroxy-stearate: evaluation of accelerated and long-term stability, Eur. J. Pharm. Biopharm., 54, 207-212 (2002)   DOI   ScienceOn