Lipid shell modified with combination of lipid and phospholipids in solid lipid nanoparticles for engineered specificity of paclitaxel in tumor bearing mice.

Sidharth Malgounda Patil, Hemant P. Joshi


Paclitaxel (PTX) is an anticancer drug belonging to the class of Taxan. It is active against various types of carcinomas. The marketed formulation of paclitaxel is associated with deleterious effects with lack of specificity to tumor. Solid lipid nanoparticles (SLN) are colloidal carriers extensively studied and developed for there potential uses especially for controlled release and site specificity. The present study was designed to develop a formulation of PTX in the form of SLN to be administered via IV route with improved tumor specificity, in which the lipid shell was modified by using combination of lipid with phospholipids. Total eight formulations were prepared and were characterized by various in vitro and in vivo parameters. The microemulsification method was used for the preparation of SLN.The production yield  of resulting process for all SLN was high. Average particle size was ranged between 209 nm to 385 nm. The developed PTX-SLN showed high percentage entrapment efficiency. The zeta potential values showed the good stable feature of the sln.The in vitro dissolution study showed that drug release was more retarded and was found to dependent on concentration of lipids employed. In vitro cytotoxicity study was performed on MCF-7 cancer cell line, which showed that formulation G2 is having more potentiating effect on cancer cell line. Tissue targeting study and tumor growth inhibition studies were performed on mice where the PTX loaded SLN from batch G2 shown more promising outcome. Results obtained from this study indicated strongly that developed SLN are having potential as an efficient drug delivery system for paclitaxel.


PTX, SLN, Modified Shell, Lipid and Phospholipids, Stearic Acid SLN

Full Text:




Rang HP, Dale MM, Ritter JM. Cancer Chemotherapy, 4th edition : Churchill Livingstone; (2001).

Cancer chemotherapy. [Online] [Cited 2010 Sep 28]; Available from URL:

Bharadwaj, Rajnish, Yu, Hongtao; The spindle checkpoint, aneuploidy, and cancer, (2004); Oncogene 23 (11): 2016–27.

Brito, D. A., Yang, Z., Rieder, C. L; Microtubules do not promote mitotic slippagewhen the spindle assembly checkpoint cannot be satisfied, The Journal of Cell Biology, (2008);182 (4): 623–9.

Cancer chemotherapy. [Online] [Cited 2010 Sep 28]; Available from URL:

Chein YW. Fundamentals of rate controlled drug delivery system.2nd edition- Revised and expanded;Newyork: Marcel dekker, inc;(1992):43-137.

Kreuter J. Colloidal drug delivery systems. Library of congress cataloging in publication data,s Marcel Dekker, INC; Newyork: 1994; 66: 219-315.

Kevin J. Kauffman,, Naveen Kanthamnenib,Samantha A. Meenach, Benjamin C. Piersona,Eric M. Bachelderb, Kristy M. Ainsliea., Optimization of rapamycin-loaded acetalated dextran microparticles for immunosuppression, International Journal of Pharmaceutics, (2012); 422: 356–363.

Francesca Cavalieri, Ali El Hamassi, Ester Chiessi, and Gaio Paradossi., Stable Polymeric Microballoons as Multifunctional Device for Biomedical Uses: Synthesis and Characterization, Langmuir ,(2005); 21: 8758-8764.

Kircheis, E. Ostermann, M.F. Wolschek, C. Lichtenberger, C. Magin-Lachmann, L. Wightman, M. Kursa and E. Wagner., Tumor-targeted gene delivery of tumor necrosis factor-alpha induces tumor necrosis and tumor regression without systemic toxicity, Cancer Gene Ther,( 2002); 9(8):673-680.

E. Garcia-Garcia , K. Andrieux, S. Gil, P. Couvreur., Colloidal carriers and blood–brain barrier (BBB) translocation: A way to deliver drugs to the brain, International Journal of Pharmaceutics , (2005); 298: 274–292.

Vighi E, Ruozi B, Montanari M, Battini R, Leo E., Re-dispersible cationic solid lipid nanoparticles (SLNs) freeze-dried without cryotectors: Characterization and ability to bind the pGEGFP, Eur J Pharm Biopharm,( 2007); 67:320-28.

Wissing SA, Kayser O, Muller RH., Solid lipid nanoparticles for parenteral drug delivery, Advanced Drug Delivery Reviews. May (2004); 56(9): 1257-72.

Jie Liu a, Wen Hub, Huabing Chena, Qian Ni b, Huibi Xua, Xiangliang Yang; Isotretinoin-loaded solid lipid nanoparticles with skin targeting for topical delivery , International Journal of Pharmaceutics, 328 (2007): 191–195.

R.H. M¨uller a, S. Rungea, V. Ravelli b, W. Mehnert a, A.F. Th¨unemannc, E.B. Souto, Oral bioavailability of cyclosporine: Solid lipid nanoparticles (SLN®) versus drug nanocrystals, International Journal of Pharmaceutics, 317 (2006): 82–89.

F.Q. Hu, Y. Hong, H. Yuan; Preparation and characterization of solid lipid nanoparticles containing peptide, International Journal of Pharmaceutics, 273 (2004): 29–35.

E.B. Souto a, C. Anselmi b, M. Centini b, R.H. M¨uller;Preparation and characterization of n-dodecyl-ferulate-loaded solid lipid nanoparticles (SLN®) International Journal of Pharmaceutics ,295 (2005):, 261–268.

Z. Ahmad, M. Maqbool ,A. F. Raja; Nanomedicine for tuberculosis: Insights from animal models , Int.J.Nano Dim, (2011); 2(1): 67-84.

Bin Lua,b, , Su-Bin Xionga, Hong Yanga, Xiao-Dong Yina, Ruo-Bing Chao; Solid lipid nanoparticles of mitoxantrone for local injection against breast cancer and its lymph node metastases, european journal of pharmaceutical sciences; ( 2 0 0 6 ),Article in press.

Anil K. Singla, Alka Garg, Deepika Aggarwal; Paclitaxel and its formulations, International Journal of Pharmaceutics, (2002); 235: 179–192.

Wolfgang Mehnert, Karsten Mader;“SLNs production, characterization and application”, Advanced Drug Delivery Review, 47:165-196,(2001).

Takeuchi H, Matsui Y, Sugihara H, Yamamoto H, Kawashima Y. ;Effectiveness of submicron-sized, chitosan-coated liposomes in oral administration of peptide drugs, Int. J. Pharm, 303:160-70,(2005).

Yogesh B. Patil , Suresh K. Swaminathan , Tanmoy Sadhukha , Linan Mac, Jayanth Panyamb; The use of nanoparticle-mediated targeted gene silencing and drug delivery to overcome tumor drug resistance, Biomaterials,;31:358–365,(2010).

Virivaroj A, Ritthidei GC.; Diazepam- glycerol behenate nanoparticles for parenteral delivery prepared by the hot homogenization process, Asian Journal of Pharmaceutical Sciences, 1: 17-30,( 2006).

Jain P, Mishra A, Yadav SK, Patil UK, Baghel US; Formulation Development and Characterization of Solid Lipid Nanoparticles Containing Nimesulide.,International Journal of Drug Delivery Technology; 1(1): 24-27,(2009).

Freshney, R. Alan R. Liss, Culture of Animal Cells: A Manual of Basic Technique, Inc. New York., 117-184, (1987).

Cristina Fonseca, Sergio Simo, Rogerio Gaspar, Paclitaxel-loaded PLGA nanoparticles: preparation,physicochemical characterization and in vitro anti-tumoral activity, Journal of Controlled Release: 83; 273–286, (2002).

Ho-Young Hwang , In-San Kim , Ick Chan Kwon , Yong-Hee Kim;Tumor targetability and antitumor effect of docetaxel-loaded hydrophobically modified glycol chitosan nanoparticles, Journal of Controlled Release;128: 23–31, (2008).

G. Arican, E. Arican;Evaluation Of the Apoptotic AND Antiproliferative Activities Of Paclitaxel in Ehrlich Ascites Tumor Cells, Biotechnol. & Biotechnol. Eq, 69-75., (2006).

Minghuang Hong , Saijie Zhu , Yanyan Jiang , Guotao Tang , Chang Sun , Chao Fang , Bin Shi , Yuanying Pei ; Novel anti-tumor strategy: PEG-hydroxycamptothecin conjugate loaded transferrin-PEG-nanoparticles, Journal of Controlled Release;141: 22–29, (2010).


  • There are currently no refbacks.

Copyright (c)

               AR Journals

18K, Street 1st, Gaytri Vihar, Pinto Park, Gwalior, M.P. India (Design) 2009-2021


Follow @arjournals on Twitter