INVESTIGATION OF EFFECT OF PHOSPHOLIPIDS ON PHYSICAL AND FUNCTIONAL CHARACTERIZATION OF PACLITAXEL LIPOSOMES
DOI:
https://doi.org/10.22159/ijpps.2017v9i12.20749Keywords:
Liposomes, Phospholipon, Entrapment efficiency, In vitro release, Hemolytic toxicityAbstract
Objective: Aim of the present investigation was to determine the effect of various synthetic grades of phospholipids on paclitaxel liposomes (PTL).
Methods: The PTL formulations using various grades of phospholipids were prepared by film hydration method. The prepared PTL formulations were physicochemically characterized by entrapment efficiency (EE, %w/w), vesicular size and particle size distribution. These formulations were also characterized for function parameters such as in vitro release and hemolytic toxicity assay.
Results: The synthetic grades of phospholipids significantly influenced PTL formulations. The stoichiometric ratio (1:1) between CH and various synthetic phospholipids was found to be optimized one, from rest of the ratios. The characterization confirmed the formation of PTL. The EE was observed to be high (86.67%) as increasing the ratios between CH and phospholipids but then declined suddenly as further increasing the ratio. The best liposomal formulations showed that the spherical shape was found to be within size ranging from<10 µm, with a higher rate and extent of the release, ~86.22% of paclitaxel from PTL formulation. The results of the hemolytic toxicity study demonstrated that PTL formulations with a ratio (1:1) exhibited a significantly lower hemolytic toxicity (2.70%), compared to all formulations.
Conclusion: The result revealed the excellent effect of phospholipids on paclitaxel liposomes. The paclitaxel liposomes prepared with CH: PL90G ratio (1:1) was found to be optimized one. The entrapment efficiency, particle size distribution, in vitro release and hemolytic activity with this ratio shown to be excellent as compared to other ratios.
Downloads
References
Brasili E, Filho VC. Metabolomics of cancer cell cultures to assess the effects of dietary phytochemicals. Crit Rev Food Sci Nutr 2017;57:1328-39.
Hanahan D, Weinberg RA. Hallmarks of cancer: the next generation. Cell 2011;144:646-74.
Cairns RA, Mak TW. The current state of cancer metabolism. Nat Rev Cancer 2016;16:613-4.
Liu QS, Deng R, Yan QF, Cheng L, Luo Y, Li K, et al. Novel beta-tubulin-immobilized nanoparticles affinity material for screening β-tubulin inhibitors from a complex mixture. ACS Appl Mater Interfaces 2017;9:5725-32.
Louage B, De Wever O, Hennink WE, De Geest BG. Developments and future clinical outlook of taxane nanomedicines. J. Controlled Release 2017;253:137-52.
Schiff PB, Horwitz SB. Taxol stabilize microtubules in mouse fibroblast cells. Proc Natl Acad Sci USA 1980;77:1561-5.
Ye J, Liu Y, Xia X, Meng L, Dong W, Wang R, et al. Improved safety and efficacy of a lipid emulsion loaded with a paclitaxel-cholesterol complex for the treatment of breast tumors. Oncol Rep 2016;36:399-409.
Kampan NC, Madondo MT, McNally OM, Quinn M, Plebanski M. Paclitaxel and its evolving role in the management of ovarian cancer. BioMed Res Int 2015;2015:1-21. http://dx.doi.org/10.1155/2015/413076
Wang L, Yu RS, Yang WL, Luan SJ, Qin BK, Pang XB, et al. Effects of paclitaxel loaded-drug micelles on cell proliferation and apoptosis of human lung cancer A549 cells. Acta Pharm Sin 2015;50:1240-5.
Lemstrova R, Melichar B, Mohelnikova-Duchonova B. Therapeutic potential of taxanes in the treatment of metastatic pancreatic cancer. Cancer Chemother Pharmacol 2016;78:1101-11.
Mullins DW, Burger CJ, Elgert KD. Paclitaxel enhances macrophage IL-12 production in tumor-bearing hosts through nitric oxide. J Immunol 1999;162:6811-8.
Glass-Marmor L, Beitner R. Taxol (paclitaxel) induces a detachment of phosphofructokinase from cytoskeleton of melanoma cells and decreases the levels of glucose 1, 6-bisphosphate, fructose 1, 6-bisphosphate and ATP. Eur J Pharmacol 1999;370:195-9.
Thanki K, Gangwal RP, Sangamwar AT, Jain S. Oral delivery of anticancer drugs: challenges and opportunities. J Controlled Release 2013;170:15-40.
Backman JT, Filppula AM, Niemi M, Neuvonen PJ. Role of cytochrome P450 2C8 in drug metabolism and interactions. Pharmacol Rev 2016;68:168-241.
Li J, Tang J, Li Y, Yu J, Zhang B, Yu C. Pharmacokinetic profile of paclitaxel in the plasma, lung, and diaphragm following intravenous or intrapleural administration in rats. Thorac Cancer 2015;6:43-8.
Webster LK, Woodcock DM, Rischin D, Millward MJ. Review: cremophor: pharmacological activity of an" inert" solubiliser. J Oncol Pharm Pract 1997;3:186-92.
Cragun JM, Baggs JH, Rollins C, Chambers SK. Case report hypersensitivity reaction to parenteral nutrition after severe hypersensitivity reaction to paclitaxel. Am J Clin Exp Obstet Gynecol 2013;1:69-75.
Singla AK, Garg A, Aggarwal D. Paclitaxel and its formulations. Int J Pharm 2002;235:179-92.
Moes J, Koolen S, Huitema A, Schellens J, Beijnen J, Nuijen B. Development of an oral solid dispersion formulation for use in low-dose metronomic chemotherapy of paclitaxel. Eur J Pharm Biopharm 2013;83:87-94.
Sandhu PS, Beg S, Mehta F, Singh B, Trivedi P. Novel dietary lipid-based self-nanoemulsifying drug delivery systems of paclitaxel with p-gp inhibitor: implications on cytotoxicity and biopharmaceutical performance. Expert Opin Drug Delivery 2015;12:1809-22.
Li J, Wang F, Sun D, Wang R. A review of the ligands and related targeting strategies for active targeting of paclitaxel to tumours. J Drug Target 2016;24:590-602.
Xu J, Zhang X, Chen Y, Huang Y, Wang P, Wei Y, et al. Improved micellar formulation for enhanced delivery for paclitaxel. Mol Pharm 2016;14:31-41.
Bonde S, Nair S. Advances in liposomal drug delivery system: fascinating types and potential applications. Int J Appl Pharm 2017;9:1-7.
Li J, Huang P, Chang L, Long X, Dong A, Liu J, et al. Tumor targeting and pH-responsive polyelectrolyte complex nanoparticles based on hyaluronic acid-paclitaxel conjugates and chitosan for oral delivery of paclitaxel. Macromol Res 2013;21:1331-7.
Teow HM, Zhou Z, Najlah M, Yusof SR, Abbott NJ, D’Emanuele A. Delivery of paclitaxel across cellular barriers using a dendrimer-based nanocarrier. Int J Pharm 2013;441:701-11.
Al-Najjar BY, Hussain SA. Chitosan microspheres for the delivery of chemotherapeutic agents: paclitaxel as a model. Asian J Pharm Clin Res 2017;10:1-5.
Kulkarni PR, Yadav JD, Vaidya KA. Liposomes: a novel drug delivery system. Int J Curr Pharm Res 2011;3:10-8.
Zhang W, Wang G, Falconer JR, Baguley BC, Shaw JP, Liu J, et al. Strategies to maximize liposomal drug loading for a poorly water-soluble anticancer drug. Pharm Res 2015;32:1451-61.
Zhang H, Gong W, Wang ZY, Yuan SJ, Xie XY, Yang YF, et al. Preparation, characterization, and pharmacodynamics of thermosensitive liposomes containing docetaxel. J Pharm Sci 2014;103:2177-83.
Bhatia A, Singh B, Raza K, Shukla A, Amarji B, Katare OP. Tamoxifen-loaded novel liposomal formulations: evaluation of anticancer activity on DMBA-TPA induced mouse skin carcinogenesis. J Drug Target 2012;20:544-50.
Parikh RS, Patel BK. Formulation development and evaluation of temozolomide loaded hydrogenated soya phosphatidyl-choline liposomes for the treatment of brain cancer. Asian J Pharm Clin Res 2016;9:340-3.
Dua JS, Rana AC, Bhandari AK. Liposome: methods of preparation and applications. Int J Pharm Stud Res 2012; 3:14-20.
Yang T, Cui FD, Choi MK, Lin H, Chung SJ, Shim CK, et al. Liposome formulation of paclitaxel with enhanced solubility and stability. Drug Delivery 2007;14:301-8.
Utreja P, Jain S, Tiwary AK. Localized delivery of paclitaxel using elastic liposomes: Formulation development and evaluation. Drug Delivery 2011;18:367-76.
Reed KW, Yalkowsky SH. Lysis of human red blood cells in the presence of various cosolvents. II. The effect of differing NaCI concentrations. PDA J Pharm Sci Technol 1986;40:88-94.
Kan P, Tsao CW, Wang AJ, Su WC, Liang HF. A liposomal formulation able to incorporate a high content of Paclitaxel and exert promising anticancer effect. J Drug Delivery 2010:1-9. http://dx.doi.org/10.1155/2011/629234
Nava G, Pinon E, Mendoza L, Mendoza N, Quintanar D, Ganem A. Formulation and in vitro, ex vivo and in vivo evaluation of elastic liposomes for transdermal delivery of ketorolac tromethamine. Pharmaceutics 2011;3:954-70.
Shanmugam S, Park JH, Chi SC, Yong CS, Choi HG, Woo JS. Physicochemical stability, pharmacokinetic, and biodistribution evaluation of paclitaxel solid dispersion prepared using supercritical antisolvent process. Drug Dev Ind Pharm 2011;37:628-37.
Published
How to Cite
Issue
Section
