Generic placeholder image

Current Nanomedicine

Editor-in-Chief

ISSN (Print): 2468-1873
ISSN (Online): 2468-1881

Research Article

Development and In Vitro Characterization of Paclitaxel Loaded Solid Lipid Nanoparticles

Author(s): R. Nithya, K. Siram, R. Hariprasad and H. Rahman*

Volume 9, Issue 1, 2019

Page: [76 - 85] Pages: 10

DOI: 10.2174/2405461503666180518093824

Price: $65

conference banner
Abstract

Background: Paclitaxel (PTX) is a potent anticancer drug which is highly effective against several cancers. Solid lipid nanoparticles (SLNs) loaded with anticancer drugs can enhance its toxicity against tumor cells at low concentrations.

Objective: To develop and characterize SLNs of PTX (PSLN) to enhance its toxicity against cancerous cells.

Method: The solubility of PTX was screened in various lipids. Solid lipid nanoparticles of PTX (PSLN) were developed by hot homogenization method using Cutina HR and Gelucire 44/14 as lipid carriers and Solutol HS 15 as a surfactant. PSLNs were characterized for size, morphology, zeta potential, entrapment efficiency, physical state of the drug and in vitro release profile in 7.4 pH phosphate buffer saline (PBS). The ability of PTX to enhance toxicity towards cancerous cells was tested by performing cytoxicity assay in MCF7 cell line.

Results: Solubility studies of PTX in lipids indicated better solubility when Cutina HR and Gelucire 44/14 were used. PSLNs were found to possess a neutral zeta potential with a size range of 155.4 ± 10.7 nm to 641.9 ± 4.2 nm. In vitro release studies showed a sustained release profile for PSLN over a period of 48 hours. SLNs loaded with PTX were found to be more toxic in killing MCF7 cells at a lower concentration than the free PTX.

Keywords: Paclitaxel, solid lipid nanoparticles, cutina HR, gelucire 44/14, solutol HS 15, solubility.

Graphical Abstract
[1]
Kim MS, Haney MJ, Zhao Y, et al. Development of exosome-encapsulated paclitaxel to overcome MDR in cancer cells. Nanomed Nanotechnol Biol Med 2016; 12: 655-64.
[2]
Koziara JM, Whisman TR, Tseng MT, Mumper RJ. In-vivo efficacy of novel paclitaxel nanoparticles in paclitaxel-resistant human colorectal tumors. J Control Release 2006; 112: 312-9.
[3]
Wong HL, Bendayan R, Rauth AM, Li Y, Wu XY. Chemotherapy with anticancer drugs encapsulated in solid lipid nanoparticles. Adv Drug Deliv Rev 2007; 59: 491-504.
[4]
Sanna V, Pala N, Sechi M. Targeted therapy using nanotechnology: Focus on cancer. Int J Nanomed 2014; 9: 467-83.
[5]
Karthik S, Raghavan CV, Marslin G, et al. Quillaja saponin: A prospective emulsifier for the preparation of solid lipid nanoparticles. Colloid Surf B Biointerfaces 2016; 142: 274-80.
[6]
Marslin G, Revina AM, Khandelwal VKM, et al. Delivery as nanoparticles reduces imatinib mesylate-induced cardiotoxicity and improves anticancer activity. Int J Nanomed 2015; 10: 3163-70.
[7]
Jain S, Patel N, Shah MK, Khatri P, Vora N. Recent advances in lipid-based vesicles and particulate carriers for topical and transdermal application. J Pharm Sci 2017; 106: 423-45.
[8]
Müller RH, Petersen RD, Hommoss A, Pardeike J. Nanostructured Lipid Carriers (NLC) in cosmetic dermal products. Adv Drug Deliv Rev 2007; 59: 522-30.
[9]
Cai S, Yang Q, Bagby TR, Forrest ML. Lymphatic drug delivery using engineered liposomes and solid lipid nanoparticles. Adv Drug Deliv Rev 2011; 63: 901-8.
[10]
Geng Y, Discher DE. Hydrolytic degradation of poly(ethylene oxide)-block-polycaprolactone worm micelles. J Am Chem Soc 2005; 127: 12780-1.
[11]
Kamaly N, Xiao Z, Valencia PM, Radovic-Moreno AF, Farokhzad OC. Targeted polymeric therapeutic nanoparticles: design, development and clinical translation. Chem Soc Rev 2012; 41: 2971-3010.
[12]
Song Z, Feng R, Sun M, et al. Curcumin-loaded PLGA-PEG-PLGA triblock copolymeric micelles: Preparation, pharmacokinetics and distribution in vivo. J Colloid Interface Sci 2011; 354: 116-23.
[13]
Qin L, Zhang F, Lu X, et al. Polymeric micelles for enhanced lymphatic drug delivery to treat metastatic tumors. J Control Release 2013; 171: 133-42.
[14]
Pettenuzzo A, Pigot R, Ronconi L. Vitamin B12 -Metal conjugates for targeted chemotherapy and diagnosis: Current status and future prospects. Eur J Inorg Chem 2017; 2017: 1625-38.
[15]
Patel KK, Kumar P, Thakkar HP. Formulation of niosomal gel for enhanced transdermal lopinavir delivery and its comparative evaluation with ethosomal gel. AAPS PharmSciTech 2012; 13: 1502-10.
[16]
Abdelbary GA, Amin MM, Zakaria MY. Ocular ketoconazole-loaded proniosomal gels: formulation, ex vivo corneal permeation and in vivo studies. Drug Deliv 2017; 24: 309-19.
[17]
Ainbinder D, Paolino D, Fresta M, Touitou E. Drug delivery applications with ethosomes. J Biomed Nanotechnol 2010; 6: 558-68.
[18]
Shah MK, Madan P, Lin S. Preparation, in vitro evaluation and statistical optimization of carvedilol-loaded solid lipid nanoparticles for lymphatic absorption via oral administration. Pharm Dev Technol 2014; 19: 475-85.
[19]
Shah MK, Madan P, Lin S. Elucidation of intestinal absorption mechanism of carvedilol-loaded solid lipid nanoparticles using Caco-2 cell line as an in-vitro model. Pharm Dev Technol 2015; 0: 1-9.
[20]
Rohit B, Pal KI. A method to prepare solid lipid nanoparticles with improved entrapment efficiency of hydrophilic drugs. Curr Nanosci 2013; 9: 211-20.
[21]
Siram K, Chellan VR, Natarajan T, et al. Solid lipid nanoparticles of diethylcarbamazine citrate for enhanced delivery to the lymphatics: In vitro and in vivo evaluation. Expert Opin Drug Deliv 2014; 11: 1351-65.
[22]
Gaspar DP, Faria V, Gonçalves LMD, Taboada P, Remuñán-López C, Almeida AJ. Rifabutin-loaded solid lipid nanoparticles for inhaled antitubercular therapy: Physicochemical and in vitro studies 2016; 497: 199-209.
[23]
Dixit AR, Rajput SJ, Patel SG. Preparation and bioavailability assessment of SMEDDS containing valsartan. AAPS PharmSciTech 2010; 11: 314-21.
[24]
Karanam V, Marslin G, Krishnamoorthy B, et al. Poly (ε-caprolactone) nanoparticles of carboplatin: Preparation, characterization and in vitro cytotoxicity evaluation in U-87 MG cell lines. Colloids Surf B Biointerfaces 2015; 130: 48-52.
[25]
Ramalingam P, Ko YT. Improved oral delivery of resveratrol from N-trimethyl chitosan-g-palmitic acid surface-modified solid lipid nanoparticles. Colloids Surf B Biointerfaces 2016; 139: 52-61.
[26]
Chambin O, Jannin V. Interest of multifunctional lipid excipients: Case of Gelucire 44/14. Drug Dev Ind Pharm 2005; 31: 527-34.
[27]
Strickley RG. Solubilizing excipients in oral and injectable formulations. Pharm Res 2004; 21: 201-30.
[28]
Craparo EF, Pitarresi G, Bondi ML, Casaletto MP, Licciardi M, Giammona G. A nanoparticulate drug-delivery system for rivastigmine: Physico-chemical and in vitro biological characterization. Macromol Biosci 2008; 8: 247-59.
[29]
Akbari J, Saeedi M, Morteza-Semnani K, et al. The design of naproxen solid lipid nanoparticles to target skin layers. Colloids Surf B Biointerfaces 2016; 145: 626-33.

Rights & Permissions Print Cite
© 2024 Bentham Science Publishers | Privacy Policy