Abstract
Objective: The current paper represents the development, optimization, and characterization of paclitaxel-loaded folate conjugated solid lipid nanoparticles (FA-SLNs).
Methods: The ligand (FA-SLNs) conjugated and non-conjugated SLNs (PTX-SLNs) were prepared by the hot homogenization method. The formulations (FA-SLNs and PTX-SLNs) were optimized with various parameters, i.e., drug loading, stirring time, stirring speed, particle size, and polydispersity index, and characterized. The in-vitro drug release study was performed in different pH environments by using the dialysis bag method. The surface morphology and particle size were determined through scanning electron microscopy and Transmission Electron Microscopy respectively. The SLNs formulations were also evaluated for the stability study.
Result: The particle size of PTX-SLNs and FA-SLNs was determined and found to be 190.1±1.9 and 231.3±2.3 nm, respectively. The surface morphology of the SLNs indicates that the prepared formulations are round-shaped and show smooth surfaces. The TEM study indicated that particles were in the range of 100-300 nm. The entrapment efficiency and drug loading capacity of FASLNs were found to be 79.42±1.6% and 17.3±1.9%, respectively. In-vitro drug release study data stated that the optimum drug release was found in an acidic environment at pH 4.0, that showed 94.21% drug release after 16 hours, and it demonstrates that FA-SLNs with an optimized formulation will provide a more sustained and effective release in tumor tissue that is exposed to an acidic environment as a result of the angiogenesis process.
Conclusion: In this research paper, different formulation parameters, found to influence the fabrication of drugs into Solid lipid nanoparticles, were optimized for high entrapment efficiency and drug loading. The most important parameters were drug:lipid ratio, drug: polymer ratio, and lipid:- surfactant ratio. Higher in-vitro drug release was observed in pH 4 as compared to pH 7.4. These result data concludes that FA-SLNs formulation was successfully prepared, optimized, and characterized.
Keywords: Solid lipid nanoparticles, folate, particle size, drug loading, paclitaxel, drug release.
Graphical Abstract
[http://dx.doi.org/10.1016/S0169-409X(02)00044-3]
[http://dx.doi.org/10.2174/156720107781023910] [PMID: 17627495]
[http://dx.doi.org/10.1073/pnas.0914585107] [PMID: 20133865]
[http://dx.doi.org/10.3402/nano.v3i0.18496] [PMID: 23240070]
[http://dx.doi.org/10.1016/j.ejpb.2014.05.004] [PMID: 24833004]
[PMID: 23444780]
[http://dx.doi.org/10.1016/j.jconrel.2010.09.003] [PMID: 20854859]
[http://dx.doi.org/10.1002/jps.22285] [PMID: 20740670]
[http://dx.doi.org/10.1016/j.ijpharm.2007.07.012] [PMID: 17714896]
[http://dx.doi.org/10.1016/j.ejps.2012.10.025] [PMID: 23178339]
[http://dx.doi.org/10.1002/jps.23758] [PMID: 24166599]
[http://dx.doi.org/10.3109/03639045.2014.891130] [PMID: 24564799]
[http://dx.doi.org/10.1002/jps.23522] [PMID: 23558514]
[http://dx.doi.org/10.1080/10611860902737938] [PMID: 19255897]
[http://dx.doi.org/10.2967/jnumed.110.076018] [PMID: 21149477]
[http://dx.doi.org/10.1016/j.ejps.2013.10.003] [PMID: 24514450]
[http://dx.doi.org/10.3390/cancers2041911] [PMID: 24281209]
[http://dx.doi.org/10.1080/10717540903047387] [PMID: 19606948]
[http://dx.doi.org/10.3109/03639045.2013.850705] [PMID: 24164469]
[http://dx.doi.org/10.1016/j.ijpharm.2015.07.012] [PMID: 26165611]
[http://dx.doi.org/10.1016/j.jcis.2017.01.092] [PMID: 28236692]
[http://dx.doi.org/10.1007/s12272-011-0220-2] [PMID: 21380818]
[http://dx.doi.org/10.1080/02652040701799598] [PMID: 18608808]
[http://dx.doi.org/10.3109/03639040903244472] [PMID: 19824865]
[http://dx.doi.org/10.4172/2157-7439.1000328]
[http://dx.doi.org/10.1016/0003-2697(78)90172-0] [PMID: 727510]