Abstract
This work was focused on identification and evaluation of process parameters of modified nanoprecipitation method, for fabrication of lomustine nanoparticles, with the aim of reducing cancer cell viability at low concentration of lomustine. The parameters controlling particle size, mostly in nanosize, were solvent/nonsolvent composition and emulsification speed of homogenizer along with aqueous phase volume. This controlled particle size is below 250 nm. The stabilizer concentration controlled particle size is within 68 nm ± 0.89 to 137 ± 0.94 nm with PDI 0.06 ± 0.008 to 0.25 ± 0.001. But, the stabilizer addition mode showed more uniform size distribution with PDI 0.085 ± 0.004. Entrapment efficiency was maintained well above 47 ± 0.23%. The drug release pattern was monophasic with controlled release over 24 hrs. In the method used, drug content was affected by ratio of polymer to drug to organic solvent, as well as homogenization speed and time. Percentage viable cells of L132 human lung cancer cell line remained, were only 5% at 100 μg/ml lomustine equivalent PLA nanoparticles.
Highlights
Biocompatible nanoparticles as drug delivery vehicles provide several advantages, including protection of the encapsulated pharmaceutical substance, improved efficacy, fewer adverse effects, controlled release and drug targeting [1]
In the nanoparticle formulation, particular interest has been focused on the use of polyesters materials such as poly (d,l-lactide) (PLA) and poly(d,llactide-co-glycolide) (PLGA), which undergo scission in the body to monomeric units of lactic acid, as a natural intermediate in carbohydrate metabolism
The degradation rate is dependent on several parameters, such as crystallinity, MW environment and particle morphology [2,3]
Summary
Biocompatible nanoparticles as drug delivery vehicles provide several advantages, including protection of the encapsulated pharmaceutical substance, improved efficacy, fewer adverse effects, controlled release and drug targeting [1]. At neutral pH (in vitro liquid environment without enzymes), PLA nanoparticles remain relatively stable over tens of days [3]. Owing to their biocompatibility and biodegradability properties, nanoparticles of these polymers are investigated for wide applications, using several preparation procedures. Particle formation is spontaneous, because the polymer precipitates in the aqueous environment. The Marangoni effect is considered to explain the process [7]: solvent flow, diffusion and surface tension at the interface of the organic solvent and the aqueous phase cause turbulences, which form small droplets containing the polymer. The size of the nanoparticles prepared by nanoprecipitation varies typically from 100 to 500 nm
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
