Development and evaluation of lipid nanoparticles for camptothecin delivery: a comparison of solid lipid nanoparticles, nanostructured lipid carriers, and lipid emulsion

Abstract

Aim: Camptothecin is an anticancer drug that acts against a broad spectrum of tumors. The clinical application of camptothecin is limited by its insolubility, instability, and toxicity problems. The aim of this study was to develop and characterize lipid nanoparticles with different lipid cores which can circumvent these problems. Methods: Lipid nanoparticles made of Precirol (solid lipid nanoparticles; SLN-P), Compritol (SLN-C), Precirol+squalene (nanostructured lipid carriers; NLC), and squalene (a lipid emulsion; LE) as the lipid core material were prepared. These systems were assessed and compared by evaluating the mean diameter, surface charge, molecular environment, camptothecin release, and cell viability against a melanoma. The safety and storage stability of these systems were also preliminarily examined. Results: The particle size ranged from 190 to 310 nm, with the NLC and LE showing the smallest and largest sizes, respectively. The in vitro drug release occurred in a sustained manner in decreasing order as follows: LE>NLC>SLN-P>SLN-C. It was found that varying the type of inner phase had profound effects on cell viability. The SLN-P generally showed higher cytotoxicity than the free control. The treatment of melanomas with the camptothecin-loaded SLN-C and NLC yielded cytotoxicity comparable to that of the free form. The percentage of erythrocyte hemolysis by all nanoparticles was ≤5%, suggesting a good tolerance to lipid nanoparticles. Conclusion: The results collectively suggest that the SLN-P may have the potential to serve as a delivery system for parenteral camptothecin administration because of the sustained drug release, strong cytotoxicity, limited hemolysis, and good storage stability. Key wordscamptothecin; solid lipid nanoparticle; nanostructured lipid carrier; lipid emulsion; drug delivery; melanoma 4 Correspondence to Prof Jia-you FANG.Phn 886-3-211-8800, ext 5521.

Formulation of a Novel Oxybenzone-Loaded Nanostructured Lipid Carriers (NLCs)

“…All NLCs were negatively charged. The negative charge was likely caused by the slightly ionized fatty acids from glycerides including the negatively charged miglyol 812 and oleic acid at their carboxylic groups (43). Values of zeta potential ranged from −10.6±0.3 mV for NLC8 using 30% oleic acid and 10% oxybenzone to −29.7± 1.8 mV for NLC5 using 15% oleic acid and 5% oxybenzone.…”

Follicular delivery of spironolactone via nanostructured lipid carriers for management of alopecia

“…30 As is presented in Table 4 and graphically illustrated in Figure 2D, increasing the liquid lipid (X 1 ) is associated with an increase in ZP, probably due to the increase in the number of ionized carboxylic groups of olive oil present at a higher oil concentration. 31 Conversely, the surfactant concentration has a significant negative effect on ZP as a result of shielding the surface charges of the nanoparticles by the nonionic surfactant molecules. The surfactant molecules decrease the electrostatic repulsion between the nanoparticles, but at the same time sterically stabilize them by forming a surfactant T r a n s c u to l ® c o n c e n tr a ti o n (% ) T r a n s c u to l ® c o n c e n tr a ti o n (% ) T r a n s c u to l ® c o n c e n tr a ti o n (% ) T r a n s c u to l ® c o n c e n tr a ti o n (% ) S u r f a c t a n t c o n c e n t r a t io n ( % ) coat layer.…”

Lipid-Based Drug Delivery Systems in Cancer Therapy: What Is Available and What Is Yet to Come

“…NLCs can be produced by several methods, most of which are adopted from polymeric nanoparticle preparations. These methods include high-pressure homogenization (Stecova et al, 2007;Huang et al, 2008;Ruktanonchai et al, 2009); microemulsion (Doktorovova et al, 2010;Souza et al, 2011); phase inversion (Souto et al, 2007); emulsification by sonication (Das and Chaudhury, 2011); emulsification-solvent-evaporation (ESE) (Lin et al, 2010); solvent diffusion and solvent injection/solvent displacement (Schubert and MullerGoymann, 2003); and the membrane contactor method (Charcosset et al, 2005). However, the most preferred method of NLC preparation is high-pressure homogenization (Iqbal et al, 2012).…”