Abstract
Objective: In current research, solid lipid nanoparticles (SLN) are formulated for the anticancer drug, nilotinib, to conquer the drawbacks associated with drug including low bioavailability and solubility. Methods: The formulation comprised of tripalmitin (lipid), poloxamer 188(surfactant) and glyceryl palmitostearate (cosurfactant) by solvent evaporation technique. The formulation and process variables of SLN were optimized by experimental design-Central composite design (CCD). The effect of drug to lipid ratio (A), concentration of Poloxamer 188 (B) and concentration of glyceryl palmitostearate(C), on particle size (Y1) and encapsulation efficiency (Y2) of SLN were evaluated. Three batches (F1-F3) of Nilotinib SLNs were formulated by desirability approach and evaluated. Results: The mean size of all the formulations ranged between 187–198 nm, PDI between 0. 291-0.652 and zeta potential between-21.8 to to-24.7 mV indicating the wide range of size distribution and stabiliity of the formulations. The total encapsulation efficiency of SLNs ranged between 85 to 86 %. The SEM analysis revealed the spherical shape of individual particles and PXRD results indicate amorphization of drug in SLN formulation. The drug release was continued for 24 h, indicative of controlled release drug delivery. Conclusion: From the above results it is concluded that the solubility and bioavailability of nilotinib is enhanced.
Highlights
The drug nilotinib is second-generation kinase inhibitor for chronic inflammatory diseases Leukemia, caused by the breakpoint cluster region of Abelson murine leukemia (BCR-ABL) gene
The results indicate that the dependent variables are sturdily dependent on chosen independent variables, as shown in all 20 batches
In the statistical analysis generated for particle size (PLS) (Y1), it was determined that the model is significant with an F-value of 810324(table 3)
Summary
The drug nilotinib is second-generation kinase inhibitor for chronic inflammatory diseases Leukemia, caused by the breakpoint cluster region of Abelson murine leukemia (BCR-ABL) gene. It inhibits tyrosine kinase activity of the BCR-ABL protein [1]. The deprived solubility of drug results in lower oral absorption [2, 3]. Nilotinib's solubility limits its therapeutic efficacy partly, due to the limited exposure it gives to the drug. Increasing interest in lipid-based pharmaceutical delivery systems has come about because they have increased bioavailability [4]. Lipid-based formulations have emerged as an effective and versatile technology for many class IV BCS drugs [5, 6]. As an alternative to emulsions, SLNs contain solid lipids instead of liquid oils
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