ABSTRACT

In the present investigation, an attempt was made to design and formulate solid lipid nanoparticles of the anticancer drug, ibrutinib, to increase their bioavailability and overcome the challenges associated with the drug. To optimize the formulation variables and process variables of these SLNs, a statistically experimental design methodology was employed properly. After selecting the critical variables affecting particle size, encapsulation efficiency, and drug loading, the response surface methodology (RSM), followed by central composite design (CCD) was employed to optimize the level of these variables. From the preliminary studies, it was found that the drug to lipid ratio (A), concentration of Poloxamer 188 (B) and concentration of soya lecithin (C), had a significant effect on the particle size (Y1) and encapsulation efficiency(Y2) of SLNs.About 20 experimental runs carried out to evaluate the effect of factors on variables chosen. The optimized levels and predicted values of Y1, and Y2 were obtained by utilizing the design software. The optimised formulation as observed at 0.23:56.37:60 ratio (A:B:C) whose particle size and encapsulation efficiency ranged between 125.42-127.74 nm and 79.12 to 80.23 mV. The PDI was ranging from 0.291 to 0.652 and zeta potential between -21.7 ± 1.22 mV to -25.3 ± 1.78 mV. The optimized formulation was evaluated for various parameters like particle size analysis, polydispersity index, zeta potential, encapsulation efficiency, drug loading capacity, SEM analysis. The results indicate spherical shape of individual particles, confirming amorphisation of drug. The dissolution studies indicated maximum release of 95% within 24h. The optimized formulation found stable for 90 days. Keywords: Ibrutinib, B cell cancers, Central composite design (CCD), Solid lipid nanoparticles (SLN), Particle size, Encapsulation efficiency
Publication date: 25/09/2021

https://ijbpas.com/pdf/2021/September/MS_IJBPAS_2021_SEPT_SPCL_1056.pdf

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https://doi.org/10.31032/IJBPAS/2021/10.9.1056