Hansen Solubility Parameter Approach in the Screening of Lipid Excipients for the Development of Lipid Nano Carriers

Background

The complex physicochemical properties of the lipids have considerable impact on the solubility and stability of the Lipid Based Nanocarriers (LBN). The major challenge in the successful development of LBN lies on the selection of suitable lipid and its ability to achieve high drug payloads. The wet lab screening of lipids is time consuming and economically not viable. Therefore, the present research aims to apply Hansen solubility parameters to predict the solubility/miscibility of 5-Fluorouracil (5FU) and curcumin in various lipids.

Materials and Methods

The apparent solubility of 5FU and curcumin in various lipids were determined by shake flask method. Theoretical predictions of Hansen Solubility Parameter (HSP) for lipids and actives were done by group contribution method proposed by van Krevelen. The various molecular descriptors of 5FU, curcumin and the range of lipids are obtained from Qikprop predictions, version 4.4, Schrodinger.

Results

Lipids exhibit low dispersion force component (δD) than 5FU and curcumin indicating that they are poor solvents; rather the polar and hydrogen bonding components might have contributed to the solubility of the actives in lipids. Hence, the actives are more soluble in those lipids with free -OH groups as in case of Maisine CC, Labrafac PG and Compritol 888 ATO which is in good correlation with the experimental values.

Conclusion

The HSP sphere radius provides an insight to screen the excipients prior to wet lab experiments. Thus, the HSP approach can be utilized as a promising tool in the preliminary screening of lipid excipients in the development of lipid nanoparticles.