Surface Modified Nanomaterials for Improving Solubility and Dissolution

Abstract

The objective of present study was to explore the application of nano crystals technology to improve the solubility and dissolution of poorly soluble drugs. Two drugs were selected for the project from synthetic as well as natural origin in order to check the versatility of application of nano crystals technology in solubility enhancement. Ball milling method was used for the preparation of nano crystals because of already proven scalability and ease in manufacturing of nano crystals. Preliminary trials in both the drugs were based on the selection of suitable stabilizer. Selection of critical process parameters as well as their optimization was done using Design of Experiment (DoE) approach. Particle size (D50 and D90) and the size distribution (SPAN) were taken as responses for the evaluation of design batches and were used as the criteria for selection of optimized batch. Optimized formulation were further characterized using SEM, XRD and DSC, depicted reduction in crystallinity of the developed nano crystals for both the drugs which resulted in their increase in solubility as well as dissolution. In vivo bio availability was performed in rat model, in case of Febuxostat nanocrystals, and was found significantly increased as compared to pure Febuxostat. While, optimized formulation of lutein was further evaluated for its anti proliferative as well as antioxidant activity in MCF7 breast cancer cell line and found higher activity as compared to lutein solution. Thus, developed nano crystals of both the drugs shows the potential of nano crystal technology in solubility and dissolution enhancement.