Surface Modified Nanomaterials for improving Solubility and Dissolution

Abstract

The objective of present study was to explore the application of nanocrystals 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 nanocrystals technology in solubility enhancement. Ball milling method was used for the preparation of nanocrystals because of already proven scalability and ease in manufacturing of nanocrystals. 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 nanocrystals for both the drugs which resulted in their increase in solubility as well as dissolution. In vivo bioavailability 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 antiproliferative as well as antioxidant activity in MCF7 breast cancer cell line and found higher activity as compared to lutein solution. Thus, developed nanocrystals of both the drugs shows the potential of nanocrystal technology in solubility and dissolution enhancement. newline newline