Mesoporous silica materials: From physico-chemical properties to enhanced dissolution of poorly water-soluble drugs

New approaches in pharmaceutical chemistry have resulted in more complex drug molecules in the quest to achieve higher affinity to their targets. However, these ‘highly active’ drugs can also suffer from poor water solubility. Hence, poorly water soluble drugs became a major challenge in drug formulation, and this problem is increasing, as currently about 40 of the marketed drugs and 90% of drug candidates are classified as poorly water soluble. Various approaches exist to circumvent poor water solubility and poor dissolution rate in aqueous environment, however, each having disadvantages and certain limitations.

Recently, mesoporous silica materials (MSMs) have been proposed to be used as matrices for enhancing the apparent solubility and dissolution rate of different drug molecules. MSMs are ideal candidates for this purpose, as silica is a “generally regarded as safe” (GRAS) material, is biodegradable, and can be readily surface-modified in order to optimize drug loading and subsequent release in the human body. The major advantage of mesoporous silica as drug delivery systems (DDSs) for poorly water soluble drugs lies in their pore size, pore morphology, and versatility in alteration of the surface groups, which can result in optimized interactions between a drug candidate and MSM carrier by modifying the pore surfaces. Furthermore, the drug of interest can be loaded into these pores in a preferably amorphous state, which can increase the drug dissolution properties dramatically.

The highlights of this review include a critical discussion about the modification of the physico-chemical properties of MSMs and how these physico-chemical modifications influence the drug loading and the subsequent dissolution of poorly water soluble drugs. It aims to further promote the use of MSMs as alternative strategy to common methods like solubility enhancement by cyclodextrins, micronization, or microemulsion techniques. This review can provide guidance on how to tailor MSMs to achieve optimized drug loading and drug dissolution.