The treatment and management of tuberculosis using conventional drug delivery systems remain challenging due to the setbacks involved. The lengthy and costly treatment regime and patients' non-compliance have led to drug-resistant tuberculosis, which is more difficult to treat. Also, anti-tubercular drugs currently used are poor water-soluble drugs with low bioavailability and poor therapeutic efficiency except at higher doses which causes drug-related toxicity. Novel drug delivery carrier systems such as mesoporous silica nanoparticles (MSNs) have been identified as nanomedicines capable of addressing the challenges mentioned due to their biocompatibility. The review discusses the sol–gel synthesis and chemistry of MSNs as porous drug nanocarriers, surface functionalization techniques and the influence of their physico-chemical properties on drug solubility, loading and release kinetics. It outlines the physico-chemical characteristics of MSNs encapsulated with anti-tubercular drugs.