In the last decade, medication research and delivery have emerged as a rapidly developing, demanding, and capital-intensive manufacturing sector. This is a time-consuming and costly technique that faces the challenges of low bioavailability, toxicity, low efficacy, biocompatibility, adverse effects, rapid excretion, and degradability. Biocompatible nanomaterials with outstanding qualities such as a high invasion rate, gradual, controlled and targeted drug release, and ease of access to receptors overcome all of these issues and outperform traditional drug formulations. Despite its significance, the toxicity of many nanoparticles used as medication delivery systems remains a big worry. This review discusses the difficulty of conventional drugs, the significance of nanoparticles in medication delivery, and their hazardous effects.