Microparticles (MPs) have great potentiality in material science- based applications. Their use in biology is however limited to clinics and has rarely been exploited in the pharmaceutical context. Unlike nanoparticles (NPs), they are amenable to routine detection by flow cytometry and confocal microscopy. Though MPs can constitute a wide variety of materials, including ceramics, glass, polymers, and metals and can be synthesized by chemical process but wet processes for the preparation of microparticles have rarely been attemped. In this paper, a thrombotic route is shown to successfully generate biocompatible MP of a model anticancer drug (doxorubicin hydrochloride). Synthesis of MPs from platelets and drug loading in to these MPs was confirmed by flow cytometry and confocal microscopy. Human cervical cancer cell line (HeLa) was treated with these drug-loaded MPs to investigate whether the loaded MPs have the capacity to deliver drug to the cancer cells. In addition, Magnetic force microscopy was used to detect the preparation of MPs loaded with magnetic NPs. The efficiency of the drug-loaded MPs in inducing cytotoxicity in cancer cell line, shown to be significantly higher than the free drug itself. The drug-loaded MP is shown to have a much higher cytotoxic propensity than the free drug applied at comparable doses. The thrombotic approach can also be applied to synthesize MP containing NPs which in turn can lead to generate a wide variety of new biocompatible materials. © 2015 The Authors. Pharmacology Research & Perspectives published by British Pharmacological Society and American Society for Pharmacology and Experimental Therapeutics and John Wiley & Sons Ltd.