Oral anticancer drugs have earned a seat at the table, as the need for homecare treatment in oncology has increased. Interest in this field is growing as a result of their proven efficacy, lower costs and positive patient uptake. However, the gastrointestinal barrier is still the main obstacle to surmount in chemotherapeutic oral delivery. Anticancer nanomedicines have been proposed to solve this quandary. Among these, lipid nanoparticles are described to be efficiently absorbed while protecting drugs from early degradation in hostile environments. Their intestinal lymphatic tropism or mucoadhesive/penetrative properties give them unique characteristics for oral administration. Considering that chronic cancer cases are increasing over time, it is important to be able to provide treatments with low toxicity and low prices. The challenges, opportunities and therapeutic perspectives of lipid nanoparticles in this area will be discussed in this review, taking into consideration the pre-clinical and clinical progress made in the last decade.