Dendrimers are versatile hyperbranched molecules, which have deserved attention especially for their potential in many applications, including biological. Peptide dendrimers comprise interesting classes of dendrimers, and their use has been emphasized as a drug/bioactive compound delivery system, mostly in the antineoplastic area. The bioactive molecules can be covalently linked or entrapped inside the peptide derivative. Self-assembled nanocarriers are a recent trend in the design of potential delivery systems, and pH-sensitive carriers, one of their methods, have been designed to control their systems. In addition, the use of targeting peptides or other specific groups that direct the drug/bioactive compounds to specific organs is an important trend in the search for better drug delivery systems. Recent examples have been given in the literature, showing that gene delivery as another important peptide dendrimer application. It is worth emphasizing that some peptide dendrimers show activity per se, without bioactive compounds. Immune compounds and vaccines are presented herein, as well as uses of other peptide dendrimers are briefly discussed in this review, which encompasses around 10 years of work.