Disclosed herein is a method for inhibiting expression of a gene of a subject comprising administering (1) a composition comprising R-(L)a-(G)b； wherein R is an oligonucleotide selected from the group consisting of DNA, RNA, siRNA, and microRNA； L is a linker and each occurrence of L is independently selected from Table 3； G is a targeting ligand and each occurrence of G is independently selected from Table 4； each of a and b is independently 0, 1, 2, 3 or 4； and (2) a composition comprising (P)c-(L)d-(G)e； wherein P is a peptide and each occurrence of P is independently selected from Table 2； L is a linker and each occurrence of L is independently selected from Table 3； G is a targeting ligand and each occurrence of G is independently selected from Table 4； d is 0, 1, 2, 3, 4, 5 or 6； and each of c and e is independently 1, 2, 3, 4, 5 or 6. Compositions in (1) and (2) can be co-administered or sequentially administered.
