The invention relates to methods of targeted drug delivery of antiviral compounds, including, chemical agents (like nucleoside analogs or protease inhibitors) and nucleic acid based drugs (like DNA vaccines, antisense oligonucleotides, ribozymes, catalytic DNA (DNAzymes) or RNA molecules, siRNAs or plasmids encoding thereof). Furthermore, the invention relates to targeted drug delivery of antiviral compounds to intracellular target sites within cells, tissues and organs, in particular to target sites within the central nervous system (CNS), into and across the blood-brain barrier, by targeting to internalizing uptake receptors present on these cells, tissues and organs. Thereto, the antiviral compounds, or the pharmaceutical acceptable carrier thereof, are conjugated to ligands that facilitate the specific binding to and internalization by these receptors.一種抗病毒化合物的目標藥物投遞方法，抗病毒化合物含化學藥劑(如核苷類似物或蛋白酶抑制劑)及核酸基藥物(如DNA疫苗、反義寡核苷酸、核糖核酸酶、催化性DNA(DNA酶)或RNA分子、siRNA或編碼其之質體)。一種將抗病毒化合物送入細胞、組織以及器官內的細胞內目標部位的目標藥物投遞，特別是將抗病毒化合物送入中樞神經系統內之目標部位以及藉由靶向上述細胞、組織及器官上的內化攝取受體使抗病毒化合物進入且穿透血腦障壁。將抗病毒化合物或其醫藥學上可接受之載體與配位體接合，配位體可與上述受體進行特異性結合且由受體進行內化。
