The positively-charged
peptide antp derived from Antennapedia transcription
protein is demonstrated to mediate the
liposome translocation across the cell membrane. In the current investigation, we prepared a stable
liposomal doxorubicin (Dox) formulation and targeted it with the antp
peptide from 0 to 200
ligand/
liposome. These antp-containing
liposomes were investigated in terms of physical stability on storage in the refrigerator and upon incubation in blood. Also, other features like cell binding, uptake, biodistribution, and treatment efficiency were evaluated in C26 colon
carcinoma BALB/c mice. The Antp in
liposomes resulted in enhanced particle growth with the development of the enormously large
liposomes from 2000 to 6000 nm. Upon incubation in blood, these large
liposomes were removed. The antp also enhanced the cell binding affinity and cell uptake rate of the
liposomes and resulted in the restriction of the
cancer cell proliferation, but it failed to improve the chemotherapeutic property of the Dox-
liposome. The i.v. injection of antp-
liposomes (15 mg Dox/kg) caused severe
body weight loss and early death incidence due to probably increased toxicity. The antp targeting offered no advantage to the Dox-
liposome in the delivery of Dox to the
tumor, and failed to enhance the treatment efficiency of the
liposomes.