Yemul S, Berger C, Estabrook A, Suarez S, Edelson R, Bayley H
Proc Natl Acad Sci U S A. 1987 Jan;84(1):246-50. doi: 10.1073/pnas.84.1.246.
Two-fold specificity in drug delivery obtained through the localized activation of drugs by physical means and the attachment of drugs to proteins that bind to target cells might be used for highly selective cancer chemotherapy or for immunosuppression. Toward this end, a monoclonal antibody against an antigen on the surface of T lymphocytes was covalently attached to liposomes containing a phototoxic drug, pyrene, bound to the lipid bilayer. When unfractionated peripheral blood lymphocytes, or B- and T-cell lines, were irradiated after treatment with these liposomes, T cells were killed while B cells were spared, demonstrating the validity of the approach in a simple in vitro assay.
通过物理手段对药物进行局部激活以及将药物附着于与靶细胞结合的蛋白质上所实现的双重药物递送特异性,可用于高度选择性的癌症化疗或免疫抑制。为此,将一种针对T淋巴细胞表面抗原的单克隆抗体共价连接到含有与脂质双层结合的光毒性药物芘的脂质体上。在用这些脂质体处理后对未分级的外周血淋巴细胞或B细胞和T细胞系进行照射时,T细胞被杀死而B细胞得以存活,这在简单的体外试验中证明了该方法的有效性。