Schäfer H, Schmidt W, Lachmann U, Bienert M
Pharmazie. 1984 Nov;39(11):765-9.
Binding of the undecapeptide substance P to unilamellar and multilamellar lipid vesicles, made from mixtures of phosphatidylcholine and phosphatidic acid, was investigated, because liposomes may be supposed to become a useful pharmaceutical tool for the delivery of low molecular mass peptide hormones. It is demonstrated that binding is largely electrostatic in nature, and that the amount of bound peptide may be varied within rather broad limits by changing the lipid matrix and/or the aqueous medium conditions. Concerning the distribution of the peptide between inner and outer surfaces of the liposomes, large differences may be realised too, as revealed by enzymatic hydrolysis of the outside bound portions of substance P. But additionally, electrostatic binding is demonstrated also to bring about peculiar, unexpected properties of the system. These imply special relevance to a potential pharmaceutical application of substance P liposomes as well as some general relevance to in vivo application of liposomes as drug carriers.
研究了由磷脂酰胆碱和磷脂酸混合物制成的单层和多层脂质体与十一肽P物质的结合情况，因为脂质体可能会成为一种用于递送低分子量肽类激素的有用药物工具。结果表明，这种结合在很大程度上是静电性质的，并且通过改变脂质基质和/或水性介质条件，结合肽的量可以在相当宽的范围内变化。关于肽在脂质体内外表面之间的分布，通过对P物质外表面结合部分的酶促水解发现，也可能实现很大差异。此外，静电结合还被证明会导致该系统具有特殊的、意想不到的性质。这些性质意味着P物质脂质体在潜在药物应用方面具有特殊意义，同时也与脂质体作为药物载体的体内应用具有一定的普遍相关性。
