Douglas S J, Davis S S, Illum L
Crit Rev Ther Drug Carrier Syst. 1987;3(3):233-61.
Alkylcyanoacrylates can be polymerized in acidified aqueous media by a process of anionic polymerization. The small particles produced tend to be monodisperse and have sizes in the range of 20 to 3000 nm depending upon the polymerization conditions and the presence of additives in the form of surfactants and other stabilizers. The polyalkylcyanoacrylate nanoparticles so produced have been studied in recent years as a possible means of targeting drugs to specific sites in the body, with particular emphasis in cancer chemotherapy. The small colloidal carriers are biodegradable and drug substances can be incorporated normally by a process of surface adsorption. The review by Davis and others considers the formulation of nanoparticles, the important physicochemical variables such as pH, monomer concentration, added stabilizers, ionic strengths, etc., as well as the characteristics of the particle so created in terms of surface charge, particle size, and molecular weight. Monodisperse particles in the range of 20 to 3000 nm can be obtained. In addition, by the use of stabilizers such as dextran and its derivatives, which can be incorporated into the nanoparticle surface by a process of polymer grafting, it is possible to make nanoparticles with interesting surface characteristics and different surface charges (sign). The stability of nanoparticles in vitro and their biodegradation in vivo are examined, and the possible formation of toxic products such as formaldehyde is highlighted. Alternative biodegradable acrylates are mentioned. Drugs can be incorporated into nanoparticles by either direct incorporation during the polymerization process or adsorption to preformed nanoparticles. The efficiency of the incorporation and the release characteristics of model compounds as well as anticancer drugs are discussed. Methods for examining these processes, including the determination of adsorption and desorption, kinetics, and isotherms, are mentioned. Selectivity in drug targeting can, in theory, be achieved by the attachment of some form of homing device, normally a monoclonal antibody or a lectin. Work in vitro and in vivo, where nanoparticles have been coated with monoclonal antibodies, is described. Finally, methods for the labeling of nanoparticles with gamma-emitting radionuclides are presented, and results obtained in animal species are given.
氰基丙烯酸烷基酯可通过阴离子聚合过程在酸化的水性介质中聚合。所产生的小颗粒往往是单分散的，其尺寸范围为20至3000纳米，这取决于聚合条件以及表面活性剂和其他稳定剂形式的添加剂的存在。近年来，如此制备的聚氰基丙烯酸烷基酯纳米颗粒已作为一种可能的将药物靶向体内特定部位的手段进行了研究，尤其在癌症化疗方面受到特别关注。这些小的胶体载体是可生物降解的，药物物质通常可通过表面吸附过程掺入其中。戴维斯等人的综述考虑了纳米颗粒的配方、重要的物理化学变量，如pH值、单体浓度、添加的稳定剂、离子强度等，以及所形成颗粒在表面电荷、粒径和分子量方面的特性。可获得20至3000纳米范围内的单分散颗粒。此外，通过使用诸如右旋糖酐及其衍生物之类的稳定剂，其可通过聚合物接枝过程掺入纳米颗粒表面，从而有可能制备出具有有趣表面特性和不同表面电荷（符号）的纳米颗粒。研究了纳米颗粒在体外的稳定性及其在体内的生物降解，并强调了可能形成的有毒产物如甲醛。提到了替代的可生物降解丙烯酸酯。药物可通过在聚合过程中直接掺入或吸附到预先形成的纳米颗粒上而掺入纳米颗粒中。讨论了掺入效率以及模型化合物和抗癌药物的释放特性。提到了用于研究这些过程的方法，包括吸附和解吸的测定、动力学和等温线。理论上，通过连接某种形式的归巢装置，通常是单克隆抗体或凝集素，可实现药物靶向的选择性。描述了在体外和体内用单克隆抗体包被纳米颗粒的工作。最后，介绍了用发射γ射线的放射性核素标记纳米颗粒的方法，并给出了在动物物种中获得的结果。
