Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard, Hamdard Nagar, New Delhi, India.
CNS Neurol Disord Drug Targets. 2011 Aug;10(5):576-88. doi: 10.2174/187152711796235023.
Most of the newly developed drugs fails to achieve sufficient bioavailability in to brain due to low water solubility and low permeability. Drug delivery systems are one method for achieving entry of molecules to their desired site of action within the body. Dendrimers are the customizable nanopolymers with uniform and well-defined particle size and shape. Dendrimers are of eminent interest for biomedical applications because of their ability to cross cell membranes. This potential pharmaceutical delivery system crosses the blood brain barrier (BBB) and other important target points. The high level of control over the dendritic architecture (size, branching density, surface functionality) make dendrimers ideal carriers in the field of brain drug delivery of anticancer, antiinflammatory, and antimicrobial agents. Examples of dendrimers such as poly(amidoamine) (PAMAM), poly(propylene imine) (PPI) and polyether-copolyester (PEPE), Glyco, PEGylated, peptide and pH dendrimers are of outmost significance. These dendrimers carry the drug molecules by physical interactions (encapsulation) or through chemical bonding (prodrug approach), while pH sensitive dendrimers are able to deliver drug molecules by alteration of ionic exchange in the brain microenvironment at the tumor site. Techniques employing dendrimers could be especially useful for drugs targeting to Alzheimer's and Prion's diseases. The present review should be of value to scientists who wish to work on the dendrimers for the delivery of molecules into the brain by systemic dosing.
由于低水溶性和低通透性,大多数新开发的药物都无法在大脑中达到足够的生物利用度。药物传递系统是使分子进入体内所需作用部位的一种方法。树突状聚合物是具有均匀和明确定义的粒径和形状的可定制纳米聚合物。由于其能够穿过细胞膜,树突状聚合物成为生物医学应用的关注焦点。这种潜在的药物传递系统可以穿过血脑屏障 (BBB) 和其他重要的靶标点。对树突状结构(大小、分支密度、表面功能)的高度控制使树突状聚合物成为抗癌、抗炎和抗菌药物脑药物输送领域的理想载体。多(聚)(酰胺)(PAMAM)、多(聚)(丙烯亚胺)(PPI)和聚醚-共聚酯(PEPE)、Glyco、PEG 化、肽和 pH 树突状聚合物等树突状聚合物的例子具有最重要的意义。这些树突状聚合物通过物理相互作用(包封)或通过化学结合(前药方法)携带药物分子,而 pH 敏感的树突状聚合物能够通过改变肿瘤部位大脑微环境中的离子交换来输送药物分子。使用树突状聚合物的技术对于希望通过系统给药将分子递送到大脑的科学家可能特别有用。本综述应该对希望通过系统给药将分子递送到大脑的科学家有价值。