Pamam dendrimer - vitamin conjugate for delivery of paclitaxel as anticancer agent

P. Tripathi
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Abstract

Background: The major issues with anticancer agent are that they randomly attack cancerous as well as healthy cell. These are injurious and its side effects can be reduced by developing a drug delivery vehicle. That is particular to tumor cells and this may be achieved by employing a strategy called active targeting strategy wherein the functionalities that respond to over expressed receptors (e.g., biotin, and folate conjunction on dendrimers surface) on tumor cells are attached to the drug carrier. Objective: In the present study, biotin- G4 PAMAM dendrimer conjugates were synthesized and structures were characterized. Materials and Methods: G4 -PAMAM Dendrimers were biotinylated using sulfo-NHS-LC-biotin and structural characterization was performed using 1 H NMR and transmission electron microscopy. The effect of generation and release rate, hemotoxicity with biotinylated dendrimer was performed. Results: The results suggested that biotinylated G4 PAMAM dendrimers may be potential drug carriers for paclitaxel targeting to cancer. Conclusion: Biotinylated G4 -PAMAM dendrimers show potential as nanocarriers in targeted drug delivery. Biotinylation of dendrimer thus reduces the distracted charge-mediated uptake and as well as also rising the in vivo biocompatibility, as seen with decrease in hemotoxicity with biotinylated dendrimers.
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Pamam树状大分子-维生素缀合物作为抗癌剂递送紫杉醇
背景:抗癌药物的主要问题是它们对癌细胞和健康细胞的攻击是随机的。这些都是有害的,其副作用可以通过开发药物运载工具来减少。这是肿瘤细胞特有的,这可以通过采用一种称为主动靶向策略的策略来实现,其中肿瘤细胞上响应过表达受体的功能(例如,树突表面的生物素和叶酸结合)被附着在药物载体上。目的:合成生物素- G4 PAMAM树状大分子缀合物并对其结构进行表征。材料和方法:采用磺胺生物素对G4 -PAMAM树状大分子进行生物素化,并采用1h NMR和透射电镜对其结构进行表征。观察了生物素化树突状分子对其产生、释放速度、血液毒性的影响。结果:生物素化的G4 PAMAM树状大分子可能是紫杉醇靶向肿瘤的潜在药物载体。结论:生物素化的G4 -PAMAM树状大分子具有作为靶向药物递送纳米载体的潜力。因此,树状大分子的生物素化减少了分散电荷介导的摄取,同时也提高了体内生物相容性,正如生物素化的树状大分子降低了血液毒性所见。
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