Xie Ying, Chen Yun, Sun Minjie, Ping Qineng
Department of Pharmaceutics, State Key Laboratory of Natural Medicines, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, PR China.
Curr Pharm Biotechnol. 2013;14(10):918-25. doi: 10.2174/1389201014666131226145441.
Nucleic acid drugs are promising new therapeutics for the treatment of various diseases including genetic diseases, viral diseases, and cancer. However, their poor intracellular bioavailability and rapid degradation hinder their development as drugs. Therefore, the main challenge is to develop an efficient delivery system. Calcium phosphate has been widely used to transfect cultured cells for 40 years, due to its safety, simply of production and noticeable efficacy of transfection. Unfortunately, calcium phosphate particles show poor colloidal stability because of uncontrolled growth, which impedes their practical use. Recently, investigators have designed a variety of biodegradable calcium phosphate nanocarriers and achieved efficient gene delivery both in vitro and in vivo with low toxicity. In this review, we focus on the current research activity in the development of calcium phosphate nanoparticlss for gene delivery. Calcium phosphate nanoparticles are mainly classified into lipid coated and polymer coated ones for discussion. In addition, cellular uptake and intracellular trafficking of calcium phosphate nanoparticles are also mentioned.
核酸药物是用于治疗包括遗传性疾病、病毒性疾病和癌症在内的各种疾病的有前景的新型治疗药物。然而，它们较差的细胞内生物利用度和快速降解阻碍了其作为药物的开发。因此，主要挑战是开发一种高效的递送系统。磷酸钙已被广泛用于转染培养细胞40年，因其安全性、生产简单以及显著的转染效果。不幸的是，由于生长不受控制，磷酸钙颗粒表现出较差的胶体稳定性，这阻碍了它们的实际应用。最近，研究人员设计了多种可生物降解的磷酸钙纳米载体，并在体外和体内实现了高效的基因递送且毒性较低。在本综述中，我们关注用于基因递送的磷酸钙纳米颗粒开发的当前研究活动。为便于讨论，磷酸钙纳米颗粒主要分为脂质包被型和聚合物包被型。此外，还提到了磷酸钙纳米颗粒的细胞摄取和细胞内运输。
