Choudhary Sonam, Gupta Lokesh, Rani Sarita, Dave Kaushalkumar, Gupta Umesh
Department of Pharmacy, School of Chemical Sciences and Pharmacy, Central University of RajasthanKishangarh, India.
Front Pharmacol. 2017 May 16;8:261. doi: 10.3389/fphar.2017.00261. eCollection 2017.
Adequate aqueous solubility has been one of the desired properties while selecting drug molecules and other bio-actives for product development. Often solubility of a drug determines its pharmaceutical and therapeutic performance. Majority of newly synthesized drug molecules fail or are rejected during the early phases of drug discovery and development due to their limited solubility. Sufficient permeability, aqueous solubility and physicochemical stability of the drug are important for achieving adequate bioavailability and therapeutic outcome. A number of different approaches including co-solvency, micellar solubilization, micronization, pH adjustment, chemical modification, and solid dispersion have been explored toward improving the solubility of various poorly aqueous-soluble drugs. Dendrimers, a new class of polymers, possess great potential for drug solubility improvement, by virtue of their unique properties. These hyper-branched, mono-dispersed molecules have the distinct ability to bind the drug molecules on periphery as well as to encapsulate these molecules within the dendritic structure. There are numerous reported studies which have successfully used dendrimers to enhance the solubilization of poorly soluble drugs. These promising outcomes have encouraged the researchers to design, synthesize, and evaluate various dendritic polymers for their use in drug delivery and product development. This review will discuss the aspects and role of dendrimers in the solubility enhancement of poorly soluble drugs. The review will also highlight the important and relevant properties of dendrimers which contribute toward drug solubilization. Finally, hydrophobic drugs which have been explored for dendrimer assisted solubilization, and the current marketing status of dendrimers will be discussed.
在为产品开发选择药物分子和其他生物活性物质时，足够的水溶性一直是理想的特性之一。药物的溶解度往往决定其药学和治疗性能。大多数新合成的药物分子由于溶解度有限，在药物发现和开发的早期阶段失败或被淘汰。药物具有足够的渗透性、水溶性和物理化学稳定性对于实现足够的生物利用度和治疗效果很重要。为了提高各种难溶性药物的溶解度，人们探索了许多不同的方法，包括助溶、胶束增溶、微粉化、pH调节、化学修饰和固体分散。树枝状聚合物作为一类新型聚合物，凭借其独特的性质，在改善药物溶解度方面具有巨大潜力。这些超支化、单分散的分子具有独特的能力，既能在外围结合药物分子，又能将这些分子包裹在树枝状结构内。有许多报道的研究成功地使用树枝状聚合物来提高难溶性药物的溶解度。这些有前景的结果鼓励研究人员设计、合成和评估各种树枝状聚合物，用于药物递送和产品开发。本综述将讨论树枝状聚合物在提高难溶性药物溶解度方面的作用和相关方面。综述还将强调有助于药物增溶的树枝状聚合物的重要和相关性质。最后，将讨论已探索用于树枝状聚合物辅助增溶的疏水性药物以及树枝状聚合物的当前市场状况。
