Phukan Kunjan, Nandy Marika, Sharma Rupanjali B, Sharma Hemanta K
Department of Pharmaceutical Sciences, Dibrugarh University, Dibrugarh, Assam, India.
Recent Pat Drug Deliv Formul. 2016;10(2):156-64. doi: 10.2174/1872211310666160321123936.
Drug targeting to brain has always been problematic due to Blood-Brain Barrier (BBB), which, does not allow most of the drugs to pass through it as they are hydrophilic and macromolecular drugs. So, in order to bypass the BBB, alternative modes of administration were searched and nasal to brain delivery route was tried by many workers. Such studies yielded patented nano-formulations with the ability to cross blood brain barrier.
Nanoparticles being smaller in size and large surface area help in increasing the rate of drug permeation to the brain. In this review work, emphasis has been laid on discussion on various works done in the field of nasal delivery of drugs to brain over the last decade.
The works that are discussed in this paper show better drug targeting of brain when given through nasal route as nanoparticles. Experiments performed in animal models have clearly exhibited that nano-sized formulations are able to facilitate the delivery of drugs to brain through nose in comparison to tantamount drug solutions.
However, it is not yet confirmed whether the drug is freed from the formulation in the nasal cavity and then absorbed or the nanoparticles themselves are absorbed and then the drug is released in the CNS. Furthermore, the toxicity studies were not carried out extensively in suitably designed model, which should be considered before going for further studies and application.
由于血脑屏障(BBB)的存在,药物靶向脑部一直存在问题,血脑屏障不允许大多数亲水性和大分子药物通过。因此,为了绕过血脑屏障,人们探索了其他给药方式,许多研究人员尝试了鼻脑给药途径。此类研究产生了具有穿越血脑屏障能力的专利纳米制剂。
纳米颗粒尺寸更小且表面积大,有助于提高药物向脑部的渗透速率。在这项综述工作中,重点讨论了过去十年中在药物鼻脑给药领域所开展的各项研究。
本文所讨论的研究表明,纳米颗粒经鼻给药时对脑部具有更好的药物靶向性。在动物模型中进行的实验清楚地表明,与等效的药物溶液相比,纳米制剂能够促进药物经鼻向脑部递送。
然而,目前尚未确定药物是在鼻腔内从制剂中释放出来然后被吸收,还是纳米颗粒本身被吸收然后药物在中枢神经系统中释放。此外,尚未在适当设计的模型中广泛开展毒性研究,在进行进一步研究和应用之前应予以考虑。