Chonkar Ankita, Nayak Usha, Udupa N
Manipal College of Pharmaceutical Sciences, Manipal University, Manipal-576 104, India.
Indian J Pharm Sci. 2015 Jul-Aug;77(4):367-75. doi: 10.4103/0250-474x.164770.
Nasal drug delivery has now been recognized as a promising route for drug delivery due to its capability of transporting a drug to systemic circulation and central nervous system. Though nasal mucosa offers improved bioavailability and quick onset of action of the drug, main disadvantage associated with nasal drug delivery is mucocilliary clearance due to which drug particles get cleared from the nose before complete absorption through nasal mucosa. Therefore, mucoadhesive polymeric approach can be successfully used to enhance the retention of the drug on nasal mucosal surface. Here, some of the aspects of the stimuli responsive polymers have been discussed which possess liquid state at the room temperature and in response to nasal temperature, pH and ions present in mucous, can undergo in situ gelation in nasal cavity. In this review, several temperature responsive, pH responsive and ion responsive polymers used in nasal delivery, their gelling mechanisms have been discussed. Smart polymers not only able to enhance the retention of the drug in nasal cavity but also provide controlled release, ease of administration, enhanced permeation of the drug and protection of the drug from mucosal enzymes. Thus smart polymeric approach can be effectively used for nasal delivery of peptide drugs, central nervous system dugs and hormones.
由于鼻内给药能够将药物输送至体循环和中枢神经系统,它如今已被公认为一种很有前景的给药途径。尽管鼻黏膜能提高药物的生物利用度并使其起效迅速,但鼻内给药的主要缺点是黏液纤毛清除作用,由于这一作用,药物颗粒在通过鼻黏膜被完全吸收之前就从鼻腔被清除了。因此,黏膜黏附聚合物方法可成功用于提高药物在鼻黏膜表面的滞留时间。在此,已讨论了刺激响应性聚合物的一些方面,这些聚合物在室温下呈液态,并且响应鼻腔温度、pH值和黏液中存在的离子,可在鼻腔内发生原位凝胶化。在这篇综述中,讨论了几种用于鼻腔给药的温度响应性、pH响应性和离子响应性聚合物及其凝胶化机制。智能聚合物不仅能够提高药物在鼻腔内的滞留时间,还能实现控释、便于给药、增强药物渗透以及保护药物免受黏膜酶的影响。因此,智能聚合物方法可有效地用于肽类药物、中枢神经系统药物和激素的鼻腔给药。