Evaluation of intestinal permeability of nifedipine cyclodextrin based nanosponges using single pass intestinal perfusion method

Abstract

Nifedipine is a BCS class II agent resulting in low bioavailability . Improving solubility and membrane permeability could lead to enhance of oral bioavailability. Novel formulations were also developed to improve therapeutic effects of nifedipine, cyclodextrin based nanosponges is one of the novel drug delivery system that can improve the nifedipine solubility and permeation, The aim of this study was the evaluation of intestinal permeability in cyclodextrin based nanosponges of nifedipine using single pass intestinal perfusion method, Nifedipines CDNSs were prepared in previous work and solubility and dissolution characteristics have been reported and the ability to permeat will investigated using single pass intestinal perfusion method in rat and compared with intestinal permeability of nifedipine solution. Aim: Evaluation of cyclodextrin based nanosponges for controlled oral delivery of nifedipine. Methods: SPIP was performed in isolated jejunal segment at CDNS formulation of nifedipine to compare intestinal permeability changes against of simple solution of nifedipine. Phenol red was used as a non-absorbable marker. Stability studies were conducted to ensure that the loss of Nifedipine could be attributed to intestinal absorption. Outlet samples were analysed using the developed HPLC method and effective permeability values were calculated by respected formula.Results: The effective permeability value of nifedipine simple solution in the jejunum was 45.9 × 10 -4 cm/min. Also the effective permeability values of CDNS nifedipine nanoparticles found to be 136 × 10 -4 cm/min. The use of nanoparticle formulations (CDN) led to a significant increase in intestinal permeability of nifedipine.Discussion and conclusion: In conclusion, the high aqueous solubility of nifedipine might be a crucial factor for its poor oral bioavailability. New techniques have shown that the use of nanoparticles like CDN can dramatically increase intestinal permeability.