Indomethacin Loaded Polybutylcyanoacrylate Nanoparticle

Indomethacin (IDM) is a powerful non-steroidal anti-inflammatory drug (NSAID) that is effective in the management of rheumatoid arthritis, ankylosing spondylitis, osteoarthritis, and acute gout. Topical NSAIDs are also widely used to prevent intraoperative miosis and ocular inflammation. However, its effectiveness is limited by the different unwanted reactions which are dose-related and associated with long-term administration. Therefore, much interest is focused on designing its new drug delivery system to reduce side effect and improve therapeutic effectNanoparticle drug delivery system which has various advantages because of their biodegradability, stability, minimum toxicity and immunological response under physiological conditions has been a considerable research interest in the area of drug delivery. Particulate systems carriers like PACA alter and improve the pharmacokinetic and pharmacodynamic properties of various types of drug molecules. They have to been used as a physical approach to increase adhesiveness to cornea and to deliver the drug at a controlled and sustained rate to the site of action. Additionally, small molecules like indomethacin can decrease cellular toxicity induced by PBCA.In the present paper, indomethacin loaded polybutylcyanoacrylate nanoparticle was prepared by the emulsion polymerization with biodegradable polybutylcyanoacrylate as carrier materials. The preparation procedure was optimized by uniform design arranged with U5(53) table associated with evaluations of drug loading, encapsulation efficiency, shape and average size. The results indicated that the optimum condition for the preparation of IMC-PBCA-NP was pH1.5, Dextran-70:Pluronic F-684:1and BCA0.7%(v/v). The nanoparticles were discrete and uniform spheres with average diameter127±3nm; the encapsulation efficiency and drug loading of IMC-PBCA-NP were88.89%and62mg-g-1, respectively. In vitro drug release revealed that indomethacin incorporation and/or adsorption led to a rapid drug release followed by a slower liberation and the release rate decreased with increasing indomethacin content in the particle. XRD experiments revealed that the amorphous fraction of crystalline indomethacin was increased in the nanoparticle.