Development of pH sensitive polymeric nanoparticle of erythromycin

Abstract

Introduction: Erythromycin is a macrolide antibiotic used for the treatment of various infections caused by bacteria. It is also used for Respiratory tract infection, skin infection, syphilis, etc. Erythromycin base was a poorly water-soluble and acid-labile drug. The bioavailability of Erythromycin was very less about (15–35%). The absorption site of Erythromycin is the small intestine. pH-responsive polymeric drug delivery system is efficient delivering the acid instable drugs. Aim: The main objective of the study is to formulate Erythromycin loaded pH-responsive polymeric nanoparticles was prepared using pHresponsive polymer to prevent the degradation of acid-labile drug and to evaluate the Polymeric nanoparticle. Materials and Methods: The Erythromycin Polymeric nanoparticles were prepared by Nano precipitation method using Eudragit L100 as a Polymer and polyvinyl alcohol (PVA) as stabilizer. The particle size, polydispersity index (PDI), zeta potential, entrapment efficiency and In-vitro drug release studies were performed for nanoparticle. The compatibility between drug and polymer was studied by Fourier transform infrared. The nanoparticle was lyophilized and surface morphology was determined by scanning electron microscope. Excipients were added and formulated into tablet. The Precompression evaluation of lyophilized powder was carried out. The post-compression evaluation for tablets and In-vitro release study was performed and compared with marketed tablet. Results: Erythromycin nanoparticle was formulated and evaluated. It showed the particle size of 270.2 nm with PDI of 0.166 and the zeta potential was found to be −32.5. The Entrapment efficiency of the ENP 9 Nanoparticle was 96%. Erythromycin loaded tablet was formulated and evaluated for hardness, weight variation, disintegration, friability, thickness, and diameter. It was present within the limit. In vitro drug release of the formulated tablet showed 91% drug release in phosphate buffer pH6.8 at the end of 60 min. Conclusion: Erythromycin nanoparticles were in the nanometer range and it was stable. Polymeric nanoparticle tablet had the ability to protect the acid-labile drug and it gets dissolved in the intestine pH 6.8. The nano particulate tablet showed the better release when compared with marketed tablet.