Amoxicillin Loaded Mucoadhesive Thiomer Based Nanoparticles for H.pylori Infection Therapy

Abstract

The aim of research project was to prepare mucoadhesive and mucopermeating carrier system based on thiomer (thiolated polycarbophil) nanoparticles incorporating amoxicillin and improve the drug stability and prolong retention in H.pylori infection. Amoxicillin (AM) loaded unmodified polycarbophil, thiolated polycarbophil and papain modified thiolated polycarbophil nanoparticles were synthesized by 1Ol11C gelation method and characterized for entrapment efficiency, particle SIze, polydispersity index, zeta potential, in-vitro drug release and mucopermeation. The sizes of all nanoparticles were in range of 111 run to 288 nm. SEM analysis confinned the spherical shape of amoxicillin loaded papain modified thiolated polycarbophil (AM-PCP-Cys-PAP) nanoparticles with average particle size less than 400 nm. Zeta potential and entrapment efficiency of AM-PCP-Cys-P AP nanoparticles were found to be - 13.4 mV and 78 ± 7.2 % respectively. The mucoadhesive property was evaluated by rheological investigation of nanoparticles. Due to presence of thiol groups in polymer backbone, thiolated polycarbophil nanoparticles displayed 2 fold higher mucoadhesive properties. Amoxicillin loaded papain modified thiolated polycarbophil (AM-PCP-Cys-PAP) nanoparticles displayed sustained drug release up to 48 hours. For ex-vivo diffusion! mucopermeation study, nanoparticles were loaded with fluorescence diacetate and silicon tube method was adopted to determine percent mucopermeation. Fluorescence diacetate is a lipophilic dye that retain in nanoparticles through temporary attachment. Papain modified nanoparticles showed deepest permeation into the mucus by cleavage of mucoglycoproteins as compared to unmodified nanoparticles. The invitro Hpylori growth inhibition activity of amoxicillin loaded papain modified thiolated polycarbophil (AM-PCP-Cys-PAP) nanoparticles and pure amoxicillin suspension was evaluated. AM-PCP-Cys-PAP nanoparticles were found to have better in-vitro efficacy based on high stability, prolong drug release and complete eradication of bacteria as compared to pure amoxicillin. Thus, from the results it is evident that amoxicillin loaded papain modified thiolated polycarbophil (PCP-Cys-PAP) nanoparticles can be an effective nanocarrier for H.pylori infection because of enhanced mucopenneation and mucoadhesion property with better stability and prolong drug release.