Conception and evaluation of suppositories loaded nanoparticulates as drug delivery system

Abstract

Rectal drug delivery system are useful delivery system for various types of drugs with narrow therapeutic window of absorption, for the drugs with pH dependent solubility, drugs which degrade in the lower pH conditions, rectal delivery system can be achieved by rectal suppositories, ointments, creams, tablets. The present dissertation aimed in conception and evaluation of novel dosage of nanoparticles loaded suppositories. Initially aspirin-chitosan nanoparticles were prepared by ionic gelation method results has shown in a good correlation in the case of chitosan-Aspirin nanoparticles with increase in the particle size there is increase in the percentage drug entrapment of aspirin nanoparticles. Compatibility study performed using Fourier transformer infrared spectroscopy (FTIR) and Differential scanning calorimeter (DSC) between Aspirin and excipients used in the formulation and proved for no incompatibility issues. The process was optimized for process related parameters effect of chitosan concentration and STPP. Based on results the best formulation was selected and in order to know the diffusion efficiency different compositions of aspirin glycerogelatin suppositories were prepared and subjected to various in-vitro evaluation studies and best composition was selected, From the evaluation studies best formulation from aspirin nanoparticles incorporated in to selected glycerol gelatin bases and evaluated for in-vitro characteristics. The results indicates that formulation Fa9 and Fb9 Aspirin nanoparticles were proved to be best formulation with 88.3±1.1 and 75±1 % of drug release at the end of 24hr, with zero drug release. iv The drug release profile was best fitted to Krosmayer s Peppas equation, the n value of (release exponent) nanoparticles were present between (0.4815 to 0.6251) and (0.511 to 0.749) which is near to 0.5 indicates the drug release follows non-fickian diffusion model. When the values are fitted to zero order the regression value (0.9926 to 0.990) and (0.978 to 0.999) which is nearer to 1 indi