Colon Targeted Protein Nanoparticles Loaded Suppositories : Effective against Intestinal Parasites

Abstract

Purpose: The aim of the present investigation was to formulate protein nanoparticles loaded suppositories for colon targeting of metronidazole (MZ), to achieve sustain release effect. Methods: Protein nanoparticles were formulated via desolvation technique by utilizing 2 3 factorial design which results into eight formulations. The synthesized protein nanoparticles were characterized for different physicochemical and in vitro parameters viz. particle size, surface morphology, entrapment efficiency and zeta potential, drug- excipients compatibility studies. Results: The formulated protein nanoparticles were found to be spherical in shape and have an average size in the range of 300.7 nm to 504.8 nm. Based on the results obtained, F7 was found to be the optimized formulation that was loaded into the suppository base. Furthermore, suppositories were also characterized for several parameters like content uniformity, weight variation and liquefaction time. Conclusion: Resultant, suppositories were free from pits, fissures and cracks. The in-vitro release data of metronidazole protein nanoparticles (MZ-PNPs) loaded suppositories were compared with the suppositories loaded with active ingredient only i.e. metronidazole. Screening against Pheretima posthuma was also conducted. The results of in vitro drug release testing proved that protein nanoparticle loaded suppositories is a better approach, compared to pure metronidazole loaded suppositories. Release kinetic study concluded that the formulation follows higuchi’s equation i.e. having a biphasic release pattern. The efficiency of the formulated dosage form was evaluated using Indian earthworms, Pheretima posthuma (P. posthuma).