Abstract
Purpose: The aim of the present investigation was to formulate protein nanoparticles (PNPs) loaded suppositories for colon targeting of metronidazole (MZ), to achieve sustain release effect. Methods: PNPs were formulated via desolvation technique by utilizing 23 factorial design which results into eight formulations. The synthesized PNPs 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 PNPs 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 MZ-PNPs loaded suppositories were compared with the suppositories loaded with active ingredient only i.e. MZ. 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 MZ 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, P. posthuma.
Highlights
In present scenario, efforts are being made to achieve more controlled drug distribution throughout the body with lessen side-effects
The formulated protein nanoparticles (PNPs) were evaluated for several physicochemical properties viz. particle size, surface morphology, zeta potential, in vitro drug release study
The optimized formulation of PNPs was loaded to a suppositories base and evaluated for weight variation, disintegration, liquefaction time and in vitro release study
Summary
Efforts are being made to achieve more controlled drug distribution throughout the body with lessen side-effects. Due to its biodegradable and non- toxic nature, it has become the most projecting macro-molecular carrier,[1] these are widely used to prepare nanospheres and nanocapsules. It is a major protein which provides benefits for ease of preparation in desired sizes and presence of reactive groups (thiols, amino or carboxylic groups) ligand binding for covalent linkage. Suppositories are chosen as dosage form to prevent drug and protein nanoparticles (PNPs) from detoriation.[4,5,6] In addition, albumin is highly soluble at pH 7.4 which is one of the reasons that rectal route was chosen so that, it is facile to release the drug at the targeted area.[7] Suppositories should have effective mucoadhesive property for their retention of drug on rectal mucosa.[8,9]. These MZ-PNPs suppositories were compared with MZ loaded suppositories to evaluate its in vitro efficacy and release kinetics pattern of the fabricated formulation
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