Design, Development and Characterization of Pyrazinamide Niosomal Dosage Form

Sanoj Thomas¹*, Bagyalakshmi J¹

1. College of Pharmacy, Sri Ramakrishna Institute of Paramedical Sciences, Coimbatore-44, Tamil Nadu, India

ABSTRACT

Pyrazinamide being a 1^st line of defense against tuberculosis is very effective for the first 2 to 3 months of treatment and helps to eradicate a major portion of the strain. But due to its increased use, there are adverse effects such as hepato-toxicity and other dose related side effects. The amount of drug used in formulation is high i.e. 500mg to 1gm. Another major disadvantage is resistance of the bacteria leading to DR-TB (drug resistant tuberculosis). The main objective of this study is to decrease the amount of drug needed for formulation and to avoid hepato-toxicity. Pyrazinamide drug formulation was prepared into a niosomal dosage form by modified ether injection method, using various concentrations of polymer and keeping cholesterol content constant. Characterization was carried out and vesicle size determination showed that the formulated vesicles were in the range of 110-350nm. FTIR results showed that drug and polymers were compatible. Drug content and entrapment efficiency were calculated using UV-spectroscopy at 268nm. In-vitro release studies were carried out for all formulations and it was seen that Span-80 formulation had the highest percentage release when compared to other formulations. The drug release was subjected to various kinetic models and it was observed that all formulations followed zero order kinetics. It can be concluded that all these polymers can be used for the successful formulation of Pyrazinamide niosomes and the surfactant that is most apt was found to be Span-80 in the ratio 1:3 as compared to other polymers in various ratios.

Keywords: Pyrazinamide, tuberculosis, hepato-toxicity, drug resistant tuberculosis, niosomes.