Kaur Gurpreet, Mehta S K, Kumar Sandeep, Bhanjana Gaurav, Dilbaghi Neeraj
Department of Chemistry and Centre of Advanced Studies in Chemistry, Panjab University, Chandigarh, 160014, Punjab, India.
Department of Bio and Nano Technology, Guru Jambheshwar University of Science and Technology, Hisar, 125001, Haryana, India.
J Pharm Sci. 2015 Jul;104(7):2203-12. doi: 10.1002/jps.24469. Epub 2015 May 7.
A microemulsion has been formulated to coencapsulate antituberculosis drugs to solve the issue of stability of rifampicin (RIF) in the presence of isoniazid (INH) and pyrazinamide (PZA). The structural transition, solubilization locus, and quantitative release of drugs without interference have been estimated. Derivative absorbance spectroscopy, especially ratio derivative and double divisor ratio derivative methods, has been employed for estimating the release. The coencapsulation of the anti-tuberculosis drugs were carried out in single, binary, or ternary mixtures and occupy the same solubilization sites in multiple drugs microemulsion systems as in the case of single drug-loaded systems. INH and PZA obey the diffusional (Fickian) release mechanism, whereas RIF shows anomalous release. Resazurin assay and agar well diffusion method were adopted for cytotoxicity analysis and antimicrobial activity, respectively. Cytotoxicity was found to be dependent on concentration and on colloidal structure of microemulsion.
已制备一种微乳液用于共包封抗结核药物，以解决利福平（RIF）在异烟肼（INH）和吡嗪酰胺（PZA）存在下的稳定性问题。已估计了结构转变、增溶位点以及无干扰情况下药物的定量释放。采用导数吸收光谱法，尤其是比率导数法和双除数比率导数法来估计释放情况。抗结核药物的共包封在单一、二元或三元混合物中进行，并且在多药物微乳液系统中占据与单药物负载系统相同的增溶位点。INH和PZA遵循扩散（菲克）释放机制，而RIF表现出异常释放。分别采用刃天青测定法和琼脂孔扩散法进行细胞毒性分析和抗菌活性测试。发现细胞毒性取决于微乳液的浓度和胶体结构。
