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Current Drug Therapy

Author(s): Swatantra Kumar Singh Kushwaha*, Awani Kumar Rai and Heena Parveen

DOI: 10.2174/1574885514666190103114200

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Development & Pharmaceutical Characterization of Isoniazid Loaded Solid Lipid Nanoparticle Drug Delivery Approach

Page: [228 - 238] Pages: 11

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Abstract

Background: Tuberculosis is a major public health problem in the world. Isoniazid is a first line antitubercular drug active against Mycobacterium species which inhibits mycolic acid synthesis.

Objective: The aim of the present investigation was the preparation of solid lipid nanoparticle containing Isoniazid to increase bioavailability, sustained release and decrease toxicity by increasing permeability.

Methods: Isoniazid was incorporated into SLN for sustained drug delivery, increasing permeability and bioavailability. SLNs were prepared by emulsification followed by the solvent evaporation technique by optimizing lipid, polymer and surfactant ratio under controlled optimized process variables i.e. temperature and stirring speed. SLNs were characterized for particle size analysis, comparative study design in different physiological pH for in-vitro drug release and drug release kinetics.

Results: The best in-vitro release for F7 was found to be 80.2% in pH-7.4 and 82.2% in pH-4.5. The particle size of the F7 formulation was found to be in the range of 200- 600nm . Among all 3 optimized formulations, i.e. F3, F7 and F8 in both the pH, F3 followed non-fickian diffusion mechanism in pH-4.5 whereas all the formulations in both pH followed super-case II diffusion mechanism. The stability studies were carried out as per ICH guidelines which signify that the SLNs were found stable in the refrigerated condition.

Conclusion: The results clearly demonstrated that SLNs drug delivery system is a promising approach for antitubercular drug delivery as it proved to sustained release, increase permeability, enhanced bioavailability and thus decreased dosing frequency. Kinetic modelling of the formulation with zero, first order, Higuchi and Korsmeyer- peppas is explained in this article.

Keywords: In-vitro release, isoniazid, macrophage, nanoparticle, solid lipid nanoparticles, drug delivery.

Graphical Abstract

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