Vol. 7, Issue 9 (2018)

Author(s):
Sunil Khatak, Uttam Prasad Semwal, Manoj Kumar Pandey and Harish Dureja

Abstract:
The patient non-compliance and emergence of multidrug resistance (MDR) have great influence on the increased incidence of tuberculosis (TB). Nanotechnology-based chemotherapy improves pharmacokinetic behaviour, antimycobacterial efficacy reduces dosing frequency and cost of therapy. The present study, a modified microemulsion technique was utilized for the preparation of first-line antitubercular drugs (ATDs). i.e. rifampicin (RIF), isoniazid (INH) and pyrazinamide (PYZ) loaded solid lipid nanoparticles (SLNs). The morphology, particle size, zeta potential was characterized and antimycobacterial activity was evaluated against Mycobacterium smegmatis mc² 155 (M. smegmatis). The resulting ATDs loaded SLNs were spherical with average particle size 195.1±11.11 nm with negative zeta potential –41.9mV and 0.229 PDI. The percentage encapsulation efficiency of RIF, INH and PYZ were 84.6±2.11, 83.3±3.75 and 76.4±3.83, and loading capacity was found to be 43.8%, 35.4% and 39.7%, respectively. The practical yield was found to be 92.6%. The ATDs loaded SLNs formulation also showed sustained drug release for 24 h. The antimycobacterial activity was greatly enhanced against M. smegmatis, and the minimum inhibitory concentration (MIC) of ATDs loaded SLNs was approximately ten-times more effective as compared to standard drugs and two-times efficacy improvement as compared to a physical mixture of ATDs solution. Drug-free SLNs showed no antimycobacterial effect. It can be concluded that the SLNs are promising vehicles for the antimycobacterial activity of ATDs.