Abstract

DEVELOPMENT AND EVALUATION OF DOTHIEPIN HCL LOADED SOLID LIPID NANOPARTICLES

Kiran B., K. Manjunath*, Suresh V. Kulkarni, Madhu G. and Chaya M.

ABSTRACT

Aim: The aim of the present study is to develop Dothiepin HCl solid lipid nanoparticles and to evaluate them. Method: Suitable lipids (Triastearin, GMS and Compritol), stabilizer (Soy lecithin) and surfactant (Tween 80) were selected. FT-IR and DSC studies were carried to check drug-excipient compatibility. In the present study nine formulations were formulated by using three lipids at various proportions. Solid lipid nanoparticles were prepared by hot homogenization followed by ultra-sonication technique. The nanoparticles were evaluated for particle size, PDI, zeta potential Drug content, percentage drug entrapment efficiency, in vitro drug release studies, release kinetics. Results: FT-IR and DSC drug-excipient compatibility studies were revealed that there was no interaction between drug and selected lipids. The particle size ranged from 57.42 to 221.85 nm, PDI of all formulations were good within the range of 0.267 to 0.578, zeta potential ranged from -10.5 to -29.6 mV, Percentage drug entrapment efficiency of all formulations were observed were in the range of 84.42 to 93.82%. The cumulative percentage release of Dothiepin HCl from different formulations varied from 75.43 to 93.59%. Among all formulations, the formulation F1-DPH-TS50 showed highest drug release of 93.59% and considered as optimized formulation. The release kinetic studies showed that the release was first order (R2 = 0.99) diffusion controlled and the ‘n’ value obtained from the Korsmeyer-Peppas model indicated the release mechanism was Anomalous diffusion (non-fickian type) (n-value of F1 was 0.5716), the particle size, PDI and zeta potential of optimized formulation was found to be 57.42 nm, 0.406, -20.9 mV. Conclusion: The developed SLNs were able to sustain the drug release for 24hrs, thus reducing dosing frequency and occurrence of side effects, thereby improving the effectiveness of the drug.

Keywords: Dothiepin HCl, solid lipid nanoparticles, FT-IR, DSC, in vitro drug release.