Abstract
The purpose of this research was to improve oral bioavailability of poorly aqueous soluble drug lopinavir using solid lipid nanoparticles (SLNs). Glyceryl behenate based SLNs of lopinavir were prepared using hot self-nanoemulsification (SNE) technique. The hot isotropic mixture of glyceryl behenate, Poloxamer 407 and polyethylene glycol 4000 was spontaneously self-nanoemulsify in hot water (80 °C) and SLNs were subsequently formed with rapid cooling. Hot SNE ability of isotropic mixture was visually assessed by ternary phase diagram study. Optimized SLNs were having particle size of 214.5 ± 4.07 nm, entrapment efficiency of 81.6 ± 2.3 % and zeta potential of −12.7 ± 0.87 mV. SLNs were evaluated by transmission electron microscopy and atomic force microscopy for morphological details. Further, differential scanning calorimetry and x-ray diffraction were also performed for solid state characterization of SLNs. Higher oral bioavailability (3.56-fold) was found for lopinavir loaded SLNs in comparison to bulk lopinavir due to higher lymphatic drug transport (p < 0.05). Results indicate that SLNs of glyceryl behenate can be successfully prepared by hot SNE technique.
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Acknowledgments
Authors are grateful to Sophisticated Analytical Instrumentation Facilities (SAIF), Panjab Univeristy for providing XRD, TEM facilities and SMITA lab, IIT Dehli for providing particle size, AFM and DSC facilities. Authors also would like to acknowledge Uttarakhand technical University, Dehradun for their kind support.
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Negi, J.S., Chattopadhyay, P., Sharma, A.K. et al. Development and evaluation of glyceryl behenate based solid lipid nanoparticles (SLNs) using hot self-nanoemulsification (SNE) technique. Arch. Pharm. Res. 37, 361–370 (2014). https://doi.org/10.1007/s12272-013-0154-y
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DOI: https://doi.org/10.1007/s12272-013-0154-y