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The purpose of the present study was to optimize lopinavir loaded solid lipid nanoparticles (SLNs) by investigating the
relationship between design factors and experimental data using response surface methodology.
Materials and Methods: SLNs were prepared by a modified method of hot homogenization ultra-sonication and low temperaturesolidification
technique using stearic acid as the solid lipid and poly vinyl alcohol as surfactant. Two statistical designs (Plackett?
Burman and Box Behnken design) were used to optimize loaded nanoparticles using Stat-Ease Design-Expert software (Version
188.8.131.52). Plackett?Burman design was used to screen ten high-risk variables obtained from risk analysis and assess their impact on
nanoparticles characteristics (drug encapsulation efficiency, particle size) followed by, Box Behnken design to further elucidate
the relationship between the factors having significant effect on the responses. Nanoparticles were evaluated for size by Malvern
Zetasizer (Zetasizer Nano ZS). Oral pharmacokinetic studies were under taken to access in vivo performance of the lopinavir
loaded SLN in male Wistar rats. Plasma samples obtained from pharmacokinetic studies were analyzed for lopinavir using HPLC
Observation and Results: It was observed that out of ten high-risk variables, only lipid amount, surfactant concentration,
homogenization time and sonicator amplitude had significant effects on the drug encapsulation efficiency and particle size.
Optimized formulation obtained from BBD (4 factors, 2 levels, 29 trials) matrix, showed high drug entrapment efficiency (81.29%
? 5.23%) and optimum particle size (250 ?10 nm) of NPs. A significant increase in oral bio-availability (p< 0.01, n= 3, 3.5 ? 0.3
folds) of lopinavir loaded SLN NPs as compared to free-lopinavir, indicating positive outcome of optimized formulation.
Conclusion: Lopinavir loaded SLN formulations were optimized using statistical screening designs (PBD and BBD). SLN could
potentially be exploited as a delivery system for improving oral bioavailability of lopinavir.
Vikas Dalal, Presenting Author is a M.Pharm student from Birla Institute Of Technology and Science, Hyderabad Campus, Jawahar Nagar,
Hyderabad, Andhra Pradesh 500078 .Rahul Vats, Aditya N, Lecturer, Birla Institute Of Technology and Science Hyderabad Campus, Jawahar Nagar,
Hyderabad, Andhra Pradesh 500078.Punna Rao Ravi, Assistant Professor, Birla Institute Of Technology and Science Hyderabad Campus, Jawahar
Nagar, Hyderabad, Andhra Pradesh 500078.
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