A hybrid design to optimize preparation of lopinavir loaded solid lipid nanoparticles and comparative pharmacokinetic evaluation with marketed lopinavir/ritonavir coformulation

Abstract

SLNs enhanced oral bioavailability and improved distribution profile of LPV to HIV reservoirs and hence could be better alternative to LPV/RTV coformulation.

Drug delivery strategies and systems for HIV/AIDS pre-exposure prophylaxis and treatment

“…In separate rats dosed intraduodenally with a solid lipid NP formulation of lopinavir, cumulative lopinavir concentrations in lymph fluid were 9.68 μg for the nanoformulation compared to 1.97 μg for the conventional formulation 6 hours after administration [106]. Negi et al reported similar observations using another solid lipid NP of lopinavir that was fabricated using a hot self nano-emulsification technique [107, 108]. Although the gut lymphatic-targeting mechanism of lipid-formulated drugs is not clear, it is believed to be similar to dietary fat absorption.…”

A Quality by Design Concept on Lipid Based Nanoformulation Containing Antipsychotic Drug: Screening Design and Optimization using Response Surface Methodology

“…As lipid concentration was increased, the entrapment efficiency was found to be increased from 18 to 95%. This was expected because at higher lipid concentration, viscosity of lipid phase will be increased which will result into faster solidification which in turn will prevent drug diffusion from inner phase to aqueous phase [20].…”

Comparative pharmacokinetic evaluation of lopinavir and lopinavir-loaded solid lipid nanoparticles in hepatic impaired rat model

“…Lopinavir‐loaded SLNs were prepared by previously reported warm oil‐in‐water (O/W) micro‐emulsion technique . Briefly, oil phase was prepared by dissolving LPV (10 mg) in molten mass of SA (100 mg) maintained at 75 °C.…”

“…To improve therapeutic effectiveness of anti‐retroviral drugs, lipid‐based nanocarrier systems like solid lipid nanoparticles (SLNs) have been extensively studied over the last decade . It is widely reported that SLNs significantly enhances the plasma exposure of poorly bioavailable compounds by increasing drug permeability or absorption and reducing drug clearance.…”

“…This is because, in the drug‐loaded nanocarrier system, the drug is not available in free form. The plasma drug exposure of drug‐loaded nanocarrier system administered through any extravascular route is dependent on the absorption and disposition properties of the carrier system and how the loaded drug releases from the carrier system in the blood …”