Background: Around 40% of newly discovered chemical entities in pharmaceutical
industries have poor water solubility and hence they suffer from low oral bioavailability owing to undesirable
physicochemical and pharmacokinetic properties. So, it is the challenge for the formulation
scientists to develop the oral formulation that can mitigate the pitfalls associated with such lipophilic
Methods: Lipid nanoparticles hold a promising tool to decrease the pitfalls of lipophilic drugs as lipid
components can effectively increase the absorption of drugs, which leads to improvement in oral
bioavailability. They are also considered as safe because they are made up of physiological lipids,
which are biocompatible and biodegradable in nature. Amongst the lipid nanoparticles, Nanostructured
Lipid Carriers (NLCs) are the second-generation lipid nanoparticles and were developed to conquer the
limitations of solid lipid nanoparticles. They increase the solubility, permeability, reduce metabolism,
P-glycoprotein efflux, and thereby increase the bioavailability of poorly soluble drugs.
Conclusion: This review highlights the various aspects of NLCs, such as structural components, types,
in vivo fate, pharmacokinetic, toxicity, recent applications, and patent reviews of NLCs in drug delivery.