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According to the list published by the WHO for global top ten causes of death, lung diseases contribute nearly one-third of the total mortality. The current treatment on lung diseases provide only symptomatic relief rather than restoring the complete lung functions. Nanostructured lipid carriers-based drug delivery system (NLCs-based DDS) provide a breakthrough in treating various lung diseases.This review provides the readers with background information for rationale behind focusing lung diseases and selection of targeted drug delivery to treat these diseases. This review discusses different hurdles in targeting the lung diseases and possible remedy in the form of NLCs-based DDS. The review gives an overview of the existing literature about the quality, safety, and efficacy of the NLCs-based DDS for pulmonary targeting.Different surface-engineered NLCs enormously proved their effectiveness in targeting the drug and other bioactive agents to the site of infection. Their results of safety and efficacy studies in in-vitro and in-vivo evaluations are encouraging. This advises the bright future of NLCs-based DDS for pulmonary targeting. To bring this optimistic NLCs-based DDS to the market, a thorough pre-clinical and clinical investigation hold prime importance.