Poly(lactic‐co‐glycolic) acid (PLGA) is one of the most versatile biomedical polymers, already approved by regulatory authorities to be used in human research and clinics. Due to its valuable characteristics, PLGA can be tailored to acquire desirable features for control bioactive payload or scaffold matrix. Moreover, its chemical modification with other polymers or bioconjugation with molecules may render PLGA with functional properties that make it the Holy Grail among the synthetic polymers to be applied in the biomedical field. In this review, the physical–chemical properties of PLGA, its synthesis, degradation, and conjugation with other polymers or molecules are revised in detail, as well as its applications in drug delivery and regeneration fields. A particular focus is given to successful examples of products already on the market or at the late stages of trials, reinforcing the potential of this polymer in the biomedical field.

Introduction: The blood-brain barrier (BBB) is a highly limiting barrier that prevents the brain from contacting with several circulating molecules, including harmful agents. However, certain systemic nutrients and macromolecules are able to cross the BBB and reach the brain parenchyma, involving the interaction with multiple receptors and/or transporters at BBB surface. Nanotechnology allows the creation of drug vehicles, functionalized with targeting ligands for binding specific BBB receptors and/or transporters, hence triggering the transport through this biobarrier. Areas covered: This review focus the BBB receptors/transporters to be exploited in regard to their overall structure and biologic function, as well as their role in the development of strategies envisaging drug delivery to the brain. Then, the interplay between the targeting of these BBB receptors/transporters and nanotechnology is explored, as they can increase by several-fold the effectiveness of brain-targeted therapies. Expert opinion: Nanomedicine may be particularly useful in brain drug delivery, mainly due to the possibility of functionalizing nanoparticles to target specific receptors/transporters. Since the BBB is endowed with numerous receptors and transporters responsible for regulating the proper metabolic activity of the brain, their targeting can be a promising bypass strategy to circumvent the hurdle that the BBB represents for brain drug delivery.