Background: Blood-brain barrier (BBB) is playing a most hindering role in drug delivery to the
brain. Recent research comes out with the nanoparticles approach, is continuously working
towards improving the delivery to the brain. Currently, polymeric nanoparticle is extensively
involved in many therapies for spatial and temporal targeted areas delivery.
Methods: We did a non-systematic review, and the literature was searched in Google, Science
Direct and PubMed. An overview is provided for the formulation of polymeric nanoparticles using
different methods, effect of surface modification on the nanoparticle properties with types of
polymeric nanoparticles and preparation methods. An account of different nanomedicine
employed with therapeutic agent to cross the BBB alone with biodistribution of the drugs.
Results: We found that various different type of polymeric nanoparticle systems are available and
they prosper in delivering the therapeutic amount of the drug to the targeted area. The effect of
physicochemical properties on nanoformulation which includes change in their size, shape,
elasticity, surface charge and hydrophobicity. Surface modification of polymers or nanocarriers is
also vital in the formulation of nanoparticles to enhance targeting efficiency to the brain.
Conclusion: More standardized methods for the preparation of nanoparticles and to assess the
relationship of surface modification on drug delivery. While the preparation and its output like
drug loading, particle size and charge, permeation is always conflicted, so it requires more
attention for the acceptance of nanoparticles for brain delivery.