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Expert Opin Drug Deliv. 2018 Jul;15(7):687-701. doi: 10.1080/17425247.2018.1496080. Epub 2018 Jul 16.

Recent advance of nanoparticle-based topical drug delivery to the posterior segment of the eye.

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a Department of Pharmaceutical, School of Pharmacy , China Pharmaceutical University , Nanjing , China.
b Department of Biologics R&D Center , Chia Tai Tianqing Pharmaceutical Group Co. Ltd , Nanjing , China.


Considering that the number of patients afflicted by posterior eye diseases is increasing, effective drug delivery is currently in high clinical demand. Topical administration has been identified as the preferred option, while sufferingfrom multiple barriers. The development of nanoparticle-based drug delivery system provides an option, which would enhance the drug permeability across the barriers and achieve the desired drug level in the targeted tissue. Areas covered: This review highlights the barrier to the posterior segment of the eye via topical administration. The up-to-date development of lipid nanoparticles, liposomes, emulsions, spanlastics, micelles, polymeric nanoparticles, layered double hydroxides (LDH), dendrimers, cyclodextrins(CDs), and prodrugs are summarized. Moreover, nanocarriers currently in clinical trials for posterior segment diseases have been discussed. Expert opinion: Topical nanoparticle-based drug delivery systems have demonstrated significant progress. An ideal formulation should prolong retention time on the surface, enhance drug permeability through the ocular tissues, and efficiently deliver drugs to the targeted site. To design the rational targeting nanoparticle-based drug delivery system, a better understanding of the distribution of transporters and receptors on the eye is required. Ultimately, there is an urgent need to develop targeting hybrid drug delivery systems with the combination of the advantages of several nanocarriers.


Topical administration; nanoparticles; ocular drug delivery; posterior segment of the eye; targeting drug delivery system

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