Your browser version may not work well with NCBI's Web applications. More information here...
1: Exp Eye Res. 2008 Sep;87(3):162-7. Epub 2008 Apr 12.Click here to read Links

Hyaluronic acid coated poly-epsilon-caprolactone nanospheres deliver high concentrations of cyclosporine A into the cornea.

Yenice I, Mocan MC, Palaska E, Bochot A, Bilensoy E, Vural I, Irkeç M, Hincal AA.

Department of Pharmaceutical Technology, Faculty of Pharmacy, Hacettepe University, 06100 Ankara, Turkey. iyenice@hacettepe.edu.tr

The objective of this study was to determine cyclosporine A (Cy A) levels in ocular tissues and fluids after topical administration of poly-epsilon-caprolactone (PCL)/benzalkonium chloride (BKC) nanospheres and hyaluronic acid (HA) coated PCL/BKC nanospheres onto healthy rabbit corneas. Nanospheres were prepared by nanoprecipitation and purified by gradient-rate centrifugation. Cy A (0.1%) in either castor oil solution (group 1), PCL/BKC nanosphere formulation (group 2) or HA coated PCL/BKC nanosphere formulation (group 3) was instilled onto rabbit corneas. Tear samples were adsorbed onto Schirmer tear strips. Cy A concentrations of fluid (blood, aqueous humor, tear) and specimen extracts (cornea, conjunctiva, iris/ciliary body) were determined by high performance liquid chromatography-mass spectrometry (LC-MS). The mean corneal Cy A concentration obtained at 0.5, 1, 2, 4, 8 and 24h following instillation of the formulations ranged between 0.12 and 1.2 ng/mg tissue for group 1, 5.9-15.5 ng/mg tissue for group 2 and 11.4-23.0 ng/mg for group 3 (one-way analysis of variance (ANOVA) and pairwise tests (SNK (Student-Newman-Keuls) and Tukey); p<0.05). Conjunctival Cy A levels of group 2 and 3 were not significantly different at any of the time points tested. However, there was a significant difference between Cy A concentration of castor oil formulation and that of PCL/BKC nanosphere formulation at 1 and 8h (p<0.05). The mean iris/ciliary body concentrations obtained with the three formulations were not significantly different at any time point with the exception of group 2 levels being higher than those of groups 1 and 3 at 1h (p<0.05). The lowest ocular tear Cy A concentrations (16-114 ng/ml) were found following the instillation of HA coated PCL/BKC nanoparticles (group 3) during the time period tested. Cy A loaded PCL/BKC and HA coated PCL/BKC nanospheres are able to achieve high levels of Cy A in the cornea that is 10-15-fold higher than that is achieved with Cy A solution in castor oil. Nanosphere formulation and HA may play an important role in delivering high levels of cyclosporine A into the cornea.

PMID: 18675411 [PubMed - indexed for MEDLINE]

Patient Drug Information

  • Cyclosporine (Neoral® , Sandimmune® , Gengraf® )

    Cyclosporine and cyclosporine (modified) are used with other medications to prevent transplant rejection (attack of the transplanted organ by the immune system of the person who received the organ) in people who have rec...

  • How to Use Eyedrops

    Wash your hands thoroughly with soap and water. Check the dropper tip to make sure that it is not chipped or cracked. Avoid touching the dropper tip against your eye or anything else—eyedrops and dropper must be k...

  • Cyclosporine Ophthalmic (Restasis® )

    Cyclosporine ophthalmic is used to increase tear production in people with dry eye disease. Cyclosporine ophthalmic is in a class of medications called immunomodulators. It works by decreasing swelling in the eye to allo...

  • Source: AHFS Consumer Medication Information