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使用 Eudragit RS100 对纳米级脂质载体的表面改性及其潜在的眼科功能

 

Authors Zhang W, Li X, Ye T, Chen F, Yu S, Chen J, Yang X, Yang N, Zhang J, Liu J, Pan W, Kong J

Published Date September 2014 Volume 2014:9(1) Pages 4305—4315

DOI http://dx.doi.org/10.2147/IJN.S63414

Received 3 March 2014, Accepted 25 May 2014, Published 11 September 2014

Abstract: This study was carried out to evaluate the ocular performance of a cationic Eudragit (EDU) RS 100-coated nanostructured lipid carrier (NLC). The genistein encapsulated NLC (GEN-NLC) was produced using the melt-emulsification technique followed by surface absorption of EDU RS 100. The EDU RS 100 increased the surface zeta potential from −7.46 mV to +13.60 mV, by uniformly forming a spherical coating outside the NLC surface, as shown by transmission electron microscopy images. The EDU RS 100 on the NLC surface effectively improved the NLC stability by inhibiting particle size growth. The obtained EDU RS 100-GEN-NLC showed extended precorneal clearance and a 1.22-fold increase in AUC (area under the curve) compared with the bare NLC in a Gamma scintigraphic evaluation. The EDU RS 100 modification also significantly increased corneal penetration producing a 3.3-fold increase in apparent permeability coefficients (Papp) compared with references. Draize and cytotoxicity testing confirmed that the developed EDU RS 100-GEN-NLC was nonirritant to ocular tissues and nontoxic to corneal cells. These results indicate that the NLC surface modified by EDU RS 100 significantly improves the NLC properties and exhibits many advantages for ocular use.
Keywords: genistein, precorneal retention, cytotoxicity






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