Research on the comparison of the demethylvancomycin's diffusion-deposition characteristics in the ocular solid tissues of sustained subtenon drug delivery with subconjunctival injection.
OBJECTIVE
To compare the demethylvancomycin's diffusion-deposition characteristics in the ocular solid tissues of sustained subtenon drug delivery with subconjunctival injection.


METHODS
Sixty adult white rabbits were randomly assigned to the subtenon drug delivery group and the subconjunctival injection group. The subtenon drug delivery group was continuously infused demethylvancomycin to the subtenon of rabbits. The subconjunctival injection group was injected demethylvancomycin to the subconjunctival of rabbits. Cornea, iris and sclera were collected for high-performance liquid chromatography analyses to determine drug concentrations at one hour, three hours, six hours, 12 h and 24 h of drug administration. WinNonlin 6.3 was used to calculate the parameters of cumulative area under the curve (AUCcum) of demethylvancomycin.


RESULTS
The peak levels of demethylvancomycin concentration of the subtenon drug delivery group and the subconjunctival injection group were 92.406 ± 21.555 and 51.778 ± 14.001 μg/g in cornea, 28.451 ± 10.229 μg/g and 42.271 ± 27.291 μg/g in iris, 153.166 ± 51.738 μg/g and 57.423 ± 18.480 μg/g in sclera. The differences of concentrations between the two groups in cornea and sclera were statistically significant (F = 487.775, p < 0.001; F = 132.748, p < 0.001). The difference in iris was not statistically significant (F = 4.848, p = 0.064). The maximum of AUCcumof the subtenon drug delivery group and the subconjunctival injection group was 1808.23 h * μg/g and 273.73 h * μg/g in cornea, 489.12 h * μg/g and 216.16 h * μg/g in iris and 2166.34 h * μg/g and 392.57 h * μg/g in sclera at 24 h of drug administration.


CONCLUSIONS
The sustained subtenon drug delivery had a better drug permeability and accumulation in the intraocular solid tissue compared to subconjunctival injection, which demonstrated it was probably a promising and effective approach for treating posterior segment diseases and endophthalmitis.
a Aier School of Ophthalmology, Central South University, ChangSha , P. R. China and.|b Changsha Aier Eye Hospital, ChangSha , P. R. China.
Yi-Qin
YQ
Duan
a Aier School of Ophthalmology, Central South University, ChangSha , P. R. China and.|b Changsha Aier Eye Hospital, ChangSha , P. R. China.
Ye-Zhen
YZ
Yang
a Aier School of Ophthalmology, Central South University, ChangSha , P. R. China and.|b Changsha Aier Eye Hospital, ChangSha , P. R. China.
Xue-Tao
XT
Huang
a Aier School of Ophthalmology, Central South University, ChangSha , P. R. China and.|b Changsha Aier Eye Hospital, ChangSha , P. R. China.
Ding
D
Lin
D000818:Animals; D000900:Anti-Bacterial Agents / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D019540:Area Under Curve; D001682:Biological Availability; D002851:Chromatography, High Pressure Liquid; D003315:Cornea / Q000378:metabolism; D003692:Delayed-Action Preparations; D004058:Diffusion; D004339:Drug Compounding; D007263:Infusions, Parenteral; D056965:Injections, Intraocular; D007498:Iris / Q000378:metabolism; D010539:Permeability; D011817:Rabbits; D012590:Sclera / Q000378:metabolism; D013678:Technology, Pharmaceutical / Q000379:methods; D014018:Tissue Distribution; D014640:Vancomycin / Q000008:administration & dosage* / Q000031:analogs & derivatives* / Q000737:chemistry / Q000493:pharmacokinetics
D000900:Anti-Bacterial Agents; D003692:Delayed-Action Preparations; C000616553:demethylvancomycin; D014640:Vancomycin
Sustained subtenon drug delivery; area under the curve; demethylvancomycin; diffusion–deposition; intraocular solid tissues