Transport Route of Fluorescent Probe via Inner Ear Administration
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1. School of Pharmacy, Guangdong Pharmaceutical University, Guangzhou 510006, China; 2. Guangdong Provincial Key Laboratory of Advanced Drug Delivery, Guangzhou 510006, China
OBJECTIVE To investigate transport route of fluorescent probe following inner ear administration. METHODS Coumarin-6 (CM) was employed as fluorescent probe and CM-loaded poly(lactic-co-glycolic acid) nanoparticles (CM-PLGA-NP) were prepared by emulsification-solvent evaporation method. Perilymph (PL), contralateral PL, cerebrospinal fluid (CSF) and plasma were collected periodically in guinea pigs after unilateral intratympanic administration of CM-PLGA-NP or CM solution. The concentrations of CM were determined by high performance liquid chromatography (HPLC), and statistic program DAS was applied to the calculation of pharmacokinetic parameters. RESULTS CM was found in PL, contralateral PL and CSF after unilateral intratympanic administration of CM-PLGA-NP or CM solution. The AUC in PL and CSF following intratympanic administration of CM-PLGA-NP were respectively 3.7 and 7.6-fold higher than those following intratympanic administration of CM solution. And the ρmax in PL and CSF were respectively 9.9 and 9.0-fold higher. Moreover, CM-PLGA-NP extended the MRT in PL and CSF by 5.1 and 9.4 times compared with CM solution. CONCLUSION Transport pathway of intra-cochlear administration is PL→CSF→contralateral PL. Nanoparticles can greatly improve drug distribution within the inner ear and CSF, and prolong the residence time.
Transport Route of Fluorescent Probe via Inner Ear Administration[J]. Chinese Pharmaceutical Journal, 2012, 47(4): 279-282
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