Ocular gelling microspheres: in vitro Precorneal retention time and drug permeation through reconstituted corneal epithelium

Lorenzo Cordone, Libero Italo Giannola, Viviana De Caro, Lorenzo Cordone, Giulia Giandalia, Libero I. Giannola, Giulia Giandalia, Maria Gabriella Siragusa

Risultato della ricerca: Articlepeer review

15 Citazioni (Scopus)


Purpose: The model drug norfloxacin (NOR)was encapsulated into trehalose (TRH) and hydroxyethylcellulose(NAT) microspheres to obtain a novel gelling ophthalmic delivery system for prolonged release on corneal tissue. Methods: We assessed NOR release from microspheres, prepared by the emulsion-solvent evaporation method. A new in vitro tear turnover model, including inserts containing reconstituted human corneal epithelium (RHC), was designed to evaluate the TRH/NAT microspheres’ precorneal retention time. Bioadhesive properties of TRH/NAT microspheres were validated by using drug-loaded microspheres prepared with gelatine (GLT) commonly used as reference material in adhesion studies. Results: In vitro drug release showed a typical trend of swelling systems. Precorneal retention tests showed that TRH/NAT microspheres maintained fluorescence in tear fluid for 81.7 min, whereas TRH/GLT microspheres and water solution maintained fluorescence for 51.8 and 22.3 min, respectively. NOR released from microspheres permeated throughout RHC slower (Js = 23.08 μ g/cm2h) than NOR from commercial eye drops Js = 42.77 μ g/cm2h) used as the control. Conclusions: Adequate drug concentrations in aqueous humor could be prolonged after the administration of TRH/NAT/NOR microspheres. Good bioadhesive properties of the system and slow drug release on corneal surface might increase ocular NOR bioavailability.
Lingua originaleEnglish
pagine (da-a)186-196
Numero di pagine11
RivistaJournal of Ocular Pharmacology and Therapeutics
Stato di pubblicazionePublished - 2008

All Science Journal Classification (ASJC) codes

  • Ophthalmology
  • Pharmacology
  • Pharmacology (medical)

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