In vitro and in vivo performance of epinastine hydrochloride-releasing contact lenses

• Published in: PloS one Vol. 14; no. 1; p. e0210362
• Main Authors: Minami, Takahiro, Ishida, Waka, Kishimoto, Tatsuma, Nakajima, Isana, Hino, Shiori, Arai, Ritsuko, Matsunaga, Toru, Fukushima, Atsuki, Yamagami, Satoru
• Format: Journal Article
• Language: English
• Published: United States Public Library of Science 30.01.2019; Public Library of Science (PLoS)
• Subjects: Allergies; Animals; Biology and Life Sciences; Care and treatment; Conjunctivitis; Conjunctivitis, Allergic - chemically induced; Conjunctivitis, Allergic - drug therapy; Contact lenses; Contact Lenses, Hydrophilic; Delayed-Action Preparations - administration & dosage; Delayed-Action Preparations - pharmacokinetics; Dibenzazepines - administration & dosage; Dibenzazepines - pharmacokinetics; Disease Models, Animal; Dosage and administration; Drug delivery; Drug Delivery Systems; Engineering and Technology; Epinastine; Functional groups; Glaucoma; Guinea Pigs; Hay fever; Histamine - toxicity; Histamine H1 Antagonists - administration & dosage; Histamine H1 Antagonists - pharmacokinetics; Hydrogels; Imidazoles - administration & dosage; Imidazoles - pharmacokinetics; In Vitro Techniques; In vivo methods and tests; Male; Medical schools; Medicine and Health Sciences; Methods; Ophthalmic agents; Ophthalmic Solutions; Osmolar Concentration; Patient compliance; Patient outcomes; Phosphates; Physical Sciences; Polymerization; Quality of life; Releasing; Research and Analysis Methods; Soft contact lenses; Surface active agents; Japan
• DOI: 10.1371/journal.pone.0210362
• ISSN: 1932-6203

A number of drug-releasing contact lenses are currently being studied to address issues inherent in eye drops as a drug delivery method. In this study, we developed epinastine hydrochloride-releasing daily soft contact lenses for treatment of allergic conjunctivitis and examined their in vitro and in vivo performance. Preformed soft contact lenses with/without ionic functional groups were soaked in a solution of epinastine hydrochloride in phosphate-buffered saline to prepare epinastine hydrochloride-releasing soft contact lenses. Among these contact lenses with different ionicities, anionic lenses demonstrated the maximum, relatively linear epinastine hydrochloride release, in vitro. The amount of epinastine hydrochloride release was directly proportional to the concentration of the epinastine hydrochloride solution used to prepare the contact lens. The epinastine hydrochloride-releasing anionic soft contact lens also demonstrated prolonged drug release and significantly greater efficacy compared with epinastine hydrochloride eye drops 12 h after treatment, in vivo. Further studies are required to determine the appropriate amount of epinastine hydrochloride to be contained in the anionic soft contact lenses.