title: Cationic lipid emulsions as potential bioadhesive carriers for ophthalmic delivery of palmatine.
abstract: Palmatine (PM) is a potent anti-infective agent used to treat eye diseases. However, PM is less effective for ocular application due to short residence time within the eyes. This study aimed to develop a cationic lipid emulsions (CLEs) for ophthalmic delivery of PM and evaluate its suitability in infection treatment. PM-loaded CLEs (PM-CLEs) were prepared through emulsifying/high-pressure homogenisation and characterised by particle size, ζ potential and morphology. The resulting PM-CLEs possessed a particle size of 192 nm and ζ potential of 45 mV around. In vitro release illustrated that PM was released less from CLEs. Corneal bioadhesion test showed that PM-CLEs exhibited an enhanced ocular residence time. Improved anti-infective activity was achieved in the model of fungus-induced keratitis. Furthermore, PM-CLEs demonstrated predominant cellular uptake and internalisation in the corneal epithelial cells. These results provide proof of concept that CLEs are promising bioadhesive carriers for ophthalmic delivery of PM.
authors.affiliation: a Department of Pharmaceutics , Huaihe Hospital Affiliated to Henan University , Kaifeng , P.R. China.
authors.forename: Juntao
authors.initials: J
authors.lastname: Yin
authors.affiliation: a Department of Pharmaceutics , Huaihe Hospital Affiliated to Henan University , Kaifeng , P.R. China.
authors.forename: Cuiyu
authors.initials: C
authors.lastname: Xiang
authors.affiliation: a Department of Pharmaceutics , Huaihe Hospital Affiliated to Henan University , Kaifeng , P.R. China.
authors.forename: Guangxiu
authors.initials: G
authors.lastname: Lu
mesh_terms: D000268:Adhesiveness; D060433:Administration, Ophthalmic; D000818:Animals; D000890:Anti-Infective Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use*; D001600:Berberine Alkaloids / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use*; D002412:Cations / Q000737:chemistry; D002460:Cell Line; D003315:Cornea / Q000378:metabolism / Q000382:microbiology; D004337:Drug Carriers / Q000737:chemistry*; D004655:Emulsions / Q000737:chemistry*; D006168:Guinea Pigs; D006801:Humans; D007634:Keratitis / Q000188:drug therapy* / Q000382:microbiology; D010316:Particle Size
chemical_list: D000890:Anti-Infective Agents; D001600:Berberine Alkaloids; D002412:Cations; D004337:Drug Carriers; D004655:Emulsions; C005413:palmatine
keywords: Palmatine; anti-infection; bioadhesion; cationic lipid emulsions; ophthalmic delivery