title: Technology of stable, prolonged-release eye-drops containing Cyclosporine A, distributed between lipid matrix and surface of the solid lipid microspheres (SLM).
abstract: The aim of this study was to prepare solid lipid microspheres (SLM) with incorporated Cyclosporine A (Cs), suitable for ocular application. For this purpose, SLM were formulated by using different lipids and three different nonionic surfactants. The SLM were produced using a hot emulsification method. The SLM dispersions contained 10, 20 or 30% of lipid (w/w) and up to 2% (w/w) of Cs. The size of the microspheres with Cs ranged from 1 to 15 μm. Physically stable SLM with Cs were prepared using Compritol, as a lipid matrix, and Tween 80, as a surfactant. In contrast, dispersion with Precirol alone, formed semi-solid gels during storage, while in formulations with Precirol and Miglyol, crystals of Cs were observed. In vitro release profile of Compritol formulations showed that 40% of Cs is released within 1h, while the release of the following 40% takes more time, depending on lipid content in the formulations. The large part of Cs, added to SLM formulations (from 45 to 80%), was found on the surface of microparticles, but no drug crystallization occurred during a long-term storage.
authors.affiliation: Department of Pharmaceutical Technology, Medical University of Gdansk, ul. Hallera 107, Gdansk 80-416, Poland.
authors.forename: Eliza
authors.initials: E
authors.lastname: Wolska
authors.forename: Małgorzata
authors.initials: M
authors.lastname: Sznitowska
mesh_terms: D003460:Crystallization; D016572:Cyclosporine / Q000008:administration & dosage / Q000737:chemistry*; D003692:Delayed-Action Preparations; D004075:Diglycerides / Q000737:chemistry; D004355:Drug Stability; D004356:Drug Storage; D005079:Excipients / Q000737:chemistry*; D005227:Fatty Acids / Q000737:chemistry; D005782:Gels; D007166:Immunosuppressive Agents / Q000008:administration & dosage / Q000737:chemistry*; D008055:Lipids / Q000737:chemistry*; D008863:Microspheres; D009883:Ophthalmic Solutions; D010316:Particle Size; D011136:Polysorbates / Q000737:chemistry; D013501:Surface-Active Agents / Q000737:chemistry; D013678:Technology, Pharmaceutical; D013997:Time Factors; D014280:Triglycerides / Q000737:chemistry
chemical_list: D003692:Delayed-Action Preparations; D004075:Diglycerides; D005079:Excipients; D005227:Fatty Acids; D005782:Gels; D007166:Immunosuppressive Agents; D008055:Lipids; D009883:Ophthalmic Solutions; D011136:Polysorbates; D013501:Surface-Active Agents; D014280:Triglycerides; C086409:glyceryl behenate; C022834:miglyol 812; D016572:Cyclosporine; C009032:precirol