title: Fabrication and characterization of silk fibroin-coated liposomes for ocular drug delivery.
abstract: The unique structure and protective mechanisms of the eye result in low bioavailability of ocular drugs. Using a mucoadhesive material is an efficient solution to improve ocular drug therapeutic efficacy. This study was designed to prepare a liposomal formulation coated by a novel adhesive excipient, silk fibroin (SF), for topical ocular drug delivery. The regenerated silk fibroins (SFs) with different dissolving time were coated onto the ibuprofen-loaded liposomes. The morphology, drug encapsulation efficiency, in vitro release and in vitro corneal permeation of SF-coated liposomes (SLs) were investigated in comparison with the conventional liposome. Cellular adhesion and cytotoxicity assay of SF and SLs were tested using human corneal epithelial cells (HCEC). SLs showed sustained drug release and in vitro corneal permeation of ibuprofen as compared to drug solution and conventional liposome. The cellular fluorescence appeared after 7 min of exposure to SF, and the intensity increased sustainedly up to 12h with no detectable cytotoxicity. Higher fluorescence intensity of Nile red in SLs was observed in a short period of 15 min showing a rapid uptake. These favorable properties make SF-coated liposome be a promising ocular drug delivery system.
authors: School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, China; Research and Development Center of Pharmaceutical Engineering, Sun Yat-sen University, Guangzhou, China.
authors: Yixuan
authors: Y
authors: Dong
authors: School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, China.
authors: Pin
authors: P
authors: Dong
authors: School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, China.
authors: Di
authors: D
authors: Huang
authors: School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, China.
authors: Liling
authors: L
authors: Mei
authors: School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, China.
authors: Yaowen
authors: Y
authors: Xia
authors: School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, China.
authors: Zhouhua
authors: Z
authors: Wang
authors: School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, China; Guangdong Research Center for Drug Delivery Systems, Guangzhou, China. Electronic address: pxin_1385@163.com.
authors: Xin
authors: X
authors: Pan
authors: Guangzhou Neworld Pharm. Co. Ltd., Guangzhou, China.
authors: Ge
authors: G
authors: Li
authors: School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, China; Research and Development Center of Pharmaceutical Engineering, Sun Yat-sen University, Guangzhou, China; Guangdong Research Center for Drug Delivery Systems, Guangzhou, China. Electronic address: chuanbin_wu@126.com.
authors: Chuanbin
authors: C
authors: Wu
mesh_terms: D000268:Adhesiveness; D060433:Administration, Ophthalmic; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000009:adverse effects / Q000737:chemistry* / Q000378:metabolism; D012831:Bombyx / Q000737:chemistry; D002470:Cell Survival / Q000187:drug effects; D002478:Cells, Cultured; D003315:Cornea / Q000166:cytology / Q000187:drug effects / Q000378:metabolism*; D003692:Delayed-Action Preparations / Q000008:administration & dosage / Q000009:adverse effects / Q000737:chemistry / Q000378:metabolism; D004339:Drug Compounding; D016503:Drug Delivery Systems / Q000009:adverse effects; D065546:Drug Liberation; D005079:Excipients / Q000009:adverse effects / Q000737:chemistry* / Q000302:isolation & purification; D005349:Fibroins / Q000009:adverse effects / Q000737:chemistry* / Q000302:isolation & purification; D006801:Humans; D007052:Ibuprofen / Q000008:administration & dosage / Q000009:adverse effects / Q000737:chemistry* / Q000378:metabolism; D008081:Liposomes; D065587:Ocular Absorption; D010316:Particle Size; D017433:Protein Structure, Secondary; D011679:Pupa / Q000737:chemistry; D013499:Surface Properties
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D003692:Delayed-Action Preparations; D005079:Excipients; D008081:Liposomes; C482288:fibroin, silkworm; D005349:Fibroins; D007052:Ibuprofen
keywords: Cell culture; Coating; Liposomes; Ocular drug delivery; Silk fibroin; Sustained release