title: The Effects of Lactidyl/Glycolidyl Ratio and Molecular Weight of Poly(D,L -Lactide-co-Glycolide) on the Tetracycline Entrapment and Release Kinetics of Drug-Loaded Nanofibers.
abstract: Electrospun tetracycline (Tet)-loaded poly(D,L-lactide-co-glycolide) (PLGA) nanofibers are considered to have great potential as local drug-delivery systems. This study was designed to explore the effects of the lactidyl/glycolidyl (LA/GA) unit ratio and molecular weight of PLGA on Tet entrapment efficiency and in vitro release kinetics. Three kinds of PLGA (PLGA75/25, M w = 100 000 or 50 000; PLGA50/50, M w = 50 000) were examined in this study. Electrospun nanofibers were fabricated containing 3, 5, 10 wt% Tet. The results showed that PLGA50/50 entrapped more Tet than both PLGA75/25 co-polymers, and the PLGA75/25 of M w = 100 000 entrapped the least amount of Tet, suggesting that the lower the molecular weight of PLGA was, the higher the GA content in PLGA was and the higher the resulting Tet entrapment. Tet loading played an important role in Tet release. Nanofibers with 3 and 5 wt% Tet loading exhibited a sustained release for more than 28 days, whereas 10 wt% Tet only lasted 14 days. Loading of 3 wt% Tet resulted in approx. 35% release in the initial 12 h, 5 wt% Tet released approx. 70% and 10 wt% Tet resulted in approx. 85% release. The integrity of Tet incorporated into electrospun PLGA nanofibers was identified by FT-IR spectrum examination and the bacterial inhibition test. The modified Kirby-Bauer test showed dose-dependent inhibition of Staphylococcus aureus growth by Tet, confirming Tet structural stability throughout the electrospinning procedure. MG-63 cells demonstrated good adhesion and proliferation on all PLGA/Tet fibrous membranes. These results indicate that Tet entrapment and release kinetics of PLGA/Tet composite fibrous scaffolds can be tailored by the LA/GA ratios, molecular weights and drug loadings. Tet-loaded fibrous scaffolds show great potential for local drug delivery and bone defect repair.
authors.affiliation: a Department of Geriatric Dentistry, Peking University School and Hospital of Stomatology, Beijing 100081, P. R. China.
authors.forename: Na
authors.initials: N
authors.lastname: Yan
authors.forename: Xuehui
authors.initials: X
authors.lastname: Zhang
authors.forename: Qing
authors.initials: Q
authors.lastname: Cai
authors.forename: Xiaoping
authors.initials: X
authors.lastname: Yang
authors.forename: Xuegang
authors.initials: X
authors.lastname: Zhou
authors.forename: Bo
authors.initials: B
authors.lastname: Wang
authors.forename: Xuliang
authors.initials: X
authors.lastname: Deng
mesh_terms: D000818:Animals; D000890:Anti-Infective Agents / Q000737:chemistry* / Q000494:pharmacology; D002448:Cell Adhesion / Q000187:drug effects; D002460:Cell Line; D049109:Cell Proliferation / Q000187:drug effects; D004146:Dioxanes / Q000737:chemistry*; D004337:Drug Carriers / Q000737:chemistry*; D065546:Drug Liberation; D004560:Electricity; D006801:Humans; D007700:Kinetics; D051379:Mice; D008970:Molecular Weight; D057139:Nanofibers / Q000737:chemistry*; D010006:Osteoblasts / Q000166:cytology / Q000187:drug effects; D011098:Polyglactin 910 / Q000737:chemistry*; D013211:Staphylococcus aureus / Q000187:drug effects; D013752:Tetracycline / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D000890:Anti-Infective Agents; D004146:Dioxanes; D004337:Drug Carriers; D011098:Polyglactin 910; C091880:dilactide; D013752:Tetracycline