Nanostructured lipid carrier (NLC) coated with Chitosan Oligosaccharides and its potential use in ocular drug delivery system.
The objective of the present investigation was to explore the potential of the Chitosan Oligosaccharides (COS)-coated NLC (nanostructured lipid carrier) for ocular drug delivery. NLC loaded with flurbiprofen was prepared by melt-ultrasonic method and then coated with COS with a molecular weight of 3000-6000kDa. After coating, the particles reflected spherical morphology with smooth surface under transmission electron microscope (TEM) analysis and a changed zeta potential from -0.446mV to +20.7mV. The ocular bioadhesion property was evaluated by Gamma scintigraphic technique, revealing that the clearance of the formulations labeled with radioactive 99(m)Tc-DTPA was significantly delayed in the presence of COS, and the AUC of the COS-coated formulation had a 7.7-fold increase comparing with non-coated ones. Additionally, enhanced transcorneal penetration was achieved by using the COS coating with a corresponding apparent permeability coefficients (P(app)) which had a 2.4-fold increase comparing with the reference. Consequently, COS coating modified the properties of NLCs and presented a series of notable advantages in ophthalmic application.
Luo
Qiuhua
Q
School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, People's Republic of China. bluer lz@163.com
Zhao
Junming
J
Zhang
Xiangrong
X
Pan
Weisan
W
D000268:Adhesiveness; D000287:Administration, Topical; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000009:adverse effects; D048271:Chitosan / Q000009:adverse effects / Q000737:chemistry*; D003315:Cornea / Q000187:drug effects / Q000378:metabolism*; D004337:Drug Carriers / Q000009:adverse effects / Q000737:chemistry*; D004339:Drug Compounding; D005480:Flurbiprofen / Q000008:administration & dosage* / Q000009:adverse effects; D066298:In Vitro Techniques; D008297:Male; D046529:Microscopy, Electron, Transmission; D049329:Nanostructures / Q000009:adverse effects / Q000737:chemistry*; D009844:Oligosaccharides / Q000009:adverse effects / Q000737:chemistry*; D010316:Particle Size; D010539:Permeability; D011817:Rabbits; D013499:Surface Properties
D000894:Anti-Inflammatory Agents, Non-Steroidal; D004337:Drug Carriers; D009844:Oligosaccharides; D005480:Flurbiprofen; D048271:Chitosan