Abstract |
The aims of this study were to design and characterize methazolamide (MTZ)-loaded solid lipid nanoparticles (SLN) with and without modification of low molecular weight chitosan (CS) and compare their potentials for ocular drug delivery. Low molecular weight CS was obtained via a modified chemical oxidative degradation method. SLN with CS (CS-SLN-MTZ) and without CS (SLN-MTZ) were prepared according to a modified emulsion- solvent evaporation method. SLN-MTZ and CS-SLN-MTZ were 199.4 ± 2.8 nm and 252.8 ± 4.0 nm in particle size, -21.3 ± 1.9 mV and +31.3 ± 1.7 mV in zeta potential, respectively. Physical stability studies demonstrated that CS-SLN-MTZ remained stable for at least 4 months at 4 °C, while SLN-MTZ no more than 2 months. A prolonged in vitro release profile of MTZ from CS-SLN-MTZ was obtained compared with SLN-MTZ. Furthermore, CS-SLN-MTZ presented a better permeation property in excised rabbit cornea. In vivo studies indicated that the intraocular pressure lowering effect of CS-SLN-MTZ (245.75 ± 18.31 mmHg × h) was significantly better than both SLN-MTZ (126.74 ± 17.73 mmHg × h) and commercial product Brinzolamide Eye Drops AZOPT® (171.17 ± 16.45 mmHg × h). The maximum percentage decrease in IOP of CS-SLN-MTZ (42.78 ± 7.71%) was higher than SLN-MTZ (27.82 ± 4.15%) and was comparable to AZOPT (38.06 ± 1.25%). CS-SLN-MTZ showed no sign of ocular irritancy according to the Draize method and the histological examination.
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Authors | Fengzhen Wang, Li Chen, Dongsheng Zhang, Sunmin Jiang, Kun Shi, Yuan Huang, Rui Li, Qunwei Xu |
Journal | Journal of drug targeting
(J Drug Target)
Vol. 22
Issue 9
Pg. 849-58
(Nov 2014)
ISSN: 1029-2330 [Electronic] England |
PMID | 25045926
(Publication Type: Journal Article, Randomized Controlled Trial, Research Support, Non-U.S. Gov't)
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Chemical References |
- Drug Carriers
- Lipids
- Chitosan
- Methazolamide
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Topics |
- Animals
- Chitosan
(chemistry)
- Cornea
(metabolism)
- Double-Blind Method
- Drug Carriers
- Drug Stability
- Female
- Glaucoma
(drug therapy)
- Hydrogen-Ion Concentration
- Lipids
(chemistry)
- Male
- Methazolamide
(administration & dosage, pharmacology)
- Molecular Weight
- Nanoparticles
(chemistry)
- Particle Size
- Rabbits
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