Mucoadhesive effect of thiolated PEG stearate and its modified NLC for ocular drug delivery
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- 作者：Jie Shen ; Yu Wang ; Qineng Ping ; Yanyu Xiao ; Xin Huang
- 关键词：Thiomers ; Polyethylene glycol stearate ; Mucoadhesive ; Nanostructured lipid carrier ; Precorneal retention
- 刊名：Journal of Controlled Release
- 出版年：2009
- 出版时间：4 August 2009
- 年：2009
- 卷：137
- 期：3
- 页码：217-223
- 全文大小：405 K
文摘
This study was to develop a thiolated non-ionic surfactant, cysteine-polyethylene glycol stearate (Cys-PEG-SA), for the assembling of nanoparticulate ocular drug delivery system with mucoadhesive property. Cys-PEG-SA was synthesized in two steps reaction involving a new derivative intermediate formation of p-nitrophenylcarbonyl-PEG-SA (pNP-PEG-SA). Up to 369.43 ± 25.54 μmol free thiol groups per gram of the conjugates was reached. The nanostructured lipid carrier (NLC) loaded cyclosporine A (CyA) was prepared by melt-emulsification method. The mucoadhesive NLC (Cys-NLC) was obtained by incubating NLC emulsion with Cys-PEG-SA. The mucoadhesive properties of these nanocarriers were examined by using mucin particles method. The particle size or zeta potential of the porcine mucin particles were changed with the added concentration of Cys-PEG-SA, and the disulphide bond breaker cysteine significantly reduced the adhesion of Cys-NLC to mucin particles (P < 0.05), whereas PEG-SA and NLC did not alternate the properties of the mucin particles. When Cys-NLC was administered topically to the rabbit eye, the encapsulated cyclosporine was found to remain on the ocular surface in the cul-de-sac for up to 6 h, both precorneal retention time and concentration were dramatically increased (P < 0.05), compared with the NLC without thiomer modification.