Stability and Drug Loading of Spontaneous Vesicles of Comb-Like PEG Derivates

✍ Scribed by Xiaolin Li; Jian Ji; Xiaoli Wang; Youxiang Wang; Jiacong Shen

• Publisher: John Wiley and Sons
• Year: 2007
• Tongue: English
• Weight: 265 KB
• Volume: 28
• Category: Article
• ISSN: 1022-1336
• DOI: 10.1002/marc.200600723

✦ Synopsis

Abstract

A novel comb‐like derivative CPEG‐g‐cholesterol was prepared by the reaction of cholesteryl chloroformate with hydroxyl groups of CPEG. The TEM and SEM results showed that CPEG‐cholesterol spontaneously aggregated vesicles with the membrane thickness of 4.27 ± 0.48 nm. Compared with the vesicles formed by comb‐like PEG (CPEG), the derivation of cholesteryl chloroformate increased the thickness of vesicle membrane and developed corrugations. The hydrophobic doxorubicin (Dox) was added into the solution of CPEG and CPEG‐g‐cholesterol to test their vesicle stability. The drug‐loaded vesicles of CPEG‐g‐cholesterol still existed but those of CPEG disappeared, which indicated that stability of vesicles was enhanced by the derived cholesteryl chloroformate. The vesicles were further cross‐linked by the reaction between divinyl sulfone (DVS) and the hydroxy groups in the side chains of the CPEG and CPEG‐g‐cholesterol. Both cross‐linked vesicles of CPEG and CPEG‐g‐cholesterol entrapped considerable hydrophobic Dox in the vesicles membrane. The spontaneous vesicles of CPEG‐g‐cholesterol and the crosslinked vesicles of CPEG and CPEG‐g‐cholesterol might have great potential as a cargo of the hydrophobic drug.

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