尾-Amino Acid and Amino-Alcohol Conjugation of a Nonsteroidal Anti-Inflammatory Drug (NSAID) Imparts Hydrogelation Displaying Remarkable Biostability, Biocompatibility, and Anti-Inflammatory Properties

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• 作者：Joydeb Majumder ; Mahua Rani Das ; Jolly Deb ; Siddhartha Sankar Jana ; Parthasarathi Dastidar
• 刊名：Langmuir
• 出版年：2013
• 出版时间：August 13, 2013
• 年：2013
• 卷：29
• 期：32
• 页码：10254-10263
• 全文大小：523K
• 年卷期：v.29,no.32(August 13, 2013)
• ISSN：1520-5827

文摘

A well-known nonsteroidal anti-inflammatory drug (NSAID), namely, naproxen (Np), was conjugated with 尾-alanine and various combinations of amino alcohols and l-alanine. Quite a few bioconjugates, thus synthesized, were capable of gelling pure water, NaCl solution (0.9 wt %), and phosphate-buffered saline (PBS) (pH 7.4). The hydrogels were characterized by rheology and electron microscopy. Hydrogelation was probed by FT-IR and temperature-variable ¹H NMR studies. Single-crystal X-ray diffraction (SXRD) of a nonhydrogelator and a hydrogelator in the series established a useful structure鈥損roperty (gelation) correlation. MTT assay of the hydrogelators in the mouse macrophage RAW 264.7 cell line showed excellent biocompatibility. The prostaglandin E₂ (PGE₂) assay of the hydrogelators revealed their anti-inflammatory response, which was comparable to that of the parent NSAID naproxen sodium (Ns).