Biocompatibility and drug release behavior of curcumin conjugated gold nanoparticles from aminosilane-functionalized electrospun poly(N-vinyl-2-pyrrolidone) fibers

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• 作者：Alfin Kurniawan^a ; Farrel Gunawan^a ; Adi Tama Nugraha^a ; Suryadi Ismadji^b ; Meng-Jiy Wang^a ; ^{mjwang@mail.ntust.edu.tw}
• 关键词：Curcumin ; Gold nanoparticles ; Aminosilane functionalization ; Sustained release ; Biocompatibility
• 刊名：International Journal of Pharmaceutics
• 出版年：2017
• 出版时间：10 January 2017
• 年：2017
• 卷：516
• 期：1-2
• 页码：158-169
• 全文大小：2395 K
• 卷排序：516

文摘

Curcumin (CUR) has a wide spectrum of biological and pharmacological activities, yet problems of its bioavailability remained a major challenge in preclinical studies. Thus, the design of the delivery systems with CUR as a model drug featuring dual release process – an initial burst followed by sustained release – to provide the optimal drug pharmacokinetics in the therapeutic region has been actively pursued. In this study, the 3-aminopropyltriethoxysilane (APTES)-functionalized electrospun poly(N-vinyl-2-pyrrolidone) fibers (NH2-PVP) were utilized as a free-standing substrate for the immobilization of CUR-PVP capped gold nanoparticles (CUR-PGNPs) conjugates. The conjugate was synthesized by sonication and the drug entrapment percentage was determined to be 54.2  ± 1.8. CUR-PGNPs immobilized on NH2-PVP fibers showed a moderate burst release during the first few hours, followed by a sustained release lasting for 2 days. The drug release was found pH-dependent (pH 5.0 > 6.0 > 7.4). The two-stage release profiles of CUR-PGNPs@NH2-PVP fibers were fitted well to Korsmeyer-Peppas model, indicating a non-Fickian diffusion mechanism for initial burst release and Fickian diffusion-controlled mechanism for the sustained release. Initial biocompatibility assessments based on lactate dehydrogenase (LDH) assay and morphological examination by SEM with L-929 mouse fibroblasts revealed that CUR-PGNPs@NH2-PVP nanofibrous scaffold was capable of supporting cell growth over a culture period of 3 days.