Scholarlink

<p>Polyphenols are natural bioactive compounds with well-documented therapeutic properties. However, their clinical application is limited by poor bioavailability and physicochemical instability. This study aimed to design and evaluate a nanocarrier system based on functionalized graphene oxide (GO) and reduced graphene oxide (rGO) to improve polyphenol delivery. GO was synthesized using a modified Hummer’s method and subsequently reduced to rGO via gamma irradiation (Co⁶⁰, 35 KGy, 6&#xa0;h). Both nanocarriers were functionalized through PEGylation following carboxylation with NaOH and TCA to introduce –COOH groups. Polyphenols were extracted from <i>Cirsium arvense</i> flowers using methanol and encapsulated into the GO and rGO matrices. In terms of characterization, SEM revealed smoother surface features for GO and a more folded, aromatic morphology for rGO. FTIR verified successful reduction and PEGylation, while EDX analysis confirmed reduced oxygen content in rGO with an increased C: O ratio from GO (72:27) to rGO and the highest carbon enrichment observed in rGO-PEG (83:16). UV–Vis spectroscopy showed that GO exhibited a characteristic absorption band at 235&#xa0;nm, corresponding to π–π* transitions of C = O groups on the surface. In contrast, rGO displayed reduced absorption in the 220–230&#xa0;nm region due to the removal of oxygen-containing functional groups. DLS showed that GO, rGO, GO-P, and rGO-P had average particle sizes in the range of 26–42&#xa0;nm with good dispersity (PDI &lt; 0.34 ± 0.13), and a net negative surface charge (-10.2 to -18.5 mV). GO-PEG showed better loading (54%) compared to rGO–PEG (31%). Polyphenol release showed time-dependent behavior, with GO-PEG exhibiting sustained release up to 86.2% at 168&#xa0;h, while rGO-PEG displayed an initial burst release followed by slower release, reaching 79% at 168&#xa0;h. GO–P achieved 87% inhibition of α-chymotrypsin at 1&#xa0;mg/mL (IC<sub>50</sub> = 40&#xa0;µg/mL), while rGO–P showed lower activity (IC<sub>50</sub> = 124&#xa0;µg/mL). Inhibition against α-amylase (IC<sub>50</sub> = 600&#xa0;µg/mL), and α-glucosidase (IC<sub>50</sub> = 300&#xa0;µg/mL) was comparatively lower. In conclusion, these preliminary findings indicate that PEGylated GO represents a promising nanosystem for sustained delivery and enhanced bioactivity of polyphenols, particularly in enzyme-targeted therapeutic applications.</p> Graphical Abstract <p></p>

错误：搜索内容不能为空，请输入英文关键词
错误：关键词超出字数限制，请精简
高级检索

PEGylated Graphene Oxide Nanocomposites Show Sustained Delivery and Enhanced Enzymatic Inhibition Potential of Cirsium Arvense Polyphenols

  • 期刊论文

  • 发表日期：

    2026年3月17日

查看全文
  • Muhammad Sohail Khan,
  • Fawad Islam,
  • Farman Ali Khan,
  • Riffat Aziz,
  • Mahmood Iqbal,
  • Shujaat Ahmad,
  • Muhammad Esa

摘要

Polyphenols are natural bioactive compounds with well-documented therapeutic properties. However, their clinical application is limited by poor bioavailability and physicochemical instability. This study aimed to design and evaluate a nanocarrier system based on functionalized graphene oxide (GO) and reduced graphene oxide (rGO) to improve polyphenol delivery. GO was synthesized using a modified Hummer’s method and subsequently reduced to rGO via gamma irradiation (Co⁶⁰, 35 KGy, 6 h). Both nanocarriers were functionalized through PEGylation following carboxylation with NaOH and TCA to introduce –COOH groups. Polyphenols were extracted from Cirsium arvense flowers using methanol and encapsulated into the GO and rGO matrices. In terms of characterization, SEM revealed smoother surface features for GO and a more folded, aromatic morphology for rGO. FTIR verified successful reduction and PEGylation, while EDX analysis confirmed reduced oxygen content in rGO with an increased C: O ratio from GO (72:27) to rGO and the highest carbon enrichment observed in rGO-PEG (83:16). UV–Vis spectroscopy showed that GO exhibited a characteristic absorption band at 235 nm, corresponding to π–π* transitions of C = O groups on the surface. In contrast, rGO displayed reduced absorption in the 220–230 nm region due to the removal of oxygen-containing functional groups. DLS showed that GO, rGO, GO-P, and rGO-P had average particle sizes in the range of 26–42 nm with good dispersity (PDI < 0.34 ± 0.13), and a net negative surface charge (-10.2 to -18.5 mV). GO-PEG showed better loading (54%) compared to rGO–PEG (31%). Polyphenol release showed time-dependent behavior, with GO-PEG exhibiting sustained release up to 86.2% at 168 h, while rGO-PEG displayed an initial burst release followed by slower release, reaching 79% at 168 h. GO–P achieved 87% inhibition of α-chymotrypsin at 1 mg/mL (IC50 = 40 µg/mL), while rGO–P showed lower activity (IC50 = 124 µg/mL). Inhibition against α-amylase (IC50 = 600 µg/mL), and α-glucosidase (IC50 = 300 µg/mL) was comparatively lower. In conclusion, these preliminary findings indicate that PEGylated GO represents a promising nanosystem for sustained delivery and enhanced bioactivity of polyphenols, particularly in enzyme-targeted therapeutic applications.

Graphical Abstract