TY - JOUR
T1 - One-Step Fabrication of Hollow Spherical Cellulose Beads Application in pH-Responsive Therapeutic Delivery
AU - Mohan, Tamilselvan
AU - Ajdnik, Urban
AU - Nagaraj, Chandran
AU - Lackner, Florian
AU - Dobaj Štiglic, Andreja
AU - Palani, Thirvengadam
AU - Amornkitbamrung, Lunjakorn
AU - Gradišnik, Lidija
AU - Maver, Uroš
AU - Kargl, Rupert
AU - Stana Kleinschek, Karin
PY - 2022/1/26
Y1 - 2022/1/26
N2 - The path to greater sustainability and the development of polymeric drug delivery systems requires innovative approaches. The adaptation and use of biobased materials for applications such as targeted therapeutic delivery is, therefore, in high demand. A crucial part of this relates to the development of porous and hollow structures that are biocompatible, pH-responsive, deliver active substances, and contribute to pain relief, wound healing, tissue regeneration, and so forth. In this study, we developed a facile single-step and water-based method for the fabrication of hollow spherical cellulose beads for targeted drug release in response to external pH stimuli. Through base-catalyzed deprotection, hydrophobic solid and spherical cellulose acetate beads are transformed into hydrophilic cellulose structures with a hollow interior (wall thickness: 150 μm and inner diameter: 650 μm) by a stepwise increment of temperature and treatment time. Besides the pH-responsive fluid uptake properties, the hollow cellulose structures exhibit a maximum encapsulation efficiency of 20-85% diclofenac (DCF), a nonsteroidal anti-inflammatory drug, used commonly to treat pain and inflammatory diseases. The maximum amount of DCF released in vitro increased from 20 to 100% when the pH of the release medium increased from pH 1.2 to 7.4. As for the DCF release patterns and kinetic models at specific pH values, the release showed a diffusion- and swelling-controlled profile, effortlessly fine-tuned by external environmental pH stimuli. Overall, we show that the modified beads exhibit excellent characteristics for transport across the gastrointestinal tract and enhance the bioavailability of the drug. Their therapeutic efficacy and biocompatibility are also evident from the studies on human fibroblast cells. We anticipate that this platform could support and inspire the development of novel sustainable and effective polysaccharide-based delivery systems.
AB - The path to greater sustainability and the development of polymeric drug delivery systems requires innovative approaches. The adaptation and use of biobased materials for applications such as targeted therapeutic delivery is, therefore, in high demand. A crucial part of this relates to the development of porous and hollow structures that are biocompatible, pH-responsive, deliver active substances, and contribute to pain relief, wound healing, tissue regeneration, and so forth. In this study, we developed a facile single-step and water-based method for the fabrication of hollow spherical cellulose beads for targeted drug release in response to external pH stimuli. Through base-catalyzed deprotection, hydrophobic solid and spherical cellulose acetate beads are transformed into hydrophilic cellulose structures with a hollow interior (wall thickness: 150 μm and inner diameter: 650 μm) by a stepwise increment of temperature and treatment time. Besides the pH-responsive fluid uptake properties, the hollow cellulose structures exhibit a maximum encapsulation efficiency of 20-85% diclofenac (DCF), a nonsteroidal anti-inflammatory drug, used commonly to treat pain and inflammatory diseases. The maximum amount of DCF released in vitro increased from 20 to 100% when the pH of the release medium increased from pH 1.2 to 7.4. As for the DCF release patterns and kinetic models at specific pH values, the release showed a diffusion- and swelling-controlled profile, effortlessly fine-tuned by external environmental pH stimuli. Overall, we show that the modified beads exhibit excellent characteristics for transport across the gastrointestinal tract and enhance the bioavailability of the drug. Their therapeutic efficacy and biocompatibility are also evident from the studies on human fibroblast cells. We anticipate that this platform could support and inspire the development of novel sustainable and effective polysaccharide-based delivery systems.
KW - beads
KW - cellulose acetate
KW - deacetylation
KW - diclofenac
KW - drug delivery
KW - fibroblast cells
KW - hollow structure
KW - targeted release
UR - http://www.scopus.com/inward/record.url?scp=85123341689&partnerID=8YFLogxK
U2 - 10.1021/acsami.1c19577
DO - 10.1021/acsami.1c19577
M3 - Article
C2 - 35014252
SN - 1944-8244
VL - 14
SP - 3726
EP - 3739
JO - ACS Applied Materials & Interfaces
JF - ACS Applied Materials & Interfaces
IS - 3
ER -