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Tailored Polymersomes for Enhanced Oral Drug Delivery: pH‐Sensitive Systems for Intestinal Delivery of Immunosuppressants: pH-Sensitive Systems for Intestinal Delivery of Immunosuppressants

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Title: Tailored Polymersomes for Enhanced Oral Drug Delivery: pH‐Sensitive Systems for Intestinal Delivery of Immunosuppressants: pH-Sensitive Systems for Intestinal Delivery of Immunosuppressants
Authors: Matteo Tollemeto, Sintija Ursulska, Pascal L. W. Welzen, Lasse H. E. Thamdrup, Atena Malakpour‐Permlid, Yudong Li, Gohar Soufi, Tania Patiño Padial, Jørn B. Christensen, Line Hagner Nielsen, Jan van Hest, Anja Boisen
Source: Tollemeto, M, Ursulska, S, Welzen, P L W, Thamdrup, L H E, Malakpour Permlid, A, Li, Y, Soufi, G, Patiño Padial, T, Christensen, J B, Hagner Nielsen, L, van Hest, J & Boisen, A 2024, ' Tailored Polymersomes for Enhanced Oral Drug Delivery : pH-Sensitive Systems for Intestinal Delivery of Immunosuppressants ', Small, vol. 20, no. 43, 2403640 . https://doi.org/10.1002/smll.202403640
Publisher Information: Wiley, 2024.
Publication Year: 2024
Subject Terms: Polymersomes, Oral, Male, Mycophenolic Acid/chemistry, Polymers, IBD, mucosal barriers, Administration, Oral, 02 engineering and technology, 01 natural sciences, Drug Delivery Systems, Polymers/chemistry, Drug Delivery Systems/methods, Humans, Animals, Mucosal barriers, Immunosuppressive Agents/administration & dosage, oral administration, Mycophenolate mofetil, mycophenolate mofetil, Hydrogen-Ion Concentration, Mycophenolic Acid, Rats, 0104 chemical sciences, Oral administration, Intestinal Absorption, polymersomes, Administration, Nanoparticles, Nanoparticles/chemistry, Caco-2 Cells, 0210 nano-technology, Immunosuppressive Agents
Description: Ensuring precise drug release at target sites is crucial for effective treatment. Here, pH‐responsive nanoparticles for oral administration of mycophenolate mofetil, an alternative therapy for patients with inflammatory bowel disease unresponsive to conventional treatments is developed. However, its oral administration presents challenges due to its low solubility in the small intestine and high solubility and absorption in the stomach. Therefore, this aim is to design a drug delivery system capable of maintaining drug solubility compared to the free drug while delaying absorption from the stomach to the intestine. Successful synthesis and assembly of a block copolymer incorporating a pH‐responsive functional group is achieved. Dynamic light scattering indicated a significant change in hydrodynamic size when the pH exceeded 6.5, confirming successful incorporation of the pH‐responsive group. Encapsulation and controlled release of mycophenolate mofetil are efficiently demonstrated, with 90% release observed at intestinal pH. In vitro cell culture studies confirmed biocompatibility, showing no toxicity or adverse effects on Caco‐2 cells. In vivo oral rat studies indicated reduced drug absorption in the stomach and enhanced absorption in the small intestine with the developed formulation. This research presents a promising drug delivery system with potential applications in the treatment of inflammatory bowel disease.
Document Type: Article
File Description: application/pdf
Language: English
ISSN: 1613-6829
1613-6810
DOI: 10.1002/smll.202403640
Access URL: https://pubmed.ncbi.nlm.nih.gov/38963162
https://research.tue.nl/en/publications/0d3e8584-eb1c-475c-b0f0-e79a8d0f518e
https://doi.org/10.1002/smll.202403640
https://orbit.dtu.dk/en/publications/fb764b4e-1544-4b25-9437-324260de2818
https://curis.ku.dk/ws/files/410622786/Small_2024_Tollemeto_Tailored_Polymersomes_for_Enhanced_Oral_Drug_Delivery_pH_Sensitive_Systems_for_Intestinal.pdf
Rights: CC BY NC ND
Accession Number: edsair.doi.dedup.....48b3185738c8006e89fd4b8e3b682e62
Database: OpenAIRE
Description
Abstract:Ensuring precise drug release at target sites is crucial for effective treatment. Here, pH‐responsive nanoparticles for oral administration of mycophenolate mofetil, an alternative therapy for patients with inflammatory bowel disease unresponsive to conventional treatments is developed. However, its oral administration presents challenges due to its low solubility in the small intestine and high solubility and absorption in the stomach. Therefore, this aim is to design a drug delivery system capable of maintaining drug solubility compared to the free drug while delaying absorption from the stomach to the intestine. Successful synthesis and assembly of a block copolymer incorporating a pH‐responsive functional group is achieved. Dynamic light scattering indicated a significant change in hydrodynamic size when the pH exceeded 6.5, confirming successful incorporation of the pH‐responsive group. Encapsulation and controlled release of mycophenolate mofetil are efficiently demonstrated, with 90% release observed at intestinal pH. In vitro cell culture studies confirmed biocompatibility, showing no toxicity or adverse effects on Caco‐2 cells. In vivo oral rat studies indicated reduced drug absorption in the stomach and enhanced absorption in the small intestine with the developed formulation. This research presents a promising drug delivery system with potential applications in the treatment of inflammatory bowel disease.
ISSN:16136829
16136810
DOI:10.1002/smll.202403640