Production and Characterization of Colon Targeted pH Sensitive Macrospheres and Investıgation of Release Kinetics

Yıl 2023, Cilt: 27 Sayı: 2, 408 - 418, 30.04.2023

Ezgi Eren Belgin , Cankız Gizem Delibalta , Hüseyin Çiçek

https://doi.org/10.16984/saufenbilder.1137591

Öz

The gastrointestinal track has different pH values at different sections. Thus, it is not easy to carry a drug to the colon for absorption. pH sensitive polymeric macrosphere drug carriers have important advantages such as being able to be taken orally, targeting the active ingredient to the desired area and dosing the active ingredient at the desired concentration for a long time in the target area. In this contex pH sensitive sodium alginate-gelatin macrospheres were produced by the dispersion phase gelling and cross-linking (complex coacervation) process method then loaded with Sternbergia lutea extract in this study. The macrosphere extract release kinetics were investigated for different pH medias that simulates different sections of the gastrointestinal track. As a result, the produced drug carrier macrospheres released the active ingredient at the colon pH (pH 7.0) while at lower pH values did not show a significant extract release. Therefore, it was reported that the produced macrospheres have potential to be used for colon diseases treatments.

Anahtar Kelimeler

Colon targeted drug delivery, macrosphere, controlled release, release kinetics, pH sensitive

Destekleyen Kurum

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Proje Numarası

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Teşekkür

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Kaynakça

• [1] S. Amidon, J. E. Brown, Dave V. S., “Colon-targeted oral drug delivery systems: design trends and approaches,”An Official Journal of the American Association of Pharmaceutical Scientists, vol. 16, 4, pp: 731-41, 2015.
• [2] G. V. D. Mooter, Kinget R., “Oral colon-specific drug delivery: a review”,Drug Delivery,vol. 2, no.2, pp.81-93, 1995.
• [3] Z. Vinarov, M., Abdallah, J. A., Agundez, K., Allegaert, A. W., Basit, M., Braeckmans, J., Ceulemans, M., Corsetti, B. T., Griffin, M., Grimm, D., Keszthelyi, M., Koziolek, C. M., Madla, C., Matthys, L. E., McCoubrey, A., Mitra C., Reppas J., Stappaerts, N., Steenackers, N. L., Trevaskis P., Augustijns, “Impact of gastrointestinal tract variability on oral drug absorption and pharmacokinetics: an UNGAP review,” European Journal of Pharmaceutical Sciences, vol. 162, 2021.
• [4] S. Adepu, Ramakrishna S., “Controlled drug delivery systems: current status and future directions,”Molecules, vol. 26, no. 19, pp. 5905, 2021.
• [5] S. Hua, “Advances in oral drug delivery for regional targeting in the gastrointestinal tract - ınfluence of physiological, pathophysiological and pharmaceutical factors,“ Frontiers in Pharmacology, vol. 11, 2020.
• [6] A. Geraili, M. Xing, K. Mequanint, "Design and fabrication of drug‐delivery systems toward adjustable release profiles for personalized treatment," View, vol. 2, no. 5, 2021.
• [7] U. Nautyal, D. G. Deepak , "Oral sustained release tablets: an overview with a special emphasis on matrix tablet," International Journal of Health and Biological Sciences, vol. 3, no.1, pp. 06-13, 2020.
• [8] A. H. Teruel, I. Gonzalez-Alvarez, M., Bermejo, V. Merino, M. D. Marcos, F. Sancenon, M. Gonzalez-Alvarez, R. Martinez-Mañez, “New insights of oral colonic drug delivery systems for inflammatory bowel disease therapy,” International Journal of Molecular Sciences, vol. 21, no. 18, pp. 6502, 2020.
• [9] K. Ulrich, M. Schwab, “Topical delivery of therapeutic agents in the treatment of ınflammatory bowel disease,” Advanced Drug Delivery Reviews, vol. 57, no. 2, pp. 267-79, 2005.
• [10] R. Lalani, R. Samant, A. Misra, "Applications of polymers in small intestinal drug delivery,"Applications of Polymers in Drug Delivery (Second Edition), pp. 105-129, 2021.
• [11] H. Zhang, C. Yang, W. Zhou, Q. Luan, , W. Li, , Q. Deng, X. Dong, H. Tang, F. Huang, “A pH-responsive gel macrosphere based on sodium alginate and cellulose nanofiber for potential intestinal delivery of probiotics,”ACS Sustainable Chemistry & Engineering, vol. 6,no. 11, pp.13924-13931, 2018.
• [12] L. Liu, W. Yao, Y. Rao, X. Lu, J. Gao, “pH-responsive carriers for oral drug delivery: challenges and opportunities of current platforms,” Drug Delivery, vol. 24, no. 1, pp. 569-581, 2017.
• [13] F. Hsu, D. Yu, C. Huang, "Development of pH-sensitive pectinate/alginate microspheres for colon drug delivery," Journal of Materials Science: Materials in Medicine, vol. 24, no. 2, pp. 317-323, 2013.
• [14] Z. Yao, L. Ji, Z. Ahmad, J. Huang, M. Chang, J. Li, “Ganoderma lucidum polysaccharide loaded sodium alginate micro-particles prepared via electrospraying in controlled deposition environments,” International Journal of Pharmaceutics, vol. 524, pp. 148–158, 2017.
• [15] Ç. Aydın, A. Ermiş, R. Mammadov, "Phenolic contents and antioxidant properties of sternbergia lutea (l.) ker-gawl. ex sprengel ethanol extract," International Journal of Secondary Metabolite, vol. 2, no. 1, pp. 18-26, 2015.
• [16] E. Eren Belgin, H. Gönen, H. Çiçek, "Production of ganoderma lucidum extract loaded kıscgelatın-sodium alginate microspheres, investigation of release kinetics at different pH values and evaluation of kinetic models," Mugla Journal Of Science And Technology, vol. 8, no. 1, pp. 41-50, 2022.
• [17] N. Bahrin, N. Muhammad, N. Abdullah, B. H. A. Talip, S. Jusoh, S. W. Theng, "Effect of processing temperature on antioxidant activity of Ficus carica leaves extract," Journal of Science and technology, vol. 10, no. 2, 2018.
• [18] R. Gong, C. Li, S. Zhu, Y. Zhang, Y. Du, J. Jiang, “A novel pH-sensitive hydrogel based on dual crosslinked alginate/N-α-glutaric acid chitosan for oral delivery of protein,” Carbohydrate polymers, vol. 85, no. 4, pp. 869-874, 2011.
• [19] Q. Wang, W. Wang, J. Wu, A. Wang, “Effect of attapulgite contents on release behaviors of a pH sensitive carboxymethyl cellulose‐g‐poly (acrylic acid)/attapulgite/sodium alginate composite hydrogel bead containing diclofenac,” Journal Of Applied Polymer Science, vol. 124, no. 6, pp. 4424-4432, 2012.
• [20] I. Colinet, V. Dulong, G. Mocanu, L. Picton, D. Le Cerf, “Effect of chitosan coating on the swelling and controlled release of a poorly water-soluble drug from an amphiphilic and pH-sensitive hydrogel,” International Journal of Biological Macromolecules, vol. 47, no. 2, pp. 120-125, 2010.
• [21] S. Wang, Q. Zhang, B. Tan, L. Liu, L. Shi, “pH-sensitive poly (vinyl alcohol)/sodium carboxymethylcellulose hydrogel beads for drug delivery,” Journal of Macromolecular Science, Part B,vol. 50, no. 12, pp. 2307-2317, 2011.
• [22] S. Banerjee, S. Singh, S. S. Bhattacharya, P. Chattopadhyay, “Trivalent ion cross-linked pH sensitive alginate-methyl cellulose blend hydrogel beads from aqueous template,” International Journal of Biological Macromolecules, vol. 57, pp. 297-307, 2013.
• [23] B. Yang, Y. Lu, T. Ren, G. Luo, “One-step synthesis of pH-sensitive poly (acrylamide-co-sodium acrylate) beads with core–shell structure,” Reactive and Functional Polymers, vol.73, no. 1, pp. 122-131, 2013.
• [24] M. S. M. Eldin, E. A. Kamoun, M. A. Sofan, and S. M. Elbayomi, “L-Arginine grafted alginate hydrogel beads: A novel pH-sensitive system for specific protein delivery,” Arabian Journal of Chemistry, vol. 8, no. 3, pp. 355-365, 2015.
• [25] L. Li, C. Dong, L. Liu, J. Li, K. Xiao, D. Zhang, X. Li “Preparation and characterization of pH-controlled-release intelligent corrosion inhibitor,” Materials Letters,vol. 116, pp. 318-321, 2014.
• [26] S. Dash, P. N. Murthy, L. Nath, P. Chowdhury, “Kinetic modeling on drug release from controlled drug delivery systems,” Acta Poloniae Pharmaceutica in Drug Research, vol. 67, no. 3, pp. 217-223, 2010.
• [27] G. Singhvi, M. Singh, “Review: In-Vitro Drug Release Characterization Models,” International Journal of Pharmaceutical Studies and Research, vol. 2, no. 1, pp. 77-84, 2011.