Fabrication, Characterization and in vitro Evaluation of Prednisolone Sustained Release Multiparticulate System for Colonic Targeting

Authors

  • Surra Lateef Abdulkadhim Department of Pharmaceutics, College of Pharmacy, Al-Mustansiriyah University, 10052 Baghdad, Iraq https://orcid.org/0009-0006-4935-8814
  • Masar Basim Mohsin Mohamed Department of Pharmaceutics, College of Pharmacy, Al-Mustansiriyah University, 10052 Baghdad, Iraq
  • Afrah Mohammed Hasan Salman Department of Pharmacology and Toxicology, College of Pharmacy, Al-Mustansiriyah University, 10052 Baghdad, Iraq

DOI:

https://doi.org/10.54133/ajms.v5i.253

Keywords:

Colon target beads, Eudragit S-100, Guar gum, Inulin, Pectin, Prednisolone

Abstract

Background: Prednisolone (PRD) is orally prescribed for inflammatory bowel syndrome (IBS) as the upper GIT is the main site of absorption; therefore, long-term PRD dosing decreases therapeutic effectiveness through systemic side effects. Objective: This work focused on formulating sustained-release alginate beads as a multiparticulate system for colon targeting using prednisolone (PRD) to be filled in an HPMC capsule. Methods: PRD beads were prepared by the ionotropic gelation technique using sodium alginate as the primary polymer and inulin, guar gum, and pectin as secondary polymers. In addition to the impact of polymer type and quantity, other factors were investigated: The CaCl2 concentration and tween 80 addition Thirteen formulations were successfully prepared, and their properties, such as bead size, morphology, percentage of encapsulation efficiency, yield, DL, in vitro release study in GIT buffer media, IBS media, SEM, and FTIR, were assessed. Results: The study showed that the beads were close in size, and the size was not an obstacle for loading the beads in HPMC capsules. Further, yield%, EE%, and DL% increased according to the bead’s content increase. Conclusions: The optimum formula was F3 that coated HPMC capsules with Eudragit S-100, which gave sustained release profiles in GIT and IBS simulating media, and F13 that could last the release in different pH media, pH 1.2, 6.8, and 7.4.

Downloads

Download data is not yet available.

References

local disorders. Polysaccharide Carriers for Drug Delivery: Elsevier; 2019. p. 737-62.

Iswandana R, Putri KSS, Putri FA, Gunawan M, Larasati SA. Challenge and development strategy for colon-targeted drug delivery system. Pharm Sci Res. 2022;9(1):17-27.

Lozoya-Agullo I, Gonzalez-Alvarez I, Merino-Sanjuan M, Bermejo M, González-Álvarez M. Preclinical models for colonic absorption, application to controlled release formulation development. Eur J Pharm Biopharm. 2018;130:247-259. doi: 10.1016/j.ejpb.2018.07.008. DOI: https://doi.org/10.1016/j.ejpb.2018.07.008

Auriemma G, Cerciello A, Aquino RP, Del Gaudio P, Fusco BM, Russo P. Pectin and zinc alginate: The right inner/outer polymer combination for core-shell drug delivery systems. Pharmaceutics. 2020;12(2):87. doi: 10.3390/pharmaceutics12020087. DOI: https://doi.org/10.3390/pharmaceutics12020087

Mehdi-alamdarlou S, Mozafari N, Daneshamooz S, Ashrafi H. Preparation and in vitro evaluation of controlled release granules of mesalazine for colon targeted drug delivery system. Trends Pharm Sci. 2022;8(1):37-42. doi: 10.30476/tips.2021.92954.1116.

Sarangi MK, Rao MB, Parcha V. Smart polymers for colon targeted drug delivery systems: a review. Int J Polym Mater Polym Biomater. 2021;70(16):1130-66. doi: 10.1080/00914037.2020.1785455. DOI: https://doi.org/10.1080/00914037.2020.1785455

Lanjhiyana S. Polysaccharides based novel and controlled released multiparticulate systems for colon-specific delivery: Contemporary scenario and future prospects. Asian J Pharmaceutics. 2020;14(4). doi: 10.22377/ajp.v14i4.3815. DOI: https://doi.org/10.22377/ajp.v14i4.3815

Cerciello A, Auriemma G, Morello S, Aquino RP, Del Gaudio P, Russo P. Prednisolone delivery platforms: Capsules and beads combination for a right timing therapy. PLoS One. 2016;11(7):e0160266. doi: 10.1371/journal.pone.0160266. DOI: https://doi.org/10.1371/journal.pone.0160266

Gunter EA, Popeyko OV. Calcium pectinate gel beads obtained from callus cultures pectins as promising systems for colon-targeted drug delivery. Carbohydr Polym. 2016;147:490-499. doi: 10.1016/j.carbpol.2016.04.026. DOI: https://doi.org/10.1016/j.carbpol.2016.04.026

Bagyalakshmi J, Raj A, Ravi T. Formulation, physical characterization and in-vitro release studies of prednisolone alginate beads for colon targeting by ionotropic gelation. Pharmacie Globale. 2011;3:1-4.

Araujo V, Gamboa A, Caro N, Abugoch L, Gotteland M, Valenzuela F, et al. Release of prednisolone and inulin from a new calcium-alginate chitosan-coated matrix system for colonic delivery. J Pharm Sci. 2013;102(8):2748-2759. doi: 10.1002/jps.23656. DOI: https://doi.org/10.1002/jps.23656

Youcef Benzine. Enzymatically triggered polymeric drug delivery systems for colon targeting. Thesis: Human health and pathology. Université de Lille, 2019.

Patel N, Lalwani D, Gollmer S, Injeti E, Sari Y, Nesamony J. Development and evaluation of a calcium alginate based oral ceftriaxone sodium formulation. Prog Biomater. 2016;5:117-133. doi: 10.1007/s40204-016-0051-9. DOI: https://doi.org/10.1007/s40204-016-0051-9

Asnani GP, Bahekar J, Kokare CR. Development of novel pH–responsive dual cross-linked hydrogel beads based on Portulaca oleracea polysaccharide-alginate-borax for colon specific delivery of 5-fluorouracil. J Drug Deliv Sci Technol. 2018;48:200-208. doi: 10.1016/j.jddst.2018.09.023. DOI: https://doi.org/10.1016/j.jddst.2018.09.023

Vecino X, Devesa-Rey R, Cruz J, Moldes A. Study of the physical properties of calcium alginate hydrogel beads containing vineyard pruning waste for dye removal. Carbohydr Polym. 2015;115:129-138. doi: 10.1016/j.carbpol.2014.08.088. DOI: https://doi.org/10.1016/j.carbpol.2014.08.088

Ansari M, Sadarani B, Majumdar A. Colon targeted beads loaded with pterostilbene: Formulation, optimization, characterization and in vivo evaluation. Saudi Pharm J. 2019;27(1):71-81. doi: 10.1016/j.jsps.2018.07.021. DOI: https://doi.org/10.1016/j.jsps.2018.07.021

Helmy AM, Elsabahy M, Soliman GM, Mahmoud MA, Ibrahim EA. Development and in vivo evaluation of chitosan beads for the colonic delivery of azathioprine for treatment of inflammatory bowel disease. Eur J Pharm Sci. 2017;109:269-279. doi: 10.1016/j.ejps.2017.08.025. DOI: https://doi.org/10.1016/j.ejps.2017.08.025

Martínez-Terán M, Hoang-Thi T, Flament M. Multiparticulate dosage forms for pediatric use. Pediatr Ther. 2017;7:314. doi: 10.4172/2161-0665.1000314. DOI: https://doi.org/10.4172/2161-0665.1000314

Kaur N, Singh B, Sharma S. Hydrogels for potential food application: Effect of sodium alginate and calcium chloride on physical and morphological properties. Pharma Innov J. 2018;7(7):142-148.

Sarangi M, Rao MB, Parcha V, Upadhyay A. Development and characterization of colon-targeting 5-fluorouracil multiparticulate beads. Indian J Pharm Sci. 2020;82(3):435-448. doi: 10.36468/pharmaceutical-sciences.666. DOI: https://doi.org/10.36468/pharmaceutical-sciences.666

Bale S, Khurana A, Reddy ASS, Singh M, Godugu C. Overview on therapeutic applications of microparticulate drug delivery systems. Crit Rev Ther Drug Carrier Syst. 2016;33(4). doi: 10.1615/CritRevTherDrugCarrierSyst.2016015798. DOI: https://doi.org/10.1615/CritRevTherDrugCarrierSyst.2016015798

Jung J, Arnold RD, Wicker L. Pectin and charge modified pectin hydrogel beads as a colon-targeted drug delivery carrier. Colloids Surf B Biointerfaces. 2013;104:116-121. doi: 10.1016/j.colsurfb.2012.11.042. DOI: https://doi.org/10.1016/j.colsurfb.2012.11.042

Jaiswal D, Bhattacharya A, Yadav IK, Singh HP, Chandra D, Jain D. Formulation and evaluation of oil entrapped floating alginate beads of ranitidine hydrochloride. Int J Pharm Pharm Sci. 2009;1(3):128-140.

Sarangi MK, Rao MB, Parcha V, Upadhyay A. Tailoring of colon targeting with sodium Alginate‐Assam bora rice starch based multi particulate system containing naproxen. Starch. 2020;72(7-8):1900307. doi: 10.1002/star.201900307. DOI: https://doi.org/10.1002/star.201900307

Atia A, Gomma AI, Fliss I, Beyssac E, Garrait G, Subirade M. Molecular and biopharmaceutical investigation of alginate–inulin synbiotic coencapsulation of probiotic to target the colon. J Microencapsul. 2017;34(2):171-184. doi: 10.1080/02652048.2017.1313330. DOI: https://doi.org/10.1080/02652048.2017.1313330

Das S. Pectin based multi-particulate carriers for colon-specific delivery of therapeutic agents. Int J Pharm. 2021;605:120814. doi: 10.1016/j.ijpharm.2021.120814. DOI: https://doi.org/10.1016/j.ijpharm.2021.120814

Osmałek T, Milanowski B, Froelich A, Szybowicz M, Białowąs W, Kapela M, et al. Design and characteristics of gellan gum beads for modified release of meloxicam. Drug Dev Indust Pharm. 2017;43(8):1314-1329. DOI: https://doi.org/10.1080/03639045.2017.1318896

Patole VC, Pandit AP. Mesalamine-loaded alginate microspheres filled in enteric coated HPMC capsules for local treatment of ulcerative colitis: in vitro and in vivo characterization. J Pharm Invest. 2018;48(3):257-267. doi: 10.1007/s40005-017-0304-1. DOI: https://doi.org/10.1007/s40005-017-0304-1

Mar JM, da Silva LS, Rabello MDS, Biondo MM, Kinupp VF, Campelo PH, et al. Development of alginate/inulin carrier systems containing non-conventional Amazonian berry extracts. Food Res Int. 2021;139:109838. doi: 10.1016/j.foodres.2020.109838. DOI: https://doi.org/10.1016/j.foodres.2020.109838

Mohamed MBM, Qaddoori ZS, Hameed GS. Study the effect of 12-hydroxyoctadecanoic acid concentration on preparation and characterization of floating organogels using cinnarizin as modeling drug. Iraqi J Pharm Sci. 2022;31(2):169-176. doi: 10.31351/vol31iss2pp169-176. DOI: https://doi.org/10.31351/vol31iss2pp169-176

Mohammed MA, Kadhim KA, Jasim GA, Fawzi HA. Metformin compared to insulin for the management of gestational diabetic. Int J Res Pharm Sci. 2018;9(3):1063-1067. DOI: https://doi.org/10.26452/ijrps.v9i3.1630

Downloads

Published

2023-09-27

How to Cite

Abdulkadhim, S. L., Mohamed, M. B. M., & Salman, A. M. H. (2023). Fabrication, Characterization and in vitro Evaluation of Prednisolone Sustained Release Multiparticulate System for Colonic Targeting. Al-Rafidain Journal of Medical Sciences ( ISSN 2789-3219 ), 5, 229–236. https://doi.org/10.54133/ajms.v5i.253

Issue

Section

Original article

Similar Articles

<< < 1 2 

You may also start an advanced similarity search for this article.