Delivery of Potential Drugs to The Colon: Challenges and Strategies
Keywords:
active compound, challenges, colon, colon-targeted drug delivery systems, strategies
Abstract
Colon-targeted drug delivery systems have been exploited to treat local diseases in the colon, systemic delivery of protein and peptide, and chronotherapeutic drugs. The upper gastrointestinal tract restricts the effective delivery of these drugs. Therefore, several strategies are needed for targeted drugs directly to the colon, such as pH-sensitive polymers, enzyme-sensitive polymers, bacterially degradable polysaccharides, time-dependent polymers, and particulate systems. However, variable physiological conditions of the gastrointestinal tract in individuals cause combinations of these strategies are needed to ensure colonic delivery of the drug. This review presents and discusses several potential drugs and their approaches used to design and develop colon-targeted drug delivery systems for medications with particular characteristics.
References
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Lu L., Chen G., Qiu Y., Li M., Liu D., Hu D., Gu X., & Xiao Z., 2016. Nanoparticle-based oral delivery systems for colon targeting: principles and design strategies. Sci. Bull. 61(9): 670–681. https://doi.org/10.1007/s11434-016-1056-4
Ma Z., Ma R., Wang X., Gao J., Zheng Y., & Sun Z., 2019. Enzyme and PH responsive 5-flurouracil (5-FU) loaded hydrogels based on olsalazine derivatives for colon-specific drug delivery. Eur. Polym. J. 118: 64–70. https://doi.org/10.1016/j.eurpolymj.2019.05.017
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Morales-Burgos AM., Carvajal-Millan E., Rascón-Chu A., Martínez-López AL., Lizardi-Mendoza J., López-Franco YL., & Brown-Bojorquez F., 2019. Tailoring reversible insulin aggregates loaded in electrosprayed arabinoxylan microspheres intended for colon-targeted delivery. J. Appl. Polym. Sci. 136(38): 1–8. https://doi.org/10.1002/app.47960
Naeem M., Bae J., Oshi, AM., Kim MS., Moon HR., Lee BL., Im E., Jung Y., & Yoo JW., 2018. Colon-targeted delivery of cyclosporine A using dual-functional Eudragit® FS30D/PLGA nanoparticles ameliorates murine experimental colitis. Int. J. Nanomed. 13: 1225–1240. https://doi.org/10.2147/IJN.S157566
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Sharma N., Sharma A., Bhatnagar A., Nishad D., Karwasra R., Khanna K., Sharma D., Kumar N., & Jain GK., 2019. Novel gum acacia based macroparticles for colon delivery of Mesalazine: Development and gammascintigraphy study. J. Drug Del. Sci. Tech. 54, 101224. https://doi.org/10.1016/j.jddst.2019.101224
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Amidon S, Brown JE., & Dave VS., 2015. Colon-targeted oral drug delivery systems: Design trends and approaches. AAPS PharmSciTech. 16(4): 731–741. https://doi.org/10.1208/s12249-015-0350-9
Ballesta A., Innominato PF., Dallmann R., Rand DA., & Lévi FA., 2017). Systems chronotherapeutics. Pharmacol. Rev. 69(2): 161–199. https://doi.org/10.1124/pr.116.013441
Cesar ALA., Abrantes FA., Farah L., Castilho RO., Cardoso V., Fernandes SO., Araújo ID., & Faraco AAG., 2018. New mesalamine polymeric conjugate for controlled release: Preparation, characterization and biodistribution study. Eur. J. Pharm. Sci. 111: 57–64. https://doi.org/10.1016/j.ejps.2017.09.037
Cook MT., Tzortzis G., Charalampopoulos D., & Khutoryanskiy VV., 2012. Microencapsulation of probiotics for gastrointestinal delivery. J. Control. Release. 162(1): 56–67. https://doi.org/10.1016/j.jconrel.2012.06.003
Date AA., Hanes J., & Ensign LM., 2016. Nanoparticles for oral delivery: Design, evaluation and state-of-the-art. J. Control. Release. 240: 504–526. https://doi.org/10.1016/j.jconrel.2016.06.016
Elkhodairy KA., Elsaghir HA., & Al-Subayiel AM., 2014. Formulation of indomethacin colon targeted delivery systems using polysaccharides as carriers by applying liquisolid technique. BioMed. Res. Int. 2014: 1–17. https://doi.org/10.1155/2014/704362
Elsayed AM., 2012. Oral delivery of insulin: Novel approaches. IntechOpen. https://doi.org/10.5772/52265
Eun CS., & Han DS., 2015. Does the cyclosporine still have a potential role in the treatment of acute severe steroid-refractory ulcerative colitis? Gut Liver. 9(5): 567-568. https://doi.org/10.5009/gnl15293
Fang Y., Wang Q., Lin X., Jin X., Yang D., Gao S., Wang X., Yang M., & Shi K., 2019. Gastrointestinal responsive polymeric nanoparticles for oral delivery of insulin: optimized preparation, characterization, and in vivo evaluation. J. Pharm. Sci. 108(9): 2994–3002. https://doi.org/10.1016/j.xphs.2019.04.020
Goodman LS., & Gilman A., 2011. Anti-inflammatory, Antipyretic, and Analgesic Agents; Pharmacotherapy of Gout. In The Pharmacological Basis of Therapeutics (12th ed., p. 985). McGraw Hill.
Handali S., Moghimipour E., Rezaei M., Ramezani Z., Kouchak M., Amini M., Angali KA., Saremy S., & Dorkoosh FA., 2018. A novel 5-Fluorouracil targeted delivery to colon cancer using folic acid conjugated liposomes. Biomed. Pharmacother. 108: 1259–1273. https://doi.org/10.1016/j.biopha.2018.09.128
Iswandana R., Putri KSS., Dwiputra R., Yanuari T., Sari SP., & Djajadisastra J. (2017a). Formulation of chitosan tripolyphosphate-tetrandrine beads using ionic gelation method: In vitro and in vivo evaluation. Int. J. Appl. Pharm. 9(5): 109–115. https://doi.org/10.22159/ijap.2017v9i5.20842
Iswandana R., Putri KSS., Sandiata CE., Triani S., Sari SP., & Djajadisastra J., 2017b. Formulation of tetrandrine beads using ionic gelation method ca-pectinate coated ph-sensitive polymers as colon-targeted dosage form. Asian J. Pharm. Clin. Res. 10(10): 90. https://doi.org/10.22159/ajpcr.2017.v10i10.19994
Iswandana R., Putri KSS., Wulandari FR., Najuda G., Sari SP., & Djajadisastra J., 2018. Preparation of calcium alginate-tetrandrine beads using ionic gelation method as colon-targeted dosage form. J. Appl. Pharm. Sci. 8(5): 68–74. https://doi.org/10.7324/JAPS.2018.8509
Iwao Y., Tomiguchi I., Domura A., Mantaira Y., Minami A., Suzuki T., Ikawa T., Kimura S., & Itai S., 2018. Inflamed site-specific drug delivery system based on the interaction of human serum albumin nanoparticles with myeloperoxidase in a murine model of experimental colitis. Eur. J. Pharm. Biopharm. 125: 141–147. https://doi.org/10.1016/j.ejpb.2018.01.016
Jain D., Verma S., & Shukla S., 2012. Formulation and characterization of calcium chloride guar gum microsphere of theophylline. Chron. Young Sci. 3(2): 137. https://doi.org/10.4103/2229-5186.98686
Leuva VR., Patel BG., Chaudhary DJ., Patel JN., & Modasiya MMK., 2012. Oral colon specific drug delivery system. J. Pharm. Res. 5(4): 2293–2297.
Lu L., Chen G., Qiu Y., Li M., Liu D., Hu D., Gu X., & Xiao Z., 2016. Nanoparticle-based oral delivery systems for colon targeting: principles and design strategies. Sci. Bull. 61(9): 670–681. https://doi.org/10.1007/s11434-016-1056-4
Ma Z., Ma R., Wang X., Gao J., Zheng Y., & Sun Z., 2019. Enzyme and PH responsive 5-flurouracil (5-FU) loaded hydrogels based on olsalazine derivatives for colon-specific drug delivery. Eur. Polym. J. 118: 64–70. https://doi.org/10.1016/j.eurpolymj.2019.05.017
Macedo A., Filipe P., Thomé NG., Vieira J., Oliveira C., Teodósio C., Ferreira R., Roque L., & Fonte P., 2020. A brief overview of the oral delivery of insulin as an alternative to the parenteral delivery. Curr. Mol. Med. 20(2): 134–143. https://doi.org/10.2174/1566524019666191010095522
Melero A., Draheim C., Hansen S., Giner E., Carreras JJ., Talens-Visconti R., Garrigues TM., Peris JE., Recio MC., Giner R., & Lehr CM., 2017. Targeted delivery of cyclosporine A by polymeric nanocarriers improves the therapy of inflammatory bowel disease in a relevant mouse model. Eur. J. Pharm. Biopharm. 119: 361–371. https://doi.org/10.1016/j.ejpb.2017.07.004
Morales-Burgos AM., Carvajal-Millan E., Rascón-Chu A., Martínez-López AL., Lizardi-Mendoza J., López-Franco YL., & Brown-Bojorquez F., 2019. Tailoring reversible insulin aggregates loaded in electrosprayed arabinoxylan microspheres intended for colon-targeted delivery. J. Appl. Polym. Sci. 136(38): 1–8. https://doi.org/10.1002/app.47960
Naeem M., Bae J., Oshi, AM., Kim MS., Moon HR., Lee BL., Im E., Jung Y., & Yoo JW., 2018. Colon-targeted delivery of cyclosporine A using dual-functional Eudragit® FS30D/PLGA nanoparticles ameliorates murine experimental colitis. Int. J. Nanomed. 13: 1225–1240. https://doi.org/10.2147/IJN.S157566
Naeem M., Cao J., Choi M., Kim WS., Moon HR., Lee BL., Kim MS., Jung Y., & Yoo JW., 2015. Enhanced therapeutic efficacy of budesonide in experimental colitis with enzyme/pH dual-sensitive polymeric nanoparticles. Int. J. Nanomed. 10: 4565–4580. https://doi.org/10.2147/IJN.S87816
Newton AMJ., Indana VL., & Kumar J., 2015. Chronotherapeutic drug delivery of tamarind gum, chitosan and okra gum controlled release colon targeted directly compressed propranolol hcl matrix tablets and in-vitro evaluation. Int. J. Biol. Macromol. 79: 290–299. https://doi.org/10.1016/j.ijbiomac.2015.03.031
Patel MM., & Amin AF., 2011. Design and optimization of colon-targeted system of theophylline for chronotherapy of nocturnal asthma. J. Pharm. Sci. 100(5), 1760–1772. https://doi.org/10.1002/jps.22406
Patel MM., 2013. Colon targeting: an emerging frontier for oral insulin delivery. Expert Opin. Drug Deliv. 10(6): 731–739. https://doi.org/10.1517/17425247.2013.782284
Philip A., & Philip B., 2010. Colon targeted drug delivery systems: a review on primary and novel approaches. Oman Med. J. 25(2): 70–78. https://doi.org/10.5001/omj.2010.24
Pithadia AB., & Jain S., 2011. Treatment of inflammatory bowel disease (IBD). Pharmacol. Rep. 63(3): 629–642. https://doi.org/10.1016/S1734-1140(11)70575-8
Quetglas EG., Armuzzi A., Wigge S., Fiorino G., Barnscheid L., Froelich M., & Danese S., 2015. Review article: The pharmacokinetics and pharmacodynamics of drugs used in inflammatory bowel disease treatment. Eur. J. Clin. Pharmacol. 71(7): 773–799. https://doi.org/10.1007/s00228-015-1862-7
Rekha MR., & Sharma CP., 2011. Chapter 8. Nanoparticle mediated oral delivery of peptides and proteins: Challenges and perspectives, edited by Chris Van Der Walle. Peptide and Protein Delivery. Academic Press. pp. 165–194. https://doi.org/10.1016/B978-0-12-384935-9.10008-2
Roberts LK., Barr LJ., Fuller DH., McMahon CW., Leese PT., & Jones S., 2005. Clinical safety and efficacy of a powdered Hepatitis B nucleic acid vaccine delivered to the epidermis by a commercial prototype device. Vaccine. 23(40): 4867–4878. https://doi.org/10.1016/j.vaccine.2005.05.026
Sahu KK., Kaurav M., & Pandey RS., 2019. Chylomicron mimicking solid lipid nanoemulsions encapsulated enteric minicapsules targeted to colon for immunization against hepatitis B. Int. Immunopharmacol. 66: 317–329. https://doi.org/10.1016/j.intimp.2018.11.041
Sahu KK., & Pandey RS., 2019. Development and characterization of HBsAg-loaded Eudragit nanoparticles for effective colonic immunization. Pharm. Dev. Tech. 24(2): 166–175. https://doi.org/10.1080/10837450.2018.1444639
Salvioni L., Fiandra L., Del Curto MD., Mazzucchelli S., Allevi R., Truffi M., Sorrentino L., Santini B., Cerea M., Palugan L., Corsi F., & Colombo M., 2016. Oral delivery of insulin via polyethylene imine-based nanoparticles for colonic release allows glycemic control in diabetic rats. Pharmacol. Res. 110: 122–130. https://doi.org/10.1016/j.phrs.2016.05.016
Sandborn WJ., Travis S., Moro L., Jones R., Gautille T., Bagin R., Huang M., Yeung P., & Ballard ED., 2012. Once-daily budesonide MMX® extended-release tablets induce remission in patients with mild to moderate ulcerative colitis: results from the CORE i study. Gastroenterology. 143(5): 1218-1226.e2. https://doi.org/10.1053/j.gastro.2012.08.003
Sardo HS., Saremnejad F., Bagheri S., Akhgari A., Afrasiabi Garekani H., & Sadeghi F., 2019. A review on 5-aminosalicylic acid colon-targeted oral drug delivery systems. Int. J. Pharm. 558: 367–379. https://doi.org/10.1016/j.ijpharm.2019.01.022
Shahiwala A., 2020. Cyclodextrin conjugates for colon drug delivery. J. Drug Del. Sci. Tech. 55: 101448. https://doi.org/10.1016/j.jddst.2019.101448
Sharma N., Sharma A., Bhatnagar A., Nishad D., Karwasra R., Khanna K., Sharma D., Kumar N., & Jain GK., 2019. Novel gum acacia based macroparticles for colon delivery of Mesalazine: Development and gammascintigraphy study. J. Drug Del. Sci. Tech. 54, 101224. https://doi.org/10.1016/j.jddst.2019.101224
Tromm A., Bunganič I., Tomsová E., Tulassay Z., Lukáš M., Kykal J., Bátovský M., Fixa B., Gabalec L., Safadi R., Kramm H., Altorjay I., Löhr H., Koutroubakis I., Bar–Meir S., Štimac D., Schäffeler E., Glasmacher C., Dilger K., … Greinwald R., 2011. Budesonide 9 mg is at least as effective as mesalamine 4.5 g in patients with mildly to moderately active crohn’s disease. Gastroenterology. 140(2): 425-434.e1. https://doi.org/10.1053/j.gastro.2010.11.004
Tummala S., Satish Kumar MN., & Prakash A, 2015. Formulation and characterization of 5-Fluorouracil enteric coated nanoparticles for sustained and localized release in treating colorectal cancer. Saudi Pharm. J., 23(3): 308–314. https://doi.org/10.1016/j.jsps.2014.11.010
Verma A., Kumar N., Malviya R., & Sharma PK., 2014. Emerging trends in noninvasive insulin delivery. J. Pharm. 2014: 1–9. https://doi.org/10.1155/2014/378048
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Published
2022-09-28
How to Cite
Iswandana, R., Putri, K. S. S., Larasati, S. A., Gunawan, M., & Putri, F. A. (2022). Delivery of Potential Drugs to The Colon: Challenges and Strategies. Indonesian Journal of Pharmacy, 33(3), 307-332. https://doi.org/10.22146/ijp.2734
Issue
Section
Review Article
