MICROSPHERE-BASED COLON-SPECIFIC DELIVERY SYSTEMS: A NOVEL APPROACH FOR DIHYDROARTEMISININ
Main Article Content
Keywords
Colon-targeted drug delivery, Microspheres, Dihydroartemisinin (DHA), Controlled release, Bioavailability enhancement, Polymer-based drug carriers, Site-specific delivery, pH-sensitive polymers, Nano carrier innovations
Abstract
Colon-targeted drug delivery has become an important strategy for improving the treatment of diseases that affect the large intestine, as well as for enhancing the systemic availability of drugs that are unstable in the upper gastrointestinal tract. Microspheres have drawn particular attention because they can protect sensitive drugs, provide controlled release, and deliver them precisely where needed. Dihydroartemisinin, a key antimalarial drug, is limited in its use due to poor solubility, rapid clearance, and instability in normal physiological conditions. Incorporating this drug into polymer-based colon-targeted microspheres offers a way to overcome these barriers, leading to better stability, prolonged release, and improved bioavailability. This review summarizes the importance of colon-targeted systems, the barriers and mechanisms of targeting, the role of microspheres, and the polymers used in their formulation. It also highlights how such approaches can specifically benefit Dihydroartemisinin therapy, while pointing toward future directions in research and clinical translation.
References
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19. Hua S, Marks E, Schneider JJ, et al. Advances in oral nano-delivery systems for colon-targeted drug delivery in inflammatory bowel disease: selective targeting to diseased versus healthy tissue. Nanomedicine (Lond). 2015;11(5):1117–1132.
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25. Yang Y, Li G, Han W, et al. Efficient porous microspheres by foam-phase evaporation. Chin J Chem Eng. 2021;29(1):409–16.
26. Prajapati ST, et al. Chitosan-based colon-targeted microparticles: preparation and characterization. AAPS PharmSciTech. 2023;24(2):73.
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28. Momin M, et al. Colon-targeted Eudragit-coated microspheres: formulation and evaluation. J Microencapsul. 2021;38(7):579–92.
29. Patil SA, et al. Advances in spray drying for microsphere fabrication. J Control Release. 2023;361:297–313.
30. Vyas D, et al. Ionotropically gelled gellan gum microparticles for colon targeting. Pharmaceutics. 2025;17(5):569.
31. Patil S, Parmar D, Amin A, et al. Carbohydrate polymer-based carriers in colon-targeted pharmaceutical formulations: a systematic review. Carbohydr Polym. 2023;299:120310.
32. Tas C, Calıskan Ö, Celebioglu A, et al. Mucoadhesive polymers for oral drug delivery: Mechanisms and design strategies. Int J Biol Macromol. 2023;234:123–138.
33. Shendge RS, et al. Polymeric microspheres redefining the landscape of colon-targeted delivery. Eur J Med Chem Rep. 2024;11:100156.
34. Kang J, Zhang J, Gao Y et al. Strategic approaches for colon-targeted drug delivery: pH-triggered and microflora-mediated release. Pharmaceutics. 2020;12(2):154.
35. Vilar G, Tulla-Puche J, Albericio F. Polymers and drug delivery systems. Curr Drug Deliv. 2012;9(4):367–94.
36. Ahmadi E, Sadrjavadi K, Mohammadi G, Fattahi A. De-Esterified tragacanth microspheres in Eudragit S100 capsules for colon-targeted delivery. Iran J Pharm Res. 2018;17(2):e124822.
37. Dos P, et al. Smart hydrogels of Eudragit S100 and acrylic acid for colon-specific delivery of losartan. Drug Deliv. 2021;28(1):1234–1246.
38. Zhang C, et al. Core–shell curcumin microparticles for site-specific release in ulcerative colitis (electrospray). Chin Med. 2021;16:92.
39. Alshammari ND, Elkanayati R, Vemula SK, et al. Advancements in colon-targeted drug delivery: Hot-melt extrusion and 3D printing. AAPS PharmSciTech. 2024;25(7):236.
40. MDPI Editorial Team. In vitro methodologies for colon-targeted drug delivery evaluation. Pharmaceutics. 2022;14(2):291.
41. Xu Y, Xu S, Li Y. Improving the solubility and bioavailability of dihydroartemisinin using solid dispersions and inclusion complexes. Drug Dev Ind Pharm. 2021;47(8):1231–8.
42. Olliaro P, Navaratnam V. Stability of the antimalarial drug dihydroartemisinin under physiologically relevant conditions; implications for clinical treatment and pharmacokinetic studies. Antimicrob Agents Chemother. 2015;59(11):7140–4.
43. Morris CA, Duparc S, Borghini-Fuhrer I, Jung D, Shin CS, Fleckenstein L. Review of the clinical pharmacokinetics of artesunate and its active metabolite dihydroartemisinin following various routes of administration. Malar J. 2011;10:263.
44. Sriwongjanya M, Mallick B, Swanson BD, et al. Development of nanoscale drug delivery systems of dihydroartemisinin for cancer therapy: A review. Asian J Pharm Sci. 2022;17(4):475–90.
45. Wong KH, Yang D, Chen S, He C, Chen M. Development of nanoscale drug delivery systems of dihydroartemisinin for cancer therapy: A review. Asian J Pharm Sci. 2022;17(4):475–90.
46. Qian S, et al. Encapsulating DHA in gelatin or hyaluronic acid nanoparticles enhanced bioavailability in lung cancer cells. J Nanobiotechnology. 2020;18:69.
47. Morris CA, et al. Clinical PK review of artesunate and DHA, pointing to short half-life and frequent dosing. Malar J. 2011;10:263. Alshammari ND, et al. Colonic drug delivery: Formulating the next generation of colon-targeted therapeutics. AAPS PharmSciTech. 2024;25(7):236.
48. Lv Y, et al. Colon-specific delivery of methotrexate using hyaluronic acid-modified pH-responsive nanocarrier for colitis therapy in mice. Carbohydr Polym. 2021;269:118325.
49. Frontiers Editorial Office. Targeted lipid nanoparticles encapsulating dihydroartemisinin and chloroquine phosphate for suppressing colorectal cancer metastasis. Front Pharmacol. 2021;12:720777.
50. Alshammari ND, Elkanayati R, Vemula SK, Al Shawakri E, Uttreja P, Almutairi M, Repka MA. Advancements in Colon-Targeted Drug Delivery: A Comprehensive Review on Recent Techniques with Emphasis on Hot-Melt Extrusion and 3D Printing Technologies. AAPS PharmSciTech. 2024;25(7):236. doi:10.1208/s12249-024-02965-w
51. Wang L, Guo B. Colonic drug delivery: Formulating the next generation of colon-targeted therapeutics. J Control Release. 2023;353:1107–1126.
52. Hussain A, Bhagat M. Challenges and advances in colon-targeted nano-drug delivery systems. Nanomedicine. 2020;15(11):951–970.
53. Iswandana R, Putri KS, Gunawan M, Larasati SA. Challenge and development strategy for colon-targeted drug delivery system. Pharm Sci Res. 2022;9:17–27.
54. Dos Santos AM, Carvalho SG, Meneguin AB, Sábio RM, Gremião MPD, Chorilli M. Oral delivery of micro/nanoparticulate systems based on natural polysaccharides for intestinal diseases therapy: Challenges, advances and future perspectives. J Control Release. 2021;334:353–366.
2. McCoubrey LE, Favaron A, Awad A, Orlu M, Gaisford S, Basit AW. Colonic drug delivery: Formulating the next generation of colon-targeted therapeutics. J Control Release. 2023;353:1107–26.
3. Yamamura R, Inoue KY, Nishino K, Yamasaki S. Intestinal and fecal pH in human health. Front Microbiomes. 2023;2:1192316.
4. Kulkarni N, Jain P, Shindikar A, Suryawanshi P, Thorat N. Advances in the colon-targeted chitosan-based multiunit drug delivery systems for the treatment of inflammatory bowel disease. Carbohydr Polym. 2022;288:119351.
5. Udaipuria N, Bhattacharya S. Novel carbohydrate polymer-based systems for precise drug delivery in colon cancer: Improving treatment effectiveness with intelligent biodegradable materials. Biopolymers. 2025;116(1):e23632.
6. “Advancements in Colon Targeted Drug Delivery: A Comprehensive Review on Recent Techniques with Emphasis on Hot Melt Extrusion and 3D Printing Technologies.” AAPS PharmSciTech. 2024;25:236.
7. Yecheng L, et al. Inulin-based colon targeted drug delivery systems: Advancing site-specific therapeutics. Discover Mater. 2025;5:114.
8. Bertin L, et al. Polysaccharide based drug delivery targeted approach for colon cancer treatment: A comprehensive review. Therap Adv Gastroenterol. 2024;17:17562848241303651.
9. Cui, M., Zhang, M., & Liu, K. Colon-targeted drug delivery of polysaccharide-based nanocarriers for synergistic treatment of inflammatory bowel disease: A review. Carbohydrate polymers. 2021,272, 118530.
10. Deljavan Ghodrati A, Çomoğlu T. Mucoadhesive polymers in colon targeted drug delivery systems: A comprehensive review. J Fac Pharm Ankara Univ. 2024;48(2):696–713.
11. Alshammari ND, Elkanayati R, Vemula SK, et al. Advancements in Colon-Targeted Drug Delivery: A Comprehensive Review on Recent Techniques with Emphasis on Hot-Melt Extrusion and 3D Printing Technologies. AAPS PharmSciTech. 2024;25:236.
12. Dos Santos AM, Carvalho SG, Meneguin AB, et al. Oral delivery of micro/nanoparticulate systems based on natural polysaccharides for intestinal disease therapy: challenges, advances, and future perspectives. J Control Release. 2021;334:353–366.
13. McCoubrey LE, Favaron A, Awad A, et al. Colonic drug delivery: Formulating the next generation of colon-targeted therapeutics. J Control Release. 2023;353:1107–1126.
14. Ghodrati A, Çomoğlu T. An overview on recent approaches for colonic drug delivery systems. Pharm Dev Technol. 2024;29(5):566–581.
15. Kumari B, Upadhyay PK, Kumar M, et al. An updated overview of recent advances on formulation development for colon targeting. Int J Pharm Sci Res. 2020;11(4):1571–1580.
16. Zheng B, Wang L, Yi Y, et al. Design strategies, advances and future perspectives of colon-targeted delivery systems for the treatment of inflammatory bowel disease. Asian J Pharm Sci. 2024;19:100943.
17. Hu S, Zhao R, Xu Y, et al. Orally-administered nanomedicine systems targeting colon inflammation for the treatment of inflammatory bowel disease: Latest advances. J Mater Chem B. 2023;12(1):13–38.
18. Ray S, Shukla S, Singhai AK, et al. Colon drug delivery system and their benefits and the carriers for delivery of drugs to colon: a review. Asian J Pharm Educ Res. 2020;9:15–26.
19. Hua S, Marks E, Schneider JJ, et al. Advances in oral nano-delivery systems for colon-targeted drug delivery in inflammatory bowel disease: selective targeting to diseased versus healthy tissue. Nanomedicine (Lond). 2015;11(5):1117–1132.
20. Ábrómez-Gálvez R, et al. Microparticles, microspheres, and microcapsules—a review. Pharmaceutics. 2020;12(3):209.
21. Butreddy A, Gaddam RP, Kommineni N, et al. PLGA/PLA-based long-acting injectable depot microspheres in clinical use. Int J Mol Sci. 2021;22(16):8884.
22. Zhang M, et al. Ethyl cellulose-based microparticles: A comprehensive review. J Drug Deliv Sci Technol. 2022;67:102911.
23. Petrovici AR, et al. Dextran formulations as delivery systems of therapeutic agents. Molecules. 2023;28(3):1086.
24. Feng T, et al. Microfluidic fabrication of microspheres for drug delivery. Front Bioeng Biotechnol. 2025;13:1551199.
25. Yang Y, Li G, Han W, et al. Efficient porous microspheres by foam-phase evaporation. Chin J Chem Eng. 2021;29(1):409–16.
26. Prajapati ST, et al. Chitosan-based colon-targeted microparticles: preparation and characterization. AAPS PharmSciTech. 2023;24(2):73.
27. Awasthi R, et al. Colon-specific drug delivery for inflammatory bowel disease. Drug Discov Today. 2022;27(2):586–97.
28. Momin M, et al. Colon-targeted Eudragit-coated microspheres: formulation and evaluation. J Microencapsul. 2021;38(7):579–92.
29. Patil SA, et al. Advances in spray drying for microsphere fabrication. J Control Release. 2023;361:297–313.
30. Vyas D, et al. Ionotropically gelled gellan gum microparticles for colon targeting. Pharmaceutics. 2025;17(5):569.
31. Patil S, Parmar D, Amin A, et al. Carbohydrate polymer-based carriers in colon-targeted pharmaceutical formulations: a systematic review. Carbohydr Polym. 2023;299:120310.
32. Tas C, Calıskan Ö, Celebioglu A, et al. Mucoadhesive polymers for oral drug delivery: Mechanisms and design strategies. Int J Biol Macromol. 2023;234:123–138.
33. Shendge RS, et al. Polymeric microspheres redefining the landscape of colon-targeted delivery. Eur J Med Chem Rep. 2024;11:100156.
34. Kang J, Zhang J, Gao Y et al. Strategic approaches for colon-targeted drug delivery: pH-triggered and microflora-mediated release. Pharmaceutics. 2020;12(2):154.
35. Vilar G, Tulla-Puche J, Albericio F. Polymers and drug delivery systems. Curr Drug Deliv. 2012;9(4):367–94.
36. Ahmadi E, Sadrjavadi K, Mohammadi G, Fattahi A. De-Esterified tragacanth microspheres in Eudragit S100 capsules for colon-targeted delivery. Iran J Pharm Res. 2018;17(2):e124822.
37. Dos P, et al. Smart hydrogels of Eudragit S100 and acrylic acid for colon-specific delivery of losartan. Drug Deliv. 2021;28(1):1234–1246.
38. Zhang C, et al. Core–shell curcumin microparticles for site-specific release in ulcerative colitis (electrospray). Chin Med. 2021;16:92.
39. Alshammari ND, Elkanayati R, Vemula SK, et al. Advancements in colon-targeted drug delivery: Hot-melt extrusion and 3D printing. AAPS PharmSciTech. 2024;25(7):236.
40. MDPI Editorial Team. In vitro methodologies for colon-targeted drug delivery evaluation. Pharmaceutics. 2022;14(2):291.
41. Xu Y, Xu S, Li Y. Improving the solubility and bioavailability of dihydroartemisinin using solid dispersions and inclusion complexes. Drug Dev Ind Pharm. 2021;47(8):1231–8.
42. Olliaro P, Navaratnam V. Stability of the antimalarial drug dihydroartemisinin under physiologically relevant conditions; implications for clinical treatment and pharmacokinetic studies. Antimicrob Agents Chemother. 2015;59(11):7140–4.
43. Morris CA, Duparc S, Borghini-Fuhrer I, Jung D, Shin CS, Fleckenstein L. Review of the clinical pharmacokinetics of artesunate and its active metabolite dihydroartemisinin following various routes of administration. Malar J. 2011;10:263.
44. Sriwongjanya M, Mallick B, Swanson BD, et al. Development of nanoscale drug delivery systems of dihydroartemisinin for cancer therapy: A review. Asian J Pharm Sci. 2022;17(4):475–90.
45. Wong KH, Yang D, Chen S, He C, Chen M. Development of nanoscale drug delivery systems of dihydroartemisinin for cancer therapy: A review. Asian J Pharm Sci. 2022;17(4):475–90.
46. Qian S, et al. Encapsulating DHA in gelatin or hyaluronic acid nanoparticles enhanced bioavailability in lung cancer cells. J Nanobiotechnology. 2020;18:69.
47. Morris CA, et al. Clinical PK review of artesunate and DHA, pointing to short half-life and frequent dosing. Malar J. 2011;10:263. Alshammari ND, et al. Colonic drug delivery: Formulating the next generation of colon-targeted therapeutics. AAPS PharmSciTech. 2024;25(7):236.
48. Lv Y, et al. Colon-specific delivery of methotrexate using hyaluronic acid-modified pH-responsive nanocarrier for colitis therapy in mice. Carbohydr Polym. 2021;269:118325.
49. Frontiers Editorial Office. Targeted lipid nanoparticles encapsulating dihydroartemisinin and chloroquine phosphate for suppressing colorectal cancer metastasis. Front Pharmacol. 2021;12:720777.
50. Alshammari ND, Elkanayati R, Vemula SK, Al Shawakri E, Uttreja P, Almutairi M, Repka MA. Advancements in Colon-Targeted Drug Delivery: A Comprehensive Review on Recent Techniques with Emphasis on Hot-Melt Extrusion and 3D Printing Technologies. AAPS PharmSciTech. 2024;25(7):236. doi:10.1208/s12249-024-02965-w
51. Wang L, Guo B. Colonic drug delivery: Formulating the next generation of colon-targeted therapeutics. J Control Release. 2023;353:1107–1126.
52. Hussain A, Bhagat M. Challenges and advances in colon-targeted nano-drug delivery systems. Nanomedicine. 2020;15(11):951–970.
53. Iswandana R, Putri KS, Gunawan M, Larasati SA. Challenge and development strategy for colon-targeted drug delivery system. Pharm Sci Res. 2022;9:17–27.
54. Dos Santos AM, Carvalho SG, Meneguin AB, Sábio RM, Gremião MPD, Chorilli M. Oral delivery of micro/nanoparticulate systems based on natural polysaccharides for intestinal diseases therapy: Challenges, advances and future perspectives. J Control Release. 2021;334:353–366.
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Sep 30, 2025
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Mr. Devarsh Maheriya, Ms. Nirzari Antani, & Dr. Pragnesh Patani. (2025). MICROSPHERE-BASED COLON-SPECIFIC DELIVERY SYSTEMS: A NOVEL APPROACH FOR DIHYDROARTEMISININ. Journal of Population Therapeutics and Clinical Pharmacology, 32(7), 1947-1956. https://doi.org/10.53555/mxe4c689
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Author Biographies
Mr. Devarsh Maheriya
Khyati College of Pharmacy, Gujarat Technology University, Ahmedabad, Gujarat, India.
Ms. Nirzari Antani
Khyati College of Pharmacy, Gujarat Technology University, Ahmedabad, Gujarat, India.
Dr. Pragnesh Patani
Khyati College of Pharmacy, Gujarat Technology University, Ahmedabad, Gujarat, India.
How to Cite
Mr. Devarsh Maheriya, Ms. Nirzari Antani, & Dr. Pragnesh Patani. (2025). MICROSPHERE-BASED COLON-SPECIFIC DELIVERY SYSTEMS: A NOVEL APPROACH FOR DIHYDROARTEMISININ. Journal of Population Therapeutics and Clinical Pharmacology, 32(7), 1947-1956. https://doi.org/10.53555/mxe4c689