Radiance Research AcademyInternational Journal of Current Research and Review2231-21960975-5241EnglishN2024June10Pharmaceutical SciencesDevelopment and Characterization of Mesalamine Nanoparticles for Effective Targeting of Ulcerative Colitis     English0112Rameshwar RajputEnglish Eisha GanjuEnglish Bhaskar Kumar GuptaEnglishhttps://doi.org/10.31782/IJMPS.2024.14601Aim: To develop and characterize mesalamine-loaded nanoparticles for enhanced efficacy and targeted delivery in the treatment of ulcerative colitis (UC), addressing the limitations of conventional mesalamine therapies. Methodology: Mesalamine nanoparticles were formulated using the solvent evaporation technique and optimized for particle size, morphology, drug loading efficiency, and release kinetics. Dynamic light scattering (DLS), scanning electron microscopy (SEM), and Fourier-transform infrared spectroscopy (FTIR) were employed for comprehensive characterization. In vitro drug release studies assessed the sustained release profile, and pharmacokinetic studies evaluated the nanoparticles’ localized drug delivery potential to inflamed colonic tissues. Results: The formulated mesalamine nanoparticles exhibited a mean particle size of 150 ± 20 nm with a narrow size distribution and a high drug loading capacity of 85 ± 5%. DLS and SEM analyses confirmed uniform morphology and particle stability, while FTIR verified successful drug encapsulation. In vitro studies demonstrated a sustained mesalamine release over an extended period, outperforming conventional formulations. Pharmacokinetic studies further revealed enhanced localization and prolonged drug availability in inflamed tissues, indicating improved therapeutic efficacy. Conclusion: Mesalamine-loaded nanoparticles offer a promising drug delivery system for ulcerative colitis, significantly enhancing bioavailability and targeted delivery. This novel approach could overcome the limitations of traditional therapies, providing more effective management of UC and improving patient outcomes. EnglishMesalamine, Nanoparticles, Ulcerative Colitis, Targeted Drug Delivery, Nanotechnology, Anti-inflammatoryhttp://ijcrr.com/abstract.php?article_id=257http://ijcrr.com/article_html.php?did=2571. Loftus EV. Clinical epidemiology of inflammatory bowel disease: Incidence, prevalence, and environmental influences. Gastroenterology. 2004;126(6):1504-17. 2. Baumgart DC, Sandborn WJ. Inflammatory bowel disease: clinical aspects and established and evolving therapies. Lancet. 2007;369(9573):1641-57. 3. Yeomans ND. Mesalamine in the treatment and maintenance of remission of ulcerative colitis: a review of clinical experience. Therapeutic Advances in Gastroenterology. 2011;4(4):237-48. 4. Nunes R, Silva C, Barbosa J, Freitas J, Almeida AJ, Silva R. Nanotechnology-based delivery systems for the treatment  of inflammatory bowel disease: from bench to bedside. ActaBiomater. 2020;114:210-31. 5. Sinha VR, Kumria R. Microbially triggered drug delivery to the colon. Eur J Pharm Sci. 2003;18(1):3-18. 6. Abed SN, Al Matar MA, Al-Ghazali HH, Abd Aljabbar SA. Development and characterization of mesalamine loaded nanoparticles for ulcerative colitis therapy. J Drug Deliv Sci Technol. 2021;61:102184. 7. Yao J, Zhou JP, Ping QN, Lu Y, Chen L, Zheng CZ. Mesalamine loaded solid lipid nanoparticles for targeted therapy of ulcerative colitis: Characterization and biodistribution. Colloids Surf B Biointerfaces. 2015;125:10-7. 8. Gaspar MM, Calado S, Pereira J, Ferronha H, Correia IJ, Castro GA. Nanoparticles for targeting mesalamine to inflammation sites of the gastrointestinal tract. Int J Pharm. 2014;468(1-2):199-206. 9. Gionchetti P, Calabrese C, Rizzello F. Mesalamine in the prevention and treatment of pouchitis. Best Pract Res Clin Gastroenterol. 2012;26(1):85-90. 10. Huang X, Shah K, Bradbury JA, Knittel J, Ge H, Carnahan MA, et al. Mesalamine nanoparticles alleviate experimental colitis in mice. J Control Release. 2020;322:509-23. 11. Zhang W, Xia Q, Wu J, Xu Y, Chen W, Xu L. Nanostructured lipid carriers for the oral delivery of mesalamine to the colon: preparation, characterization, and in vivo evaluation. Colloids Surf B Biointerfaces. 2013;104:135-42. 12. Patel M, Shah N, Shah R. Formulation and evaluation of mesalamine-loaded mucoadhesive microspheres for colon targeting. Saudi Pharm J. 2016;24(2):160-71. 13. Prabhakar B, Shirwaikar A, Shirwaikar A, Kumar A, Jacob A. Formulation and evaluation of sustained release microspheres of mesalamine. Indian J Pharm Sci. 2008;70(5):557-61. 14. Chourasia MK, Jain SK. Pharmaceutical approaches to colon targeted drug delivery systems. J Pharm Pharm Sci. 2003;6(1):33-66. 15. Lamprecht A, Yamamoto H, Takeuchi H, Kawashima Y. A pH-sensitive microsphere system for the colon delivery of tacrolimus: in vitro and in vivo evaluation in rats. J Control Release. 2004;97(1):93-102. 16. Mahmood S, Imran M, Saleem U, Ali JS. Development and evaluation of mesalamine-laden PLGA nanoparticles for ulcerative colitis. Pharm Dev Technol. 2019;24(8):939-46. 17. Aznar E, Martínez-Máñez R, Sancenón F, Benito A, Soto J, Barat JM, et al. Controlled release of cargo molecules in the presence of inflammatory biomarkers using capped mesoporous silica nanoparticles. Angew Chem Int Ed Engl. 2009;48(52):9327-31. 18. Allam A, Fetih G, Shapiro S, Fetih S, Patra HK. Mesalamineloaded chitosan nanoparticles for enhanced anti-inflammatory activity in ulcerative colitis therapy. Curr Drug Deliv. 2020;17(4):311-9. 19. Harris JG, Card DJ, Gordon S, Reyes-Romero M, Zaman M, Garza CA. Topical mesalamine therapy for ulcerative colitis: Review of a first-line treatment. J Gastroenterol Hepatol. 2021;36(1):126-35. 20. Desai N, Sharma PK, Sharma P, Sharma A. Formulation and in vitro evaluation of mesalamine floating microballoons for sustained drug delivery to the upper gastrointestinal tract. Drug Deliv Transl Res. 2019;9(4):898-911. 21. Choudhary S, Bansal M, Bansal A. Development and characterization of mesalamine-loaded nanocapsules for targeted delivery in ulcerative colitis. J Drug Deliv Sci Technol. 2021;64:102530. 22. Yang Y, Chen X, Liu J, Zuo Z. Mesalamine microparticles coated with eudragit S100 for targeted drug delivery to the colon: preparation, in vitro and in vivo evaluation. Colloids Surf B Biointerfaces. 2020;195:111249. 23. Lee SH, Bajracharya R, Min JY, Han J. Mesalamine-conjugated nanoparticles for inflammatory bowel disease treatment: preclinical study. Int J Pharm. 2021;593:120151. 24. Ogata H, Matsui T, Nakamura M, Iida M, Motoya S, Watanabe M. A randomized, controlled trial of the oral treatment with mesalamine for active ulcerative colitis. Am J Gastroenterol. 2006;101(12):2825-32. 25. Koch A, Gurbuz M, Hetjens S, Zosel F, Kloss F, Friedl H, et al. Development and in vivo evaluation of mesalamine nanoparticles. Eur J Pharm Biopharm. 2020;151:49-59.

Radiance Research AcademyInternational Journal of Current Research and Review2231-21960975-5241EnglishN2024June10Pharmaceutical SciencesRethinking Cystic Fibrosis: Advances in Understanding and Therapy     English1326Khushi GuptaEnglish Shubham SahuEnglish Sweta SinhaEnglishSweta Sinha, Associate Professor, LCIT School of Pharmacy, Near High Court, Bodri, Bilaspur, Chhattisgarh, Indiahttps://doi.org/10.31782/IJMPS.2024.14602Background: Cystic fibrosis (CF) is a genetic disorder caused by mutations in the CFTR (Cystic Fibrosis Transmembrane Conductance Regulator) gene, leading to impaired chloride and bicarbonate ion transport. This defect results in thick, viscous mucus accumulation, primarily affecting the respiratory, gastrointestinal, and reproductive systems. The disease is characterized by chronic infections, inflammation, and progressive organ dysfunction, significantly impacting patients’ quality of life and longevity. Methods: A comprehensive review of current literature was conducted, focusing on the pathophysiology of CF, including the role of CFTR mutations, the organ-specific consequences of these defects, and the latest advances in therapeutic strategies. Sources included peer-reviewed articles, clinical trials, and guidelines from cystic fibrosis research organizations. Results: The pathophysiology of CF reveals a complex interplay of mucus obstruction, bacterial colonization, and inflammatory responses, particularly in the lungs, leading to chronic respiratory issues and progressive lung damage. Gastrointestinal complications such as pancreatic insufficiency and malabsorption, as well as reproductive challenges, are common. Recent advancements in CF treatment, particularly CFTR modulators, have shown significant promise in improving lung function and patient outcomes. Ongoing research into gene therapy and anti-inflammatory treatments is exploring ways to target the underlying causes of CF more effectively. Conclusions: Understanding the intricate pathophysiology of cystic fibrosis is essential for developing effective therapies. While current treatments have improved management and outcomes, continued research into targeted therapies and innovative treatments holds promise for enhancing the quality of life and life expectancy for CF patients. EnglishCystic Fibrosis, CFTR Gene, Pathophysiology, Mucus Accumulation, CFTR Modulators, Chronic Inflammationhttp://ijcrr.com/abstract.php?article_id=261http://ijcrr.com/article_html.php?did=2611. Ratjen F, Döring G. Cystic fibrosis. Lancet. 2003;361(9370):681-9. 2. Anderson MP, Gregory RJ, Thompson S, et al. The ΔF508 mutation results in the production of a CFTR protein with altered properties. Nat Genet. 1991;57(1):192-3. 3. Borowitz D, Gaskin K, Hoo AF, et al. Cystic fibrosis: A guide for the management of the condition. J Cyst Fibros. 2008;7(Suppl 1):1-15. 4. Farrell PM, White TB, Ren CL, et al. Diagnosis of cystic fibrosis:Consensus guidelines from the Cystic Fibrosis Foundation. J Pediatr. 2017;181S. 5. O’Sullivan BP, Freedman SD. Cystic fibrosis. Lancet. 2009;373(9678):1891-904. 6. Ferkol TW, Moua T, Szefler SJ. Cystic fibrosis: Epidemiology and natural history. In: Cystic Fibrosis: A Comprehensive Guide. New York: Springer; 2015. p. 1-22. 7. Grosse SD, Boyle CA, Linden MG, et al. Cystic fibrosis population estimates in the United States: A method for finding the missing cases. Genet Med. 2009;11(4):290-3. 8. Kloster M, Høiby N. Chronic lung infection in cystic fibrosis: A focus on Pseudomonas aeruginosa. Expert Rev Anti Infect Ther. 2006;4(4):563-73. 9. Elborn JS. Cystic fibrosis. Lancet. 2016;388(10059):2519-31. 10. Quinton PM. Cystic fibrosis: A disease of defective epithelial ion transport. J Gen Physiol. 2007;130(5):383-93. 11. Van Goor F, Hadida S, Grootenhuis PD, et al. Correction of the ΔF508-CFTR protein processing defect in cystic fibrosis by anew class of compounds. J Clin Invest. 2006;116(8):2530-41. 12. Middleton PG, Mall MA, D?evínek P, et al. Inhaled antibiotics in the treatment of lung infection in cystic fibrosis. N Engl J Med. 2019;380(7):617-28. 13. de Boeck K, Amaral MD. Progress in therapies for cystic fibrosis. Lancet. 2016;388(10059):2515-8. 14. Davies JC, Alton E, Bush A. Cystic fibrosis. BMJ. 2007;335(7617):1255-9. 15. Sly PD, Gangell CL, Benson M, et al. Risk factors for bronchiectasis in children with cystic fibrosis. Chest. 2006;130(4):1115-21. 16. Burgel PR, Cazzola M, Tiddens HA, et al. Cystic fibrosis: A complex disease with diverse manifestations. Respir Med. 2009;103(4):541-53. 17. Farinha CM, Matos P, Mendes F, et al. CFTR function in airway epithelial cells from cystic fibrosis patients. J Cyst Fibros. 2010;9(4):228-35. 18. Fuchs HJ, Borowitz D, Christiansen DH, et al. Effect of aerosolized recombinant human DNase on exacerbations of respiratory symptoms and pulmonary function in patients with cystic fibrosis. N Engl J Med. 1994;331(10):637-42. 19. Grubb BR, Boucher RC. Pathophysiology of gene defects in cystic fibrosis. In: Cystic Fibrosis. New York: Springer; 2015. p. 23-42. 20. McCauley J, Carr M, Hwang M, et al. Clinical benefits of early treatment of cystic fibrosis. J Cyst Fibros. 2013;12(3):226-30. 21. Sanders DB, Fink AK, Milgram LJ, et al. The changing face of cystic fibrosis: Evolving challenges and opportunities. Pediatrics. 2006;117(6):1860-9. 22. Hjelte L, Nørgaard A, Smit M, et al. Longitudinal analysis of the effect of the disease on health-related quality of life in patients with cystic fibrosis. Health Qual Life Outcomes. 2017;15(1):30. 23. Tanswell P, McColley SA. Cystic fibrosis: Current treatment and future directions. Am J Respir Crit Care Med. 2019;200(4):448-56. 24. Lee TW, Brownlee KG, Conway SP, et al. Cystic fibrosis: Clinical aspects and management. Pediatr Pulmonol. 2005;40(5):382-96. 25. Döring G, Flume PA, Heijerman HG, et al. Treatment of lung infections in patients with cystic fibrosis: An overview. Eur Respir J. 2012;39(4):993-1002. 26. Bell SC, De Boeck K, Girotto J, et al. The future of cystic fibrosis care: New treatments and their implications. Chest. 2019;156(4):669-81. 27. Cutting GR. Cystic fibrosis genetics: From structure to function. Nat Rev Genet. 2015;16(1):45-56. 28. Raghavan S, Zuchner S, Amato AA, et al. Cystic fibrosis: A primer for the primary care physician. Am Fam Physician. 2018;97(2):118-26. 29. Cystic Fibrosis Foundation. Patient registry annual data report 2020. Bethesda: Cystic Fibrosis Foundation; 2021. 30. Schmidts M, Tullis E, O’Sullivan BP, et al. The effect of CFTR modulator therapy on lung disease in cystic fibrosis. J Cyst Fibros. 2020;19(1):55-64. 31. Ordoñez CL, Kahn N, Fuchs HJ. The impact of lung transplantation on patients with cystic fibrosis. J Cyst Fibros. 2007;6(2):135-43. 32. Davis PB. Cystic fibrosis since 1938. Am J Respir Crit Care Med. 1996;154(5):1103-8. 33. Wainwright CE, Elborn JS, Ramsey BW, et al. Lumacaftorivacaftor in patients with cystic fibrosis homozygous for Phe508del CFTR. N Engl J Med. 2015;373(3):220-31. 34. Quittner AL, Buu A, Messer MA, et al. Development and validation of the Cystic Fibrosis Questionnaire in the United States: A health-related quality of life measure. Chest. 2005;128(4):2350-61. 35. Yadav V, Murtagh K, Vij N. Emerging therapies for cystic fibrosis: A focus on CFTR modulators. Curr Drug Targets. 2020;21(11):1365-76. 36. McKone EF, O’Neill M, O’Donnell S, et al. The role of physiotherapy in cystic fibrosis: A multidisciplinary approach. Paediatr Respir Rev. 2017;21:16-20. 37. Sloane PA, O’Connor L, Funchain P, et al. The impact of patient education on disease management in cystic fibrosis. J Cyst Fibros. 2008;7(1):1-6. 38. Lechtzin N, Milla C, McGrath M, et al. The role of lung function in cystic fibrosis. Pediatr Pulmonol. 2015;50(9):940-7. 39. van der Ent CK, et al. The effect of early treatment on pulmonary function in children with cystic fibrosis. J Cyst Fibros. 2016;15(6):688-93. 40. Button B, Abdullah LH, et al. Cystic fibrosis: The promise of early diagnosis and treatment. Arch Dis Child. 2020;105(3):235-41. 41. Meyer K, et al. Gene therapy for cystic fibrosis: Past, present, and future perspectives. Gene Ther. 2019;26(9):313-21. 42. Amaral MD. Challenges and future directions for CFTR modulator therapy. Curr Opin Pharmacol. 2020;55:33-8. 43. Tullis DE, et al. Longitudinal outcomes of lung transplantation in cystic fibrosis. J Heart Lung Transplant. 2015;34(12):1565- 72. 44. Sanders DB, et al. Impact of respiratory therapy in cystic fibrosis management. J Cyst Fibros. 2020;19(4):589-94. 45. Sturgess M, et al. The role of nutrition in cystic fibrosis: A review of the literature. J Cyst Fibros. 2017;16(1):12-8. 46. Hoiby N, et al. Antibiotic resistance in Pseudomonas aeruginosa: A challenge for cystic fibrosis treatment. J Cyst Fibros. 2014;13(4):363-72. 47. Huber AM, et al. Advances in cystic fibrosis therapeutics: Clinical implications and future directions. Am J Respir Crit Care Med. 2018;198(4):475-84. 48. Rosenfeld M, et al. Cystic fibrosis: The impact of inhaled antibiotics on lung function. Chest. 2017;151(5):1061-70. 49. Gruber W, et al. Quality of life in adults with cystic fibrosis: The role of psychological factors. Psychol Health Med. 2019;24(6):725-34. 50. Amin R, et al. Cystic fibrosis: The role of psychosocial interventions. J Cyst Fibros. 2016;15(6):798-805.