Development and Evaluation of Floating Alginate Beads of Esomeprazole

The aim of the study was the Development and Evaluation of Floating alginate beads of Esomeprazole. The floating alginate beads of Esomeprazole (F1–F6) were prepared in six different batches using varying concentration of sodium alginate and HPMC K4M using inotropic gelation technique. The floating alginate beads of Esomeprazole (F1–F6) were extensively evaluated. Micrometric properties such as angle of repose, bulk density, tapped density, Carr’s index, and Hausner’s ratio confirmed good flow and packing behavior across all formulations, with F5 exhibiting the most favorable characteristics. The drug entrapment efficiency increased with polymer concentration, reaching a maximum of 87.96 ± 1.05% for F5.Floating lag time decreased with increasing polymer content, with F5 showing the shortest lag time (33.8 ± 1.4 sec).The total floating duration improved significantly with HPMC content, with F5 and F6 maintaining buoyancy for over 12 hours.Particle size analysis revealed a trend of decreasing size with increasing polymer content, with F5 having the smallest average size (190.1 ± 2.3 µm). Additionally, percent yield improved with higher polymer concentrations, with F5 again demonstrating the highest yield (89.62 ± 1.10%).The optimized formulation F5, containing 2% sodium alginate and 1% HPMC K4M, exhibited maximum sustained release (98.26% over 12 hours), balancing matrix stability and drug dissolution

Alginate beads, Floating Drug Delivery, Esomeprazole, Micrometric properties

1. Singh, B., Kim, K. H., & Floating Drug Delivery Systems: A Review. Journal of Pharmaceutical Investigation. 41(8), 485–495. (2011). [Google Scholar] [Crossref]

2. Agrawal, A. K., Harikumar, S. L., Sharma, P. K., & Singh, R. P. Floating drug delivery systems: A review. International Journal of Pharmaceutical Sciences Review and Research. 7(1), 180-186. (2011). [Google Scholar] [Crossref]

3. Bharat W. Tekade, Umesh T. Jadhao, Pankaj H. Bari, Vijay R Patil., A comprehensive review on gastro-retentive drug delivery system. Innovations in Pharmaceuticals and Pharmacotherapy. 5 (2), 94-102, 2017. [Google Scholar] [Crossref]

4. Akhtar, N., & Ahuja, A. Application of floating drug delivery systems in the development of novel anti-retroviral drug combinations for HIV treatment. Journal of Pharmacy & Bioallied Sciences. 4(2), 124–129. (2012). [Google Scholar] [Crossref]

5. Jadhao, U. T., Thakare, V. M., Tekade, B.W., Chaudhari, K. P., Patil, V. R., 2013. Development and in-vitro Evaluation of Intra Gastric Cefadroxil Monohydrate Floating Tablet. Pelagia Research Library. 4,4,141-150. [Google Scholar] [Crossref]

6. Sánchez, F. M., Navarro, L. G., & Pérez, R. D. Floating drug delivery systems: a review. American Journal of Pharmaceutical Sciences and Nanotechnology. 6(1), 29-38. (2019). [Google Scholar] [Crossref]

7. Jadhao, U. T., Thakare, V. M., Chaudhari, K. P., Tekade, B. W., Chaudhari, C. S., Patil, V. R. 2013. Design and Evaluation of Famotidine Matrix Tablet Using 32 Factorial Designs. Research Journal of Pharmaceutical, Biological and Chemical Sciences. July-September RJPBCS 4, 3, 1441-1451. [Google Scholar] [Crossref]

8. Arora S, Ahuja A. Floating drug delivery system: a review. J AAPS PharmSciTec h 2005;6:372–90. [Google Scholar] [Crossref]

9. El-Kamel, A.H., Sokar, M.S., Al Gamal, S.S., Naggar. Preparation and evaluat ion of ketoprofen floating oral delivery system. Int J Pharm. 2001; 220, 13-21. [Google Scholar] [Crossref]

10. Groning R, Heun G. Oral dosage forms with controlled gastrointestinal transit. Drug Dev Ind Pharm. 1984; 10: 527-539. [Google Scholar] [Crossref]

11. Tekade B. W., Jadhao U. T., Thakare V. M., Yogita A. Chaudhari., Vaishali D. Patil, Chaudhari C. S. Design and In-vitro Evaluation of Ethyl Cellulose Based Floating Microspheres Containing Antidiabetic Drug. Asian Journal of Biomedical and Pharmaceutical Sciences; 3(23) 2013, 33-37. [Google Scholar] [Crossref]

12. Kawashinia Y, Niwa T. Takcuchi H. Hino T, Itoh Y. Hallow microspheres for use as a floating controlled drug delivery system in the stomach. J.Pharm.Sci.1992; 81(2): 135- 140. [Google Scholar] [Crossref]

13. Chikhalikar SS and Wakade RB: Floating Drug Delivery System – An Approach To Oral Controlled Drug Delivery. International Journal of PharmTech Research 2012; 4(4) 1812-26. [Google Scholar] [Crossref]

14. Hwang S, Park H, Park K. Gastric retentive drug-delivery systems. Crit Rev Ther Drug Carr Syst 1998;15:243-83. [Google Scholar] [Crossref]

15. Rouge N, Buri P, Doelker E. Drug absorption sites in the gastrointestinal tract and dosage forms for site specific delivery. Int J Pharm. 1996; 136:117-139. [Google Scholar] [Crossref]

16. Sharma S, Garg S. Gastroretentive drug delivery system in drug delivery oral, Business Brief : Pharmatech 2003 :160- 166. [Google Scholar] [Crossref]

17. Bharat W. Tekade, Umesh T. Jadhao, Vinod M. Thakre, Leena R. Bhortake., Formulation and evaluation of diclofenac sodium effervescent tablet. Innovations in Pharmaceuticals and Pharmacotherapy. 2 (2), 350-358, 2014. [Google Scholar] [Crossref]

18. Bechgaard H., Ladefoged K. Distribution of pellets in the gastrointestinal tract: The influence on transit time exerted by density or diameter of pellets. J.Pharm. Pharmacol. 1978; 30:690-692. [Google Scholar] [Crossref]

19. Deshpande A.A., Shah N.H., Rhodes C.T., Malick W.,Development of a novel controlled release system for gastric retention, Pharm. Res. 1997; 14: 815-819. [Google Scholar] [Crossref]

20. Thanoo B.C, Sunny M.C. and Jayakrishnan A., Oral sustained-release drug delivery systems using polycarbonate microspheres capable of floating on the gastric fluid, J.Pharm. Pharmacol. 1993,45,21-24. [Google Scholar] [Crossref]

21. Rathod Sayali P, Jadhao Umesh T, Lokhande Sneha S, Panchal Pranita P., Design and Development of Multiparticulate Floating Drug Delivery System Containing Lisinopril., Sch Acad J Pharm, Mar, 2021; 10(3): 54-59. [Google Scholar] [Crossref]

22. Takka S, Gürel A. Evaluation of chitosan/alginate beads using experimental design: formulation and in vitro characterization. AAPS PharmSciTech. 2010 Mar;11(1):460-6. [Google Scholar] [Crossref]

23. B.Y. Choi, H.J. Park, S.J. Hwang, J.B. Park, Preparation of alginate beads for floating drug delivery system: effects of CO2 gas-forming agents, Internatio nal Journal of Pharmaceutics, Volume 239, Issues 1–2, 2002, Pages 81-91. [Google Scholar] [Crossref]

• Determination of pKa Value for Ranolazine and Atenolol Using UV Spectroscopy
• The Science of Sustained-Release Medications
• Development of Proteomics in Clinical Medicine
• Advances on Quinoline Derivatives: A Review of Synthesis and Biological Activities
• “Review on Development and Validation of RP-HPLC Method, And Techniques for Vorasidenib in Bulk Drug and Pharmaceutical Dosage Forms”