DEVELOPMENT AND CHARACTERIZATION OF GASTRO RETENTIVE MUCOADHESIVE MICROBEADS CONTAINING SIMVASTATIN WITH DIFFERENT CROSS LINKING AGENTS

  • VENKATA RAMANA REDDY K. Department of Pharmaceutics, KVK College of Pharmacy, Ranga Reddy Dist, Telangana State, India 501512
  • NAGABHUSHANAM M. V. Department of Pharmaceutics, Hindu College of Pharmacy, Guntur Dist, Andhra Pradesh State, India 522003
  • PAMULA REDDY B. Department of Pharmaceutics, Nirmala College of Pharmacy, Guntur District, Andhra Pradesh, India 522503
  • RAVINDAR NAIK E. Department of Pharmaceutics, KVK College of Pharmacy, Ranga Reddy Dist, Telangana State, India 501512

Abstract

Objective: The aim of the present work was to prepare and examine drug release of the oral controlled release microbeads using different curing agents by emulsification internal ionic gelation technique.


Methods: Cross-linked alginate microbeads were prepared with different cross linking agents by using mucoadhesive properties. The formation and compatibility of microbeads were confirmed by compatibility studies. Prepared microbeads evaluated for encapsulated efficiency, micromeritic properties, drug loading, in vitro wash off studies, in vitro dissolution studies, drug release kinetics and stability studies


Results: The in vitro drug release was influenced by both type of curing agents and type of polymers and no significant changes in characterization parameters was observed after 3 mo stability studies. The sustained release profile of optimized batch was found to be 99.66±0.18% in comparison to pure drug profile of 28.64±0.02% at 12 h release study. Results of both wash-off and in vitro studies suggests that batch (SF2) prepared with aluminium chloride has shown better mucoadhesive property. Drug release of optimized batch follows zero order with non fickian mechanism according to Korsmeyer-Peppas equation.


Conclusion: The data suggest the use of simvastatin mucoadhesive cross linked microbeads to offer the potential for oral controlled drug delivery with improved gastric retention and capable to provide sustained drug release by using cross linking agents.

Keywords: Simvastatin, Emulsification internal ionic gelation, Gatro-retentive drug delivery system, Mucoadhesive microbeads, In vitro study

References

1. Shirodker A, Rajashree Gude, Shreya Acharya, Shraddha Bhangle, Steffi Parab, Nidhi Gadi, et al. Formulation and evaluation of gastroretentive mucoadhesive tablets of nizatidine. Int J Res Pharm Sci 2019;10:31-9.
2. Silvina A, Bravo R, Claudio J. In vitro studies of diclofenac sodium controlled from bio-polymeric hydrophilic matrices. J Pharm Pharm Sci 2002;5:213-9.
3. Ravikumar MNV. Nano and micro-particles as controlled drug deliverydevices. J Pharm Pharm Sci 2000;3:234-58.
4. Schachter M. Chemical, pharmacokinetic and pharmacodynamic properties of statins: an update. Fundam Clin Pharmacol 2005;19:117-25.
5. Mishra B, Jayanth P, Shankar C. Development of chitosan-alginate microcapsule for colon specific delivery of metronidazole. Ind Drugs 2003;40:695-70.
6. Davis SS, Hardy JG, Taylor MJ, Whalley DR, Wilson CG. Comparative study of gastrointestinal transit of a pellet and tablet formulation. Int J Pharm 1984;21:167-77.
7. Davidovich Pinhas M, Harari O, Bianco Peled H. Evaluating the mucoadhesive properties of drug delivery systems based on hydrated thiolated alginate. J Controlled Release 2009;136:38-44.
8. Majithiya RJ, Raval AJ, Umrethia ML, Ghosh PK, Murthy RS. Enhancement of mucoadhesion by blending anionic, cationic and nonionic polymers. Drug Delivery Technol 2008;8:40-5.
9. Ford JL, Rubinstein MH, Hogan JE. Formulation of sustained release promethazine hydrochloride tablets using hydroxypropyl-methylcellulose matrices. Int J Pharm 1985;24:327-38.
10. Shah HP, Prajapati ST, Patel C. Gastroretentive drug delivery systems: from conception to commercial success. J Crit Rev 2017;4:10-21.
11. Gnanasekaran John Selvaraj, Balasubramanian A, Ramalingam K. Alteration of pharmacokinetic parameters of pentoxifylline using natural mucoadhesive polymers. Int J Appl Pharm 2020;12:153-7.
12. Vivek Puri, Ameya Sharma, Paramjot Maman, Nishant Rathore, Inderbir Singh. Overview of mucoadhesive biopolymers for buccal drug delivery systems. Int J Appl Pharm 2019;11:18-29.
13. Kavanagh N, Corrigan OI. Swelling and erosion properties of hydroxyl propyl methyl cellulose (Hypromellose) matrices-influence of agitation rate and dissolution medium composition. Int J Pharm 2004;279:141-52.
14. Chowhan ZT. Moisture, hardness, disintegration and dissolution interrealationships in compressed tablets prepared by the wet granulation process. Drug Dev Ind Pharm 1979;5:41-62.
15. Balaji A, Radhika V, Goud V. Formulation and evaluation of mucoadhesive buccal tablets by using natural polymer. Int J Pharm Sci Res 2014;5:4699-708.
16. Venkata Ramana Reddy K, Nagabhushanam MV. Fabrication and evaluation of oral controlled release of mucoadhesive alginate microbeads containing fluvastatin sodium. Asian J Pharm Clin Res 2019;12:101-12.
17. Chng, HS, Park H, Kelly P, Robinson JR. Bioadhesive polymers as platforms for oral controlled drug delivery II: synthesis and evaluation of some swelling, water-insoluble bioadhesive polymers. J Pharm Sci 1985;74:399-405.
18. Shweta Agarwal, Murthy RSR. Effect of different polymer concentration on drug release rate and physicochemical properties of mucoadhesive gastroretentive tablets. Indian J Pharm Sci 2015;77:705-14.
19. Ravi Kumar K, Suresh G. Development and characterization of alginate microspheres containing olmesartan by ionotropic gelation method. Int J Pharm Sci Drug Res 2018;10:335-41.
20. Morch YA, Donati I, Strand BL, Skjak Brek G. Effect of Ca2+, Ba2+, and Sr2+on alginate microbeads. Biomacro-molecules 2006;7:1471-80.
21. Liu Y Tong, Wang S, Deng Q, Chen A. Influence of different divalent metal ions on the properties of alginate microcapsules and microencapsulated cells. J Sol Gel Sci Techn 2013;67:66-76.
22. Shu Ling Huang, Yung Sheng Lin. The size stability of alginate beads by different ionic crosslinkers. Adv Mater Sci Eng 2017:1-8. https://doi.org/10.1155/2017/9304592
23. Swati Chaturvedi, Sharma PK, Sharad Visht, Shanu Tyagi. Comparison of emulsification and ionic gelation method of preparation of mucoadhesive microsphere. Pharma Innovation 2012;1:1-9.
24. Chaiyasan W, Srinivas SP, Tiyaboonchai W. Development and characterization of topical ophthalmic formulations containing lutein-loaded mucoadhesive nanoparticles. Int J Pharm Pharm Sci 2016;8:261-6.
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K., V. R. R., M. V., N., B., P. R., & E., R. N. (2020). DEVELOPMENT AND CHARACTERIZATION OF GASTRO RETENTIVE MUCOADHESIVE MICROBEADS CONTAINING SIMVASTATIN WITH DIFFERENT CROSS LINKING AGENTS. International Journal of Applied Pharmaceutics, 12(6), 118-126. https://doi.org/10.22159/ijap.2020v12i6.38913
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