SYNTHESIS AND CHARACTERIZATION OF A NOVEL MUCOADHESIVE DERIVATIVE OF PSYLLIUM SEED POLYSACCHARIDE

  • Monica R.p. Rao Department of Pharmaceutics, AISSMS College of Pharmacy, near RTO, Kennedy Road, Pune 411001, Maharashtra, India
  • Snehal R. Gaikwad Department of Pharmaceutics, AISSMS College of Pharmacy, near RTO, Kennedy Road, Pune 411001, Maharashtra, India
  • Prachi M. Shevate Department of Pharmaceutics, AISSMS College of Pharmacy, near RTO, Kennedy Road, Pune 411001, Maharashtra, India

Abstract

Objective: In the present study, thiol-functionalization of psyllium seed polysaccharide (PSY) was cross-linked with thioglycolic acid by esterification in an attempt to reveal the mucoadhesive properties of thiolated psyllium seed polysaccharide (TPSY).

Methods: The crosslinking was carried out by the microwave-assisted method. A simplex centroid design was employed to systematically study the mucoadhesive strength, mucoadhesive retention time and drug release profile. Comparative evaluation of carbopol-based ciprofloxacin hydrochloride (HCl) tablets containing PSY and TPSY was carried out. Acute oral toxicity studies and repeated oral toxicity for TPSY were also conducted.

Results: Thiol-functionalization was confirmed by-SH stretch in Fourier Transform infra-red spectra at 2353 cm-1. Thiolation was observed in thiolated PSY (TPSY) by a change in the surface morphology of psyllium from fibrous to granular and resulted in 82 %swelling in deionized water. TPSY was found to contain 102.35 mmol of thiol groups/g as determined by the Ellman’s method. The percent increase in mucoadhesive strength of TPSY was found to be 50.31 % as compared to PSY and 128.30 % as compared to carbopol. The percent increase in mucoadhesive retention time of TPSY was found to be 110 % as compared to PSY and 50 % as compared to carbopol.

Conclusion: Mucoadhesion strength and mucoadhesive retention time were greater of tablets containing a higher amount of TPSY. Further, the acute oral toxicity studies and repeated oral toxicity for TPSY proved it as non-toxic and hence safe for human use.

Keywords: Psyllium seed polysaccharide, Crosslinking, Microwave assisted, Thiolated psyllium seed polysaccharide

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References

1. Chauhan P, Mehta N. Probiotic assisted colon targeted drug delivery system: research scope. Asian J Pharm Clin Res 2011;4:12-5.
2. Khan M, Ansari V, Kushwaha P, Kumar A, Akhtar J. Mucoadhesive microspheres for controlled delivery of drugs. Asian J Pharm Clin Res 2015;8:1-20.
3. Kumar R, Setia A, Mahadevan N. Grafting modification of the polysaccharide by the use of microwave irradiation–a review. Int J Recent Adv Pharm Res 2012;2:45-53.
4. Aminabhavi T, Chaturvedi K, Ganguly K, Nadagouda M. Polymeric hydrogels for oral insulin delivery. J Controlled Release 2013;165:129–38.
5. Singh B. Psyllium as therapeutic and drug delivery agent. Int J Pharm 2007;334:1–14.
6. Rao MRP, Warrier D, Rao S. Evaluation of phosphorylated psyllium seed polysaccharides a release retardant. Indian J Pharm Sci 2015;77:605-12.
7. Singh B, Sharma V. Design of psyllium–PVA–acrylic acid based novel hydrogels for use in antibiotic drug delivery. Int J Pharm 2010;389:94–106.
8. Singh B, S Kumar. Synthesis and characterization of psyllium-NVP based drug delivery system through radiation crosslinking polymerization. Nuclear Instrum Methods Phys Res 2008; 266:3417–30.
9. Lalge M, Sharma P, Bhandari A, Garud A, Garud N. Mucoadhesive drug delivery system: a review. Crit Rev Pharm Sci 2014;3:17-29.
10. Sarti F, Staaf A. Thiolated hydroxyethylcellulose: synthesis and in vitro evaluation. Eur J Pharm Biopharm 2010;76:421-7.
11. Roldoa M, Hornof M. Mucoadhesive thiolated chitosans as platforms for oral controlled drug delivery: synthesis and in vitro evaluation. Eur J Pharm Biopharm 2004;57:115–21.
12. Shahnaz G, Perera G. Synthesis, characterization, mucoadhesion and biocompatibility of thiolated carboxymethyl dextran–cysteine conjugate. J Controlled Release 2010;144:32-8.
13. Kaur H, Yadav S. Synthesis, characterization and evaluation of thiolated tamarind seed polysaccharide as a mucoadhesive polymer. Carb Poly 2012;90:1543-9.
14. Bhosale R, Gangadharappa H, Moin A, Gowda D, Osmani R. A review on grafting modification of polysaccharides by microwave irradiation-distinctive practice for application in drug delivery. Int J Curr Pharm Rev Res 2015;6:8-17.
15. Divate V, Dhongade Desai S. An efficient microwave assisted multicomponent synthesis of some 7-amino-3-(substituted phenyl)-5-(substituted phenyl)-[1,2, 4]triazolo [4,3a] pyrimidine-6-carbonitrile derivatives. Int J Curr Pharm Res 2014;6:20-4.
16. Bhatia M, Ahuja M. Thiol modification of psyllium husk mucilage and evaluation of its mucoadhesive applications. Hindawi Publishing Corporation Sci World J 2013;1-7. http://dx.doi.org/10.1155/2013/284182
17. Sena G, Mishra S. Microwave initiated synthesis of polyacrylamide grafted psyllium and its application as a flocculant. Int J Biol Macromol 2012;50:369-75.
18. Berg J, Tymoczko J, Stryer L. Biochemistry 5th ed. WH Freeman. New York; 2002.
19. Khandelwal KR, Practical pharmacognosy, Techniques and experiments. 19th ed. Nirali Prakashan, Pune; 2008. p. 159.
20. Rao MRP, Khambete M, Lunavat H. Study of rheological properties of psyllium polysaccharide and its evaluation as a suspending agent. Int J PharmTech Res 2011;3:1191-7.
21. Patrick S. Martin’s physical pharmacy and pharmaceutical sciences. 5th ed. Lippincott Williams and Wilkins, Philadelphia; 2000. p. 587-8.
22. Krishnarajan D. Effect of cellulose and non-cellulose polymers on ciprofloxacin extended-release tablets. J Chem Pharm Res 2012;4:3617-23.
23. Surawase R, Maru A. Formulation and evaluation of metoprolol succinate buccal tablet containing tamarind seed polysaccharides. Int J Pharm Pharm Sci 2011;3:1491.
24. OECD guideline for testing of chemicals-423 Acute Oral Toxicity–Acute Toxic Class Method; 2001.
25. Madgulkar A, Bhalekar M. Optimization of carboxymethyl-xyloglucan-based tramadol matrix tablets using simplex centroid mixture design. Hindawi Publishing Corporation J of Pharma 2013;1-11. http://dx.doi.org/10.1155/2013/396468
26. Indian Pharmacopoeia. The government of India, Ministry of Health and Family Welfare. Vol. 3. Published by the Indian Pharmacopoeia Commission; 2010. p. 1247.
27. Singh V, Kumara P, Sanghi R. Use of microwave irradiation in the grafting modification of the polysaccharides–a review. Prog Polym Sci 2012;37:340–64.
28. Bhattarai N, Ramay H. PEG-grafted chitosan as an injectable thermosensitive hydrogel for sustained protein release. J Controlled Release 2005;103:609–24.
29. Sravani B, Deveswaran R, Bharath S, Basavaraj B, Madhavan V. Development of sustained release metformin hydrochloride tablets using a natural polysaccharide. Int J Appl Pharm 2012;4:23-9.
30. Tangri P, Khurana S, Madhav S. Mucoadhesive drug delivery: mechanism and methods of evaluation. Int J Pharmacol Biol Sci 2011;3:458.
31. Muraleedhara KK. Mucoadhesive vaginal drug delivery system: a review on advanced status. Int J Pharm Res Anal 2013;3:33-46.
32. Coviello T, Matricardi P, Marianecci C, Alhaique F. Polysaccharide hydrogels for modified release formulations. J Controlled Release 2007;119:5–24.
33. Chaturvedi K, Ganguly K. Polymeric hydrogels for oral insulin delivery. J Controlled Release 2013;165:129–38.
34. Patrick S, Martin’s physical pharmacy and pharmaceutical sciences. 5thed. Lippincott Williams and Wilkins, Philadelphia; 2000. p. 581.
35. Huang Y, Leobandung W. Molecular aspects of muco and bio-adhesion: tethered structures and site-specific surfaces. J Controlled Release 2000;65:63-71.
36. Qaqish R, Amiji M. Synthesis of a fluorescent chitosan derivative and its application for the study of chitosan-mucin interactions. Carbohydr Polym 1999;38:99-107.
37. Bernkop Schnurch A. Thiomers: a new generation of mucoadhesive polymers. Adv Drug Delivery Rev 2005;58:1569-82.
38. Patrick S. Martin’s physical pharmacy and pharmaceutical sciences. 5th ed. Lippincott Williams and Wilkins, Philadelphia; 2000. p. 26, 67.
39. http://plc.cwru.edu/tutorial/enhanced/files/polymers/orient/orient.htm [Last accessed on 20 Apr 2017]
40. https://en.wikipedia.org/wiki/Enthalpy. [Last accessed on 20 Apr 2017]
41. Madgulkar A, Bhalekar M. Synthesis and characterization of a novel mucoadhesive derivative of xyloglucan. Carbohydr Polym 2016;135:356–62.
42. Kaur H, Yadav S. Synthesis, characterization and evaluation of thiolated tamarind seed polysaccharide as a mucoadhesive polymer. Carbohydr Polym 2012;90:1543–9.
43. Kottke K, Edward M. Tablet dosage forms. In: Banker GS, Rhodes CT. ed. Modern Pharmaceutics. New York: Marcel Dekker, Inc; 2002;1:287-333.
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Rao, M. R., S. R. Gaikwad, and P. M. Shevate. “SYNTHESIS AND CHARACTERIZATION OF A NOVEL MUCOADHESIVE DERIVATIVE OF PSYLLIUM SEED POLYSACCHARIDE”. International Journal of Pharmacy and Pharmaceutical Sciences, Vol. 9, no. 6, June 2017, pp. 166-75, doi:10.22159/ijpps.2017v9i6.14221.
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