DESIGN, DEVELOPMENT, AND CHARACTERIZATION OF OCIMUM BASILICUM MUCILAGE-BASED, MODIFIED RELEASE MUCOADHESIVE GASTROSPHERES OF CARVEDILOL
OCIMUM BASILICUM MUCILAGE BASED GASTROSPHERES OF CARVEDILOL
Objective: The present investigations aim to develop mucoadhesive gastrospheres of carvedilol using sodium alginate and Ocimum basilicum seed mucilage combination blend oral use.
Methods: The gastrospheres were prepared by ionotropic gelation method using 32 factorial designs, the concentration of sodium alginate and O. basilicum mucilage was independent variables while % drug content (DC), % entrapment efficiency, and % drug release at 12 h were dependent variables. The gastrospheres were evaluated for other parameters such as Fourier-transform infrared (FTIR), powder X-ray diffraction, differential scanning calorimetric, and in vitro mucoadhesion studies.
Results: In optimization studies from statistical second-order complete model equation among the polymers used O. basilicum mucilage had a more profound effect on DC and % encapsulation efficiency as compared to sodium alginate. The mean particle size of gastrospheres when measured by optical microscopy technique ranged from 774 to 882 μm. The percentage of gastrosphere adhering to goat intestinal mucosal tissue varied from 10% to 65% over 8 h in 0.1N HCl, whereas this was varied from 40% to 60% in phosphate buffer pH 6.8 with provided 12 h of controlled release following zero-order release pattern.
Conclusion: Studies conclude that mucilage of O. basilicum can be used as controlled release mucoadhesive material in the formulation of gastrospheres.
2. Wong CY, Al-Salami H, Dass CR. Microparticles, microcapsules and microspheres: A review of recent developments and prospects for oral delivery of insulin. Int J Pharm 2018;537:223-44.
3. Patel MM. Formulation and development of di-dependent microparticulate system for colon-specific drug delivery. Drug Deliv Transl Res 2017;7:312-24.
4. Oliveira MB, da Silva JB, Montanha MC, Kimura E, Diniz A, Bruschi ML, et al. Design and characterization of mucoadhesive gelatin-ethylcellulose microparticles for the delivery of curcumin to the bladder. Curr Drug Deliv 2018;15:1112-22.
5. Di Prima G, Conigliaro A, De Caro V. Mucoadhesive polymeric films to enhance barbaloin penetration into buccal mucosa: A novel approach to chemoprevention. AAPS PharmSciTech 2019;20:18.
6. Sakhare SS, Yadav AV, Jadhav PD. Design, development and characterization of mucoadhesive gastro spheres of carvedilol. Int J Appl Pharm 2016;8:37-42.
7. Leichner C, Jelkmann M, Bernkop-Schnürch A. Thiolated polymers: Bioinspired polymers utilizing one of the most important bridging structures in nature. Adv Drug Deliv Rev 2019; S0169- 409X(19)30049-3.
8. Patil PS. Natural excipients: Uses of pharmaceutical formulations. Int J PharmTech Res 2014;6:21-8.
9. Kamble MS, Mendake SD, Chaudhari PD, Aute PP. Evaluation of binding property of Ocimum tenuiflorum Linn. Seed mucilage isolated by defatting method. J Biomed Pharm Res 2012;3:22-7.
10. Jania GK, Shah DP, Prajapatia VD, Jain VC. Gums and mucilages: Versatile excipients for pharmaceutical formulations. Asian J Pharm Sci 2009;4:308-22.
11. Malviya R, Srivastava P, Kulkarni GT. Applications of mucilages in drug delivery-a review. Adv Biol Res 2011;5:1-7.
12. Osano JP, Hosseini-Parvar SH, Matia-Merino L, Golding M. Emulsifying properties of a novel polysaccharide extracted from basil seed (Ocimum basilicum L.): Effect of polysaccharide and protein content. Food Hydrocoll 2014;37:40-8.
13. Khazaei N, Esmaiili M, Djomeh ZE, Ghasemlou M, Jouki M. Characterization of new biodegradable edible film made from basil seed (Ocimum basilicum L.) gum. Carbohydr Polym 2014;102:199-206.
14. Bal T, Sengupta S, Padala S, Murthy N. Formulation and evaluation of carvedilol microcapsules using eudragit NE30D and sodium aliginate. Braz J Pharm Sci 2013;49:879-900.
15. Yelugam M, Koteshwara KB, Reddy MS. Gastroretentive floating microspheres of carvedilol: Formulation, characterization and in vitro evaluation. Int J Pharm Pharm Sci 2013;5:686-90.
16. Sayyad FJ, Sakhare SS. Isolation, characterization and evaluation of Ocimum basilicum seed mucilage for tableting performance. Indian J Pharm Sci 2018;80:282-90.
17. Prajapati VD, Jani GK, Moradiya NG, Randeria NP, Maheriya PM, Nagar BJ, et al. Locust bean gum in the development of sustained release mucoadhesive macromolecules of aceclofenac. Carbohydr Polym 2014;113:138-48.
18. Joshi P, Patel MR, Patel KR. Design and development of carvedilol phosphate floating microsphere. Int J Pharmamedix India 2013;1:557-71.
19. Singh B, Sharma V, Chauhan D. Gastroretentive floating sterculia– alginate beads for use in antiulcer drug delivery. Chem Eng Res Des 2010;88:997-1012.
20. Nayaka AK, Pal D, Das S. Calcium pectinate-fenugreek seed mucilage mucoadhesive beads for controlled delivery of metformin HCl. Carbohydr Polym 2013;96:349-57.
21. Manohar SD, Dhake AS, Mallikarjuna SC. A research article on solubility and dissolution enhancement of carvedilol by solid dispersion technique using gelucire 50/13. Int J Pharm Sci Rev Res 2014;29:161-5.
22. Brahmankar DM, Jaiswal SB. Biopharmaceutics and Pharmacokinetics a Treaties. New Delhi: Vallabh Prakashan; 2013.
23. Wittaya-areekul S, Kruenate J, Prahsarn C. Preparation and in vitro evaluation of mucoadhesive properties of alginate/chitosan microparticles containing prednisolone. Int J Pharm 2006;312:113-8.
24. Jaswir I, Noviendri D, Taher M, Mohamed F, Octavianti F, Lestari W, et al. Optimization and formulation of fucoxanthin-loaded microsphere (F-LM) using response surface methodology (RSM) and analysis of its fucoxanthin release profile. Molecules 2019;24:E947.
25. Patil S, Babbar A, Mathur R, Mishra A, Sawant K. Mucoadhesive chitosan microspheres of carvedilol for nasal administration. J Drug Target 2010;18:321-31.
26. Riekes MK, Barboza FM, Veccia DD, Bohatch M Jr., Farago VV, Farnandes D, et al. Evaluation of oral carvedilol microparticles prepared by simple emulsion technique using poly (3-hydroxybutyrate-co-3-hydroxyvalerate) and polycaprolactone as polymers. Mater Sci Eng C 2011;31:962-8.
27. Gada S, Anandkumar Y, Settee M. Drumstick mucilage microspheres for controlled release of lamivudine: Design, optimization and in vitro evaluation. Int J Pharm Pharm Sci 2019;11:60-8.
28. Chakra BP, Saumen K, Das B, Debnath S, Chatterjee TK. Controlled release microsphere formulation of an anti-diabetic drug and characterization of the microsphere. Int J Pharm Pharm Sci 2018;10:30-8.
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