DESIGN, DEVELOPMENT AND CHARACTERIZATION OF MUCOADHESIVE GASTRO SPHERES OF CARVEDILOL

Authors

  • S. S. Sakhare Department of Pharmaceutics, Gourishankar Institute of Pharmaceutical Education and Research, Limb, Satara, Shivaji University, Kolhapur
  • A. V. Yadav Department of Pharmaceutics, Gourishankar Institute of Pharmaceutical Education and Research, Limb, Satara, Shivaji University, Kolhapur
  • P. D. Jadhav Department of Pharmaceutics, Gourishankar Institute of Pharmaceutical Education and Research, Limb, Satara, Shivaji University, Kolhapur

DOI:

https://doi.org/10.22159/ijap.2016v8i3.11276

Keywords:

Carvedilol, Mucoadhesive, Gastro spheres, Factorial design

Abstract

Objective: The purpose of this study was to design mucoadhesive gastro spheres of carvedilol targeting to upper GIT, and optimize it in terms of its entrapment efficiency and drug release. A 32 full factorial design was employed to study the effect of independent variables like sodium alginate and sodium carboxyl methyl cellulose on entrapment efficiency and in vitro drug release.

Methods: Mucoadhesive gastro spheres were prepared by Orifice-Ionic gelation method, in which drug is uniformly distributed in the polymer solution so drug can be loaded easily in the polymer.32 full factorial designs were used to study the effect of process variables on formulation characteristics by applying statistical analysis.

Results: FTIR, XRD and DSC analyses apparently did not indicate any interaction of the drug with the polymers. However, the drug content, drug entrapment efficiency and morphology of the gastro spheres were found to be influenced by the method of preparation, composition of gastro spheres as well as exposure to the cross linking agent. In vitro drug release study showed that drug release can be modified by varying drug to polymer ratio. The release rate was found to be decreased in accordance with the increase in the ratio of polymer used.

Conclusion: From the study, we successfully developed carvedilol gastro spheres by using mucoadhesive polymer like SCMC and rate retardant sodium alginate polymer.

Downloads

Download data is not yet available.

References

Patwekar S, Baramade MK. Controlled release approach to novel multi particulate drug delivery system. Int J Pharm Pharm Sci 2012;4:757-63.

Kumar BP, Chandiran IS. Microparticulate drug delivery system: a review. Int J Pharma Sci Res 2011;1:19-37.

Balaji A, Uma Shankar MS. Microspheres as a promising mucoadhesive drug delivery system review. Int J Pharm Sci Rev Res 2013;23:8-14.

Kasim NA, Whitehouse M, Ramachandran C, Bermejo M, Lennernas H, Hussain AS, et al. Molecular properties of WHO essential drugs and provisional biopharmaceutical classification. Mol Pharm 2004;1:85–96.

Ruffolo RR, Jr Feuerstein GZ. Carvedilol: a novel multiple action antihypertensive drug that provides major organ protection. Cardiovasc Drugs Ther 1997;11:247–56.

Thummel KE, Shen DD. 10th ed. New York: McGraw-Hill companies. Goodman and Gilman's The Pharmacological Basis of Therapeutics; 2001. p. 1936.

Bal T, Sengupta S, Murthy PN. Formulation and evaluation of Carvedilol microcapsules using Eudragit NE30D and sodium alginate, Braz. J Pharm Sci 2013;49:889-900.

Nayaka AK, Pal D, Das S. Calcium pectinate-fenugreek seed mucilage mucoadhesive beads for controlled delivery of metformin HCl. Carbohydr Polym 96;2013:349–57.

Prajapatia VD, Jania GK, Moradiya NG. Locust bean gum in the development of sustained release mucoadhesive macromolecules of aceclofenac. Carbohydr Polym 2014;113:138–48.

Joshi P, Patel MR, Patel KR. Design and development of carvedilol phosphate are floating microsphere. Int J Pharmamedix India 2013;1:557-71.

Giri IC, Satyabrata B, Ellaiah P, Martha SK, Sahu PK, Tiwari P, et al. Design and evaluation of acyclovir mucoadhesive microcapsules. Int J Pharm Sci Rev Res 2010;5:0976–044X.

Ramana Reddy KV, Patra PK, Divakar K. Original article on the formulation and in vitro studies of carvedilol microspheres with its characterization. Int J Pharm Pharm Sci 2014;l6:975-1491.

Menon TV, Sajeeth CI. Formulation and evaluation of sustained release sodium alginate microbeads of carvedilol. Int J PharmTech Res 2013;5:746-53.

Patil S, Babbar A, Mathur R. Mucoadhesive chitosan microspheres of carvedilol for nasal administration research. J Drug Target 2010;184:321–31.

Indian Pharmacopoeia; 2014;2:1284-5, 244.

Patel B, Modi V, Patel Komal, Patel Manisha. Preparation and evaluation of ethyl cellulose microspheres prepared by emulsification solvent evaporation method. Int J Res Management Pharm 2012;1:82-91.

Yadav G, Jain A, Sutar N. Development of evaluation of oral mucoadhesive microcapsules of ketorolac tromethamine. Int J Pharm Res Dev 2014;6:122-31.

Sharma A, Jain CP. Preparation and characterization of solid dispersions of carvedilol with PVP K30. Res Pharm Sci 2010;5:49–56.

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.

Nayaka AK, Pal D, Santra K. Artocarpus heterophyllus L. seed starch blended gellan gum mucoadhesive beads of metformin HCl. Int J Biol Macromol 2014;65:329-39.

Published

03-05-2016

How to Cite

Sakhare, S. S., Yadav, A. V., & Jadhav, P. D. (2016). DESIGN, DEVELOPMENT AND CHARACTERIZATION OF MUCOADHESIVE GASTRO SPHERES OF CARVEDILOL. International Journal of Applied Pharmaceutics, 8(3), 37–42. https://doi.org/10.22159/ijap.2016v8i3.11276

Issue

Section

Original Article(s)