FORMULATION AND EVALUATION OF STABILIZED EPROSARTAN NANOSUSPENSION

  • M. SANTHOSH RAJA University College of Pharmaceutical Sciences, Acharya Nagarjuna University, Guntur 522510, India
  • K. VENKATARAMANA A. S. N. Pharmacy College, Burripalem Road, Tenali, Guntur 522201, India

Abstract

Objective: The objective of the current study is to enhance the solubility of Eprosartan mesylate a BCS Class II drug by employing the nanoprecipitation technique.


Methods: Polymeric nanoparticles of Eprosartan mesylate were prepared by precipitation technique with various polymers like PVP K30, HPMC K15M, and Eudragit L100 in various ratios. The incompatibility issues which may arise between the drug and polymers were tested by differential scanning calorimetry (DSC). The formed nanosuspensions were evaluated for various parameters like particle size, zeta potential, drug content, and dissolution testing.


Results: Among all the nanosuspension formulations, E12 formulation prepared with Eudragit L 100 showed better evaluation characteristics. SEM and DSC analysis showed no major interactions with the excipients. The maximum drug release was showed at 12h. The formulation E12 showed the particle size of 81.5±5.5 nm and zeta potential of-55.1mv.


Conclusion: The nano-precipitation method improved the dissolution as well as the bioavailability of Eprosartan mesylate nanosuspension.

Keywords: Bioavailability, Dissolution, Nanoprecipitation, Eprosartan mesylate, Eudragit

References

1. Ramaiyan D, Vijaya Ratna J. Nanosuspensions technology in drug delivery–a review. Int J Pharm Rev Res 2012;2:46-52.
2. Murthy RSR. In vitro evaluation of NPDDS. In: Yashwant Pathak, Deepak Thassu. editors. Drug Delivery Nanoparticles Formulation and Characterization. London: Informa Health Care; 2009. p. 156-68.
3. Vishal RP, Agrawal YK. Nanosuspension: an approach to enhance solubility of drugs. J Adv Pharm Tech Res 2011;2:81-7.
4. Barrett E Rabinow. Nanosuspensions in drug delivery. Nat Rev 2004;3:785-96.
5. Sumathi R, Tamizharasi S, Sivakumar T. Formulation and evaluation of polymeric nanosuspension of naringenin. Int J Appl Pharm 2017;9:60-70.
6. Aher SS, Malsane ST, Saudagar RB. Nanosuspension: an overview. Int J Curr Pharm Sci 2017;9:19-3.
7. Deore S, Shahi SR, Dabir P. Nanoparticle: as a targeted drug delivery system for depression. Int J Curr Pharm Res 2016;8:7-11.
8. Muller RH, Dingler A, Schneppe T, Gohla S. Large-scale production of solid lipid nanoparticles (SLN) and nanosuspensions (DissoCubes). In: Donald L Wise. editor. Handbook of pharmaceutical controlled release technology. New York: Marcel Dekker; 2000. p. 359-75.
9. Amidon GL, Lennarnas H, Shah VP, Crison JR. A theoretical basis for a biopharmaceutical classification: the correlation of in vitro product dissolution and in vivo bioavailability. Pharm Res 1995;12:413-20.
10. Muddana EB Rao, Suryakanta Swain, Chinam N Patra, Shakti P Mund. Formulation design, optimization and characterization of eprosartan mesylate nanoparticles. Nanosci Nanotechnol Asia 2018;8:130-43.
11. Upasana Yadav, Nuzhat Husain, Qamar Rehman. Formulation of nanoparticles of Eprosartan mesylate for better drug delivery by improving solubility. Asian J Pharm Clin Res 2018;11:260-3.
12. Prachi Shekhawat, Milind Bagul, Diptee Edwankar, Varsha Pokharkar. Enhanced dissolution/caco-2 permeability, pharmacokinetic and pharmacodynamic performance of re-dispersible eprosartan mesylate nanopowder. Eur J Pharm Sci 2019;132:72-85.
13. Prachi Shekhawat, Varsha Pokharkar. Risk assessment and QbD based optimization of an eprosartan mesylate nanosuspension: in vitro characterization, PAMPA and in vivo assessment. Int J Pharm 2019;567:118415.
14. Sabitri Bindhani, Snehamayee Mohapatra, Rajat Ku Kar, Utkalika Mahapatra. Preparation of self micro emulsifying drug delivery system (SMEDDS) of poorly soluble drug Eprosartan mesylate and its in vitro evaluation. Int J Res Pharm Sci 2019;10:3304-14.
15. Pankaj Dangre, Ritu Gilhotra, Shashikant Dhole. Formulation and statistical optimization of self-microemulsifying drug delivery system of eprosartan mesylate for improvement of oral bioavailability. Drug Delivery Transl Res 2016;6:610–62.
16. Pankaj Vijay Dangre, Mangesh Dinanath Godbole, Priyanka Vijay Ingale, Debarshi Kar Mahapatra. Improved dissolution and bioavailability of eprosartan mesylate formulated as solid dispersions using conventional methods. Ind J Pharm Edu Res 2016;50:209-17.
17. Pradeep Kumar M, Chandrasekhar KB. Formulation and in vitro and in vivo characterization of nifedipine stabilized nanosuspensions by nanoprecipitation method. Int J Res Pharm Sci 2017;8:759-66.
18. Higuchi T. Mechanism of sustained-action medication, theoretical analysis of rate of release of solid drugs dispersed in solid matrices. J Pharm Sci 1963;52:1145-9.
19. John Pugh Kinetics. In: ME Aulton, KMG Taylor. editors. Aulton’s pharmaceutics, the design and manufacture of medicines. 4th ed. Edinburgh: Churchill Livingstone; 2013. p. 115-25.
20. Patrick J Sinko. Micromeritics. In: Patrick J Sinko. editor. Martin's physical pharmacy and pharmaceutical sciences. 6th ed. Philadelphia: Lippincott Williams and Wilkins; 2011. p. 442-68.
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RAJA, M. S., & VENKATARAMANA, K. (2020). FORMULATION AND EVALUATION OF STABILIZED EPROSARTAN NANOSUSPENSION. International Journal of Applied Pharmaceutics, 12(6), 83-87. https://doi.org/10.22159/ijap.2020v12i6.39123
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