ATENOLOL MICROPARTICLES BY TWO-FACTOR TWO-LEVEL CENTRAL COMPOSITE DESIGN

  • ARTI SHARMA Department of Pharmaceutics, Hindu College of Pharmacy, Sonipat, Haryana, India.
  • SUNIL K BATRA Department of Pharmaceutics, Hindu College of Pharmacy, Sonipat, Haryana, India.

Abstract

Objective: The objective of this research was to formulation, optimization, and evaluation of gastric-mucoadhesive microparticles which contains selective β1 receptor antagonist atenolol.


Methods: The following chemicals were used, atenolol (Gangwal Chemicals Pvt. Ltd., Mumbai), ethyl cellulose (EC) (Loba Chemie Pvt. Ltd., Mumbai), Carbopol 940 (Loba Chemie Pvt. Ltd., Mumbai), liquid paraffin (Arora Pharmaceuticals Pvt. Ltd., New Delhi), and Span 80 (Central Drug House (P) Ltd., New Delhi). Microparticles were prepared by the emulsification solvent evaporation technique using polymers of Carbomer 934p (CP) and EC. Disc formulations were prepared by direct compression technique from microparticles. Microparticles of combined polymers were designed according to 22 factorial central composite design (CCD), taking EC concentration and surfactant concentration as the independent variables. A total of 13 batches were prepared. The dependent variables were percentage of % drug released and % entrapment efficiency.


Results and Discussion: All evaluation tests were done for the prepared 13 formulations, such as percentage entrapment efficiency, percentage drug release, swelling index, percentage yield, and particle size analysis. The entrapment efficiency of optimized formulation was found to be 72.02%. The entrapment efficiency increases with increase in EC concentration and stirring speed. Optimized formulation was further subjected to study of drug release kinetics based on the R2 value; it was observed that Korsmeyer Peppas release kinetic model was found to be best suited for formulation of atenolol with EC: carbopol 934 by solvent evaporation method.


Conclusion: The optimized formulation of microparticles containing atenolol was found to be homogeneous, good appearance and had well flow properties and better release kinetics.

Keywords: Selective β1 receptor antagonist, Entrapment efficiency, Design–Expert, evaporation, Variables, Central composite design

References

1. Nayak AK, Maji R, Das B. Gastroretentive drug delivery systems: A review. Asian J Pharm Clin Res 2010;3:1-10.
2. Meenakshi J, Ujjwal N, Jyotsana K, Devendra S. A review: Gastroretentive drug delivery system (grdds). Indian J Pharm Biol Res 2015;3:82-92.
3. Havaldar VD, Kulkarni AS, Dias RJ, Aloorkar NH, Mali KK. Floating matrix tablets of atenolol: Formulation and in vitro evaluation. Asian J Pharm 2009;3:284-91.
4. Pranati S, Rishabha M, Sharad V. Formulation development and evaluation of atenolol fast disintegrating tablets for treatment of hypertension. J Chronother Drug Deliv 2010;1:36-42.
5. Yadava N, Mohiteb DD, Pawarb KR, Pawarb UR, Bhiseb SB, Sande TA. Synthesis and characterization of sustained release atenolol microspheres by solvent evaporation technique. J Pharm Sci Technol 2011;3:559-62.
6. Tadwee IK, Sadhana S, Shekhar T, Gupta SK, Suhas V, Ashok S. Formulation development and evaluation of spray dried nasal mucodhesive microspheres of atenolol. Int J Pharm Res All Sci 2011;1:34-40.
7. Shahi SR, Tribhuwan SD, Tadwee IK, Gupta SK, Zadbuke SN, Shivanikar SS. Formulation of atenolol mucoadhesive microspheres for nasal delivery by spray drying technique: In vitro/ex vivo evaluation. Pharm Sin 2011;2:54-63.
8. Patil PB, Gawali VU, Patil HN, Hardikar SR, Bhosale AV. Preparation and evaluation of mucoadhesive microspheres of atenolol and propranolol. Int J Pharm Tech Res 2009;1:639-43.
9. Sanjay D, Sankha C, Bhaskar M. Formulation and evaluation of fixed-dose combination of bilayer gastroretentive matrix tablet containing atorvastatin as fast-release and atenolol as sustained-release. Biomed Res Int 2014;2014:396106.
10. Adity B, Sultana NR, Tajnin A, Sharmin S. Design and development of atenolol matrix tablet employing natural and synthetic polymers. J Appl Pharm Sci 2013;3:103-8.
11. Badola A, Chakraborthy GS. Development and characterization of atenolol and indapamide in their combined dosage form using different polymers. World J Pharm Pharm Sci 2014;3:1206-27.
12. Anepu S, Duppala L, Nikhil J, Devi SJ. Formulation and evaluation of gastro retentive matrix tablets of atenolol using melt granulation technique. Int J Pharm Sci Res 2016;7:1081-92.
13. Anepu S, Duppala L, Nikhil J, Devi SJ. Formulation and evaluation of gastro retentive matrix tablets of atenolol using melt granulation technique. Int J Pharm Sci Res 2016;7:1081-92.
14. Jaybir S, Meenakshi B. Formulation and evaluation of atenolol mouth dissolving tablet. Chem Biol Interface 2017;7:323-7.
15. Khonsari F, Zakeri-Milani P, Jelvehgari M. Formulation and evaluation of in vitro characterization of gastic-mucoadhesive microparticles/discs containing metformin. Iran J Pharm Res 2014;13:67-80.
16. Surendranaths B, Mohan VM, Abbulu K. Formulation and evaluation of sustained release microspheres of propranolol. World J Pharm Pharm Sci 2017;6:1497-507.
17. Shivpoojan K, Jony G, Shweta S, Narendra PK, Mahendra T. Method development and validation of atenolol drug by spectrophotometric and HPLC technique in forensic application. Int J Sci Res 2013;2013:1731-5.
18. Gite S, Shinkar DM, Saudagar RB. Development and evaluation of mucoadhesive tablets of atenolol and its ?-cyclodextrin complex. Asian J Biomed Pharm Sci 2014;4:25-32.
19. Venkatalakshmi R, Sasikala C, Yajaman S. Formulation and evaluation of bioerodible bilayered buccal tablets containing atenolol. J Chem Pharm Sci 2017;10:1170-3.
20. Perumal D. Microencapsulation of ibuprofen and Eudragit RS 100 by the emulsion solvent diffusion technique. Int J Pharm 2001;218:1-11.
21. Kuldip P, Tekade BW, Thakare VM, Patil VR. Formulation and evaluation of atenolol floating microsphere. Pharmatutor 2018;???:1-10.
22. Reddy AP, Shaik US, Moodu M, Gaddam S, Anga M. Development and evaluation of sustained release microparticles of atenolol of gastrointestinal delivery. GSC Biol Pharm Sci 2018;3:1-5.
23. Kumar S, Reddy J, Sekhar PC. Design, development and characterisation of mucoadhesive microsphere of naproxen sodium by HPMC K15M as polymer. J Pharm Res 2011;4:3943-7.
24. Satyanasrayana L, Sandeepthi N. Formulation and evaluation of atenolol floating microspheres. Indo Am J Pharm Sci 2018;5:135-40.
25. Mankala SK, Korla AC, Gade S. Development and evaluation of aceclofenac-loaded mucoadhesive microcapsules. J Adv Pharm Technol Res 2011;2:245-54.
26. Tarun P, Nardev S. Formulation and in vitro evaluation of bilayer tablet of atenolol for biphasic drug release. Asian J Pharm Clin Res 2018;11:114-9.
27. Haritha S, Kotla NG, Balaji M, Sima S, Omprakash S, Kumar A, et al. Formulation and evaluation of atenolol floating bioadhesive system using optimized polymer blends. Int J Pharm Investig 2016;6:116-22.
28. Balagani PK, Chandiran IS, Jayaveera KN. Formulation development and evaluation of glibenclamide loaded Eudragit RLPO microparticles. Int Curr Pharm J 2013;2:196-201.
29. Melike U, Karaman EF. Preliminary studies on solid lipid microparticles of loratadine for the treatment of allergic reactions via the nasal route. Trop J Pharm Res 2013;12:287-93.
30. Shih-Mo Y, Tung-Ming Y, Ming-Huei L, Long H, Cheng-Hsien L.Moldless PEGDA-based optoelectrofluidic platform for microparticle selection. Adv Optoelectron 2011;2011:1-9.
31. Abhay K, Sonali D, Ghatuary SK, Subhasri M. Design and evaluation of progesterone microparticles using biodegradable polymers. IOSR J Pharm 2013;3:26-8.
32. Josephine LJ, Yathish M, Wilson B, Kumari KB. Formulation and evaluation of microparticles containing curcumin for colorectal cancer. J Drug Deliv Ther 2012;2:125-8.
33. Madan JR, Kadam V, Bandavane S, Dua, K. Formulation and evaluation of microspheres containing ropinirole hydrochloride using biodegradable polymers. Asian J Pharm 2014;7:184-8.
34. Gantala V, Ramanathan S, Mansor SM, Nair NK, Sattar MA, Croft SL, et al. Development and validation of RP-HPLC-UV method for simultaneous determination of buparvaquone, atenolol, propranolol, quinidine and verapamil: A tool for the standardization of rat in situ intestinal permeability studies. J Pharm Biomed Anal 2007;43:1546-51.
35. Natarajan R, Elishaba G, Rangapriya M, Rajendran N. Optimization and evaluation of mucoadhesive microspheres of atenolol. Int J Res Pharm Chem 2011;1:722-9.
36. Nappinnai M, Kishore VS. Formulation and evaluation of microspheres of diltiazem hydrochloride. Indian J Pharm Sci 2007;69:511-4.
37. Reddy JR, Gnanaprakash K, Badarinath AV, Chetty CM. Formulation and evaluation of microparticles of metronidazole. J Pharm Sci Res 2009;1:131-6.
38. Dalu D, Kumar YG. Formulation design and development of gastro retentive floating tablets of atenolol. J Pharm Res 2017;11:479-84.
39. Yagnesh B, Dushyant S. Influence of additives on fabrication and release from protein loaded PLGA microparticles. J Chem Pharm Res 2012;4:1708-15.
40. Ahmed N, Hasan I, Saifuddin M, Chowdhury JA, Reza MS. Formulation and optimization of carbamazepine microspheres by 2 factor 2 level central composite design. Bangladesh Pharm J 2016;19:152-60.
Statistics
63 Views | 77 Downloads
Citatons
How to Cite
SHARMA, A., and S. K BATRA. “ATENOLOL MICROPARTICLES BY TWO-FACTOR TWO-LEVEL CENTRAL COMPOSITE DESIGN”. Asian Journal of Pharmaceutical and Clinical Research, Vol. 13, no. 4, Apr. 2020, pp. 192-01, doi:10.22159/ajpcr.2020.v13i4.36467.
Section
Original Article(s)