FORMULATION AND EVALUATION OF GASTRORETENTIVE MICROBALLOONS OF ACEBROPHYLLINE FOR THE TREATMENT OF BRONCHIAL ASTHMA
Objective: Gastroretentive dosage forms are an approach for prolonged and predictable drug delivery in the upper gastrointestinal tract to control
the gastric residence time. Microballoons are considered as one of the most promising buoyant drug delivery systems as they possess the advantages
of both multiple-unit systems and good floating properties. Acebrophylline is a xanthine derivative with potent bronchodilator, mucosecretolytic, and
anti-inflammatory property. It is used to treat bronchial asthma and chronic obstructive pulmonary diseases.
Methods: Microballoons of acebrophylline were prepared by emulsion solvent diffusion method using hydroxypropyl methylcellulose (HPMC) and
ethyl cellulose (EC) as polymer. The microballoons were evaluated with their micromeritic properties, particle size, tapped density, compressibility
index, angle of repose, percentage yield, in vitro buoyancy, entrapment efficiency, drug-polymer compatibility, scanning electron microscopy (SEM),
and drug release kinetics.
Results: The mean particle size of the microballoons formulation MB1 to MB6 containing HPMC and EC was in the range between 226Â±16 and 577Â±10,
respectively. The mean particle size of microballoons was found to increase with increasing polymer concentration. The micromeritic properties were
found be good, and SEM confirmed their hollow structure with smooth and dense which helped to prolong floating to increase residence time in
stomach. The in vitro drug release studies showed controlled release of acebrophylline microballoons in the simulated gastric fluid more than 12 hrs.
Conclusions: The results showed that the prepared floating microballoons of acebrophylline prove to be potential multiple-unit delivery devices
adaptable for safe and effective sustained drug delivery.
Keywords: Microballoons, Acebrophylline, Bronchial asthma, Hydroxypropyl methylcellulose, Ethyl cellulose.
2. Nayak AK, Maji R, Das B. Gastroretentive drug delivery systems: A review. Asian J Pharm Clin Res 2010;3(1):1-10.
3. Kiss D, ZelkÃ³ R. Gastroretentive dosage forms. Acta Pharm Hung 2005;75(3):169-76.
4. Hou SY, Cowles VE, Berner B. Gastric retentive dosage forms: A review. Crit Rev Ther Drug Carrier Syst 2003;20(6):459-97.
5. Kawashima Y, Niwa T, Takeuchi H, Hino T, Itoh Y. Hollow microspheres for use as a floating controlled drug delivery system in the stomach. J Pharm Sci 1992;81(2):135-40.
6. Pujara ND, Patel NV, Thacker AP, Raval BK, Doshi SM, Parmar RB. Floating microspheres: A novel approach for gastro retention. World J Pharm Pharm Sci 2012;1(3):872-95.
7. The Global Asthma Report 2011. Paris, France: The International Union against Tuberculosis and Lung Disease; 2011.
8. Gopinath H, Vedanthan C, Kumar PB. Formulation and evaluation of acebrophylline sustained release matrix tablets. J Chem Pharm Sci 2012;5(2):56-61.
9. Pozzi E. Acebrophylline: An airway mucoregulator and anti-inflammatory agent. Monaldi Arch Chest Dis 2007;67(2):106-15.
10. Bauskar MD, Nandedkar SY, Wagh RD. Formulation design and optimization of pulsatile release tablet of acebrophylline with swelling and erodible layers for treatment of nocturnal bronchial asthma. Int J Pharm Sci Res 2011;2(12):3100-8.
11. Streubel A, Siepmann J, Bodmeier R. Multiple unit gastroretentive drug delivery systems: A new preparation method for low density microparticles. J Microencapsul 2003;20(3):329-47.
12. Charulatha R, Damodharan N, Sundaramoorthy R, Abhilash G. Design and evaluation of acebrophylline sustained release matrix tablets. Der Pharm Lett 2012;4(2):530-5.
13. Trivedi P, Verma AM, Garud N. Preparation and characterization of aceclofenac microspheres. Asian J Pharm 2008;2(2):110-5.
14. Martin A, Butamante P, Chun AH. Physical Pharmacy. 4th ed. Philadelphia, PA: Lea & Febiger; 1993. p. 431.
15. Manavalen R, Ramasamy C. Physical Pharmaceutics. 2nd ed. Tamil Nadu: Vignesh Publisher; 2001. p. 456.
16. Sinha VR, Agrawal MK, Kumria R. Influence of formulation and excipient variables on the pellet properties prepared by extrusion spheronization. Curr Drug Deliv 2005;2(1):1-8.
17. Gattani YS, Bhagwat DA, Maske AP. Formulation and evaluation of intragastric floating drug delivery system of diltiazem hydrochloride. Asian J Pharm 2008;2(4):228-31.
18. USP. The United States Pharmacopoeia XXIV. Rockville, MD: United States Pharmacopoeial Convention; 2000. p. 1941.
19. Sato Y, Kawashima Y, Takeuchi H, Yamamoto H. Physicochemical properties to determine the buoyancy of hollow microspheres (microballoons) prepared by the emulsion solvent diffusion method. Eur J Pharm Biopharm 2003;55(3):297-304.
20. Garg R, Gupta GD. Gastroretentive floating microspheres of Silymarin: Preparation and in vitro evaluation. Trop J Pharm Res 2010;9(1):59-66.
21. Jagtap YM, Bhujbal RK, Ranade AN, Ranpise NS. Effect of various polymers concentrations on physicochemical properties of floating microspheres. Indian J Pharm Sci 2012;74(6):512-20.
22. Garg R, Gupta GD. Progress in controlled gastroretentive delivery systems. Trop J Pharm Res 2008;7(3):1055-66.
23. Mohan Kamila M, Mondal N, Kanta Ghosh L, Kumar Gupta B. Multiunit floating drug delivery system of rosiglitazone maleate: Development, characterization, statistical optimization of drug release and in vivo evaluation. AAPS PharmSciTech 2009;10(3):887-99.
24. Reddy P, Dorle AK, Krishna DK. Albumin microspheres: Effect of process variables on the distribution and in vitro release. Drug Dev Ind Pharm 1990;16:1781-803.
25. Hafeez A, Maurya A, Singh J, Rana L. In vitro evaluation of floating microsphere of Ketoprofen. J Sci Innov Res 2013;2(3):714-22.
26. Perumandla PK, Priya S. Formulation and in vitro evaluation of floating microspheres of dextromethorphan hydrobromide. Int J Pharm Pharm Sci 2014;6(4):206-10
27. Tripathi M, Radhika PR, Sivakumar T. Formulation and evaluation of glipzide hollow microbaloons for floating drug delivery. Bull Pharm Res 2011;1(1):67-74.
28. Srivastava AK, Ridhurkar DN, Wadhwa S. Floating microspheres of cimetidine: Formulation, characterization and in vitro evaluation. Acta Pharm 2005;55(3):277-85.
29. Dash S, Murthy PN, Nath L, Chowdhury P. Kinetic modeling on drug release from controlled drug delivery systems. Acta Pol Pharm 2010;67(3):217-23.
30. Bajaj S, Singla D, Sakhuja N. Stability testing of pharmaceutical products. J Appl Pharm Sci 2012;2(3):129-38.
The publication is licensed under CC By and is open access. Copyright is with author and allowed to retain publishing rights without restrictions.