STUDY OF INFLUENCE OF FORMULATION AND PROCESS VARIABLES ON ENTRAPMENT EFFICIENCY AND PARTICLE SIZE OF FLOATING MICRO BALLOONS OF DIPYRIDAMOLE BY DOE

  • SEELAM RAMYA KRISHNA Department of Pharmaceutics, Chebrolu Hanumaiah Institute of Pharmaceutical Sciences; Acharya Nagarjuna University
  • A. RAMU Department of Pharmaceutics, Chebrolu Hanumaiah Institute of Pharmaceutical Sciences; Acharya Nagarjuna University
  • S. VIDYADHARA Department of Pharmaceutics, Chebrolu Hanumaiah Institute of Pharmaceutical Sciences; Acharya Nagarjuna University

Abstract

Objective: In the current research work, dipyridamole, a BCS class–II drug, was aimed to be formulated as floating controlled release microballoons using ethyl cellulose as polymer and span 80 as surfactant to improve the gastric retention of drug as the multi-particulate dosage forms have tremendous advantages over single unit dosage forms.


Methods: Microballoons were prepared by the emulsion solvent evaporation method. Prepared microballoons were characterized for entrapment efficiency, particle size, floating behavior and drug release studies. The study of effect of various formulation and process parameters like surfactant concentration, solvent volume, the volume of internal phase, polymer concentration, rotation speed on the drug entrapment efficiency and particle size of the microballoons were carried by using Box–Benhken to optimize the formulated microballoons.


Results: The smallest particle size of the microballoons was found to be 205.9 µm in the F32 formulation. The highest drug entrapment efficiency was found to be 93.4% in the F34 formulation. Buoyancy studies showed all the formulations have good floating characteristics that lasted for a minimum of 24 h. The maximum yield of microballoons was found in the F7 formulation with 91.8% yield. The final results were statistically treated using ANOVA and were found to be significant (p value<0.05).


Conclusion: Thus, the obtained results and their statistical interpretations indicated floating microballoons of dipyridamole were formulated effectively.

Keywords: Optimization, Gastric emptying, Dipyridamole, Gastric transit time, Box–Benhken design, Microballoons

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References

1. Foda NH, Ali SM. Gastroretentive drug delivery systems as a potential tool for enhancing the efficacy of antibiotics: a review. Int J Pharm Bio Sci 2011;2:94-104.
2. Anepu S, Duppala L, Sundari MS. Formulation development, characterization, and in vitro evaluation of floating matrix dosage form of tramadol hydrochloride using various polymers. Asian J Pharm Clin Res 2017;10:281-90.
3. Mohanraj Palanisamy, Jasmina Khanam, N Arun Kumar, C Rani. Chitosan microspheres encapsulated with metoprolol succinate: formulation and in vitro evaluation. Res J Pharm Tech 2009;2:349-52.
4. Pandey A, Kumar G, Kothiyal P, Barshiliya Y. A review on current approaches in gastro retentive drug delivery system. Asian J Pharm Nursing Med Sci 2012;2:60-77.
5. Chinna Gangadhar B, Shyam Sunder R, Vimal Kumar Varma M, Sleeva Raju M, Sai Kiran M. Formulation and evaluation of indomethacinmicrospheres using natural and synthetic polymers as controlled release dosage forms. Int J Drug Discovery 2010;2:8-16.
6. Patil UK, Sahu R, Yadav SK. Formulation and evaluation of controlled release microspheres containing metformin hydrochloride. Res J Pharm Tech 2009;2:176-9.
7. Kawatra M, Jain U, Ramana J. Recent advances in floating microspheres as a gastro-retentive drug delivery system: a review. Int J Adv Pharm Res 2012;2:5-23.
8. Ritesh Kumar, Surbhi Kamboj, Amrish Chandra, Pawan Kumar Gautam, Vijay Kumar Sharma. Microballoons: an advance avenue for gastroretentive drug delivery system-a review. UK J Pharm Bio Sci 2016:4;29-40.
9. Bhuvaneswari S, Manivannan S, Akshay M, Nify F. Formulation and evaluation of gastroretentive microballoons of acebrophylline for the treatment of bronchial asthma. Asian J Pharm Clin Res 2016;9:105-11.
10. Kouchak Maryam, Ali Badrian. Preparation and in vitro evaluation of a microballoon delivery system for theophylline. Int J Pharm Res 2007;6:35-42.
11. Durgapal S, Mukhopadhyay S, Goswami L. Preparation, characterization and evaluation of floating microparticles of ciprofloxacin. Int J Appl Pharm 2017;9:1-8.
12. Chaturvedi AK, Verma A, Singh A, Kumar A. Formulation and characterization of microballoons of norfloxacin. J Drug Delivery Ther 2011;1:21-6.
13. Bhardwaj P, Chaurasia H, Chaurasia D, Prajapati SK, Singh S. Formulation and in vitro evaluation of floating microballoons of indomethacin. Acta Pol Pharm 2010;67:291-8.
14. Jain A, Pandey V, Ganeshpurkar A, Dubey N, Bansal D. Formulation and characterization of floating microballoons of nizatidine for effective treatment of gastric ulcers in the murine model. Drug Delivery 2015;22:306-11.
15. Yadav A, Jain DK. Gastroretentive microballoons of metformin: formulation development and characterization. J Adv Pharm Technol Res 2011;2:51–5.
16. Soni M, Majumdar A, Malviya N. Mucoadhesive chitosan microspheres of gefitinib. Int J Curr Pharm Res 2018;10:9-19.
17. Srivastava AK, Ridhurkar DN, Wadhwa S. Floating microspheres of Cimetidine: Formulation, characterization and in vitro evaluation. Acta Pharm 2005;55:277–85.
18. Gidwani B, Vyas A, Ahirwar K, Shukla S. Factorial design and a practical approach for gastro–retentive drug delivery system. Res J Pharm Tech 2016;9:641-9.
19. Srikar G, Rani AP. Study on infuence of polymer and surfactant on in vitro performance of biodegradable aqueous-core nanocapsules of tenofovirdisoproxil fumarate by response surface methodology. Braz J Pharm Sci 2019;55:e18736.
20. Shende MA, Marathe RP. Development and optimization of oral gastroadhesive matrices for diltiazem hydrochloride using some natural materials. Res J Pharm Tech 2016;9:817–30.
21. Grandhi S, Rani AP, Pathuri R. Voriconazole solid lipid nanoparticles: Optimization of formulation and process parameters. Res J Pharm Tech 2018;11:2829-35.
22. Krishnamachari Y, Madan P, Lin S. Development of pH-and time-dependent oral microparticles to optimize budesonide delivery to ileum and colon. Int J Pharm 2007;338:238-47.
23. Dinarvand R, Moghadam SH, Sheikhi A, Atyabi F. Effect of surfactant HLB and different formulation variables on the properties of poly-D, L-lactide microspheres of naltrexone prepared by double emulsion technique. J Microencapsul 2005;22:139-51.
24. Rojas J, Pinto Aiphandary H, Leo E, Pecquet S, Couvreur P, Gulik A, et al. A polysorbate-based non-ionic surfactant can modulate loading and release of ?-lactoglobulin entrapped in multiphase poly (dl-lactide-co-glycolide) microspheres. Pharm Res 1999;16:255-60.
25. Sharma N, Madan P, Lin S. Effect of process and formulation variables on the preparation of parenteral paclitaxel-loaded biodegradable polymeric nanoparticles: a co-surfactant study. Asian J Pharm Sci 2016;11:404-16.
26. Srikar G, Shanthi D, Ramesh J, Kalyani V, Nagamma I. Floating microspheres: a prevailing trend in the development of gastroretentive drug delivery system. Asian J Pharm 2018;12:235-42.
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KRISHNA, S. R., A. RAMU, and S. VIDYADHARA. “STUDY OF INFLUENCE OF FORMULATION AND PROCESS VARIABLES ON ENTRAPMENT EFFICIENCY AND PARTICLE SIZE OF FLOATING MICRO BALLOONS OF DIPYRIDAMOLE BY DOE”. International Journal of Pharmacy and Pharmaceutical Sciences, Vol. 12, no. 10, Sept. 2020, pp. 85-91, doi:10.22159/ijpps.2020v12i10.35995.
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