• Noor Mohammed Dawood Department of Pharmaceutics, College of Pharmacy, University of Baghdad, Iraq-Baghdad
  • Shaimaa Nazar Abdal-hammid Department of Pharmaceutics, College of Pharmacy, University of Baghdad, Iraq-Baghdad
  • Ahmed Abbas Hussien Department of Pharmaceutics, College of Pharmacy, University of Baghdad, Iraq-Baghdad


Objective: The objective of this study was to prepare nanosuspension of a practical water insoluble antiulcer drug which is lafutidine to enhance the solubility, dissolution rate with studying the effect of different formulation variables to obtain the best formula with appropriate physical properties and higher dissolution rate.

Methods: Nanosuspension of lafutidine was prepared using solvent anti-solvent precipitation method using Polyvinylpyrrolidone K-90(PVP K-90) as the stabilizer. Ten formulations were prepared to show the effect of different variables in which two formulations showed the effect of stabilizer type, three formulations showed the effect of stabilizer concentration, two formulations showed the effect of combination of polymer with surfactant such as tween 80, three formulations show the effect of stirring speed and three formulations prepare to show the effect of addition of co-surfactant such as tween 20. All these formulations are evaluated for their particle size and entrapment efficiency and in vitro release. The selected one was evaluated for zeta potential, scanning electron microscope, atomic force microscopy, Fourier transforms infrared spectroscopy, differential scanning calorimetry, saturation solubility and stability study.

Results: The formulations (F3-F10) were in the nano size. The optimum concentration of the stabilizer was in the formulation when the drug: polymer: surfactant ratio 1:4:4 and the optimum stirring speed was 1500 rpm. Dramatic effect on the particle size reduction was found by the addition of co-surfactant (tween 20) in formulation F7 that has a particle size 15.89±1.8 nm. The selected formula F7 showed an enhanced dissolution profile (10 min) compared to the pure drug at all-time intervals.

Conclusion: The results show that the formulation that contains drug: PVP-K90: tween 80: tween 20 in ratio 1:4:2:2 is the best one and can be utilized to formulate lafutidine nanosuspension.


Keywords: Lafutidine, Solubility, Dissolution rate, Bioavailability


1. Marano S, Barker SA, Raimi-Abraham BT, Missaghi S, Rajabi-Siahboomi A, Craig DQ. Development of micro-fibrous solid dispersions of poorly water-soluble drugs in sucrose using temperature-controlled centrifugal spinning. Eur J Pharm Biopharm 2016;103:84-94.
2. Martin’s physical pharmacy and pharmaceutical sciences. 4th Edition; 2006. p. 220.
3. Loh ZH, Samanta AK, Heng PW. Overview of milling techniques for improving the solubility of poorly water-soluble drugs. Asian J Pharm Sci 2015;10:255-74.
4. K Ramesh B, Chandra S, Podile K. Formulation and evaluation of poorly soluble etravirine by spray drying method. Int J Pharm Pharm Sci 2015;7:98-103.
5. Bhairav BA, Bachhav JK, Saudagar RB. Review on solubility enhancement techniques. Asian J Pharm Res 2016;6:175-80.
6. Khadka P, Ro J, Kim H, Kim I, Kim JT, Kim H, et al. Pharmaceutical particle technologies: an approach to improve drug solubility, dissolution, and bioavailability. Asian J Pharm Sci 2014;9:304-16.
7. Kayaert P, Van den Mooter G. Is the amorphous fraction of a dried nanosuspension caused by milling or by drying? a case study with naproxen and cinnarizine. Eur J Pharm Biopharm 2012;81:650-6.
8. Amin MA, Osman SK, ALY UF. Preparation and characterization of ketoprofen nanosuspension for solubility and dissolution velocity enhancement. Int J Pharm Bio Sci 2013;4:768-80.
9. Sutradhar KB, Khatun S, Luna IP. Increasing possibilities of nanosuspension. J Nanotech 2013.
10. Agrawal G, Atrey R, Mishra P. A stability-indicating high performance liquid chromatographic analytical method for the determination of lafutidine in the tablet. Der Pharm Lett 2015;7:38-43.
11. Parveen A, Reddy RS. Formulation and in vitro evaluation of gastroretentive bilayer floating tablets of clarithromycin and lafutidine. Int J Pharm Tech 2014;6:6651-70.
12. Lolitas D. Design and evaluation of lafutidine floating tablets for controlled release by using semi-synthetic and natural polymer. J Drug Discovery Ther 2014;24:2.
13. Sravanthi N, Bandari D. Effect of super disintegrants on solubility and dissolution rate of lafutidine. Int J Adv Tech Eng Sci 2015;3:275-89.
14. Patel MD, Patel GD, Patel NC. Formulation and optimization of the raft-forming chewable tablet containing lafutidine. Int J Pharm Sci Drug Res 2015;7:229-34.
15. Patel DM, Patel DG, Patel CN. Formulation and optimization of a raft-forming chewable tablet containing lafutidine. Int J Pharm Sci Drug Res 2015;7:229-34.
16. Pandya VM, Patel JK, Patel DJ. Formulation, optimization and characterization of simvastatin nanosuspension prepared by nanoprecipitation technique. Pharm Lett 2011;3:129-40.
17. Jassim ZE, Hussein AA. Formulation and evaluation of clopidogrel tablet incorporating drug nanoparticles. Int J Pharm Pharm Sci 2014;6:838-51.
18. Shid RL, Dhole SN, Kulkarni N, Shid SL. Formulation and evaluation of nanosuspension formulation for drug delivery of simvastatin. Int J Pharm Sci Nanotech 2014;7:2650-65.
19. Sahu BP, Das MK. Nanosuspension for enhancement of oral bioavailability of felodipine. Appl Nanosci 2014;4:189-97.
20. Papdiwal A, Pande V, Aher S. Investigation of an effect of different stabilizers on a formulation of zaltoprofen nanosuspension. Int J Pharm Sci Rev Res 2014;27:244-9.
21. Deore S, Nerkar P, Mahajan H, Ige P. Formulation and evaluation of nanosuspension formulations polymers. Int J Pharm Sci Nanotechnol 2014;8:5-14.
22. Gadad AP, Naik SS, Dandagi PM, Bokmal UB. Formulation and evaluation of gastroretentive floating microspheres of lafutidine. Indian J Pharm Educ Res 2016;50Suppl:76-81.
23. Kakran M, Sahoo GN, Li L. Fabrication of nanoparticles of silymarin, hesperetin and glibenclamide by evaporative precipitation of nanosuspension for fast dissolution. Pharm Anal Acta 2015;6:2.
24. Jassem NA, Rajab NA. Formulation and in vitro evaluation of azilsartan medoxomil nanosuspension. Int J Pharm Pharm Sci 2017;9:110-9.
25. Wu L, Zhang J, Watanabe W. Physical and chemical stability of drug nanoparticles. Adv Drug Delivery Rev 2011;63:456-69.
26. Sinha B, Müller RH, Möschwitzer JP. Bottom-up approaches for preparing drug nanocrystals: formulations and factors affecting particle size. Int J Pharm 2013;453:1-15.
27. Amin MA, Osman SK, AlyUF. Preparation and characterization of ketoprofen nanosuspension for solubility and dissolution velocity enhancement. Int J Pharm Bio Sci 2013;4:768-80.
28. Krishna K, Hiral K, Navin S, Mahesh D. The impact of critical variables on properties of nanosuspension: a review. Int J Drug Dev Res 2015;7:150-61.
29. Rachmawati H, Shaal LA, Müller RH, Keck CM. Development of curcumin nanocrystal: physical aspects. J Pharm Sci 2013;102:204-14.
30. Zu Y, Sun W, Zhao X, Wang W, Li Y, Ge Y, et al. Preparation and characterization of amorphous amphotericin B nanoparticles for oral administration through liquid anti-solvent precipitation. Eur J Pharm Sci 2014;53:109-17.
31. Senthil Kumar P, Arivuchelvan A, Jagadeeswaran A, Subramanian N, Senthil Kumar C, Mekala P. Formulation, optimization and evaluation of enrofloxacin solid lipid nanoparticles for sustained oral delivery. Asian J Pharm Clin Res 2015;8:231-6.
32. Yeole BD, Patil RP, Lone KD, Tekade AR. Preparation of nanoparticles of poorly water-soluble dronedarone by antisolvent addition technique using the natural polymer as a stabilizer. J Pharm Res Clin Prac 2016;6:8-16.
33. Gera S, Talluri S, Rangaraj N, Sampathi S. Formulation and evaluation of naringenin nanosuspensions for enhancement. AAPS PharmSciTech 2017;18:3151-62.
34. Maaz A, Abdelwahed W, Tekko IA, Trefi S. Influence of nanoprecipitation method parameters on nanoparticles loaded with gatifloxacin for ocular drug delivery. Int J Acad Sci Res 2014;3:1-2.
35. Jünemann D, Dressman J. Analytical methods for dissolution testing of nanosized drugs. J Pharm Pharmacol 2012;64:931-43.
36. Ahuja BK, Jena SK, Paidi SK, Bagri S, Suresh S. Formulation, optimization and in vitro–in vivo evaluation of febuxostat nanosuspension. Int J Pharm 2015;478:540-52.
37. Junyaprasert VB, Morakul B. Nanocrystals for enhancement of oral bioavailability of poorly water-soluble drugs. Am J Pharmacol Sci 2015;10:13-23.
38. Fu X, Kong W, Zhang Y, Jiang L, Wang J, Lei J. Novel solid-solid phase change materials with biodegradable trihydroxy surfactants for thermal energy storage. RSC Adv 2015;5:68881-9.
39. Mishra B, Sahoo J, Dixit PK. Fabrication of cinnarizine nanosuspensions by ultrasonication technique: a systematic study of formulation parameters on particle size and in vitro dissolution. Biopharm J 2017;1:12-21.
40. Vora C, Patadia R, Mittal K, Mashru R. Preparation and characterization of dipyridamole solid dispersions for stabilization of supersaturation: effect of precipitation inhibitors type and molecular weight. Pharm Dev Tech 2016;21:847-55.
608 Views | 1671 Downloads
How to Cite
Dawood, N. M., Abdal-hammid, S. N., & Hussien, A. A. (2018). FORMULATION AND CHARACTERIZATION OF LAFUTIDINE NANOSUSPENSION FOR ORAL DRUG DELIVERY SYSTEM. International Journal of Applied Pharmaceutics, 10(2), 20-30.
Original Article(s)