ENCAPSULATION OF IBUPROFEN INTO SOLID LIPID NANOPARTICLES FOR CONTROLLED AND SUSTAINED RELEASE USING EMULSIFICATION SOLVENT EVAPORATION TECHNIQUE

  • WESLEY N OMWOYO Department of Chemistry, Vaal University of Technology, Private Bag X021, Vanderbijlpark, South Africa.
  • MAKWENA J MOLOTO Department of Chemistry, Vaal University of Technology, Private Bag X021, Vanderbijlpark, South Africa.

Abstract

Objective: The objective of the study was to encapsulate ibuprofen (IBU) into solid lipid nanoparticles (SLNs) for enhanced dissolution and achieving a sustained and controlled release of the drug from the nanocarrier.


Methods: IBU loaded nanoparticles were prepared by emulsification solvent evaporation technique and characterized by Fourier Transform Infrared spectroscopy, Thermogravimetric Analysis, X-ray diffraction (XRD), and transmission electron microscopy. Release kinetics on the drug-loaded nanoparticles was carried out in phosphate buffer pH 6.8 using pharma test dissolution apparatus adopting shaking basket method at 37°C.


Results: The optimized IBU-loaded SLNs had a particle size of 76.40 nm, polydispersity index of 0.275, and zeta potential of −41.3 mV. The encapsulation efficiency (EE) and DL were 99.73% and 2.31%, respectively. The Fourier transform infrared spectroscopy (FTIR) spectra confirmed successful encapsulation of the drug inside the nanocarrier as only peaks responsible for the emulsifier and the binder could be identified. This corroborated well with XRD spectra which showed a completely amorphous state of the drug-loaded nanoparticles as compared to the crystalline nature of the pure drug. The IBU-SLNs showed a release profile of up to 8 h which is a great improvement from other reported works. The drug release pattern of IBU-SLNs was best fitted with Higuchi square root model and followed the Higuchi drug release kinetics. Korsmeyer-Peppas model confirmed a non-Fickian diffusion model for the release of the drug from the matrix system.


Conclusion: IBU-loaded SLNs were successfully prepared which had a sustained and controlled release. It was observed that the release of the drug from the matrix was diffusion controlled and time dependent.

Keywords: Cyclooxygenase, Nociceptors, Inflammation, Ibuprofen, Nanomedicine

Author Biography

WESLEY N OMWOYO, Department of Chemistry, Vaal University of Technology, Private Bag X021, Vanderbijlpark, South Africa.

Postdoctoral Fellow, Department of Chemistry

References

1. Yiyun C, Tongwen X. Dendrimers as potential drug carriers. Part I. Solubilization of non-steroidal anti-inflammatory drugs in the presence of polyamidoamine dendrimers. Eur J Med Chem 2005;40:1188-92.
2. Reis CP, Ferreira JP, Candeias S. Ibuprofen nanoparticles for oral delivery : Proof of concept. Biotherapeutic Discov 2013;4:1-5.
3. Jiang B, Hu L, Gao C, Shen J. Ibuprofen-loaded nanoparticles prepared by a co-precipitation method and their release properties. Int J Pharm 2005;304:220-30.
4. Zhu KJ, Li Y, Jiang HL, Yasuda H, Ichimaru A, Yamamoto K, et al. Preparation, characterization and in vitro release properties of ibuprofen-loaded microspheres based on polylactide, poly(epsilon-caprolactone) and their copolymers. J Microencapsul 2005;22:25-36.
5. Kumar S, Rajkumar S, Ruckmani K. Formulation and evaluation of ibuprofen loaded nanoparticles for improved anti-inflamatory activity. Acta pharm Turc 2003;45:125-30.
6. Potthast H, Dressman JB, Junginger HE, Midha KK, Oeser H, Shah VP, et al. Biowaiver monographs for immediate release solid oral dosage forms: Ibuprofen. J Pharm Sci 2005;94:2121-31.
7. Sweetman CS. Martindale: The Complete Drug Reference. Scriba GKE. Vol. 74. London, UK: Pharmaceuticl Press; 2011. p. 647-8.
8. Moore N. Ibuprofen: A journey from prescription to over-the-counter use. J R Soc Med 2007;100 Suppl 48:2-6.
9. Borhade N, Pathan AR, Halder S, Karwa M, Dhiman M, Pamidiboina V, et al. NO-NSAIDs. Part 3: Nitric oxide-releasing prodrugs of non-steroidal anti-inflammatory drugs. Chem Pharm Bull (Tokyo) 2012;60:465-81.
10. Shimpi S, Chauhan B, Shimpi P. Cyclodextrins: Application in different routes of drug administration. Acta Pharm 2005;55:139-56.
11. Mansouri M, Pouretedal HR, Vosoughi V. Preparation and characterization of ibuprofen nanoparticles by using solvent/antisolvent precipitation. Open Conf Proc J 2011;2:88-94.
12. Nada A, Bandarkar F, Al-basarah Y. Formulation of ibuprofen nanoparticles. Asian J Pharm 2017;11:4-10.
13. Csóka G, Marton S, Zelko R, Otomo N, Antal I. Application of sucrose fatty acid esters in transdermal therapeutic systems. Eur J Pharm Biopharm 2007;65:233-7.
14. Mehnert W, Mäder K. Solid lipid nanoparticles: Production, characterization and applications. Adv Drug Deliv Rev 2001;47:165-96.
15. Sreelola V, Sailaja AK. Preparation and characterisation of ibuprofen loaded polymeric nanoparticles by solvent evaporation technique. Int J Pharm Pharm Sci 2014;6:6-11.
16. Jan SU, Khan GM, Hussain I. Formulation development and investigation of ibuprofen controlled release tablets with hydrophilic polymers and the effect of co-excipients on drug release patterns. Pak J Pharm Sci 2012;25:751-6.
17. Omwoyo WN, Ogutu B, Oloo F, Swai H, Kalombo L, Melariri P, et al. Preparation, characterization, and optimization of primaquine-loaded solid lipid nanoparticles. Int J Nanomedicine 2014;9:3865-74.
18. Potta SG, Minemi S, Nukala RK, Peinado C, Lamprou DA, Urquhart A, et al. Preparation and characterization of ibuprofen solid lipid nanoparticles with enhanced solubility. J Microencapsul 2011;28:74-81.
19. Omwoyo WN, Melariri P, Gathirwa JW, Oloo F, Mahanga GM, Kalombo L, et al. Development, characterization and antimalarial efficacy of dihydroartemisinin loaded solid lipid nanoparticles. Nanomedicine 2016;12:801-9.
20. Giri TK, Kumar K, Alexander A, Ajazuddin AA, Badwaik H, Tripathi DK. A novel and alternative approach to controlled release drug delivery system based on solid dispersion technique. Bull Fac Pharm Cairo Univ 2012;50:147-59.
21. Westesen K, Bunjes H, Koch MH. Physicochemical characterization of lipid nanoparticles and evaluation of their drug loading capacity and sustained release potential. J Control Release 1997;48:223-36.
22. Begum N, Sailaja KA. Effect of formulation variables on the preparation of ibuprofen loaded polymeric nanoparticles. Pharm Nanotechnol 2016;3:111-21.
23. Cooper DL, Harirforoosh S. Design and optimization of PLGA-based diclofenac loaded nanoparticles. PLoS One 2014;9:e87326.
24. Akbari Z, Amanlou M, Karimi-Sabet J, Golestani A, Niassar MS. Production of ibuprofen-loaded solid lipid nanoparticles using rapid expansion of supercritical solution. J Nano Res 2015;31:15-29.
25. Sastre V, Ghaly ES. Controlled release ibuprofen nanoparticles : Physico-chemical characterization and drug release. Int J Pharm Pharm Sci 2014;6:99-107.
26. Hasnain MS, Nayak AK. Solubility and dissolution enhancement of ibuprofen by solid dispersion technique using PEG 6000-PVP K 30 combination carrier. Bulg J Sci Educ 2012;21:118-32.
27. Kotcherlakota R, Barui AK, Prashar S, Fajardo M, Briones D, Rodríguez-Diéguez A, et al. Curcumin loaded mesoporous silica: An effective drug delivery system for cancer treatment. Biomater Sci 2016;4:448-59.
28. Patil SJ, Kumar SY, Mokale JV, Naik BJ. Development of surfactant free nanoparticles by a single emulsion high pressure homogenization technique and effect of formulation parameters on the drug entrapment and release. Int J Pharm 2013;3:843-52.
29. Vineeth P, Rao PR, Kumar K, Babu BD, Veerabhadra RA, Suresh BK. Influence of organic solvents on nanoparticle formation and surfactants on release behaviour in-vitro using costunolide as model anticancer agent. Int J Pharm Pharm Sci 2014;6:638-45.
30. Gouda R, Baishya H, Quing Z. Application of mathematical models in drug release kinetics of carbidopa and levodopa ER tablets. J Dev Drugs 2017;6:1-8.
31. Dash S, Murthy PN, Nath L, Chowdhury P. Kinetic modeling on drug release from controlled drug delivery systems. Acta Pol Pharm 2010;67:217-23.
32. 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.
33. Owuor J, Oloo F, Ngetich J, Nyaigoti W, Gathirwa J. Comparison of freeze and spray drying to obtain primaquine-loaded solid lipid nanoparticles. Drug Des Dev Ther Comp 2017;1:1-8.
34. Ritger P, Peppas NA. A simple equation for description of solute release I. Fickian and non-fickian release from non-swellable devices in the form of slabs, spheres, cylinders or discs. J Control Release 1987;5:23-6.
35. Peppas NA, Khare AR. Preparation, structure and diffusional behavior of hydrogels in controlled release. Adv Drug Deliv Rev 1993;11:1-35.
36. Basak SC, Kumar KS, Ramalingam M. Design and release characteristics of sustained release tablet containing metformin HCl. Rev Bras Cienc Farm J Pharm Sci 2008;44:477-83.
37. Jana U, Mohanty AK, Manna PK, Mohanta GP. Preparation and characterization of nebivolol nanoparticles using eudragit® RS100. Colloids Surf B Biointerfaces 2014;113:269-75.
38. Arifin DY, Lee LY, Wang CH. Mathematical modeling and simulation of drug release from microspheres: Implications to drug delivery systems. Adv Drug Deliv Rev 2006;58:1274-325.
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How to Cite
WESLEY N OMWOYO, and MAKWENA J MOLOTO. “ENCAPSULATION OF IBUPROFEN INTO SOLID LIPID NANOPARTICLES FOR CONTROLLED AND SUSTAINED RELEASE USING EMULSIFICATION SOLVENT EVAPORATION TECHNIQUE”. Asian Journal of Pharmaceutical and Clinical Research, Vol. 12, no. 8, June 2019, pp. 74-81, https://innovareacademics.in/journals/index.php/ajpcr/article/view/33652.
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