DESIGN, OPTIMIZATION AND IN VITRO EVALUATION OF ANTIFUNGAL ACTIVITY OF NANOSTRUCTURED LIPID CARRIERS OF TOLNAFTATE

  • AHMED GARDOUH Department of Pharmaceutics, Faculty of Pharmacy, Suez Canal University, Ismailia, Egypt
  • Samar H. Faheim Department of Pharmaceutics, Faculty of Pharmacy, Horus University, New Damietta, Egypt https://orcid.org/0000-0002-5112-0710
  • Samar M. Solyman Department of Microbiology and Immunology, Faculty of Pharmacy, Suez Canal University, Ismailia, Egypt https://orcid.org/0000-0002-8450-5940

Abstract

Objective: The main purpose of this work was to prepare tolnaftate (TOL) loaded nanostructured lipid carriers (NLCs), Evaluate its characteristics and in vitro release study.


Methods: Tolnaftate loaded Nanostructured lipid carriers were prepared by the high shear homogenization method using different liquid lipids types (DERMAROL DCO® and DERMAROL CCT®) and concentrations, different concentration ratios of tween80® to span20® and different homogenization speeds. All the formulated nanoparticles were subjected to particle size (PS), zeta potential (ZP), polydispersity index (PI), drug entrapment efficiency (EE), Differential Scanning Calorimetry (DSC), Transmission Electron microscopy (TEM), release kinetics and in vitro release study was determined.


Results: The results revealed that NLC dispersions had spherical shapes with an average size between 154.966±1.85 nm and 1078.4±103.02 nm. High entrapment efficiency was obtained with negatively charged zeta potential with PDI value ranging from 0.291±0.02 to 0.985±0.02. The release profiles of all formulations were characterized by a sustained release behavior over 24 h and the release rates increased as the amount of surfactant decreased. The release rate of TOL is expressed following the theoretical model by Higuchi.


Conclusion: From this study, It can be concluded that NLCs are a good carrier for tolnaftate delivery

Keywords: Nanostructured lipid carriers, High shear homogenization method, Topical antifungal drug

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Author Biography

AHMED GARDOUH, Department of Pharmaceutics, Faculty of Pharmacy, Suez Canal University, Ismailia, Egypt

Pharmaceutics. highly ranked work done.

References

1. Mehnert W, Mäder K. Solid lipid nanoparticles: production, characterization and applications. Adv Drug Delivery Rev 2001;47:165-96.
2. Lee CM, Maibach HI. Deep percutaneous penetration into muscles and joints. J Pharm Sci 2006;95:1405-13.
3. Akhtar N, Verma A, Pathak K. Topical delivery of drugs for the effective treatment of fungal infections of skin. Curr Pharm Des 2015;21:2892-913.
4. Gungor S, Erdal MS, Aksu B. New formulation strategies in topical antifungal therapy. J Cosmet Dermatol Sci Appl 2013;3:56.
5. Battaglia L, Serpe L, Foglietta F, Muntoni E, Gallarate M, Del Pozo Rodriguez A, et al. Application of lipid nanoparticles to ocular drug delivery. Expert Opin Drug Delivery 2016;13:1743-57.
6. Jores K, Haberland A, Wartewig S, Mäder K, Mehnert W. Solid lipid nanoparticles (SLN) and oil-loaded SLN studied by spectrofluorometry and Raman spectroscopy. Pharm Res 2005;22:1887-97.
7. Muller R, Petersen R, Hommoss A, Pardeike J. Nanostructured lipid carriers (NLC) in cosmetic dermal products. Adv Drug Delivery Rev 2007;59:522-30.
8. Putranti AR, Primaharinastiti R, Hendradi E. Effectivity and physicochemical stability of nanostructured lipid carrier coenzyme Q10 in different ratio of lipid cetyl palmitate and alpha tocopheryl acetate as carrier. Asian J Pharm Clin Res 2017;10:146-52.
9. Duarah S, Pujari K, Durai R, Narayanan V. Nanotechnology-based cosmeceuticals: a review. Int J Appl Pharm 2016;8:1-12.
10. Abdelgawad R, Nasr M, Hamza M, Awad G. Topical and systemic dermal carriers for psoriasis. Int J Curr Pharm Res 2016;8:4-9.
11. Gunda SRC, Ganesh G. Formulation and evalutation of tolnaftate loaded topical liposomal gel for effective skin drug delivery to treat fungal diseases. J Chem Pharm Res 2014;6:856-66.
12. Kumar JR, Muralidharan S, Parasuraman S. Antifungal agents: new approach for novel delivery systems. J Pharm Sci Res 2014;6:229.
13. Meghana G, Karri VNR, Talluri SV, Trivedi D, Ganesh G. In vitro and in vivo behavior of liposomal gel for the treatment of topical fungal diseases. Int J PharmTech Res 2015;7:814-20.
14. Suraweera R, Pasansi H, Sakeena M. Assessing the characterizations of Ketoprofen loaded and unloaded virgin coconut oil based creamy nanoemulsion. Asian J Pharm Clin Res 2015;8:275-9.
15. Uner M. Preparation, characterization and physicochemical properties of solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC): their benefits as colloidal drug carrier systems. Die Pharmazie An Int J Pharm Sci 2006;61:375-86.
16. Devarajan PV, Sonavane GS. Preparation and in vitro/in vivo evaluation of gliclazide loaded Eudragit nanoparticles as a sustained release carrier. Drug Dev Ind Pharm 2007;33:101-11.
17. Kumar VV, Chandrasekar D, Ramakrishna S, Kishan V, Rao YM, Diwan PV. Development and evaluation of nitrendipine loaded solid lipid nanoparticles: influence of wax and glyceride lipids on plasma pharmacokinetics. Int J Pharm 2007;335:167-75.
18. Yasir M, Sara UVS. Solid lipid nanoparticles for nose to brain delivery of haloperidol: in vitro drug release and pharmacokinetics evaluation. Acta Pharm Sin B 2014;4:454-63.
19. Barry AL, Brown SD. Fluconazole disk diffusion procedure for determining the susceptibility of Candida species. J Clin Microbiol 1996;34:2154-7.
20. Wayne P. USA: CLSI. Clinical and Laboratory Standards Institute. Performance Standards for Antimicrobial Susceptibility Testing. Twenty-Second Informational Supplement. CLSI Document; 2012. p. M100-S22.
21. Kushwaha AK, Vuddanda PR, Karunanidhi P, Singh SK, Singh S. Development and evaluation of solid lipid nanoparticles of raloxifene hydrochloride for enhanced bioavailability. BioMed Res Int 2013. http://dx.doi.org/10.1155/2013/584549
22. Thatipamula R, Palem C, Gannu R, Mudragada S, Yamsani M. Formulation and in vitro characterization of domperidone loaded solid lipid nanoparticles and nanostructured lipid carriers. Daru: J Fac Pharm Tehran Univ Med Sci 2011;19:23.
23. Khalil RM, Abd Elbary A, Kassem MA, Ghorab MM, Basha M. Nanostructured lipid carriers (NLCs) versus solid lipid nanoparticles (SLNs) for topical delivery of meloxicam. Pharm Dev Technol 2014;19:304-14.
24. Saparia B, Murthy RR, Solanki A. Preparation and evaluation of chloroquine phosphate microspheres using cross-linked gelatin for long-term drug delivery. Indian J Pharm Sci 2002;64:48.
25. Haznedar S, Dortunc B. Preparation and in vitro evaluation of Eudragit microspheres containing acetazolamide. Int J Pharm 2004;269:131-40.
26. 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.
27. Ritger PL, 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 Controlled Release 1987;5:23-36.
28. Meleson K, Graves S, Mason TG. Formation of concentrated nanoemulsions by extreme shear. Soft Materials 2004;2:109-23.
29. Wulff Perez M, Torcello Gomez A, Galvez Ruiz M, Martin Rodriguez A. Stability of emulsions for parenteral feeding: preparation and characterization of o/w nanoemulsions with natural oils and Pluronic f68 as surfactant. Food Hydrocolloids 2009;23:1096-102.
30. Centis V, Vermette P. Physico-chemical properties and cytotoxicity assessment of PEG-modified liposomes containing human hemoglobin. Colloids Surf B Biointerfaces 2008;65:239-46.
31. Shakeel F, Baboota S, Ahuja A, Ali J, Aqil M, Shafiq S. Nanoemulsions as vehicles for transdermal delivery of aceclofenac. AAPS PharmSciTech 2007;8:191.
32. Muller R, Jacobs C, Kayser O. Nanosuspensions as particulate drug formulations in therapy: rationale for development and what we can expect for the future. Adv Drug Delivery Rev 2001;47:3-19.
33. Gaba B, Fazil M, Khan S, Ali A, Baboota S, Ali J. Nanostructured lipid carrier system for topical delivery of terbinafine hydrochloride. Bull Fac Pharm Cairo Univ 2015;53:147-59.
34. Schwarz C, Mehnert W, Lucks J, Müller R. Solid lipid nanoparticles (SLN) for controlled drug delivery. I. Production, characterization and sterilization. J Controlled Release 1994;30:83-96.
35. Higuchi WI. Analysis of data on the medicament release from ointments. J Pharm Sci 1962;51:802-4.
36. Uner M, Yener G. Importance of solid lipid nanoparticles (SLN) in various administration routes and future perspectives. Int J Nanomed 2007;2:289.
37. Liu M, Dong J, Yang Y, Yang X, Xu H. Characterization and release of triptolide-loaded poly (D, L-lactic acid) nanoparticles. Eur Polymer J 2005;41:375-82.
38. Nayak AP, Tiyaboonchai W, Patankar S, Madhusudhan B, Souto EB. Curcuminoids-loaded lipid nanoparticles: novel approach towards malaria treatment. Colloids Surf B: Biointerfaces 2010;81:263-73.
39. Dora CP, Singh SK, Kumar S, Datusalia AK, Deep A. Development and characterization of nanoparticles of glibenclamide by the solvent displacement method. Acta Pol Pharm 2010;67:283-90.
40. Hou D, Xie C, Huang K, Zhu C. The production and characteristics of solid lipid nanoparticles (SLNs). Biomater 2003;24:1781-5.
41. Gonzalez Mira E, Egea M, Garcia M, Souto E. Design and ocular tolerance of flurbiprofen loaded ultrasound-engineered NLC. Colloids Surf B: Biointerfaces 2010;81:412-21.
42. Jenning V, Mäder K, Gohla SH. Solid lipid nanoparticles (SLN™) based on binary mixtures of liquid and solid lipids: a 1H-NMR study. Int J Pharm 2000;205:15-21.
43. Segal E. Candida, still number one–what do we know and where are we going from there? Mycoses 2005;48:3-11.
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GARDOUH, A., S. H. Faheim, and S. M. Solyman. “DESIGN, OPTIMIZATION AND IN VITRO EVALUATION OF ANTIFUNGAL ACTIVITY OF NANOSTRUCTURED LIPID CARRIERS OF TOLNAFTATE”. International Journal of Pharmacy and Pharmaceutical Sciences, Vol. 11, no. 7, May 2019, pp. 109-15, doi:10.22159/ijpps.2019v11i7.33115.
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