SOLID LIPID NANOPARTICLES AND NANOSTRUCTURED LIPID CARRIERS OF TOLNAFTATE: DESIGN, OPTIMIZATION AND IN-VITRO EVALUATION
Objective: The target of our work is the preparation of tolnaftate (TOL) loaded solid lipid nanoparticles (SLNs) as well as nanostructured lipid carriers (NLCs).
Methods: The high shear homogenization method was chosen for the preparation of nanoparticles. The nanoparticle dispersions were prepared using Compritol 888ATO, Tefose 63, MiglyolÂ® 812, Poloxamer188, and Tween80. Particle size (PS), zeta potential (ZP), polydispersity index (PDI), drug entrapment efficiency (EE) and in vitro release study were determined. Differential Scanning Calorimetry (DSC) analysis and morphological transmission electron microscopy (TEM) examination were conducted. A stability study for 3 mo was performed.
Results: The results revealed that NLC and SLN dispersions had spherical shapes with an average size between 41.10Â±1.92 nm and 98.85Â±1.01 nm. High entrapment efficiency was obtained with negatively charged zeta potential with PDI value ranging from 0.251Â±0.012 to 0.759Â±0.028. The release profiles of all formulations were characterized by a sustained release behavior over 24â€‰h and the release rates increased as the amount of liquid lipid in lipid core increased. Tolnaftate loaded NLC showed more stability than its corresponding SLN.
Conclusion: It can be fulfilled from this work that NLCs may represent a promising carrier for tolnaftate delivery offering both sustained release and stability.
2. Dubey A, Kamath J. Nanostructured lipid carriers: a novel topical drug delivery system. Int J PharmTech Res 2012;4:705-14.
3. Hadgraft J. Passive enhancement strategies in topical and transdermal drug delivery. Int J Pharm 1999;184:1-6.
4. Kreilgaard M. Influence of microemulsions on cutaneous drug delivery. Adv Drug Delivery Rev 2002;54:77-98.
5. MÃ¼ller R, Radtke M, Wissing S. Solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) in cosmetic and dermatological preparations. Adv Drug Delivery Rev 2002;54:131-55.
6. Liu J, Du Z, Bin Z. Preparation and pharmacokinetic evaluation of tanshinone IIA solid lipid. Drug Dev Ind Pharm 2005;31:551-6.
7. Prow T, Grice J, Lim L, Faye R, Butler M, Becker W, et al. Nanoparticles and microparticles for skin drug delivery. Adv Drug Delivery Rev 2011;63:470-91.
8. Luo D, Guo J, Wang F, Jin Z, Cheng X, Zhu J, et al. Anti-fungal efficacy of poly butyl cyanoacrylate nanoparticles of allicin and comparison with pure allicin. J Biomater Sci Polym Ed 2009;20:21-31.
9. Zhang N, Ping Q, Huang G, Xu W, Cheng Y, Han X. Lectin-modified solid lipid nanoparticles as carriers for oral administration of insulin. Int J Pharm 2006;327:153-9.
10. Bhaskar K, Krishna M, Lingam M, Prabshakar R, Venkateswardu V, Madhusudan R. Development of nitrendipine controlled release formulations based on SLN and NLC for topical delivery: in vitro and ex vivo characterization. Drug Dev Ind Pharm 2008;34:719-25.
11. Muller R, Mader K, Gohla S. Solid lipid nanoparticles (SLN) for controlled drug delivery a review of the state of the art. Eur J Pharm Biopharm 2000;50:161-77.
12. Mehnert W, Mader K. Solid lipid nanoparticlesâ€”production, characterization, and applications. Adv Drug Delivery Rev 2001;47:165-96.
13. Ryder N, Frank I, Dupont M. Ergosterol biosynthesis inhibition by the thiocarbamate antifungal agents tolnaftate and tolciclate. Antimicrob Agents Chemother 1986;29:858-60.
14. Noguchi T, Igarashi Y, Shigematsu A, Taniguchi K. Antitrichophyton activity of naphthiomate. Antimicrob Agents Chemother 1962;25:259-67.
15. Weinstein M, Oden E, Moss E. Antifungal properties of tolnaftate in vitro and in vivo. Antimicrob Agents Chemother 1964;10:595-601.
16. Meghana G, Siddhartha V, Raviteja G, Saikrishna R, Ganesh G. Formulation and evaluation of tolnaftate loaded topical liposomal gel for effective skin drug delivery to treat fungal diseases. J Chem Pharm Res 2014;6:856-66.
17. Upadhyay S, Patel J, Patel V, Saluja A. Effect of different lipids and surfactants on the formulation of solid lipid nanoparticles incorporating tamoxifen citrate. J Pharm Bioallied Sci 2012;4:112-3.
18. Bhaskar K, Krishna M, Lingam M, Prabshakar R, Venkateswardu V, Madhusudan R, et al. Development of SLN and NLC enriched hydrogels for transdermal delivery of nitrendipine: in vitro and in vivo characteristics. Drug Dev Ind Pharm 2009;35:98-113.
19. Neves A, Lucio M, Martin S, Lima JL, Reis S. Novel resveratrol nanodelivery systems based on lipid nanoparticles to enhance its oral bioavailability. Int J Nanomed 2013;8:177-87.
20. Sandri G, Bonferoni MC, Gokce EH, Ferrari F, Rossi S, Patrini M, et al. Chitosan-associated SLN: in vitro and ex vivo characterization of cyclosporine a loaded ophthalmic systems. J Microencapsul 2010;27:735-46.
21. Kumar V, 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.
22. 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 2013:1-9. doi: 10.1155/2013/584549. [Epub 20 Oct 2013].
23. Thatipamula R, Palem C, Gannu R, Mudragada S, Yamsami M. Formulation and in vitro characterization of domperidone loaded solid lipid nanoparticles and nanostructured lipid carriers. Daru 2011;19:23-32.
24. Khalil R, Abd-Elbary A, Kassem M, Ghorab M, Basha M. Nanostructured lipid carriers (NLCs) versus solid lipid nanoparticles (SLNs) for topical delivery of meloxicam. Pharm Dev Technol 2014;19:304-14.
25. Hao J, Fang X, Zhou Y, Wang J, Guo F, Li F, et al. Development and optimization of solid lipid nanoparticle formulation for ophthalmic delivery of chloramphenicol using a Box-Behnken design. Int J Nanomed 2011;6:683-92.
26. Ekambaram P, Abdul H. Formulation and evaluation of solid lipid nanoparticles of ramipril. J Young Pharm 2011;3:216-20.
27. Abdelbary G, Fahmy R. Diazepam-loaded solid lipid nanoparticles: design and characterization. AAPS PharmSciTech 2009;10:211-9.
28. Muller R, Radtke M, Wissing S. Nanostructured lipid matrices for improved microencapsulation of drugs. Int J Pharm 2002;242:121-8.
29. Patel D, Dasqupta S, Dey S, Ramani YR, Ray S, Mazumder B. Nanostructured lipid carriers (NLC)-based gel for the topical delivery of aceclofenac: preparation, characterization, and in vivo evaluation. Sci Pharm 2012;80:749-64.
30. Vijayan V, Jayachandran E, Anburaj J. Preparation and characterization of anti diabetic drug loaded solid lipid nanoparticles. J Pharm Res 2010;8:324.
31. Dandagi P, Dessai G, Gadad A, Desai V. Formulation and evaluation of nanostructured lipid carrier (NLC) of lornoxicam. Int J Pharm Pharm Sci 2014;6:73-7.
32. Centis V, Vermette P. Physico-chemical properties and cytotoxicity assessment of PEG-modified liposomes containing human hemoglobin. Colloids Surf B 2008;65:239-46.
33. Shakeel F, Ahuja A, Ali J, Aqil M, Shafik S. Nanoemulsions as vehiclesfor transdermal delivery of aceclofenac. AAPS PharmSciTech 2007;8:191-9.
34. Muller R, Kayser O. Nanosuspensions a particulate drug formulations in therapy: rationale for development and what we can expect for the future. Adv Drug Delivery Rev 2001;47:3-19.
35. Levy M, Schutze W, Fuhrer C, Benita S. Characterization of diazepam submicron emulsion interface: role of oleic acid. J Microencapsulation 1994;11:79-92.
36. Kumar PP, Gayatri P, Sunil R, Jaganmohan S, Rao YM. Atorvastatin loaded solidlipid nanoparticles: formulation, optimization, and in-vitro characterization. IOSR J Pharm 2012;2:23-32.
37. Uner M, Yener G. Importance of solid lipid nanoparticles (SLN) in various administration routes and future perspectives. Int J Nanomed 2007;2:289-300.
38. Liu M, Yang Y, Yang X, Xu H. Characterization and release of triptolide-loaded poly (d, l-lactic acid) nanoparticles. Eur Polym J 2005;41:375-82.
39. Nayak AP, T Patankar S, Madhusudhan B, Souto EB. Curcuminoids-loaded lipid nanoparticles: novel approach towards malaria treatment. Colloids Surf B 2010;81:263-73.
40. Hou D, Huang K, Zhu C. The production and characteristics of solid lipid nanoparticles (SLNs). Biomaterials 2003;24:1781â€“5.
41. Gonzalez-Mira E, Garcia ML, Souto EB. Design and ocular tolerance of flurbiprofen loaded ultrasound-engineered NLC. Colloids Surf B 2010;81:412â€“21.
42. Venkateswarlu V, Manjunath K. Preparation, characterization and in vitro release kinetics of clozapine solid lipid nanoparticle. J Controlled Release 2004;95:627â€“38.
43. Jenning V, Mader K, Gohla S. Solid lipid nanoparticles (SLN) based on binary mixtures of liquid and solid lipids: a H-NMR study. Int J Pharm 2000;205:15-21.
44. zur Muhlen A, Schwarz C, Mehnert W. Solid lipid nanoparticles (SLN) for controlled drug delivery--drug release and release mechanism. Eur J Pharm Biopharm 1998;45:149-55.
45. Higuchi W. Analysis of data on the medicament release from ointments. J Pharm Sci 1962;51:802-4.