• RAJKUMAR ALAND Department of Pharmacy, Jawaharlal Nehru Technological University, Kakinada, Andhra Pradesh, India.
  • GANESAN M Dr. Reddy’s Laboratories Limited, Hyderabad, Telangana, India.
  • RAJESWARA RAO P Department of Pharmacy, Andhra University, Visakhapatnam, Andhra Pradesh, India.


Objective: Psoriasis is an unswervingly recurring, inflammatory, autoimmune disorder of the skin, disturbing about 2–5% of the world population. The main objective for this investigation is to develop and optimize the solid lipid nanoparticles (SLN) formulation of tazarotene for effective drug delivery.

Methods: Tazarotene SLNs were fabricated by hot homogenization followed by the ultrasonication using Taguchi’s orthogonal array with eight parameters that could affect the particle size and entrapment efficiency (EE). In view of the outcomes from the examinations of the responses acquired from Taguchi design, three diverse independent variables including sonication time (s), lipid to drug ratio (w/w), and surfactant concentration (%) were carefully chosen for further investigation utilizing central composite design. The lipid dynasan-116, surfactant poloxamer-188, and cosurfactant egg lecithin resulted in better percent drug loading and evaluated for particle size, drug EE, zeta potential, in vitro drug release, and stability.

Results: The prepared nanoformulations were evaluated for different parameters and found to be in an acceptable range. In vitro drug release of optimized SLN formulation (F1) was found to be 98.12±1.52%, whereas pure drug release was 42.12 after 60 min, and the major mechanism of drug release follows zero-order kinetics release data for optimized formulation (F1) with non-Fickian (anomalous) with a strong correlation coefficient (R2=0.98598) of Korsmeyer-Peppas model. Transmission electron microscopy analysis has demonstrated the presence of individual nanoparticles in spherical shape, and the results were also compatible with particle size measurements. The drug content of tazarotene gel formulation was found to 98.96±0.021%, and the viscosity of gel formulation at 5 rpm was found to be 5.98×103±0.34×103 cp. The release rate (flux) of tazarotene across the membrane and expunged skin diverges pointedly, which specifies the barrier nature of skin. The flux value for SLN based gel formulation (193.454±4.324 μg/cm2/h) was found to be higher than that for marketed gel (116.345±2.238 μg/cm2/h). The higher flux and Kp values of SLN based gel suggest that it might be able to enter the skin easily as compared with marketed gel with an advantage of low interfacial tension of the emulsifier film that ensures an excellent contact to the skin.

Conclusion: From the obtained results, the topically oriented SLN-based gel formulation of tazarotene could be useful in providing effective and site-specific psoriasis treatment.

Keywords: Tazarotene, Psoriasis, Taguchi design, SLN, Topical gel, Flux


1. Mehnert W, Mader K. Solid lipid nanoparticles: Production, characterization and applications. Adv Drug Deliv Rev 2012;64:83-101.
2. Rohit B, Pal KI. A method to prepare solid lipid nanoparticles with improved entrapment efficiency of hydrophilic drugs. Curr Nanosci 2013;9:21120.
3. das Neves J, Amiji MM, Bahia MF, Sarmento B. Nanotechnology-based systems for the treatment and prevention of HIV/AIDS. Adv Drug Deliv Rev 2010;62:458-77.
4. Priya S, Marina K, Kumari NS. Formulation and characterization of ropinirole hydrochloride loaded solid lipid nanoparticles. Int J Pharm Pharm Sci 2015;7:85-9.
5. Perugini P, Tomasi C, Vettor M, Dazio V, Conti B, Genta I, et al. Influence of sln matrix modification on “in vitro” and “in vivo”nanoparticle performances. Int J Pharm Pharm Sci 2010;2:37-43.
6. Parisi R, Symmons DP, Griffiths CE, Ashcroft DM, Identification and Management of Psoriasis and Associated ComorbidiTy (IMPACT) project team. Global epidemiology of psoriasis: A systematic review of incidence and prevalence. J Invest Dermatol 2013;133:377-85.
7. Cameron JB, Voohees AS. History of Psoriasis. London: Springer; 2014.
8. Perera GK, Di Meglio P, Nestle FO. Psoriasis. Annu Rev Pathol 2012;7:385-422.
9. Raychaudhuri SK, Maverakis E, Raychaudhuri SP. Diagnosis and classification of psoriasis. Autoimmun Rev 2014;13:490-5.
10. Griffiths CE, Barker JN. Pathogenesis and clinical features of psoriasis. Lancet 2007;370:263-71.
11. Aqel B, Bishop M, Krishna M, Cangemi J. Collagenous colitis evolving into ulcerative colitis: A case report and review of the literature. Dig Dis Sci 2003;48:2323-7.
12. Russell JJ. Topical therapy for acne. Am Fam Phys 2000;61:1-13.
13. Zaenglein AL. Topical retinoids in the treatment of acne vulgaris. Semin Cutan Med Surg 2008;27:177-82.
14. Patel MR, Patel RB, Parikh JR, Patel BG. HPTLC method for estimation of tazarotene in topical gel formulations and in vitro study. Anal Methods 2010;2:275-81.
15. Manjunath K, Venkateswarlu V. Pharmacokinetics, tissue distribution and bioavailability of clozapine solid lipid nanoparticles after intravenous and intraduodenal administration. J Control Release 2005;107:215-28.
16. Müller RH, Mäder 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.
17. Roy A. Primer on the Taguchi Method. New York: Van Nostrand Reinhold; 1990.
18. Sharma P, Verma A, Sidhu RK, Pandey OP. Process parameter selection for strontium ferrite sintered magnets using Taguchi L9 orthogonal design. J Mater Process Technol 2005;168:147-51.
19. El-Moslamy SH, Elkady MF, Rezk AH, Abdel-Fattah YR. Applying taguchi design and large-scale strategy for mycosynthesis of nano-silver from endophytic trichoderma harzianum SYA.F4 and its application against phytopathogens. Sci Rep 2017;7:45297.
20. Chen YH. Application of Taghuchi method in the optimization of laser micro-engineering of photomasks. Int J Mater Prod Technol 1996;11:333-44.
21. Noordin MY, Venkatesh VC, Sharif S, Elting S, Abdullah A. Application of response surface methodology in describing the performance of coated carbide tools when turning AISI 1045 steel. J Mater Process Technol 2004;145:46-58.
22. Khosla A, Kumar S, Aggarwal KK. Identification of strategy parameters for particle swarm optimizer through Taguchi method. J Zhejiang Univ Sci 2006;7:1989-94.
23. Ba-Abbad MM, Kadhum AA, Mohamad AB, Takriff MS, Sopian K. Optimization of process parameters using D-optimal design for synthesis of ZnO nanoparticles via sol gel technique. J Ind Eng Chem 2013;19:99-105.
24. Hu C, Rhodes DG. Proniosomes: A novel drug carrier preparation. Int J Pharm 1999;185:23-35.
25. Maia CS, Mehnert W, Schäfer-Korting M. Solid lipid nanoparticles as drug carriers for topical glucocorticoids. Int J Pharm 2000;196:165-7.
26. Bachhav YG, Patravale VB. Microemulsion based vaginal gel of fluconazole: Formulation, in vitro and in vivo evaluation. Int J Pharm 2009;365:175-9.
27. El Laithy HM, El-Shaboury KM. The development of cutina lipogels and gel microemulsion for topical administration of fluconazole. AAPS PharmSciTech 2002;3:E35.
28. Yang RD, Mather RR, Fortheringham AF. The application of factorial experimental design to the processing of polypropylene fibres. J Mater Sci 2001;36:3097-101.
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