DEVELOPMENT AND IN VITRO EVALUATION OF NANOLIPID CARRIERS OF CLOBETASOL PROPIONATE AND PRAMOXINE HYDROCHLORIDE FOR TOPICAL DELIVERY
Objective: Formulation and characterization of clobetasol propionate (CP) and pramoxine hydrochloride (PH) loaded nanostructured lipid carriers (NLC) offering improved performance in terms of drug loading and long-term stability for topical drug delivery.
Methods: Drug-loaded NLC formulation was designed by melt-emulsification ultrasonication technique, by fluctuating the concentration of stearic acid and oleic acid. Poloxamer F68 and tween 80 were used as surfactants in the formulation and soya lecithin was used as stabilizer and co-surfactant. Differential scanning calorimetry (DLS), scanning electron microscopic studies (SEM), transmission electron microscopy (TEM), fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), x-ray diffraction (XRD), are the techniques used to characterize the preparations. Optimized drug-loaded formulations were evaluated for particle size, zeta potential, entrapment efficiency, in vitro drug release, hemocompatibility assay and cytotoxicity screening.
Results: For drug loaded formulation the particle size was found in nanometric range. In vitro drug release was carried out using dialysis membrane and drug release after 24h was found to be 90.98 %Â±1.89 for CP and 79.81 %Â±4.20 for PH.
Conclusion: The formulated NLC is a potential approach for sustained release of drug which may reduce systemic side effects, increase skin retention time and duration of action. Further in vivo studies will confirm the effect of NLC to increase skin retention time, decreases systemic absorption of the corticosteroid thereby avoiding side effects.
2. Finlay AY. Quality of life in atopic dermatitis. J Am Academy Dermatol 2001;45:64-6.
3. Beiber T. Atopic dermatitis. N Engl J Med 2008;358:1483-94.
4. Levy RM, Gelfand JM, Yan AC. The epidemiology of atopic dermatitis. Clin Dermatol 2003;21:109-15.
5. Zauner W, Farrow NA, Haines AM. In vitro uptake of polystyrene microspheres: effect of particle size cell line and cell density. J Controlled Release 2001;7:39-51.
6. Sahu MK, Soni GC, Prajapati Sk. Nanostructured lipid carrier; The second generation of solid lipid nanoparticle. Int J Pharm Res Scholars 2012;1:224-35.
7. Muller R, H Petersen, RD Hommoss, A Pardeike. Lipid nanoparticles: recent advances. J Adv Drug Delivery Rev 2007;1:522-9.
8. So Hee Nam, Xu Ying Ji, Jong-Sang Park. Investigation of tacrolimus loaded nanostructured lipid carriers for topical drug delivery. Bull Korean Chem Soc 2011;32:956-60.
9. Luis Antonio Dantas Silva, Stephania Fleury Taveira, Eliana Martins Lima, Ricardo Neves Marreto. In vitro skin penetration of clobetasol from lipid nanoparticles: drug extraction and quantitation in different skin layers. Braz J Pharm Sci 2012;48:48-57.
10. Date AA, Nagarsenker MS. Design and evaluation of selfnanoemulsifying drug delivery systems (SNEDDS) for cefpodoximeproxetil. Int J Pharm 2007;329:166-72.
11. Neda Naseri, Hadi Valizadeh, Parvin Zakeri-Milani. Solid lipid nanoparticles and nanostructuredlipid carriers: structure, preparation and application. Adv Pharm Bull 2015;5:305-13.
12. EB Souto, SA Wissing, CM Barbosa, RH MÃ¼ller. Development of a controlled release formulation based on sln and nlc for topical clotrimazole delivery. Int J Pharm 2004;278:71â€“7.
13. Ruma Maji, Niladri Shekhar Dey, Bhabani Sankar Satapathy, Biswajit Mukherjee, Subhasish Mondal. Preparation and characterization of tamoxifen citrate loaded nanoparticles for breast cancer therapy. Int J Nanomed 2017;9:3107-18.
14. Shubham Uprit, Ram Kumar Sahu, Amit Roy, Aniruddha Pare. Preparation and characterization of minoxidil loaded nanostructured lipid carrier gel for the eï¬€ective treatment of alopecia. Saudi Pharma J 2013;21:379â€“85.
15. Shu-Ben Sun, Ping Liu, Fa-Ming Shao, Qi-Long Miao. Formulation and evaluation of PLGA nanoparticles loaded capecitabine for prostate cancer. Int J Clin Exp Med 2015;8:19670-81.
16. G Divya, Rajitha Panonnummal, Swati Gupta, R Jayakumar, M Sabitha. Acitretin and aloe-emodin loaded chitin nanogel for the treatment of psoriasis. Eur J Pharm Biopharm 2016;107:97-109.
17. Rajitha Panonnummal, R Jayakumar, M Sabitha. Comparative anti-psoriatic efficacy studies of clobetasol loaded chitin nanogel and marketed cream. Eur J Pharm Sci 2016;96:193-206.
18. Reshmi KP, Subin Mary Zachariah, Vidya Viswanad. Formulation and evaluation of novel chromene derivatives as an anti-inflammatory agent used for inflammatory bowel diseases. Asian J Pharm Clin Res 2017;10:213-24.
19. J Smith, E Wood, M Dornish. Effect of chitosan on epithelial cell tight junctions. Pharm Res 2004;21:43-9.
20. Shammika P, Aneesh TP, Vidya Viswanad. Solubility enhancement of synthesized quinazolinone derivative by solid dispersion technique. Int J Pharm Sci Rev Res 2016;41:197-206.
21. Guiling Li, Yating Fanb, Chao Fanb, Xinru Li, Xiaoning Wang Mei Li a, YanLiub. Tacrolimus-loaded ethosomes: physicochemical characterization and in vivo evaluation. Eur J Pharm Biopharm 2012;82:49-57.
22. Pranav V Patel, Hitesh K Patel, Shital S Panchal, Tejal A Mehta. Self-micro emulsifying drug delivery system of tacrolimus: formulation, in vitro evaluation and stability studies. Int J Pharma Investig 2013;3:95-104.
23. Freitas C, Muller RH. Effect of light and temperature on zeta potential and physical stability in solid lipid nanoparticle (SLNâ„¢) dispersions. Int J Pharm 1998;168:221-9.
24. Xiao Ying Ying, Yong Zhong Du, Wan Wei Chen, Hong Yuan, Fu-Qiang Hu. Preparation and characterization of modified lipid nanoparticles for doxorubicin controlled release. Pharmazie 2008;63:878-82.
25. Dilip Patel, Sandipan Dasgupta, Sanjay Dey, Y Roja Ramani, Subhabrata Ray, Bhaskar Mazumder. Nanostructured lipid carriers (nlc)-based gel for the topical delivery of aceclofenac: preparation, characterization, and in vivo evaluation. Sci Pharm 2012;80:749â€“64.
26. Biancamaria Baroli, Maria Grazia Ennas, Felice Loffredo, Michela Isola, Raimondo Pinna, M Arturo, et al. Penetration of metallic nanoparticles in the human full-thickness skin. J Inv Derm 2007;127:1701â€“12.