NLC as a potential carrier system for transdermal delivery of forskolin*
* Preliminary report presented at 6th Central European Congress of Life Sciences. EUROBIOTECH, 11–14 September, 2017. Kraków, Poland
NLC (nanostructured lipid carriers), composed with substances of GRAS (generally recognized as safe) status, were obtained by using the hot high pressure homogenization technique (HPH). The influence of number of homogenization cycles and concentration of a surfactant (decyl glucoside) on NLC properties were studied. The systems stability was assessed by macroscopic observation, light backscattering and zeta potential measurements. NLC particle size was measured by means of dynamic light scattering (DLS). The kinetically stable formulations were loaded with forskolin and selected for in vitro drug permeation study (Franz cell method). The concentration of forskolin in the receptor solution (i.e. Ethanol/PBS mixture) was analyzed by high performance liquid chromatography (HPLC) with UV detection. The obtained results have shown that NLC formulations could be used as effective carriers for forskolin permeation through the skin.
Burlando B, et al, (2010), Herbal Principles in Cosmetics: Properties and Mechanisms of Action, CRS Press Taylor & Francis Group, 212-216.
Caldero G, Garcia-Celma MJ, Solans C, (2011) Formation of polymeric nano-emulsions by a low-energy method and their use for nanoparticle preparation. J Colloid Interface Sci., 353(2): 406–411. DOI: 10.1016/j.jcis.2010.09.073
Chen H, Chang X, Du D, Liu W, Liu J, Weng T, Yang Y, Xu H, Yang X, (2006), Podophyllotoxin-loaded solid lipid nanoparticles for epidermal targeting, J. Control. Release, 110: 296–306. https://doi.org/10.1016/j.jconrel.2005.09.052
Chen Y, Zhu X, Zhang X, Liu B, Huang L, (2010), Nanoparticles modified with tumor-targeting scFv deliver siRNA and miRNA for cancer therapy, Mol Ther., 18(9):1650-6. DOI: 10.1038/mt.2010.136
Dhar S, Kolishetti N, Lippard SJ, Farokhzad OC, (2011), Targeted delivery of a cisplatin prodrug for safer and more effective prostate cancer therapy in vivo, Proc Natl Acad Sci., 108(5): 1850-5. DOI: 10.1073/pnas.1011379108
Han F, Li S, Yin R, Liu HZ, Xu L, (2008), Effect of surfactant on the formation and characterization of a new type of colloidal drug delivery system: nanostructured lipid carriers, Colloids Surf. A, 315: 210-216. DOI: 10.1016/j.colsurfa.2007.08.005
Jenning V., Schäfer-Korting M., Gohla S., (2000), Vitamin A-loaded solid lipid nanoparticles for topical use: drug release properties, J. Control. Release, 66: 115–126. https://doi.org/10.1016/S0168-3659(99)00223-0
Junyapraserta VB, Teeranachaideekula V, Souto EB, Boonmed P, Müller RH, (2009), Q10-loaded NLC versus nanoemulsions: Stability, rheology and in vitro skin permeation, Int. J. Pharm., 377: 207-214. DOI: 10.1016/j.ijpharm.2009.05.020
Liu J, Hu W, Chen H, Ni Q, Xu H, Yang X, (2007), Isotretinoin-loaded solid lipid nanoparticles with skin targeting for topical delivery, Int. J. Pharm., 328: 191–195. DOI: 10.1016/j.ijpharm.2006.08.007
Mulla JS, Khazi IM, (2009), Influence of process variables on particle size of solid lipid nanoparticles, Indian Journal of Novel Drug Delivery, 1(1): 47-49
Müller RH, Mehnert W, Lucks JS, Schwarz C, zur Muhlen A, Weyhers H, Freitas C, Ruhl D, (1995), Solid lipid nanoparticles (SLN): an alternative colloidal carrier system for controlled drug delivery, Eur. J. Pharm. Biopharm.41, 62–69.
Müller RH, Petersen RD, Hommoss A, Pardeike J, (2007), Nanostructured lipid carriers (NLC) in cosmetic dermal products, Adv. Drug Deliv. Rev.59: 522–530. DOI: 10.1016/j.addr.2007.04.012
Müller RH, Radtke M, Wissing SA, (2002a), Nanostructured lipid matrices for improved microencapsulation of drugs, Int. J. Pharm.242: 121–128. https://doi.org/10.1016/S0378-5173(02)00180-1
Okamoto, Kamatsu H, Hashida M, Sezaki H, (1986), Effects of β-cyclodextrin and di-o-methyl-β-cyclodextrin on the percutaneous absorption of butylparaben, indomethacin and sulfanylic acid. Int. J. Pharm, 30: 34-35
Paolino D, Stancampiano AHS, Cilurzo F, Cosco D, Puglisi G, Pignatello R, (2011), Nanostructured Lipid Carriers (NLC) for the Topical Delivery of Lutein, Drug Delivery Letters, 1: 32-39. DOI: 10.2174/2210304x11101010032
Pardeike J, Hommos A, Müller RH, (2009), Lipid nanoparticles (SLN, NLC) in cosmetic and pharmaceutical dermal products, Int. J. Pharm. 366: 170-184. DOI: 10.1016/j.ijpharm.2008.10.003
Passeron T, Namiki T, Passeron H, Le Pape E, Hearing VJ, (2009), Forskolin protects keratinocytes from ultraviolet (UV) B-induced apoptosis and increases DNA repair independent of its effects on melanogenesis, J Invest Dermatol. Jan., 129(1): 162–166. DOI: 10.1038/jid.2008.182
Schwarz C, Menhert W, (1999), Solid lipid nanoparticles (SLN) for the controlled drug delivery. II. Drug incorporation and physicochemical characterization, J. Microencapsul., 16: 205-213. DOI: 10.1080/026520499289185
Selzer D, Abdel-Mottaleb MMA, Hahn T, Schaefer UF, Neumann D, (2013) Finite and infinite dosing: difficulties in measurements, evaluations and predictions. Adv Drug Deliv Rev., 65(2): 278-94. DOI: 10.1016/j.addr.2012.06.010
Souto EB, Müller RH, (2005), SLN and NLC for topical delivery of ketoconazole, J. Microencapsul., 22: 501–510. DOI: 10.1080/02652040500162436
Souto EB, Wissing SA, Barbosa CM, Müller RH, (2004), Development of a controlled release formulation based on SLN and NLC for topical clotrimazole delivery, Int. J. Pharm., 278: 71–77. DOI: 10.1016/j.ijpharm.2004.02.032
Spry ML, Vanover JC, Scott T, et al. (2009), Prolonged treatment of fair-skinned mice with topical forskolin causes persistent tanning and UV protection. Pigment Cell Melanoma Res., 22: 219–229.
Üner M, Wissing SA, Yener G, Müller RH, (2005), Solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) for application of ascorbyl palmitate, Pharmazie, 60: 577–582.
Vyas A, Kisore Das S, Singh D, Sonker A, Gidwani B, Jain V, Singh M, (2012), Recent Nanoparticulate Approaches of Drug Delivery for Skin Cancer, Trends in Applied Sciences Research 7 (8): 620-635. DOI: 10.3923/tasr.2012.620.635
Wissing SA, Müller RH, (2003), The influence of solid lipid nanoparticles on skin hydration and viscoelasticity - in vivo study, Eur J Pharm Biopharm. 56: 67-72. https://doi.org/10.1016/S0939-6411(03)00040-7
Zheng M, Falkeborg M, Zheng Y, Yang T, Xu X (2013) Formulation and characterization of nanostructured lipid carriers containing a mixed lipids core. Colloids Surf A 430: 76–84. https://doi.org/10.1016/j.colsurfa.2013.03.070
Copyright (c) 2018 Elwira Lasoń, Elżbieta Sikora, Małgorzata Miastkowska, Elvira Escribano, Maria Jose Garcia-Celma, Conxita Solans, Meritxell Llinas, Jan Ogonowski
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