Thermodynamic behavior of lipid nanoparticles upon delivery of Vitamin E derivatives into the skin: in vitro studies
Tóm tắt
This article reports the thermodynamic changes of lipid nanoparticles (LN) upon delivery of lipophilic vitamin E derivatives to the skin. Skin penetration of α-tocopherol (α-T) and α-tocopherol acetate (α-Ta) into and across porcine ear skin was investigated in vitro using tape-stripping test in modified Franz diffusion cells. Wide angle X-ray scattering (WAXS) and differential scanning calorimetry (DSC) have been used to characterize the polymorphism of the solid matrix of LN before and after in vitro skin penetration assay. Cetyl palmitate LN with a loading capacity of 20% of vitamin E derivatives (with regard to the lipid matrix) have shown the typical β’ modification of waxes, with a crystallinity index (%CI) between 30 and 40%. Mean particle size and shelf life stability was assessed by static (laser diffractometry, LD) and dynamic (photon correlation spectroscopy, PCS) light scattering techniques. Submicron-sized LN were produced, i.e., 99% of LN showed a size below 600 nm immediately after production. A mean size between 180 and 350 nm (polydispersity index < 0.25) was obtained for LN stored at both 8 and 22 °C, and this size range was kept constant for at least 20 days of shelf life. Quantification of α-T and α-Ta in the skin using tape-stripping provided a 3.4-fold increase in the level of actives within the stratum corneum (SC) and 1.3-fold increase in the viable epidermis (VE). LN increased skin penetration of both actives, following a cumulative release during 8 h in modified Franz diffusion cells. The differences in the distribution levels observed between α-T and α-Ta when delivered via LN was due to the different thermodynamic activity of both actives, i.e., following increased partition coefficient of α-Ta into SC and VE, in comparison to α-T.
Tài liệu tham khảo
Burton GW, Ingold KU. Vitamin E as in vitro and in vivo antioxidants. Ann N Y Acad Sci. 1989;570:7–22.
Kalka K, Mukhtar H, Turowski-Wanke A, Merk H. Biomelanin antioxidants in cosmetics: assessment based on inhibition of lipid peroxidation. Skin Pharmacol Appl Skin Physiol. 2000;13:143–9.
Burgess C. Topical vitamins. J Drugs Dermatol. 2008;7:s2–6.
Van Haaften RIM, Evelo CTA, Penders J, Eijnwachter MPF, Haenen GRMM, Bast A. Inhibition of human glutathione S-transferase P1-1 by tocopherol and α-tocopherol derivatives. Biochim Biophys Acta. 2001;1548:23–8.
Lam PY, Yan CW, Chiu PY, Leung HY, Ko KM. Schisandrin B protects against solar irradiation-induced oxidative stress in rat skin tissue. Fitoterapia. 2011;82:393–400.
Doktorovova S, Souto EB. Nanostructured lipid carrier-based hydrogel formulations for drug delivery: a comprehensive review. Expert Opin Drug Deliv. 2009;6:165–76.
Souto EB, Muller RH. Lipid nanoparticles: effect on bioavailability and pharmacokinetic changes. Handb Exp Pharmacol. 2010;197:115–41.
Müller RH, Mehnert W, Souto EB. Solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) for dermal delivery. In: Bronaugh L, editor. Percutaneous absorption. New York: Marcel Dekker, Inc.; 2005. p. 719–38.
Souto EB, Doktorovova S. Chapter 6—solid lipid nanoparticle formulations pharmacokinetic and biopharmaceutical aspects in drug delivery. Methods Enzymol. 2009;464:105–29.
Mehnert W, Mäder K. Solid lipid nanoparticles—production, characterization and applications. Adv Drug Deliv Rev. 2001;47:165–96.
Müller RH, Mäder K, Gohla S. Solid lipid nanoparticles (SLN) for controlled drug delivery—a review of the state of art. Eur J Pharm Biopharm. 2000;50:161–77.
Müller RH, Radtke M, Wissing SA. Solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) in cosmetic and dermatological preparations. Adv Drug Deliv Rev. 2002;54:S131–55.
Dingler A, Gohla S. Production of solid lipid nanoparticles (SLN): scaling up feasibilities. J Microencapsul. 2002;19:11–6.
Wissing SA, Lippacher A, Müller RH. Investigations on the occlusive properties of solid lipid nanoparticles (SLN). J Cosmet Sci. 2001;52:313–24.
Wissing SA, Müller RH. A novel sunscreen system based on tocopherol acetate incorporated into solid lipid nanoparticles. Int J Cosmet Sci. 2001;23:233–43.
Wissing SA, Müller RH. The influence of the crystallinity of lipid nanoparticles on their occlusive properties. Int J Pharm. 2002;242:377–9.
Pilgram GSK, van Pelt AME, Bouwstra JA, Koerten HK. Electron diffraction provides new information on human stratum corneum lipid organization studied in relation to depth and temperature. J Investig Dermatol. 1999;113:403–9.
Gonzalez-Mira E, Nikolic S, Garcia ML, Egea MA, Souto EB, Calpena AC. Potential use of nanostructured lipid carriers for topical delivery of flurbiprofen. J Pharm Sci. 2011;100:242–51.
Freitas C, Müller RH. Correlation between long-term stability of solid lipid nanoparticles (SLN™) and crystallinity of the lipid phase. Eur J Pharm Biopharm. 1999;47:125–32.
Egorova EM. The validity of the Smoluchowski equation in electrophoretic studies of lipid membranes. Electrophoresis. 1994;15:1125–31.
Martins S, Silva AC, Ferreira DC, Souto EB. Improving oral absorption of Salmon calcitonin by trimyristin lipid nanoparticles. J Biomed Nanotechnol. 2009;5:76–83.
Weyhers H. Feste Lipid Nanopartikel (SLN) für die gewebsspezifische Arzneistoffapplikation, Herstellung, Charakterisierung oberflächenmodifizierter Formulierungen. PhD Thesis, Freie Universität Berlin, Berlin; 1995.
Nielsen PB, Müllertz A, Norling T, Kristensen HG. The effect of α-tocopherol on the in vitro solubilisation of lipophilic drugs. Int J Pharm. 2001;222:217–24.
Souto EB, Müller RH. SLN and NLC for topical delivery of ketoconazole. J Microencapsul. 2005;22:501–10.
Alvarez-Roman R, Naik A, Kalia YN, Guy RH, Fessi H. Skin penetration and distribution of polymeric nanoparticles. J Control Release. 2004;99:53–62.
Short SM, Paasch BD, Turner JH, Weiner N, Daugherty AL, Mrsny RJ. Percutaneous absorption of biologically-active interferon-gamma in a human skin graft-nude mouse model. Pharm Res. 1996;13:1020–7.
Short SM, Rubas W, Paasch BD, Mrsny RJ. Transport of biologically active interferon-gamma across human skin in vitro. Pharm Res. 1995;12:1140–5.
Downing DT, Strauss JS. On the mechanism of sebaceous secretion. Arch Dermatol Res. 1982;272:343–9.