Thermodynamic behavior of lipid nanoparticles upon delivery of Vitamin E derivatives into the skin: in vitro studies

被引:6
作者
Fangueiro, J. F. [1 ]
Macedo, A. S. [1 ]
Jose, S. [2 ]
Garcia, M. L. [3 ,4 ]
Souto, S. B. [5 ]
Souto, E. B. [1 ,6 ]
机构
[1] Fernando Pessoa Univ, Fac Hlth Sci, P-4200150 Oporto, Portugal
[2] Mahatma Gandhi Univ, Dept Pharmaceut Sci, Ettumanoor 686631, Kerala, India
[3] Univ Barcelona, Fac Pharm, Dept Phys Chem, E-08028 Barcelona, Spain
[4] Univ Barcelona, Inst Nanosci & Nanotechnol, E-08028 Barcelona, Spain
[5] Hosp Sao Joao, Dept Endocrinol, P-4200319 Oporto, Portugal
[6] Univ Tras Os Montes & Alto Douro CGB UTAD IBB, Ctr Genom & Biotechnol, Inst Biotechnol & Bioengn, P-5001801 Vila Real, Portugal
关键词
Vitamin E; Tocopherol; Vitamin E-acetate; Tocopherol-acetate; Lipid nanoparticles; LN; Porcine ear skin; ACTIVE INTERFERON-GAMMA; DRUG-DELIVERY; OCCLUSIVE PROPERTIES; TOPICAL DELIVERY; ALPHA-TOCOPHEROL; SLN; CRYSTALLINITY; FORMULATIONS; INHIBITION; ABSORPTION;
D O I
10.1007/s10973-011-1645-z
中图分类号
O414.1 [热力学];
学科分类号
摘要
This article reports the thermodynamic changes of lipid nanoparticles (LN) upon delivery of lipophilic vitamin E derivatives to the skin. Skin penetration of alpha-tocopherol (alpha-T) and alpha-tocopherol acetate (alpha-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 beta' 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 degrees C, and this size range was kept constant for at least 20 days of shelf life. Quantification of alpha-T and alpha-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 alpha-T and alpha-Ta when delivered via LN was due to the different thermodynamic activity of both actives, i.e., following increased partition coefficient of alpha-Ta into SC and VE, in comparison to alpha-T.
引用
收藏
页码:275 / 282
页数:8
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