Transdermal solid delivery of epigallocatechin-3-gallate using self-double-emulsifying drug delivery system as vehicle: Formulation,evaluation and vesicle-skin interaction
Restricted accessResearch articleFirst published online February, 2016
Transdermal solid delivery of epigallocatechin-3-gallate using self-double-emulsifying drug delivery system as vehicle: Formulation,evaluation and vesicle-skin interaction
The present study investigated a self-double-emulsifying drug delivery system loaded with epigallocatechin-3-gallate to improve epigallocatechin-3-gallate skin retention. The long chain solid lipids (cetostearyl alcohol) and macadamia oil were utilized as a carrier to deliver the bioactive ingredient. Response surface methodology was used to optimize the formulation, and the solid lipid to total lipid weight ratio, concentration of epigallocatechin-3-gallate and hydrophilic surfactant on skin retention were found to be the principal factors. The optimum formulation with high encapsulation efficiency (95.75%), self-double-emulsification performance (99.58%) and skin retention (87.24%) were derived from the fitted models and experimentally examined, demonstrating a reasonable agreement between experimental and predicted values. Epigallocatechin-3-gallate-self-double-emulsifying drug delivery system was found to be stable for 3 months. Transdermal studies could explain a higher skin diffusion of epigallocatechin-3-gallate from the self-double-emulsifying drug delivery system compared with EGCG aqueous solution. In vitro cytotoxicity showed that epigallocatechin-3-gallate-self-double-emulsifying drug delivery system did not exert hazardous effect on L929 cells up to 1:10.
ElsnerPMaibachHI. Cosmeceuticals drugs vs. cosmetics, New York: Marcel Dekker, Inc, 2002.
2.
DonaMDell'aicaICalabreseF. Neutrophil restraint by green tea: inhibition of inflammation, associated angiogenesis, and pulmonary fibrosis. J Immunol2003; 170: 4335–4341.
3.
AgarwalRKatiyarSKZaidiSI. Inhibition of skin tumor promoter-caused induction of epidermal ornithine decarboxylase in SENCAR mice by polyphenolic fraction isolated from green tea and its individual epicatechin derivatives. Cancer Res1992; 52: 3582–3588.
4.
ChungJHHanJHHwangE. Dual mechanisms of green tea extract (EGCG)-induced cell survival in human epidermal keratinocytes. FASEB J2003; 17: 1913–1915.
5.
HigdonJVFreiB. Tea catechins and polyphenols: health effects, metabolism, and antioxidant functions. Crit Rev Food Sci Nutr2003; 43: 89–143.
6.
BatchelderRJCalderRJThomasCP. In vitro transdermal delivery of the major catechins and caffeine from extract of Camellia sinensis. Int J Pharm2004; 283: 45–51.
7.
ChoiWILeeJHKimJ-Y. Efficient skin permeation of soluble proteins via flexible and functional nano-carrier. J Controlled Release2012; 157: 272–278.
8.
HoppelMReznicekGKahligH. Topical delivery of acetyl hexapeptide-8 from different emulsions: influence of emulsion composition and internal structure. Eur J Pharm Sci2015; 68: 27–35.
9.
HoppelMMahrhauserDStallingerC. Natural polymer stabilized multiple water in oil in water emulsions: a novel dermal drug delivery system for 5 fluorouracil. J Pharm Pharmacol2014; 66: 658–667.
10.
HoppelMBaurechtDHolperE. Validation of the combined ATR-FTIR/tape stripping technique for monitoring the distribution of surfactants in the stratum corneum. Int J Pharm2014; 472: 88–93.
11.
LutzRAserinAWickerL. Release of electrolytes from W/O/W double emulsions stabilized by a soluble complex of modified pectin and whey protein isolate. Colloids Surf B: Biointerface2009; 74: 178–185.
12.
ZhaoGHuCSunR. Development of novel composite antioxidant multiple lipid particles from combination of W/O/W multiple emulsions and solid lipid nanoparticles. European J Lipid Sci Technol2015; 117: 1056–1065.
13.
LvL-ZTongC-QLvQ. Enhanced absorption of hydroxysafflor yellow A using a self-double-emulsifying drug delivery system: in vitro and in vivo studies. Int J Nanomed2012; 7: 4099–4099.
14.
QiXWangLZhuJ. Self-double-emulsifying drug delivery system (SDEDDS): a new way for oral delivery of drugs with high solubility and low permeability. Int J Pharm2011; 409: 245–251.
15.
HuCZhaoGXiaQ. Development and characterization of a self-double-emulsifying drug delivery system containing both epigallocatechin-3-gallate and α-lipoic acid. J Mater Sci2015; 50: 6567–6577.
16.
GascoMRGallarateMPattarinoF. In vitro permeation of azelaic acid from viscosized microemulsions. Int J Pharm1991; 69: 193–196.
17.
ŠpiclinPHomarMZupančič-ValantA. Sodium ascorbyl phosphate in topical microemulsions. Int J Pharm2003; 256: 65–73.
18.
ComunianTAThomaziniMAlvesAJG. Microencapsulation of ascorbic acid by complex coacervation: protection and controlled release. Food Res Intl2013; 52: 373–379.
19.
MancaMLCastangiaICaddeoC. Improvement of quercetin protective effect against oxidative stress skin damages by incorporation in nanovesicles. Colloids Surf B: Biointerfaces2014; 123: 566–574.
20.
KawashimaYHinoTTakeuchiH. Shear-induced phase inversion and size control of water/oil/water emulsion droplets with porous membrane. J Colloid Interface Sci1991; 145: 512–523.
21.
MatosMGutiérrezGCocaJ. Preparation of water-in-oil-in-water (W1/O/W2) double emulsions containing trans-resveratrol. Colloids Surf A: Physicochem Eng Aspects2014; 442: 69–79.
22.
SchambilFJostFSchwugerMJInterfacial and colloidal properties of cosmetic emulsions containing fatty alcohol and fatty alcohol polyglycol ethers. In: HoffmannH (ed). New trends in colloid science, Steinkopff, 1987.
23.
KanouniMRosanoHNaouliN. Preparation of a stable double emulsion (W 1/O/W 2): role of the interfacial films on the stability of the system. Adv Colloid Interface Sci2002; 99: 229–254.
24.
GershanikTBenitaS. Self-dispersing lipid formulations for improving oral absorption of lipophilic drugs. European J Pharm Biopharm2000; 50: 179–188.
25.
TriplettMIIRathmanJ. Optimization of β-carotene loaded solid lipid nanoparticles preparation using a high shear homogenization technique. J Nanopart Res2009; 11: 601–614.
26.
SchwarzJCKlangVKarallS. Optimisation of multiple W/O/W nanoemulsions for dermal delivery of aciclovir. Int J Pharm2012; 435: 69–75.
27.
PardeikeJWeberSHaberT. A. Development of an itraconazole-loaded nanostructured lipid carrier (NLC) formulation for pulmonary application. Int J Pharm2011; 419: 329–338.
28.
OttoADu PlessisJWiechersJ. Formulation effects of topical emulsions on transdermal and dermal delivery. Int J Cosm Sci2009; 31: 1–19.
29.
MüllerRHPetersenRDHommossA. Nanostructured lipid carriers (NLC) in cosmetic dermal products. Adv Drug Deliv Rev2007; 59: 522–530.
30.
MorganCJRenwickAGFriedmannPS. The role of stratum corneum and dermal microvascular perfusion in penetration and tissue levels of water-soluble drugs investigated by microdialysis. Br J Dermatol2003; 148: 434–443.
31.
RodríguezGBarbosa-BarrosLRubioL. Conformational changes in stratum corneum lipids by effect of bicellar systems. Langmuir2009; 25: 10595–10603.
32.
HasanovicAWinklerRReschGP. Modification of the conformational skin structure by treatment with liposomal formulations and its correlation to the penetration depth of aciclovir. Eur J Pharm Biopharm2011; 79: 76–81.
33.
DamienFBonchevaM. The extent of orthorhombic lipid phases in the stratum corneum determines the barrier efficiency of human skin in vivo. J Invest Dermatol2010; 130: 611–614.
34.
AdlerSBasketterDCretonS. A. Alternative (non-animal) methods for cosmetics testing: current status and future prospects—2010. Archiv Toxicol2011; 85: 367–485.
35.
BasketterDAlépéeNCasatiS. Skin sensitisation – moving forward with non-animal testing strategies for regulatory purposes in the EU. Regulat Toxicol Pharmacol2013; 67: 531–535.
36.
MurgiaSFalchiAMManoM. Nanoparticles from lipid-based liquid crystals: emulsifier influence on morphology and cytotoxicity. J Phys Chem B2010; 114: 3518–3525.
37.
LeeJKKimDBKimJI. In vitro cytotoxicity tests on cultured human skin fibroblasts to predict skin irritation potential of surfactants. Toxicol Vitro2000; 14: 345–349.
38.
WeisburgJHWeissmanDBSedaghatT. In vitro cytotoxicity of epigallocatechin gallate and tea extracts to cancerous and normal cells from the human oral cavity. Basic Clinc Pharmacol Toxicol2004; 95: 191–200.
