Development and characterization of a self-double-emulsifying drug delivery system containing both epigallocatechin-3-gallate and α-lipoic acid
Source abstract
Abstract
The present study investigated a self-double-emulsifying drug delivery system (SDEDDS) loaded with epigallocatechin-3-gallate (EGCG) and α-lipoic acid to improve EGCG photostability and possess a sustained release behavior. The long chain solid lipids (cetostearyl alcohol) and macadamia oil were utilized as a carrier to co-deliver the two bioactive ingredients. The prepared EA-SDEDDS for topical application was formulated using modified two-step method and characterized by confocal microscopy, in vitro release, and antioxidant effects. EA-SDEDDS was found to be stable under simulated sunlight for 1 month (at room temperature). In vitro cell culture studies, EA-SDEDDS provided protection for 3t3 fibroblasts that underwent H2O2 oxidative stress due to sustained release property. Cellular antioxidant activity assay indicated that EA-SDEDDS showed anti-oxidative capacity with the same efficacy compared to EGCG-α-lipoic acid solution.
Source: openaire · Quality: candidate unverified · Source record ↗
Research context
OpenAlex topics: Biochemical Acid Research Studies · Tea Polyphenols and Effects · Muscle metabolism and nutrition
SciVX discovery tags are terminology-based. OpenAlex topics are source-provided classifications.
References (50)
Show source-provided references
1. Bansal S, Syan N, Mathur P, Choudhary S (2012) Pharmacological profile of green tea and its polyphenols: a review. Med Chem Res 21(11):3347–336010.1007/s00044-011-9800-4 ↗
2. Yuan JM, Sun C, Butler LM (2011) Tea and cancer prevention: epidemiological studies. Pharmacol Res 64(2):123–13510.1016/j.phrs.2011.03.002 ↗
3. Primavesi L, Piantanida M, Pravettoni V (2014) Chapter 66—Studying tea polyphenols and their protective effects on skin. In: Watson RR, Preedy VR, Zibadi S (eds) Polyphenols in human health and disease. Academic Press, San Diego
4. Meltzer SM, Monk BJ, Tewari KS (2009) Green tea catechins for treatment of external genital warts. Am J Obstet Gynecol 200(3):233.e1–233.e710.1016/j.ajog.2008.07.064 ↗
5. Yiannakopoulou E (2014) Effect of green tea catechins on breast carcinogenesis: a systematic review of in vitro and in vivo experimental studies. Eur J Cancer Prev 23(2):84–8910.1097/CEJ.0b013e328364f23e ↗
6. Kataoka H (1998) Chromatographic analysis of lipoic acid and related compounds. J Chromatogr B Biomed Sci Appl 717(1):247–26210.1016/S0378-4347(97)00628-2 ↗
7. Leu J-G, Lin C-Y, Jian J-H, Shih C-Y, Liang Y-J (2013) Epigallocatechin-3-gallate combined with alpha lipoic acid attenuates high glucose-induced receptor for advanced glycation end products (RAGE) expression in human embryonic kidney cells. Anais da Academia Brasileira de Ciências 85(2):745–75210.1590/S0001-37652013005000023 ↗
8. Leu J-G, Chen S-A, Chen H-M et al (2012) The effects of gold nanoparticles in wound healing with antioxidant epigallocatechin gallate and α-lipoic acid. Nanomed Nanotechnol Biol Med 8(5):767–77510.1016/j.nano.2011.08.013 ↗
9. Bianchi A, Marchetti N, Scalia S (2011) Photodegradation of (−)-epigallocatechin-3-gallate in topical cream formulations and its photostabilization. J Pharm Biomed Anal 56(4):692–69710.1016/j.jpba.2011.07.007 ↗
10. Ruktanonchai U, Bejrapha P, Sakulkhu U et al (2009) Physicochemical characteristics, cytotoxicity, and antioxidant activity of three lipid nanoparticulate formulations of alpha-lipoic acid. AAPS PharmSciTech 10(1):227–23410.1208/s12249-009-9193-6 ↗
11. Scalia S, Marchetti N, Bianchi A (2013) Comparative evaluation of different co-antioxidants on the photochemical- and functional-stability of epigallocatechin-3-gallate in topical creams exposed to simulated sunlight. Molecules 18(1):574–58710.3390/molecules18010574 ↗
12. Hombreiro-Perez M, Siepmann J, Zinutti C et al (2003) Non-degradable microparticles containing a hydrophilic and/or a lipophilic drug: preparation, characterization and drug release modeling. J Control Release 88(3):413–42810.1016/S0168-3659(03)00030-0 ↗
13. Vicentini FTMC, Vaz MM, Fonseca YM, Bentley MVLB, Fonseca MJV (2011) Characterization and stability study of a water-in-oil microemulsion incorporating quercetin. Drug Dev Ind Pharm 37(1):47–5510.3109/03639045.2010.491078 ↗
14. Lyons KC, Charman WN, Miller R, Porter CJH (2000) Factors limiting the oral bioavailability of N-acetylglucosaminyl-N-acetylmuramyl dipeptide (GMDP) and enhancement of absorption in rats by delivery in a water-in-oil microemulsion. Int J Pharm 199(1):17–2810.1016/S0378-5173(00)00349-5 ↗
15. Kofuji K, Qian C-J, Murata Y, Kawashima S (2005) Preparation of chitosan microparticles by water-in-vegetable oil emulsion coalescence technique. React Funct Polym 62(1):77–8310.1016/j.reactfunctpolym.2004.09.002 ↗
16. Hibberd D, Holmes A, Garrood M et al (1997) Ultrasonic monitoring of oil-in-water emulsions undergoing depletion flocculation. J Colloid Interface Sci 193(1):77–8710.1006/jcis.1997.5057 ↗
17. Zhao G, Hu C, Sun R, Ni S, Xia Q (2015) Effect of emulsification process on multiple lipid particles encapsulating both coenzyme Q10 and tea polyphenols. J Food Process Eng 38(2):144–15410.1111/jfpe.12138 ↗
18. Frasch-Melnik S, Norton IT, Spyropoulos F (2010) Fat-crystal stabilised w/o emulsions for controlled salt release. J Food Eng 98(4):437–44210.1016/j.jfoodeng.2010.01.025 ↗
19. Melzer E, Kreuter J, Daniels R (2003) Ethylcellulose: a new type of emulsion stabilizer. Eur J Pharm Biopharm 56(1):23–2710.1016/S0939-6411(03)00025-0 ↗
20. Špiclin P, Homar M, Zupančič-Valant A, Gašperlin M (2003) Sodium ascorbyl phosphate in topical microemulsions. Int J Pharm 256(1–2):65–7310.1016/S0378-5173(03)00063-2 ↗
21. Li J, Qiao Z, Tatsumi E et al (2013) A novel approach to improving the quality of bittern-solidified tofu by W/O controlled-release coagulant. 1: preparation of W/O bittern coagulant and its controlled-release property. Food Bioprocess Technol 6(7):1790–180010.1007/s11947-012-0896-4 ↗
22. Patel MJ, Patel SS, Patel NM, Patel MM (2010) A self-microemulsifying drug delivery system (SMEDDS). Int J Pharm Sci Rev Res 4(3):29–35
23. Kommuru TR, Gurley B, Khan MA, Reddy IK (2001) Self-emulsifying drug delivery systems (SEDDS) of coenzyme Q10: formulation development and bioavailability assessment. Int J Pharm 212(2):233–24610.1016/S0378-5173(00)00614-1 ↗
24. Julianto T, Yuen KH, Noor AM (2000) Improved bioavailability of vitamin E with a self emulsifying formulation. Int J Pharm 200(1):53–5710.1016/S0378-5173(00)00337-9 ↗
25. Khoo S-M, Humberstone AJ, Porter CJH, Edwards GA, Charman WN (1998) Formulation design and bioavailability assessment of lipidic self-emulsifying formulations of halofantrine. Int J Pharm 167(1):155–16410.1016/S0378-5173(98)00054-4 ↗
26. Gao Z-G, Choi H-G, Shin H-J et al (1998) Physicochemical characterization and evaluation of a microemulsion system for oral delivery of cyclosporin A. Int J Pharm 161(1):75–8610.1016/S0378-5173(97)00325-6 ↗
27. Qi X, Wang L, Zhu J, Hu Z, Zhang J (2011) Self-double-emulsifying drug delivery system (SDEDDS): a new way for oral delivery of drugs with high solubility and low permeability. Int J Pharm 409(1):245–25110.1016/j.ijpharm.2011.02.047 ↗
28. Lutz R, Aserin A, Wicker L, Garti N (2009) Release of electrolytes from W/O/W double emulsions stabilized by a soluble complex of modified pectin and whey protein isolate. Colloids Surf B 74(1):178–18510.1016/j.colsurfb.2009.07.014 ↗
29. Shpigelman A, Cohen Y, Livney YD (2012) Thermally-induced β-lactoglobulin–EGCG nanovehicles: loading, stability, sensory and digestive-release study. Food Hydrocoll 29(1):57–6710.1016/j.foodhyd.2012.01.016 ↗
30. Lee Y-K, Ahn S-I, Kwak H-S (2013) Optimizing microencapsulation of peanut sprout extract by response surface methodology. Food Hydrocoll 30(1):307–31410.1016/j.foodhyd.2012.06.006 ↗
31. Comunian TA, Thomazini M, Alves AJG et al (2013) Microencapsulation of ascorbic acid by complex coacervation: protection and controlled release. Food Res Int 52(1):373–37910.1016/j.foodres.2013.03.028 ↗
32. Dvorakova K, Dorr RT, Valcic S, Timmermann B, Alberts DS (1999) Pharmacokinetics of the green tea derivative, EGCG, by the topical route of administration in mouse and human skin. Cancer Chemother Pharmacol 43(4):331–33510.1007/s002800050903 ↗
33. Ikuta N, Sugiyama H, Shimosegawa H et al (2013) Analysis of the enhanced stability of r(+)-alpha lipoic acid by the complex formation with cyclodextrins. Int J Mol Sci 14(2):3639–365510.3390/ijms14023639 ↗
34. Fan H, Liu G, Huang Y, Li Y, Xia Q (2014) Development of a nanostructured lipid carrier formulation for increasing photo-stability and water solubility of Phenylethyl Resorcinol. Appl Surf Sci 288:193–20010.1016/j.apsusc.2013.10.006 ↗
35. Shete H, Patravale V (2013) Long chain lipid based tamoxifen NLC. Part I: preformulation studies, formulation development and physicochemical characterization. Int J Pharm 454(1):573–58310.1016/j.ijpharm.2013.03.034 ↗
36. Barbosa RM, Silva CMGD, Bella TS et al (2013) Cytotoxicity of solid lipid nanoparticles and nanostructured lipid carriers containing the local anesthetic dibucaine designed for topical application. J Phys 429(1):012035
37. Kasugai S, Hasegawa N, Ogura H (1990) A simple in vito cytotoxicity test using the MTT (3-(4,5)-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide) colorimetric assay: analysis of eugenol toxicity on dental pulp cells (RPC-C2A). Jpn J Pharmacol 52(1):95–10010.1254/jjp.52.95 ↗
38. Wolfe KL, Liu RH (2007) Cellular antioxidant activity (CAA) assay for assessing antioxidants, foods, and dietary supplements. J Agric Food Chem 55(22):8896–890710.1021/jf0715166 ↗
39. Marcos D, Haran M. (2010) Foamable topical composition for treating or preventing skin condition, e.g. diaper rash, psoriasis, and eczema, comprises water in oil emulsion, where the emulsion comprises oil, water or hydrophilic liquid, and at least one surfactant. Patent WO 2010103505A1
40. Márquez AL, Medrano A, Panizzolo LA, Wagner JR (2010) Effect of calcium salts and surfactant concentration on the stability of water-in-oil (w/o) emulsions prepared with polyglycerol polyricinoleate. J Colloid Interface Sci 341(1):101–10810.1016/j.jcis.2009.09.020 ↗
41. Akhtar M, Murray BS, Afeisume EI, Khew SH (2014) Encapsulation of flavonoid in multiple emulsion using spinning disc reactor technology. Food Hydrocoll 34:62–6710.1016/j.foodhyd.2012.12.025 ↗
42. Pardeike J, Weber S, Haber T et al (2011) Development of an Itraconazole-loaded nanostructured lipid carrier (NLC) formulation for pulmonary application. Int J Pharm 419(1–2):329–33810.1016/j.ijpharm.2011.07.040 ↗
43. Gasco MR, Gallarate M, Pattarino F (1991) In vitro permeation of azelaic acid from viscosized microemulsions. Int J Pharm 69(3):193–19610.1016/0378-5173(91)90361-Q ↗
44. Gaspar LR, Maia Campos PMBG (2003) Rheological behavior and the SPF of sunscreens. Int J Pharm 250(1):35–4410.1016/S0378-5173(02)00462-3 ↗
45. Matos M, Gutiérrez G, Coca J, Pazos C (2014) Preparation of water-in-oil-in-water (W1/O/W2) double emulsions containing trans-resveratrol. Colloids Surf A 442:69–7910.1016/j.colsurfa.2013.05.065 ↗
46. Akoh CC, Min DB, Akoh AC (2002) Food lipids: chemistry, nutrition, and biotechnology. Marcel Dekker Inc, New York10.1201/9780203908815 ↗
47. Cichewicz A, Pacleb C, Connors A, Hass MA, Lopes LB (2013) Cutaneous delivery of α-tocopherol and lipoic acid using microemulsions: influence of composition and charge. J Pharm Pharmacol 65(6):817–82610.1111/jphp.12045 ↗
48. Kosmidis K, Argyrakis P, Macheras P (2003) Fractal kinetics in drug release from finite fractal matrices. J Chem Phys 119(12):6373–637710.1063/1.1603731 ↗
49. Weisburg JH, Weissman DB, Sedaghat T, Babich H (2004) In vitro cytotoxicity of epigallocatechin gallate and tea extracts to cancerous and normal cells from the human oral cavity. Basic Clin Pharmacol Toxicol 95(4):191–20010.1111/j.1742-7843.2004.pto_950407.x ↗
50. Wolfe KL, Liu RH (2008) Structure–activity relationships of flavonoids in the cellular antioxidant activity assay. J Agric Food Chem 56(18):8404–841110.1021/jf8013074 ↗