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Vesicular systems, ethosomes, LAA
Background: Vesicular system is a good approach to improve hydrophilic drug permeability using phospholipids as Nanocarriers to increase lipophilicity and reduce vesicle size. L-ascorbic acid is a water soluble vitamin with antioxidant activity with poor skin permeability. Aim: The purpose of this work is to prepare LAA-containing ethosomes formulations utilizing a modified thin film hydration approach. Methods: eight formulas were prepared using different types of phospholipids (egg yolk lecithin and soya lecithin), different volumes of ethanol (2 and 3mL), and tween 80 as a surfactant. The prepared formulas (F1, F2, F3, F4, F5, F6, F7 and F8) were characterized to detect the best one regarding the physical appearance, pH, average vesicle size, polydispersity index (PDI) and entrapment efficiency. Scanning electron microscope (SEM) and transmission electron microscope (TEM) were used to evaluate the morphological properties Results: The best prepared ethosomal formula was F3 which contains (1.5g) LAA, (0.1 g) egg yolk lecithin, (2 mL) ethanol, 0.025 mL tween 80 and (q.s.10mL) of distilled water. Its average vesicle size value (176nm), PDI = 0.243, high entrapment efficiency (89.8%) and good physical stability. The morphological properties showing spherical, smooth, and devoid of drug crystalline structures. The drug-excipient compatibility is confirmed using (FTIR, DSC and PXRD) analyses. Additionally, the Ex-vivo drug permeation investigation demonstrated that the prepared formula of LAA had flux and permeability coefficients that were two times higher than the control. Conclusions: The average vesicle size and PDI are affected by, the volume of ethanol, type of lecithin and presence of solubilizing agent.
2. Monisha C, Ganesh GNK, Mythili L, Radhakrishnan K. A review on ethosomes for transdermal application. Res J Pharm Technol. 2019;12(7):3133–43.
3. Abdulbaqi IM, Darwis Y, Khan NAK, Abou Assi R, Khan AA. Ethosomal nanocarriers: the impact of constituents and formulation techniques on ethosomal properties, in vivo studies, and clinical trials. Int J Nanomedicine. 2016;11:2279.
4. Maxwell A, Priya S. Nanosized ethosomes - a promising vesicular drug carrier for transdermal drug delivery. Res J Pharm Technol. 2019;12(2):876–80.
5. Roig MG, Rivera ZS, Kennedy JF. L-ascorbic acid: an overview. Int J Food Sci Nutr. 1993;44(1):59–72.
6. Abdel Messih HA, Ishak RAH, Geneidi AS, Mansour S. Nanoethosomes for transdermal delivery of tropisetron HCl: multi-factorial predictive modeling, characterization, and ex vivo skin permeation. Drug Dev Ind Pharm. 2017;43(6):958–71.
7. Indora N, Kaushik D. Design, development and evaluation of ethosomal gel of fluconazole for topical fungal infection. Int J Eng Sci Invent Res Dev. 2015;1(8):280–306.
8. Kucinska-Lipka J, Gubanska I, Strankowski M, Cieśliński H, Filipowicz N, Janik H. Synthesis and characterization of cycloaliphatic hydrophilic polyurethanes, modified with L-ascorbic acid, as materials for soft tissue regeneration. Mater Sci Eng C. 2017;75:671–81.
9. Castro RN, Azeredo LC, Azeredo MAA, De Sampaio CST. HPLC assay for the determination of ascorbic acid in honey samples. J Liq Chromatogr Relat Technol. 2001;24(7):1015–20.
10. Hu L, Li L, Luo Z, Yang J, Liu W. Determination of trace vitamin C by ion-pair HPLC with UV detection in calcium gluconate and vitamin C compound oral solution. J Chromatogr Sci. 2012;50(2):102–7.
11. CHEN J, LAI W, JIANG Y. Preparation of curcumin ethosomes. African J Pharm Pharmacol. 2013;7(31):2246–51.
12. Sakdiset P, Amnuaikit T, Pichayakorn W, Pinsuwan S. Formulation development of ethosomes containing indomethacin for transdermal delivery. J Drug Deliv Sci Technol. 2019;52:760–8.
13. Marto J, Vitor C, Guerreiro A, Severino C, Eleutério C, Ascenso A, et al. Ethosomes for enhanced skin delivery of griseofulvin. Colloids Surfaces B Biointerfaces. 2016;146:616–23.
14. Niu X-Q, Zhang D-P, Bian Q, Feng X-F, Li H, Rao Y-F, et al. Mechanism investigation of ethosomes transdermal permeation. Int J Pharm X. 2019;1:100027.
15. Viscosity—Capillary Methods. USP-NF. Rockville, MD: United States Pharmacopeia.
16. Zhai Y, Xu R, Wang Y, Liu J, Wang Z, Zhai G. Ethosomes for skin delivery of ropivacaine: preparation, characterization and ex vivo penetration properties. J Liposome Res. 2015;25(4):316–24.
17. Mallick S, Pradhan SK. Characterization of Particle Packing and Drug Release Studies After Solvent Evaporation of Ibuprofen, Avicel, and Aerosil. Part Sci Technol. 2013;31(3):301–8.
18. Nair RS, Billa N, Leong C-O, Morris AP. An evaluation of tocotrienol ethosomes for transdermal delivery using Strat-M® membrane and excised human skin. Pharm Dev Technol. 2021;26(2):243–51.
19. Zhang J-P, Wei Y-H, Zhou Y, Li Y-Q, Wu X-A. Ethosomes, binary ethosomes and transfersomes of terbinafine hydrochloride: a comparative study. Arch Pharm Res. 2012;35(1):109–17.
20. Akhtar N, Rehman MU, Khan HMS, Rasool F, Saeed T, Murtaza G. Penetration enhancing effect of polysorbate 20 and 80 on the in vitro percutaneous absorption of L-ascorbic acid. Trop J Pharm Res. 2011;10(3):281–8.
21. Abbas S, Da Wei C, Hayat K, Xiaoming Z. Ascorbic acid: microencapsulation techniques and trends—a review. Food Rev Int. 2012;28(4):343–74.
22. Limsuwan T, Amnuaikit T. Development of ethosomes containing mycophenolic acid. Procedia Chem. 2012;4:328–35.
23. Luki M. Towards Optimal pH of the Skin and Topical Formulations : From the Current State of the Art to Tailored Products. 2021;
24. Danaei M, Dehghankhold M, Ataei S, Hasanzadeh Davarani F, Javanmard R, Dokhani A, et al. Impact of particle size and polydispersity index on the clinical applications of lipidic nanocarrier systems. Pharmaceutics. 2018;10(2):57.
25. Maher EM, Mahmoud A, Ali A, Farouk H, Abdelrahman AA. In vitro / in vivo evaluation of an optimized fast dissolving oral film containing olanzapine co- amorphous dispersion with selected carboxylic acids. 2016;(March). Available from: http://dx.doi.org/10.3109/10717544.2016.1153746
26. Peram MR, Jalalpure S, Kumbar V, Patil S, Joshi S, Bhat K, et al. Factorial design based curcumin ethosomal nanocarriers for the skin cancer delivery: in vitro evaluation. J Liposome Res. 2019;29(3):291–311.