CHARACTERIZATION OF GLYCOLIC ACID ETHOSOMES AS ANTIBACTERIAL WITH VARIATION ETHANOL AS VESICLE FORMANT
Abstract
Glycolic acid has antibacterial properties and is hydrophilic which makes it difficult to penetrate through skin lipids to reach target cells. Thus, it is necessary to develop a delivery system in the form of ethosomes containing glycolic acid to increase drug penetration. The method used was hot preparation by varying ethanol concentrations of 20, 30 and 40% as vesicle formers with observations of organoleptics, homogeneity, pH, viscosity, flow properties and cyling tests. The results obtained with the variation of ethanol concentration can affect the characterization of glycolic acid ethosomes. However, no significant changes occurred during 28 days storage (p>0.005).
Keywords:
Ethosomes, Glycolic Acid, Characterization
References
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[2] S. Zsikó, E. Csányi, A. Kovács, M. Budai-Szűcs, A. Gácsi, and S. Berkó, “Methods to evaluate skin penetration in vitro,” Sci. Pharm., vol. 87, no. 3, 2019, doi: 10.3390/scipharm87030019.
[3] P. Makvandi et al., Engineering Microneedle Patches for Improved Penetration: Analysis, Skin Models and Factors Affecting Needle Insertion, vol. 13, no. 1. Springer Singapore, 2021. doi: 10.1007/s40820-021-00611-9.
[4] D. W. Osborne and J. Musakhanian, “Skin Penetration and Permeation Properties of Transcutol®—Neat or Diluted Mixtures,” AAPS PharmSciTech, vol. 19, no. 8, pp. 3512–3533, 2018, doi: 10.1208/s12249-018-1196-8.
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[7] A. Czajkowska-Kośnik, M. Szekalska, and K. Winnicka, “Nanostructured lipid carriers: A potential use for skin drug delivery systems,” Pharmacol. Reports, vol. 71, no. 1, pp. 156–166, 2019, doi: 10.1016/j.pharep.2018.10.008.
[8] N. Nainwal, S. Jawla, R. Singh, and V. A. Saharan, “Transdermal applications of ethosomes–a detailed review,” J. Liposome Res., vol. 29, no. 2, pp. 103–113, 2019, doi: 10.1080/08982104.2018.1517160.
[9] S. Nasri, B. Ebrahimi-Hosseinzadeh, M. Rahaie, A. Hatamian-Zarmi, and R. Sahraeian, “Thymoquinone-loaded ethosome with breast cancer potential: optimization, in vitro and biological assessment,” J. Nanostructure Chem., vol. 10, no. 1, pp. 19–31, 2020, doi: 10.1007/s40097-019-00325-w.
[10] Y. Zhang et al., “Design, characterization and comparison of transdermal delivery of colchicine via borneol-chemically-modified and borneol-physically-modified ethosome,” Drug Deliv., vol. 26, no. 1, pp. 70–77, 2019, doi: 10.1080/10717544.2018.1559258.
[11] H. M. Lin, L. F. Lin, M. Y. Sun, J. Liu, and Q. Wu, “Topical delivery of four neuroprotective ingredients by ethosome-gel: Synergistic combination for treatment of oxaliplatin-induced peripheral neuropathy,” Int. J. Nanomedicine, vol. 15, pp. 3251–3266, 2020, doi: 10.2147/IJN.S233747.
[12] P. R. Amarachinta, G. Sharma, N. Samed, A. K. Chettupalli, M. Alle, and J. C. Kim, “Central composite design for the development of carvedilol-loaded transdermal ethosomal hydrogel for extended and enhanced anti-hypertensive effect,” J. Nanobiotechnology, vol. 19, no. 1, pp. 1–15, 2021, doi: 10.1186/s12951-021-00833-4.
[13] S. Singh, “Formulation and Evaluation of Hand Wash,” Age (Omaha)., vol. 20, no. 7, p. 60yrs, 2015, doi: 10.20959/wjpr20167-6663.
[14] C. Delivery, “Quality by Design for Development , Optimization and,” 2021.
[15] E. R. Valle-González, J. A. Jackman, B. K. Yoon, N. Mokrzecka, and N. J. Cho, “pH-Dependent Antibacterial Activity of Glycolic Acid: Implications for Anti-Acne Formulations,” Sci. Rep., vol. 10, no. 1, pp. 1–8, 2020, doi: 10.1038/s41598-020-64545-9.
[16] E. M. Elmowafy, M. Tiboni, and M. E. Soliman, Biocompatibility, biodegradation and biomedical applications of poly(lactic acid)/poly(lactic-co-glycolic acid) micro and nanoparticles, vol. 49, no. 4. Springer Singapore, 2019. doi: 10.1007/s40005-019-00439-x.
[17] K. T. Kim, J. Y. Lee, D. D. Kim, I. S. Yoon, and H. J. Cho, “Recent progress in the development of poly(lactic-co-glycolic acid)-based nanostructures for cancer imaging and therapy,” Pharmaceutics, vol. 11, no. 6, 2019, doi: 10.3390/pharmaceutics11060280.
[18] G. Ceselin, Z. Salta, J. Bloino, N. Tasinato, and V. Barone, “Accurate Quantum Chemical Spectroscopic Characterization of Glycolic Acid: A Route Toward its Astrophysical Detection,” J. Phys. Chem. A, vol. 126, no. 15, pp. 2373–2387, 2022, doi: 10.1021/acs.jpca.2c01419.
[19] M. Yuen, S. Gianturco, L. Pavlech, and K. Storm, “Glycolic Acid: Summary Report,” 2020, [Online]. Available: https://archive.hshsl.umaryland.edu/handle/10713/12115
[20] N. Nurleni, Iskandarsyah, and A. Aulia, “Formulation and penetration testing of ethosome azelaic acid on abdominal skin white male rats (Rattus norvegicus) with franz diffusion cell,” Asian J. Pharm. Clin. Res., vol. 11, no. 4, pp. 327–330, 2018, doi: 10.22159/ajpcr.2018.v11i4.22193.
[21] E. F. Apriani, N. Nurleni, H. N. Nugrahani, and Iskandarsyah, “Stability testing of azelaic acid cream based ethosome,” Asian J. Pharm. Clin. Res., vol. 11, no. 5, pp. 270–273, 2018, doi: 10.22159/ajpcr.2018.v11i5.23218.
[22] N. I. Akib, I. Septiani, W. O. S. Zubaydah, H. R, and R. Mahmudah, “Preparasi Salbutamol Sulfat dalam Pembawa Vesikuler Etosom,” Maj. Farmasetika, vol. 6, no. 2, p. 129, 2021, doi: 10.24198/mfarmasetika.v6i2.29890.
[23] M. Saeedi, M. Eslamifar, and K. Khezri, “Kojic acid applications in cosmetic and pharmaceutical preparations,” Biomed. Pharmacother., vol. 110, no. November 2018, pp. 582–593, 2019, doi: 10.1016/j.biopha.2018.12.006.
[24] S. R. Zahid, N. Upmanyu, S. Dangi, S. K. Ray, P. Jain, and G. Parkhe, “Journal of Drug Delivery and Therapeutics Ethosome : a novel vesicular carrier for transdermal drug delivery,” vol. 8, no. 6, pp. 318–326, 2018.
[25] N. Akhtar et al., “Fabrication of Ethosomes Containing Tocopherol Acetate to Enhance Transdermal Permeation: In Vitro and Ex Vivo Characterizations,” Gels, vol. 8, no. 6, 2022, doi: 10.3390/gels8060335.
[26] M. Costanzo et al., “Formulative study and intracellular fate evaluation of ethosomes and transethosomes for vitamin D3 delivery,” Int. J. Mol. Sci., vol. 22, no. 10, 2021, doi: 10.3390/ijms22105341.
[27] S. Surini and S. Joshita Djajadisastra, “Formulation and in vitro penetration study of transfersomes gel containing gotu kola leaves extract (Centella Asiatica L. Urban),” J. Young Pharm., vol. 10, no. 1, pp. 27–31, 2018, doi: 10.5530/jyp.2018.10.8.
[28] NIH, “Natonal Library of Medicine. 2024. Pubchem h ps://pubchem.ncbi.nlm.nih.gov/compound/Glycolic- Acid,” National Center for Biotechnology Information, 2024.
[29] G. Kishore, A. Karthik, S. V. Gopal, A. Ranjith, M. Bhat, and N. Udupa, “Development of RP-HPLC method for simultaneous estimation of lactic acid and glycolic acid,” Der Pharma Chem., vol. 5, no. 4, pp. 335–340, 2013, [Online]. Available: http://derpharmachemica.com/vol5-iss4/DPC-2013-5-4-335-340.pdf
[30] Z. Moldovan, D. E. Popa, I. G. David, M. Buleandra, and I. A. Badea, “A Derivative Spectrometric Method for Hydroquinone Determination in the Presence of Kojic Acid, Glycolic Acid, and Ascorbic Acid,” J. Spectrosc., vol. 2017, 2017, doi: 10.1155/2017/6929520.
[31] D. Wulandari, G. Gusrizal, and T. A. Zaharah, “Optimasi dan Validasi Metode Penentuan Kadar Asam Glikolat dan Asam Laktat Dalam Krim Menggunakan Kromatografi Cair Kinerja Tinggi,” ALCHEMY J. Penelit. Kim., vol. 16, no. 1, p. 10, 2020, doi: 10.20961/alchemy.16.1.34008.10-24.
[32] Scientific Committee on Consumer Safety, “OPINION on the safety of alpha-arbutin and beta-arbutin in cosmetic products,” Eur. Comm., no. January, pp. 1–74, 2023.
[33] L. S. Joseph C. Dinardo, Gary L. Grove, Clinical and Histological Effects of Glycolic Acid at Different Concentrations and pH Levels. 1996.
[34] L. Nurdianti, R. Clara, H. Suhendy, F. Setiawan, and K. Idacahyati, “Formulation, Characterization, and Determination of the Diffusion Rate Study of Antioxidant Serum Containing Astaxanthin Nanoemulsion,” Int. J. Appl. Pharm., vol. 13, no. Special Issue 4, pp. 200–204, 2021, doi: 10.22159/IJAP.2021.V13S4.43859.
[35] O. Wallevik, “Rheology - A scientific approach to develop self-compacting concrete,” 3rd Int. RILEM Symp. Self-Compacting Concr., no. January 2003, pp. 23–31, 2003.
[36] J. H. Wood and E. A. Lapham, “Adaptation of commercial viscometers for special applications in pharmaceutical rheology. III. The tackmeter,” J. Pharm. Sci., vol. 53, no. 7, pp. 825–826, 1964, doi: 10.1002/jps.2600530730.
[37] S. K. Kawatra, A. K. Bakshi, and T. E. Miller, “Rheological characterization of mineral suspensions using a vibrating sphere and a rotational viscometer,” Int. J. Miner. Process., vol. 44–45, no. SPEC. ISS., pp. 155–165, 1996, doi: 10.1016/0301-7516(95)00026-7.
[38] Depkes RI, Farmakope Indonesia edisi VI. 2023.
[39] S. M. Fahira, A. Dwi Ananto, and W. Hajrin, “Analisis Kandungan Hidrokuinon dalam Krim Pemutih yang Beredar di Beberapa Pasar Kota Mataram dengan Spektrofotometri Ultraviolet-Visible,” SPIN J. Kim. dan Pendidik. Kim., vol. 3, no. 1, pp. 75–84, 2021, doi: 10.20414/spin.v3i1.3299.
[40] D. Akiladevi and S. Basak, “Ethosomes - a Noninvasive Approach for Transdermal Drug Delivery,” Int. J. Curr. Pharm. Res., vol. 2, no. 4, pp. 2–5, 2010.
[41] A. Dhiman, D. Singh, M. Bala, and K. Sharma, “Journal of Pharmaceutical and Scientific Innovation Re view Article,” vol. 1, no. 5, pp. 26–30, 2012.
[42] Ž. Vanić, “Phospholipid vesicles for enhanced drug delivery in dermatology,” J. Drug Discov. Dev. Deliv., vol. 2, no. 1, pp. 1–9, 2015.
Published
2025-11-28
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