Nur Illiyyin Akib, Cici Novianti, Halimahtussaddiyah Ritonga, Suryani, Andi Nafisah Tendri Adjeng
Nur Illiyyin Akib1, Cici Novianti1, Halimahtussaddiyah Ritonga2, Suryani1, Andi Nafisah Tendri Adjeng1*
1Department of Pharmacy, Faculty of Pharmacy, Universitas Halu Oleo, Jl. HEA. Mokodompit, Anduonohu, Kendari-South East Sulawesi, Indonesia, 93232.
2Mathematics and Natural Science, Universitas Halu Oleo, Jl. HEA. Mokodompit, Anduonohu, Kendari-South East Sulawesi, Indonesia, 93232.
Volume - 13,
Issue - 11,
Year - 2020
Kojic acid is a metabolite of Acetobacter, Asperigillus, and Penicillium fungi species that can prevent skin hyperpigmentation. Kojic acid is prepared in ethosome vesicles to increase its penetration into the skin and reduce the irritant effect. The aim of this research was to obtain the optimum content of kojic acid in ethosome vesicles. Methods: Kojic acid at a concentration of 1% was prepared in ethosome vesicles by hot (40oC) and cold methods (30oC). Phosphatidylcholine concentrations during vesicle formation were 2% and 3%. Ethanol concentrations as penetration enhancer were 20%, 25%, 30%, 35%, and 40%. Characterizations of vesicles included analysis of shape and size by using optical microscope and efficiency of entrapment was measured by using spectrophotometer at ? max 268nm. Kojic acid content that was optimized was 0.5%, 1%, 1.5%, 2%, and 2.5%. Results: The best formula obtained was phosphatidylcholine 2% and ethanol 40% which were prepared by the hot method. Shape of ethosome vesicles was large unilamellar vesicle, the smallest size was 281 nm and entrapment efficiency were 47.7%. The optimum content of kojic acid was 2% with 429.6 nm for size and entrapment efficiency was 73.0%. Conclusion: We conclude that kojic acid can be used in preparation of ethosome vesicles and future research may use this approach for clinical research.
Cite this article:
Nur Illiyyin Akib, Cici Novianti, Halimahtussaddiyah Ritonga, Suryani, Andi Nafisah Tendri Adjeng. Optimization of Method and Proportion of Phosphatidylcholine and Ethanol for Preparation of Kojic Acid Ethosome. Research J. Pharm. and Tech. 2020; 13(11):5251-5256. doi: 10.5958/0974-360X.2020.00918.X
1 Cayce KA, McMichael AJ, Feldman SR. Hyperpigmentation: an overview of the common afflictions. Dermatology Nursing / Dermatology Nurses’ Association 2004; 16:401–13.
2 Woolery-Lloyd H, Kammer JN. Treatment of Hyperpigmentation. Seminars in Cutaneous Medicine and Surgery 2011; 30:171–5.
3 Gazali M, P. Zamani N, Batubara I. Potensi limbah kulit buah Nyirih Xylocarpus granatum sebagai inhibitor tirosinase. Jurnal Ilmu Perairan, Pesisir, Dan Perikanan (DEPIK) 2014; 3:187–94.
4 Burnett CL, Bergfeld WF, Belsito D V., Hill RA, Klaassen CD, Liebler DC, et al. Final report of the safety assessment of kojic acid as used in cosmetics. International Journal of Toxicology 2010; 29:244S-273S.
5 Chang TS. An updated review of tyrosinase inhibitors. International Journal of Molecular Sciences 2009; 10:2440–75.
6 Suryani, Musnina WOS, Ruslin, Nisa M, Aprianti R, Hasanah M, et al. Formulation and physical characterization of curcumin nanoparticle transdermal patch. International Journal of Applied Pharmaceutics 2019; 11:217–21.
7 Javadzadeh Y, Azharshekoufeh Bahari L. Therapeutic Nanostructures for Dermal and Transdermal Drug Delivery. Nano- Microscale Drug Deliv. Syst. Des. Fabr., 2017, p. 131–46.
8 Jondhalekar TM, Aher SS, Saudagar RB. Transethosome: Novel vesicular carrier for enhanced transdermal drug delivery system. Research Journal of Pharmacy and Technology 2017; 10:1816.
9 Paolino D, Lucania G, Mardente D, Alhaique F, Fresta M. Ethosomes for skin delivery of ammonium glycyrrhizinate: In vitro percutaneous permeation through human skin and in vivo anti-inflammatory activity on human volunteers. Journal of Controlled Release 2005; 106:99–110.
10 Pandey S, Misra SK, Sharma N. Ethosomes-a novelize vesicular drug delivery system. Research Journal of Pharmacy and Technology 2017; 10:3223–32.
11 Rakesh R, Anoop KR. Ethosomes for transdermal and topical drug delivery. International Journal of Pharmacy and Pharmaceutical Sciences 2012; 4:17–24.
12 Chandel A, Patil V, Goyal R, Dhamija H, Parashar B. Ethosomes: A Novel Approach towards Transdermal Drug Delivery. International Journal of Pharmaceutical and Chemical Sciences 2012; 11:219–26.
13 Patidar V, Sharma D, Maliwal D, Chatap V. Penetration Enhancement Techniques for Transdermal Drug Delivery System. Research Journal of Pharmacy and Technology 2009; 2:28–33.
14 El Nagar MH, Mahdy M, Selem M, El Maghraby G. Transdermal delivery of kojic acid from microemulgel. Journal of Applied Pharmaceutical Science 2016; 6:8–16.
15 Nisa M, Radhia R, Gani SA, Aisyah A, Nursamsiar N. Uji Efektifitas Beberapa Senyawa Sebagai Peningkat Penetrasi Terhadap Laju Difusi Krim Asam Kojat Tipe Minyak dalam Air Secara in Vitro. Pharmacy: Jurnal Farmasi Indonesia 2013; 10:15–27.
16 Aggarwal D, Nautiyal U. Ethosomes : A review 2016; 4:354–63.
17 Maxwell A, Priya S. Nanosized Ethosomes-A Promising Vesicular Drug Carrier for Transdermal Drug Delivery. Research Journal of Pharmacy and Technology 2019; 12:876–80.
18 Couteau C, Coiffard L. Overview of Skin Whitening Agents: Drugs and Cosmetic Products. Cosmetics 2016; 3:27.
19 Akib NI, Suryani, Ritonga H, Prawesti N. Preparasi fenilbutazon dalam pembawa vesikular etosom dengan berbagai variasi konsentrasi fosfatidilkolin dan etanol. Medula 2014; 2:112–8.
20 Sindhu RK, Chitkara M, Kaur G, Jaiswal P, Kalra A, Singh I, et al. Skin Penetration Enhancer’s in Transdermal Drug Delivery Systems. Research Journal of Pharmacy and Technology 2017; 10:1809.
21 Akib NI, Latifah R, A. MM. Uji Permeasi In Vitro Gel Etosom Vitamin C. Majalah Farmasi Dan Farmakologi 2012; 16:1–6.
22 Patel A, Sharma RK, Trivedi M, Panicker A. Ethosomes: A Novel Tool for Transdermal Drug Delivery. Research Journal of Pharmacy and Technology 2013; 6:838.
23 Mistry A, Ravikumar P. Development and evaluation of azelaic acid based ethosomes for topical delivery for the treatment of acne. Indian Journal of Pharmaceutical Education and Research 2016; 50:S232–43.
24 Mishra AD, Khunt DM, Ghayal AH, Patel CN, Shah DR. Formulation and optimization of ethosomes for transdermal delivery of felodipine. Research Journal of Pharmacy and Technology 2012; 5:1509–17.
25 Sahu SK, Ram A. Evaluation of Linezolid Loaded Ethosomes for Treatment of Deep Skin Infections in Diabetic Model. Research Journal of Pharmacy and Technology 2018; 11:3023–30.
26 Barel AO, Paye M, Maibach HI. Handbook of Cosmetic Science and Technology. 2009.
27 Akib NI, Suryani S, Prawesti N. Preparasi Fenilbutazon dalam Pembawa Vesikular Etosom dengan Berbagai Variasi Konsentrasi Fosfatidilkolin dan Etanol. Medula 2015; 2:112–8.
28 Monisha C, Ganesh GNK, Mythili L, Radhakrishnan K. A Review on Ethosomes for Transdermal Application. Research Journal of Pharmacy and Technology 2019; 12:3133–43.
29 Voigt. Buku Pelajaran Teknologi Farmasi. 1995.
30 Benson HJ. Dasar-dasar Praktikum Mikrobiologi. 1973.
31 Philippot JR, Schuber F. Liposomes as tools in basic research and industry. 2017.
32 Bendas ER, Tadros MI. Enhanced transdermal delivery of salbutamol sulfate via ethosomes. AAPS PharmSciTech 2007; 8:E1–8.
33 Rohit B, Pal KI. A Method to Prepare Solid Lipid Nanoparticles with Improved Entrapment Efficiency of Hydrophilic Drugs. Current Nanoscience 2013; 9:211–20.
34 Mishra AD, Khunt DM, Ghayal AH, Patel CN, Shah DR. Formulation and optimization of ethosomes for transdermal delivery of felodipine. Research Journal of Pharmacy and Technology 2012; 5:VI.
35 Transdermal Delivery H, Kumar P, Patel AK, Prasad RK, Gautam SS. Formulation and Evaluation of Ethosome for Econazole Nitrate A Model Drug to Enhanced Transdermal Delivery. International Journal of Pharmaceutics and Drug 2016; 4:140–6.
36 Chowdhury WK, Wahab MA, Khondker L, Anwar MH, Khan MSI. Efficacy and safety of hydroquinone, kojic acid and glycolic acid combination in the treatment of melasma. Bangladesh Journal of Medical Science 2012; 11:191–6.