A Kojic Acid Containing Novel Drug Delivery System on Facial Dyschromia: Characterization and Their Evaluation
Prantika Mondal*, Vijay Bhalla, Reena Tyagi
Department of Pharmaceutics, SGT College of Pharmacy, SGT University, Gurgaon, Haryana, India.
Received: 17th November, 2023; Revised: 28th March, 2024; Accepted: 23rd April, 2024; Available Online: 25th June, 2024
ABSTRACT
Stubborn skin pigmentation issues like post-inflammatory hyperpigmentation (PIH) and melasma are the primary reasons people seek cosmetic consultations. Treating these conditions topically is challenging, as it involves inhibiting various stages of production of the pigment process. A powerful tyrosinase inhibitor like, kojic acid (KA) is employed as a formulation to regulate pigmentation production by suppressing the melanogenesis process. It’s important to note that the application of KA has been approved by the Food and Drug Administration (FDA), US, for dermatological treatments. The goal of this investigation was to formulate a nanoemulsion containing kojic acid for skin delivery using an emulsification method. The characteristics of the KA nanoemulsion were thoroughly examined through techniques like fourier transform infrared spectroscopy, (FTIR) particle size analysis and transmission electron microscopy (TME). In addition, the formulation’s performance was evaluated through both ex-vivo permeation study and in-vitro release study. Analysis of the FTIR, X-ray diffraction (XRD), and differential scanning calorimetry (DSC) results revealed that kojic acid with other ingredients in the formulation did not exhibit any chemical interactions. The kojic acid nanoparticles that were produced exhibited a spherical shape and were uniformly distributed, with an average size diameter of 184 nm. In in-vitro tests, it was observed that 87.67% of the drug was released within 12 hours. Moreover, ex-vivo permeation evaluation demonstrated that 81.24% of the drug permeated the skin within 8 hours of application. The thermal stability studies confirmed the stability of the kojic acid nanoemulsion, with no signs of creaming, cracking, or phase separation in the formulation. In conclusion, the findings of this study suggest that the kojic acid nanoemulsion holds great promise as an effective means for delivering kojic acid within the upper layers of the skin for treating of facial dyschromia.
Keywords: Hyperpigmentation, Nanoemulsion, Facial dyschromia, Kojic acid. International Journal of Drug Delivery Technology (2024); DOI: 10.25258/ijddt.14.2.04
How to cite this article: Mondal P, Bhalla V, Tyagi R. A Kojic Acid Containing Novel Drug Delivery System on Facial Dyschromia: Characterization and Their Evaluation. International Journal of Drug Delivery Technology. 2024;14(2):639-643.
REFERENCES
- Victor FC, Gelber J, Rao B. Melasma: a review. Journal of Cutaneous Medicine and Surgery: Incorporating Medical and Surgical Dermatology. 2004 Apr;8:97-102.
- Grimes PE. Melasma: etiologic and therapeutic considerations. Archives of dermatology. 1995 Dec 1;131(12):1453-7.
- Miot LD, Miot HA, Silva MG, Marques ME. Physiopathology of melasma. Brazilian annals of dermatology. 2009;84:623-35.
- Perper M, Eber AE, Fayne R, Verne SH, Magno RJ, Cervantes J, ALharbi M, ALOmair I, Alfuraih A, Nouri K. Tranexamic acid in the treatment of melasma: a review of the literature. American journal of clinical dermatology. 2017 Jun;18:373-81.
- Taraz M, Niknam S, Ehsani AH. Tranexamic acid in treatment of melasma: A comprehensive review of clinical studies. Dermatologic therapy. 2017 May;30(3):e12465.
- Molinar VE, Taylor SC, Pandya AG. What’s new in objective assessment and treatment of facial hyperpigmentation?. Dermatologic clinics. 2014 Apr 1;32(2):123-35.
- Sofen B, Prado G, Emer J. Melasma and post inflammatory hyperpigmentation: management update and expert opinion. Skin therapy letter. 2016 Jan 1;21(1):1-7.
- Shankar K, Godse K, Aurangabadkar S, Lahiri K, Mysore V, Ganjoo A, Vedamurty M, Kohli M, Sharad J, Kadhe G, Ahirrao P. Evidence-based treatment for melasma: expert opinion and a review. Dermatology and therapy. 2014 Dec;4:165-86.
- Deo KS, Dash KN, Sharma YK, Virmani NC, Oberai C. Kojic acid vis-a-vis its combinations with hydroquinone and betamethasone valerate in melasma: a randomized, single blind, comparative study of efficacy and safety. Indian journal of dermatology. 2013 Jul;58(4):281.
- Monteiro RC, Kishore BN, Bhat RM, Sukumar D, Martis J, Ganesh HK. A comparative study of the efficacy of 4% hydroquinone vs 0.75% kojic acid cream in the treatment of facial melasma. Indian journal of Dermatology. 2013 Mar;58(2):157.
- Navarrete-Solís J, Castanedo-Cázares JP, Torres-Álvarez B, Oros-Ovalle C, Fuentes-Ahumada C, González FJ, Martínez- Ramírez JD, Moncada B. A double-blind, randomized clinical trial of niacinamide 4% versus hydroquinone 4% in the treatment of melasma. Dermatology research and practice. 2011 Jan 1;2011.
- Rolfe HM. A review of nicotinamide: treatment of skin diseases and potential side effects. Journal of cosmetic dermatology. 2014 Dec;13(4):324-8.
- Tse TW, Hui E. Tranexamic acid: an important adjuvant in the treatment of melasma. Journal of cosmetic dermatology. 2013 Mar;12(1):57-66.
- Burdock GA, Soni MG, Carabin IG. Evaluation of health aspectsof kojic acid in food. Regulatory toxicology and pharmacology. 2001 Feb 1;33(1):80-101.
- Cabanes J, Chazarra S, Garcia-Carmona F. Kojic acid, a cosmetic skin whitening agent, is a slow-binding inhibitor of catecholase activity of tyrosinase. Journal of Pharmacy and Pharmacology. 1994 Dec;46(12):982-5.
- Gonçalez ML, Correa MA, Chorilli M. Skin delivery of kojic acid-loaded nanotechnology-based drug delivery systems for the treatment of skin aging. BioMed Research International. 2013 Jan 1;2013.
- Andrade GF, Lima GD, Gastelois PL, Assis Gomes D, Macedo WA, de Sousa EM. Surface modification and biological evaluation of kojic acid/silica nanoparticles as platforms for biomedical systems. International Journal of Applied Ceramic Technology. 2020 Jan;17(1):380-91.
- Saeedi M, Eslamifar M, Khezri K. Kojic acid applications in cosmetic and pharmaceutical preparations. Biomedicine and Pharmacotherapy. 2019 Feb 1;110:582-93.
- Burdock GA, Soni MG, Carabin IG. Evaluation of health aspects of kojic acid in food. Regulatory toxicology and pharmacology. 2001 Feb 1;33(1):80-101.
- Andrade GF, Lima GD, da Silva MA, de Sousa EM, Takahashi JA. Novel kojic acid-based functionalized silica nanoparticles for tyrosinase and ache inhibition and antimicrobial applications. Chemical Engineering Transactions. 2018.
- Abhinav M, Neha J, Anne G, Bharti V. Role of novel drug delivery systems in bioavailability enhancement: At a glance. International Journal of Drug Delivery Technology. 2016;6(1):7- 26.
- Khezri K, Saeedi M, Morteza- Semnani K, Akbari J, Rostamkalaei SS. An emerging technology in lipid research for targeting hydrophilic drugs to the skin in the treatment of hyperpigmentation disorders: kojic acid-solid lipid nanoparticles. Artificial cells, nanomedicine, and biotechnology. 2020 Jan 1;48(1):841-53.
- Ayumi NS, Sahudin S, Hussain Z, Hussain M, Samah NH. Polymeric nanoparticles for topical delivery of alpha and beta arbutin: preparation and characterization. Drug delivery and translational research. 2019 Apr 15;9:482-96.
- Hadi AS, Ghareeb MM. Rizatriptan benzoate nanoemulsion for intranasal drug delivery: preparation and characterization. International Journal of Dr ug Delivery Technology. 2022;12(2):546-52
- Gupta A, Eral HB, Hatton TA, Doyle PS. Nanoemulsions: formation, properties and applications. Soft matter. 2016;12(11):2826-41.
- Itsuo IC, Hiroo UE. Studies on Kojic Acid and its Related γ-Pyrone Compounds. Bulletin of the Agricultural Chemical Society of Japan. 1965;29(2):94-8.
- Nagai S, Izumi T, inventors; Sansho Pharmaceutical Co Ltd, assignee. Cosmetic composition containing kojic acid ester. United States patent US 4,369,174. 1983 Jan 18.
- Izadifar M, Kelly ME, Haddadi A, Chen X. Optimization of nanoparticles for cardiovascular tissue engineering. Nanotechnology. 2015 May 19;26(23):235301.
- Lawrence MJ, Rees GD. Microemulsion-based media as novel drug delivery systems. Advanced drug delivery reviews. 2012 Dec 1;64:175-93.