New topical microemulsions of etofenamate as sufficient management of osteoarthritis

Autores

  • Neslihan Üstündağ Okur University of Health Sciences, Faculty of Pharmacy, Department of PharmaceuticalTechnology, Istanbul, Turkey https://orcid.org/0000-0002-3210-3747
  • Ecehan Onay Ege University, School of Pharmacy, Department of PharmaceuticalTechnology, Izmir, Turkey
  • Beril Kadıoğlu Yaman Yeditepe University, School of Pharmacy, Department of Pharmacology, Istanbul, Turkey
  • Hande Sipahi editepe University, School of Pharmacy, Department of Toxicology, Istanbul, Turkey

DOI:

https://doi.org/10.1590/s2175-97902022e20123

Palavras-chave:

Etofenamate, Nonsteroidal anti-inflammatory drug, Microemulsion, Ex vivo, Cytotoxicity, Anti-inflammatory activity

Resumo

In this study, microemulsions containing etofenamate were prepared and evaluated as dermal delivery carriers. The developed microemulsions consist of oleic acid, Span 80, Tween 20, Cremophor EL, Transcutol and ethanol. The percentage of etofenamate loading in the microemulsions was 5% (w/w). The characterization of formulations included droplet size, zeta potential, pH, conductivity, PDI, refractive index and viscosity. Moreover, ex vivo penetration study was carried out using mice abdominal skin. The developed formulations were analyzed for their cytotoxicity via MTT assay and tested for their anti-inflammatory properties opposed to LPS-stimulated nitrite prοduction in RAW 264.7 cells. As ideal formulation, M2ETF, was

chosen due to its greater permeation, lower penetration as well as higher anti-inflammatory

activity compared to other microemulsions.

Downloads

Os dados de download ainda não estão disponíveis.

Referências

Abd-Allah FI, Dawaba HM, Ahmed AM. Development of a microemulsion-based formulation to improve the availability of poorly water-soluble drug. Drug Discov Ther. 2010;4(4):257-66.

Abd-Elsalam WH, El-Zahaby SA, Al-Mahallawi AM. Formulation and in vivo assessment of terconazole-loaded polymeric mixed micelles enriched with Cremophor EL as dual functioning mediator for augmenting physical stability and skin delivery. Drug Deliv. 2018;25(1):484-92.

Aksu NB, Yozgatlı V, Okur ME, Ayla Ş, Yoltaş A, Üstündağ Okur N. Preparation and evaluation of QbD based fusidic acid loaded in situ gel formulations for burn wound treatment. J Drug Deliv Sci Technol. 2019;52:110-21.

Ali SM, Yosipovitch G. Skin pH: From basic science to basic skin care. Acta Derm Venereol. 2013;93(3):261-7.

Aydin A, Reis R, Sipahi H, Zeybekoðlu G, Çelik N, Kírmízíbekmez H, et al. Hydroxytyrosol: The Phytochemical Responsible for Bioactivity of Traditionally used Olive Pits. Euroasian J Hepato-Gastroenterology. 2018;8(2):126-32.

Brown MB, Martin GP, Jones SA, Akomeah FK. Dermal and transdermal drug delivery systems: current and future prospects. Drug Deliv . 2006;13(3):175-87.

Üstündağ-Okur N, Çağlar EŞ, Pekcan AN, Okur ME, Ayla Ş. Preparation, optimization and in vivo anti-inflammatory evaluation of hydroquinone loaded microemulsion formulations for melasma treatment. J Res Pharm 2019;23:662-70.

Haque T, Talukder MMU. Chemical enhancer: A simplistic way to modulate barrier function of the stratum corneum. Adv Pharm Bull. 2018;8(2):169-79.

Herndon CM. Topical Delivery of Nonsteroidal Anti- inflammatory Drugs for Osteoarthritis. J Pain Palliat Care Pharmacother. 2012;26(1):18-23.

Kajbafvala A, Salabat A, Salimi A. Formulation, characterization and in-vitro/ex-vivo evaluation of quercetin- loaded microemulsion for topical application. Pharm Dev Technol. 2018;23(8):741-750.

Karadağ AE, Demirci B, Çaşkurlu A, Demirci F, Okur ME, Orak D, et al. In vitro antibacterial, antioxidant, anti- inflammatory and analgesic evaluation of Rosmarinus officinalis L. flower extract fractions. South African J Bot. 2019;125:214-20.

Koksal M, Ozkan-Dagliyan I, Ozyazici T, Kadioglu B, Sipahi H, Bozkurt A, et al. Some Novel Mannich Bases of 5-(3,4-Dichlorophenyl)-1,3,4-oxadiazole-2(3H)-one and Their Anti-Inflammatory Activity. Arch Pharm (Weinheim). 2017;350(9):1-8.

Lu GW, Gao P. Emulsions and microemulsions for topical and transdermal drug delivery. handb. Non-Invasive Drug Deliv. Syst., Elsevier; 2010, p. 59-94.

Marto J, Baltazar D, Duarte A, Fernandes A, Gouveia L, Militão M, et al. Topical gels of etofenamate : in vitro and in vivo evaluation. Pharm Dev Technol . 2015;20(6):710-5.

Mura S, Manconi M, Valenti D, Sinico C, Vila AO, Fadda AM. Transcutol containing vesicles for topical delivery of minoxidil. J Drug Target. 2011;19(3):189-96.

Okur ME, Ayla Ş, Batur Ş, Yoltaş A, Genç E, Pertek S, et al. Evaluation of In Situ Gel Containing Pycnogenol for Cutaneous Wound Healing. Medeni Med J. 2019;34(1):67-75.

Okur ME, Ayla Ş, Yozgatlı V, Aksu NB, Yoltaş A, Orak D, et al. Evaluation of burn wound healing activity of novel fusidic acid loaded microemulsion based gel in male Wistar albino rats. Saudi Pharm J. 2020a;28(3):338-48.

Okur ME, Karantas ID, Şenyiğit Z, Üstündağ Okur N, Siafaka PI. Recent trends on wound management; new therapeutic choices based on polymeric carriers. Asian J Pharm Sci. 2020b;15(6):661-684.

Peraman R, Nayakanti D, Theja Dugga HH, Kodikonda S. Development and validation of a stability-indicating assay of etofenamate by RP-HPLC and characterization of degradation products. Sci Pharm. 2013;81(4):1017-28.

Pillai AB, Nair J V., Gupta NK, Gupta S. Microemulsion- loaded hydrogel formulation of butenafine hydrochloride for improved topical delivery. Arch Dermatol Res. 2015;307(7):625-33.

Plotnikoff R, Karunamuni N, Lytvyak E, Penfold C, Schopflocher D, Imayama I, et al. Osteoarthritis prevalence and modifiable factors: a population study. BMC Public Health. 2015;15:1195.

Prausnitz MR, Elias PM, Franz TJ, Schmuth M, Tsai J-C, Menon GK, et al. Skin Barrier and Transdermal Drug Delivery. Dermatology. 2012:2065-73.

Siafaka PI, Barmbalexis P, Bikiaris DN. Novel electrospun nanofibrous matrices prepared from poly(lactic acid)/ poly(butylene adipate) blends for controlled release formulations of an anti-rheumatoid agent. Eur J Pharm Sci. 2016a;88:12-25.

Siafaka PI, Bülbül EÖ, Mutlu G, EvrenOkur M, Karantas ID, Üstündag Okur N. Transdermal drug delivery systems and their potential on Alzheimer’s disease management. CNS Neurol Disord - Drug Targets. 2020;19(5):360-373.

Siafaka PI, Okur ME, Ayla Ş, Er S, Cağlar EŞ, Üstündag Okur N. Design and characterization of nanocarriers loaded with Levofloxacin for enhanced antimicrobial activity; physicochemical properties, in vitro release and oral acute toxicity. Braz J Pharm Sci. 2019;55:1-13.

Siafaka PI, Zisi AP, Exindari MK, Karantas ID, Bikiaris DN. Porous dressings of modified chitosan with poly(2- hydroxyethyl acrylate) for topical wound delivery of levofloxacin. Carbohydr Polym. 2016b;143:90-9.

Telaprolu K, Mohammed YH, Grice JE, Roberts MS. Skin models for the testing of transdermal drugs. Clin Pharmacol Adv Appl. 2016;8:163-76.

Tuncay S, Özer Ö. Investigation of different emulsion systems for dermal delivery of nicotinamide. Pharm Dev Technol . 2013;18(6):1417-23.

Üstündag N, Özdemir Dİ, Görgülü Ş, Şenyiğit ZA, Aşıkoğlu M, Genç L, et al. Assessment of aprotinin loaded microemulsion formulations for parenteral drug delivery : Preparation, characterization, in vitro release and cytotoxicity studies. Curr Drug Deliv . 2015;12(6):668-79.

Üstündaǧ-Okur N, Ege MA, Karasulu HY. Preparation and characterization of naproxen loaded microemulsion formulations for dermal application. Int J Pharm. 2014a;4(4):33-42.

Üstündag-Okur N, Gökçe EH, Eğrilmez S, Özer Ö, Ertan G. Novel Ofloxacin-Loaded Microemulsion Formulations for Ocular Delivery. J Ocul Pharmacol Ther. 2014b;30(4):319- 32.

Ustündağ Okur N, Apaydın S, Karabay Yavaşoğlu NÜ, Yavaşoğlu A, Karasulu HY. Evaluation of skin permeation and anti-inflammatory and analgesic effects of new naproxen microemulsion formulations. Int J Pharm . 2011;416(1):136-44.

Üstündağ Okur N, Çağlar EŞ, Siafaka PI. Novel ocular drug delivery systems: An update on microemulsions. J Ocul Pharmacol Ther . 2020;36(6):342-354 - jop.2019.0135.

Üstündağ Okur N, Hökenek N, Okur ME, Ayla Ş, Yoltaş A, Siafaka PI, et al. An alternative approach to wound healing field; new composite films from natural polymers for mupirocin dermal delivery. Saudi Pharm J . 2019a;27(5):738-52.

Ustündağ Okur N, Yavaşoğlu A, Karasulu HY. Preparation and evaluation of microemulsion formulations of naproxen for dermal delivery. Chem Pharm Bull. 2014c;62(2):135-43.

Üstündağ Okur N, Yozgatlı V, Okur ME, Yoltaş A, Siafaka PI. Improving therapeutic efficacy of voriconazole against fungal keratitis: Thermo-sensitive in situ gels as ophthalmic drug carriers. J Drug Deliv Sci Technol. 2019b;49:323-33.

Vicentini FTMC, Vaz MMOLL, Fonseca YM, Bentley MVLB, Fonseca MJV. Characterization and stability study of a water-in-oil microemulsion incorporating quercetin. Drug Dev Ind Pharm. 2011;37(1):47-55.

Xavier-Junior FH, Vauthier C, Morais ARV, Alencar EN, Egito EST. Microemulsion systems containing bioactive natural oils: an overview on the state of the art. Drug Dev Ind Pharm . 2017;43(5)700-14.

Downloads

Publicado

2022-12-23

Edição

Seção

Original Article

Como Citar

New topical microemulsions of etofenamate as sufficient management of osteoarthritis. (2022). Brazilian Journal of Pharmaceutical Sciences, 58. https://doi.org/10.1590/s2175-97902022e20123