Araştırma Makalesi
BibTex RIS Kaynak Göster

Preparation, optimization and in vivo anti-inflammatory evaluation of hydroquinone loaded microemulsion formulations for melasma treatment

Yıl 2019, Cilt: 23 Sayı: 4, 662 - 670, 27.06.2025

Neslihan Üstündağ , Emre Şefik Çağlar , Ahmet Nezihi Pekcan Mehmet Evren Okur , Şule Ayla

Öz

The aim of the study is to evaluate the strengthening of penetration of the epidermis through the formulas containing hydroquinone in melasma treatment and development of alternative new carrier systems. During preparation of hydroquinone loaded microemulsions, isopropyl myristate (IPM) as oil phase, Cremophor EL, Span 20, Span 80 and Tween 20 as surfactant, ethanol as co-surfactant, distilled water as aqueous phase were used. Furthermore, in vitro drug release studies were performed. As results of the study, it was measured that conductivity between 16 ± 2.51 and 42.1 ± 2.67, viscosity between 8.97 ± 0.082 and 51.76 ± 0.04, pH between 3.3 ± 0.436 and 5.7 ± 0.2 and refractive index between 1.4032 ± 0.0002 and 1.4299 ± 0.0002. Formulations showed that zeta potential between -0.461 ± 0.009 and 0.359 ± 0.223, PDI between 0.08 ± 0.02 and 0.196 ± 0.067, and droplet size between 24.27 ± 3.559 and 324.9 ± 16.8 nm. Moreover, in vitro drug release studies showed that formulation M2 released 87.405 % of the drug at the end of the 24h. According to results of histopathological analysis, formulations were found convenient for the usage. According to results of our study, hydroquinone loaded microemulsions can be seen as a promising alternative for the treatment of melasma disease.

Anahtar Kelimeler

Hydroquinone melasma microemulsion topical mice skin irritation

Kaynakça

  • [1] Ghanbarzadeh S, Hariri R, Kouhsoltani M, Shokri J, Javadzadeh Y, Hamishehkar H. Enhanced stability and dermal delivery of hydroquinone using solid lipid nanoparticles. Colloids Surf B Biointerfaces. 2015; 136: 1004–1110. [CrossRef]
  • [2] Cohen PR. Melasma treatment: A novel approach using a topical agent that contains an anti-estrogen and a vascular endothelial growth factor inhibitor. Med Hypotheses. 2017; 101: 1–5. [CrossRef]
  • [3] Ogbechie-Godec OA, Elbuluk N. Melasma: An up to date comprehensive review. Dermatol Ther (Heidelb). 2017; 7(3): 305–318. [CrossRef]
  • [4] Kim H, Moon S, Cho S, Lee J, Kim H. Efficacy and safety of tranexamic acid in melasma: a meta-analysis and systematic review. Acta Derm Venereol. 2017; 97(7): 776–781. [CrossRef]
  • [5] Padhi T, Pradhan S. Oral tranexamic acid with fluocinolone-based triple combination cream versus fluocinolone-based triple combination cream alone in melasma: An open labeled randomized comparative trial. Indian J Dermatol. 2015; 60(5): 520. [CrossRef]
  • [6] Rigopoulos D, Gregoriou S, Katsambas A. Hyperpigmentation and melasma. J Cosmet Dermatol. 2007; 6(3): 195–202. [CrossRef]
  • [7] Palumbo A, d’Ischia M, Misuraca G, Prota G. Mechanism of inhibition of melanogenesis by hydroquinone. Biochim Biophys Acta - Gen Subj. 1991; 1073(1): 85–90. [CrossRef]
  • [8] Jimbow K, Obata H, Pathak MA, Fitzpatrick TB. Mechanism of depigmentation by hydroquinone. J Invest Dermatol. 1974; 62(4): 436–449. [CrossRef]
  • [9] Bandyopadhyay D. Topical treatment of melasma. Indian J Dermatol. 2009; 54(4): 303–309. [CrossRef]
  • [10] Üstündaǧ-Okur N, Ege MA, Karasulu HY. Preparation and characterization of naproxen loaded microemulsion formulations for dermal application. Int J Pharm. 2014; 4: 33–42. [CrossRef]
  • [11] Üstündağ Okur N, Çağlar EŞ, Arpa MD, Karasulu HY. Preparation and evaluation of novel microemulsion-based hydrogels for dermal delivery of benzocaine. Pharm Dev Technol. 2017; 22(4): 500–510. [CrossRef]
  • [12] Üstündaǧ Okur N, Apaydin Ş, Karabay Yavaşoǧlu NÜ, Yavaşoǧlu A, Karasulu HY. Evaluation of skin permeation and anti-inflammatory and analgesic effects of new naproxen microemulsion formulations. Int J Pharm. 2011; 416(1): 136–144. [CrossRef]
  • [13] Martins VMR, Sousa ARD de, Portela N de C, et al. Exogenous ochronosis: Case report and literature review. An Bras Dermatol. 2012; 87(4): 633–636. [CrossRef]
  • [14] Üstündağ Okur N, Er S, Çağlar EŞ, Ekmen TZ, Sala F. Formulation of microemulsions for dermal delivery of Cephalexin. Acta Pharm Sci. 2017; 55(4): 27–40. [CrossRef]
  • [15] Kreilgaard M. Influence of microemulsions on cutaneous drug delivery. Adv Drug Deliv Rev. 2002; 54(Suppl. 1): S77–S98. [CrossRef]
  • [16] Patel J, Patel A, Raval M, Sheth N. Formulation and development of a self-nanoemulsifying drug delivery system of irbesartan. J Adv Pharm Technol Res. 2011; 2(1): 9–16. [CrossRef]
  • [17] Li X, Yin Q, Chen W, Wang J. Solubility of hydroquinone in different solvents from 276.65 K to 345.10 K. J Chem Eng Data. 2006; 51: 127–129. [CrossRef]
  • [18] Haddad AL, Matos LF, Brunstein F, et al. A clinical, prospective, randomized, double-blind trial comparing skin whitening complex with hydroquinone vs. placebo in the treatment of melasma. Int J Dermatol. 2003; 42(2): 153–156. [CrossRef]
  • [19] Smiles KA, Dong KK, Canning MT, et al. A hydroquinone formulation with increased stability and decreased potential for irritation. J Cosmet Dermatol. 2007; 6(2): 83–88. [CrossRef]
  • [20] Wortzman MS, Gordon P, Gans E, Patel B. Process for stabilizing hydroquinone. European Patent Application. 15.04.2009 Bulletin 2009/16.
  • [21] Shinde U, Pokharkar S, Modani S. Design and evaluation of microemulsion gel systems of nadifloxacin. Indian J Pharm Sci. 2012; 74(3): 237–247. [CrossRef]
  • [22] Zala BH, Pandya RB, Prajapat MD, et al. Formulation and development of microemulsion drug delivery system of acyclovir for enhancement of permeability. J Pharm Res. 2011; 4(3): 934–937.
  • [23] Yue Y, San-ming L, Pan D, Da-fang Z. Physicochemical properties and evaluation of microemulsion systems for transdermal delivery of meloxicam. Chem Res Chin Univ. 2007; 23(1): 81–86. [CrossRef]
  • [24] Akhavan A, Levitt J. Assessing retinol stability in a hydroquinone 4%/retinol 0.3% cream in the presence of antioxidants and sunscreen under simulated-use conditions: A pilot study. Clin Ther. 2008; 30(3): 543–547. [CrossRef]
  • [25] Üstündağ-Okur N, Gökçe EH, Bozbıyık DI, et al. Novel nanostructured lipid carrier-based inserts for controlled ocular drug delivery: evaluation of corneal bioavailability and treatment efficacy in bacterial keratitis. Expert Opin Drug Deliv. 2015; 12(11): 1791–1807. [CrossRef]
  • [26] Üstündağ Okur N, Yoltaş A, Yozgatli V. Development and characterization of voriconazole loaded in situ gel formulations for ophthalmic application. Turkish J Pharm Sci. 2016; 13(3): 311–317. [CrossRef]
  • [27] Üstündag-Okur N, Gökçe EH, Eğrilmez S, et al. Novel ofloxacin-loaded microemulsion formulations for ocular delivery. J Ocul Pharmacol Ther. 2014; 30(4): 319–332. [CrossRef]
  • [28] Üstündağ Okur N, Filippousi M, Okur ME, et al. A novel approach for skin infections: Controlled release topical mats of poly(lactic acid)/poly(ethylene succinate) blends containing voriconazole. J Drug Deliv Sci Technol. 2018; 46: 74–86. [CrossRef]
  • [29] Okur ME, Ayla Ş, Çiçek Polat D, et al. Novel insight into wound healing properties of methanol extract of Capparis ovata Desf. var. palaestina Zohary fruits. J Pharm Pharmacol. 2018; 70(10): 1401–1413. [CrossRef]

Yıl 2019, Cilt: 23 Sayı: 4, 662 - 670, 27.06.2025

Neslihan Üstündağ , Emre Şefik Çağlar , Ahmet Nezihi Pekcan Mehmet Evren Okur , Şule Ayla

Öz

Kaynakça

  • [1] Ghanbarzadeh S, Hariri R, Kouhsoltani M, Shokri J, Javadzadeh Y, Hamishehkar H. Enhanced stability and dermal delivery of hydroquinone using solid lipid nanoparticles. Colloids Surf B Biointerfaces. 2015; 136: 1004–1110. [CrossRef]
  • [2] Cohen PR. Melasma treatment: A novel approach using a topical agent that contains an anti-estrogen and a vascular endothelial growth factor inhibitor. Med Hypotheses. 2017; 101: 1–5. [CrossRef]
  • [3] Ogbechie-Godec OA, Elbuluk N. Melasma: An up to date comprehensive review. Dermatol Ther (Heidelb). 2017; 7(3): 305–318. [CrossRef]
  • [4] Kim H, Moon S, Cho S, Lee J, Kim H. Efficacy and safety of tranexamic acid in melasma: a meta-analysis and systematic review. Acta Derm Venereol. 2017; 97(7): 776–781. [CrossRef]
  • [5] Padhi T, Pradhan S. Oral tranexamic acid with fluocinolone-based triple combination cream versus fluocinolone-based triple combination cream alone in melasma: An open labeled randomized comparative trial. Indian J Dermatol. 2015; 60(5): 520. [CrossRef]
  • [6] Rigopoulos D, Gregoriou S, Katsambas A. Hyperpigmentation and melasma. J Cosmet Dermatol. 2007; 6(3): 195–202. [CrossRef]
  • [7] Palumbo A, d’Ischia M, Misuraca G, Prota G. Mechanism of inhibition of melanogenesis by hydroquinone. Biochim Biophys Acta - Gen Subj. 1991; 1073(1): 85–90. [CrossRef]
  • [8] Jimbow K, Obata H, Pathak MA, Fitzpatrick TB. Mechanism of depigmentation by hydroquinone. J Invest Dermatol. 1974; 62(4): 436–449. [CrossRef]
  • [9] Bandyopadhyay D. Topical treatment of melasma. Indian J Dermatol. 2009; 54(4): 303–309. [CrossRef]
  • [10] Üstündaǧ-Okur N, Ege MA, Karasulu HY. Preparation and characterization of naproxen loaded microemulsion formulations for dermal application. Int J Pharm. 2014; 4: 33–42. [CrossRef]
  • [11] Üstündağ Okur N, Çağlar EŞ, Arpa MD, Karasulu HY. Preparation and evaluation of novel microemulsion-based hydrogels for dermal delivery of benzocaine. Pharm Dev Technol. 2017; 22(4): 500–510. [CrossRef]
  • [12] Üstündaǧ Okur N, Apaydin Ş, Karabay Yavaşoǧlu NÜ, Yavaşoǧlu A, Karasulu HY. Evaluation of skin permeation and anti-inflammatory and analgesic effects of new naproxen microemulsion formulations. Int J Pharm. 2011; 416(1): 136–144. [CrossRef]
  • [13] Martins VMR, Sousa ARD de, Portela N de C, et al. Exogenous ochronosis: Case report and literature review. An Bras Dermatol. 2012; 87(4): 633–636. [CrossRef]
  • [14] Üstündağ Okur N, Er S, Çağlar EŞ, Ekmen TZ, Sala F. Formulation of microemulsions for dermal delivery of Cephalexin. Acta Pharm Sci. 2017; 55(4): 27–40. [CrossRef]
  • [15] Kreilgaard M. Influence of microemulsions on cutaneous drug delivery. Adv Drug Deliv Rev. 2002; 54(Suppl. 1): S77–S98. [CrossRef]
  • [16] Patel J, Patel A, Raval M, Sheth N. Formulation and development of a self-nanoemulsifying drug delivery system of irbesartan. J Adv Pharm Technol Res. 2011; 2(1): 9–16. [CrossRef]
  • [17] Li X, Yin Q, Chen W, Wang J. Solubility of hydroquinone in different solvents from 276.65 K to 345.10 K. J Chem Eng Data. 2006; 51: 127–129. [CrossRef]
  • [18] Haddad AL, Matos LF, Brunstein F, et al. A clinical, prospective, randomized, double-blind trial comparing skin whitening complex with hydroquinone vs. placebo in the treatment of melasma. Int J Dermatol. 2003; 42(2): 153–156. [CrossRef]
  • [19] Smiles KA, Dong KK, Canning MT, et al. A hydroquinone formulation with increased stability and decreased potential for irritation. J Cosmet Dermatol. 2007; 6(2): 83–88. [CrossRef]
  • [20] Wortzman MS, Gordon P, Gans E, Patel B. Process for stabilizing hydroquinone. European Patent Application. 15.04.2009 Bulletin 2009/16.
  • [21] Shinde U, Pokharkar S, Modani S. Design and evaluation of microemulsion gel systems of nadifloxacin. Indian J Pharm Sci. 2012; 74(3): 237–247. [CrossRef]
  • [22] Zala BH, Pandya RB, Prajapat MD, et al. Formulation and development of microemulsion drug delivery system of acyclovir for enhancement of permeability. J Pharm Res. 2011; 4(3): 934–937.
  • [23] Yue Y, San-ming L, Pan D, Da-fang Z. Physicochemical properties and evaluation of microemulsion systems for transdermal delivery of meloxicam. Chem Res Chin Univ. 2007; 23(1): 81–86. [CrossRef]
  • [24] Akhavan A, Levitt J. Assessing retinol stability in a hydroquinone 4%/retinol 0.3% cream in the presence of antioxidants and sunscreen under simulated-use conditions: A pilot study. Clin Ther. 2008; 30(3): 543–547. [CrossRef]
  • [25] Üstündağ-Okur N, Gökçe EH, Bozbıyık DI, et al. Novel nanostructured lipid carrier-based inserts for controlled ocular drug delivery: evaluation of corneal bioavailability and treatment efficacy in bacterial keratitis. Expert Opin Drug Deliv. 2015; 12(11): 1791–1807. [CrossRef]
  • [26] Üstündağ Okur N, Yoltaş A, Yozgatli V. Development and characterization of voriconazole loaded in situ gel formulations for ophthalmic application. Turkish J Pharm Sci. 2016; 13(3): 311–317. [CrossRef]
  • [27] Üstündag-Okur N, Gökçe EH, Eğrilmez S, et al. Novel ofloxacin-loaded microemulsion formulations for ocular delivery. J Ocul Pharmacol Ther. 2014; 30(4): 319–332. [CrossRef]
  • [28] Üstündağ Okur N, Filippousi M, Okur ME, et al. A novel approach for skin infections: Controlled release topical mats of poly(lactic acid)/poly(ethylene succinate) blends containing voriconazole. J Drug Deliv Sci Technol. 2018; 46: 74–86. [CrossRef]
  • [29] Okur ME, Ayla Ş, Çiçek Polat D, et al. Novel insight into wound healing properties of methanol extract of Capparis ovata Desf. var. palaestina Zohary fruits. J Pharm Pharmacol. 2018; 70(10): 1401–1413. [CrossRef]
Toplam 29 adet kaynakça vardır.

Ayrıntılar

Birincil Dil İngilizce
Konular Eczacılık ve İlaç Bilimleri (Diğer)
Bölüm Articles
Yazarlar

Neslihan Üstündağ

Emre Şefik Çağlar

Ahmet Nezihi Pekcan

Mehmet Evren Okur

Şule Ayla

Yayımlanma Tarihi 27 Haziran 2025
Yayımlandığı Sayı Yıl 2019 Cilt: 23 Sayı: 4

Kaynak Göster

APA Üstündağ, N., Çağlar, E. Ş., Pekcan, A. N., Okur, M. E., vd. (2025). Preparation, optimization and in vivo anti-inflammatory evaluation of hydroquinone loaded microemulsion formulations for melasma treatment. Journal of Research in Pharmacy, 23(4), 662-670.
AMA Üstündağ 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. Haziran 2025;23(4):662-670.
Chicago Üstündağ, Neslihan, Emre Şefik Çağlar, Ahmet Nezihi Pekcan, Mehmet Evren Okur, ve Şule Ayla. “Preparation, Optimization and in Vivo Anti-Inflammatory Evaluation of Hydroquinone Loaded Microemulsion Formulations for Melasma Treatment”. Journal of Research in Pharmacy 23, sy. 4 (Haziran 2025): 662-70.
EndNote Üstündağ N, Çağlar EŞ, Pekcan AN, Okur ME, Ayla Ş (01 Haziran 2025) Preparation, optimization and in vivo anti-inflammatory evaluation of hydroquinone loaded microemulsion formulations for melasma treatment. Journal of Research in Pharmacy 23 4 662–670.
IEEE N. Üstündağ, E. Ş. Çağlar, A. N. Pekcan, M. E. Okur, ve Ş. Ayla, “Preparation, optimization and in vivo anti-inflammatory evaluation of hydroquinone loaded microemulsion formulations for melasma treatment”, J. Res. Pharm., c. 23, sy. 4, ss. 662–670, 2025.
ISNAD Üstündağ, Neslihan vd. “Preparation, Optimization and in Vivo Anti-Inflammatory Evaluation of Hydroquinone Loaded Microemulsion Formulations for Melasma Treatment”. Journal of Research in Pharmacy 23/4 (Haziran 2025), 662-670.
JAMA Üstündağ 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. 2025;23:662–670.
MLA Üstündağ, Neslihan vd. “Preparation, Optimization and in Vivo Anti-Inflammatory Evaluation of Hydroquinone Loaded Microemulsion Formulations for Melasma Treatment”. Journal of Research in Pharmacy, c. 23, sy. 4, 2025, ss. 662-70.
Vancouver Üstündağ 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. 2025;23(4):662-70.