Preparation, optimization and in vivo anti-inflammatory Preparation, optimization and in vivo anti-inflammatory evaluation of hydroquinone loaded microemulsion formulations for melasma treatment
Preparation, optimization and in vivo anti-inflammatory Preparation, optimization and in vivo anti-inflammatory evaluation of hydroquinone loaded microemulsion formulations for melasma treatment
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 vitrodrug 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 ourstudy, hydroquinone loaded microemulsions can be seen as a promising alternative for the treatment of melasma disease.
___
- 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]
- 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]
- Ogbechie-Godec OA, Elbuluk N. Melasma: An up to date comprehensive review. Dermatol Ther (Heidelb). 2017; 7(3): 305–18. [CrossRef]
- 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): 776–81. [CrossRef]
- Padhi T, Pradhan S. Oral tranexamic acid with fluocinolone-based triple combination cream versus fluocinolonebased triple combination cream alone in melasma: An open labeled randomized comparative trial. Indian J Dermatol. 2015; 60(5): 520. [CrossRef]
- Rigopoulos D, Gregoriou S, Katsambas A. Hyperpigmentation and melasma. J Cosmet Dermatol. 2007; 6(3): 195– 202. [CrossRef]
- 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]
- 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): 303–9. [CrossRef]
- Üstündaǧ-Okur N, Ege MA, Karasulu HY. Preparation and characterization of naproxen loaded microemulsion formulations for dermal application. Int J Phar. 2014; 4: 33-42. [CrossRef]
- 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]
- 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): 136–44. [CrossRef]
- Martins VMR, Sousa ARD de, Portela N de C, Tigre CAF, Gonçalves LMS, Castro Filho RJ de L. Exogenous ochronosis: Case report and literature review. An Bras Dermatol. 2012; 87(4): 633–636. [CrossRef]
- 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]
- Kreilgaard M. Influence of microemulsions on cutaneous drug delivery. Adv Drug Deliv Rev. 2002; 54(Suppl. 1), S77-S98. [CrossRef]
- 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]
- 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] Haddad AL, Matos LF, Brunstein F, Ferreira LM, Silva A, Costa D. A clinical, prospective, randomized, doubleblind trial comparing skin whitening complex with hydroquinone vs. placebo in the treatment of melasma. Int J Dermatol. 2003; 42(2): 153–156. [CrossRef]
- Smiles KA, Dong KK, Canning MT, Grimson R, Walfield AM, Yarosh DB. A hydroquinone formulation with increased stability and decreased potential for irritation. J Cosmet Dermatol. 2007; 6(2): 83-88. [CrossRef]
- Wortzman MS, Gordon P, Gans E, Patel B. Process for stabilizing hydroquinone. European Patent Application. 15.04.2009 Bulletin 2009/16.
- 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]
- Zala BH, Pandya RB, Prajapat MD, Ramkisham A, Parikh RK, Gobel MC. Formulation and development of microemulsion drug delivery system of acyclovir for enhancement of permeability. J Pharm Res. 2011; 4(3): 934-937.
- 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]
- Akhavan A, Levitt J. Assesing 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]
- Üstündağ-Okur N, Gökçe EH, Bozbıyık DI, Eğrilmez S, Ertan G, Özer Ö. 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): 1791–807. [CrossRef]
- 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]
- Üstündag-Okur N, Gökçe EH, Eğrilmez S, Özer Ö, Ertan G. Novel ofloxacin-loaded microemulsion formulations for ocular delivery. J Ocul Pharmacol Ther. 2014; 30(4): 319–32. [CrossRef]
- Üstündağ Okur N, Filippousi M, Okur ME, Ayla Ş, Çağlar EŞ, Yoltaş A, 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]
- Okur ME, Ayla Ş, Çiçek Polat D, Günal MY, Yoltaş A, Biçeroğlu Ö. 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]