Anayatollah SALİMİ, Ramin NOORAFROOZ, Maryam FOULADİ, Saeed MOHAMMAD SOLEYMANİ

Design and Assessment of a Microemulsion-Based Transdermal Drug Delivery System for Meloxicam; Examination of Formulation Ingredients

Background: The goal of creating meloxicam-loaded microemulsion formulations was to increase meloxicam permeability through the skin. Using pseudo-ternary phase diagram construction and full factorial design, eight formulations with three independent variables (water percent, oil percent, and surfactant/co-surfactant percent) were selected to be prepared. Methods: This research evaluated the formulation's characteristics, including particle size, viscosity, and release profile. FT-IR and DSC techniques were also utilized to investigate the effect of microemulsion components on rat abdomen skin, and the permeability of meloxicam-loaded microemulsions via rat abdomen skin was also evaluated by calculating permeability parameters such as Jss, Dapp, Tlag, ERflux, ERD, and ERP. Results: When compared to a saturated aqueous solution of meloxicam as a reference, the findings showed that all microemulsion (ME) formulations considerably increased meloxicam permeability through rat skin. Water percent had a direct and significant relationship with Jss, and oil percent had a direct and significant relationship with Dapp, according to analysis regression. Conclusion: ME components also caused alterations in the skin's lipoprotein bilayers, which might enhance formulation permeability through the skin.

Keywords:

Meloxicam Microemulsion, Formulation, NSAID, Permeability,

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1. Prausnitz MR, Langer R. Transdermal drug delivery. Nature biotechnology. 2008;26(11):1261-8.
2. McNeill SC, Potts RO, Francoeur ML. Local enhanced topical delivery (LETD) of drugs: does it truly exist? Pharmaceutical Research. 1992;9(11):1422-7.
3. Mason L, Moore RA, Edwards JE, Derry S, McQuay HJ. Topical NSAIDs for chronic musculoskeletal pain: systematic review and meta-analysis. BMC Musculoskeletal Disorders. 2004;5(1):28.
4. Solanki D, Kushwah L, Motiwale M, Chouhan V. TRANSFEROSOMES-A REVIEW. 2016.
5. Lapina V, Vorobey A, Pavich T, Opitz J. Targeting diamond nanoparticles into folate-receptor expressing HeLa cells. Journal of Applied Spectroscopy. 2013;80(3):414-8.
6. Kogan A, Garti N. Microemulsions as transdermal drug delivery vehicles. Advances in colloid and interface science. 2006;123:369-85.
7. Mohammad Soleymani S, Salimi A. Enhancement of Dermal Delivery of Finasteride Using Microemulsion Systems. Adv Pharm Bull. 2019;9(4):584-92. doi:10.15171/apb.2019.067. [PubMed:31857962].
8. Lawrence MJ, Rees GD. Microemulsion-based media as novel drug delivery systems. Adv Drug Deliv Rev. 2000;45(1):89-121. doi:10.1016/s0169-409x(00)00103-4. [PubMed:11104900].
9. Čižinauskas V, Elie N, Brunelle A, Briedis V. Skin Penetration Enhancement by Natural Oils for Dihydroquercetin Delivery. Molecules. 2017;22(9):1536.
10. Leanpolchareanchai J, Padois K, Falson F, Bavovada R, Pithayanukul P. Microemulsion system for topical delivery of Thai mango seed kernel extract: development, physicochemical characterisation and ex vivo skin permeation studies. Molecules. 2014;19(11):17107-29.
11. Pang J, Dong W, Li Y, Xia X, Liu Z, Hao H, et al. Purification of Houttuynia cordata Thunb. Essential Oil Using Macroporous Resin Followed by Microemulsion Encapsulation to Improve Its Safety and Antiviral Activity. Molecules. 2017;22(2):293.
12. Salimi A, Moghimipour E, Tavakolbekhoda N. Transdermal delivery of celecoxib through rat skin from various microemulsions. skin. 2013;8:9.
13. Moghimipour E, Salimi A, Zadeh BSM. Effect of the Various Solvents on the In Vitro Permeability of Vitamin B 12 through Excised Rat Skin. Tropical Journal of Pharmaceutical Research. 2013;12(5):671-7.
14. Obata Y, Utsumi S, Watanabe H, Suda M, Tokudome Y, Otsuka M, et al. Infrared spectroscopic study of lipid interaction in stratum corneum treated with transdermal absorption enhancers. International journal of pharmaceutics. 2010;389(1):18-23.
15. Amin S, Kohli K, Khar RK, Mir SR, Pillai KK. Mechanism of In Vitro Percutaneous Absorption Enhancement of Carvedilol by Penetration Enhancers. Pharmaceutical Development and Technology. 2008;13(6):533-9. doi:10.1080/10837450802309646.
16. Salimi A, Mohammad Soleymani H, Mohammad Soleymani S. Altered Skin Permeation of Finasteride Using Clove Oil, Urea, and Lyophilized Powder of Grape Seed Extract. doi:10.34172/apb.2023.010.
17. Golden GM, Guzek DB, Harris RR, McKie JE, Potts RO. Lipid thermotropic transitions in human stratum corneum. Journal of Investigative Dermatology. 1986;86(3):255-9.