Preparation and characterization of vemurafenib microemulsion
DOI:
https://doi.org/10.31351/vol32issSuppl.pp316-325Keywords:
spseudoternary phase diagramAbstract
Human melanoma is the most common and malignant type of skin cancer. Vemurafenib has been used for the treatment of malignant or metastatic melanoma. Oral vemurafenib has serious adverse drug reactions including
QTc sigment prolongation of heart ECG that may result in discontinuation of treatment. The aim of study was to prepare o/w vemurafenib microemulsion to be used for topical administration. Saturated solubility of vemurafenib were performed in different oils, surfactants and co-surfactants. Peppermint oil, Tween 20 and PEG 400 were chosen to be the oil phase, surfactant and co-surfactant repectively. Since, vemurafenib had the highest solubility in these materials. Six fromulas (F1- F6) of vemurafenib microemulsion were prepared by simple titration method and characterized for their particle size, polydipersity (PDI), zeta potential, microemulsion morphology, dilution test, conductivity, thermodynamic stability and drug release. Formula F3 was chosen since it exhibits the lowest particle size (11.83 nm ± 0.55 nm), zeta potential -2.57 mV, passed the thermodynamic stability tests and had significantly higher (P < 0.05) release percent for vemurafenib (91% within 24 h). As a conclusion, microemulsion is considered as a poweful and promising drug delivery system for topical administation
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35. Baroli B, López-Quintela MA, Delgado-Charro MB, Fadda, AM, & Blanco-Méndez J. Microemulsions for topical delivery of 8-methoxsalen. Journal of Controlled Release. 2000;69(1):209-218.
36. Sun J, Wang F, Sui Y, She Z, Zhai W, Wang C, & Deng Y. Effect of particle size on solubility, dissolution rate, and oral bioavailability: evaluation using coenzyme Q10 as naked nanocrystals. International journal of nanomedicine. 2012;5733-5744.
2. Ellenberger DJ, Miller DA, Kucera SU, et al. Improved vemurafenib dissolution and pharmacokinetics as an amorphous solid dispersion produced by KinetiSol® processing. AAPS PharmSciTech. 2018;19(5): 1957-1970.
3. Zhang W, Heinzmann D, Grippo JF. Clinical pharmacokinetics of vemurafenib. Clinical pharmacokinetics. 2017;56:1033-43.
4. Yamaguchi K, Mitsui T, Aso Y, & Sugibayashi K. Structure–permeability relationship analysis of the permeation barrier properties of the stratum corneum and viable epidermis/dermis of rat skin. Journal of Pharmaceutical Sciences, 2008; 97(10), 4391-4403.
5. Ngawhirunpat T, Worachun N, Opanasopit P, Rojanarata T, & Panomsuk S. Cremophor RH40-PEG 400 microemulsions as transdermal drug delivery carrier for ketoprofen. Pharmaceutical development and technology, 2013;18(4), 798-803.
6. Al-Rubaye RA & Al-Kinani KK. Formulation and Evaluation of Prednisolone Acetate Microemulsion Ocular Gel. The Egyptian Journal of Hospital Medicine. 2023;90(1):1744-1751.
7. Yang J, Xu H, Wu S, Ju B, Zhu D, Yan Y and et al. Preparation and evaluation of microemulsion-based transdermal delivery of Cistanche tubulosa phenylethanoid glycosides. Molecular Medicine Reports, 2017;15(3), 1109-1116.
8. Moulik SP, Rakshit AK. Physicochemistry and applications of microemulsions. Journal of Surface Science and Technology. 2006;22(3–4):159–186.
9. Artiga-Artigas M, Acevedo-Fani A & Martín-Belloso O. Effect of sodium alginate incorporation procedure on the physicochemical properties of nanoemulsions. Food Hydrocolloids. 2017;70: 191-200.
10. Smail, SS, Ghareeb MM, Omer HK, Al-Kinani AA & Alany RG. Studies on surfactants, cosurfactants, and oils for prospective use in formulation of ketorolac tromethamine ophthalmic nanoemulsions. Pharmaceutics. 2021;13(4): 467.
11. Srikanth, K, Gupta VR M, Manvi SR, & Devanna N. INTERNATIONAL RESEARCH JOURNAL OF PHARMACY. 2012; 3 (11):22-26.
12. Kreilgaard M. Influence of microemulsions on cutaneous drug delivery. Advanced drug delivery reviews. 2002;54: S77-S98.
13. Taher SS, Al-Kinani KK, Hammoudi ZM, Ghareeb MM. Co-surfactant effect of polyethylene glycol 400 on microemulsion using BCS class II model drug. J Adv Pharm Educ Res. 2022;12(1):63-9.
14. Nastiti, CM, Ponto T, Abd E, Grice JE, Benson HA & Roberts MS. Topical nano and microemulsions for skin delivery. Pharmaceutics. 2017;9(4): 37.
15. Juškaitė V, Ramanauskienė K & Briedis V. Design and formulation of optimized microemulsions for dermal delivery of resveratrol. Evidence-Based Complementary and Alternative Medicine, 2015.
16. Morlière P, Boscá F, Silva A M S, Teixeira A, Galmiche A, Mazière JC, et al. A molecular insight into the phototoxic reactions observed with vemurafenib, a first-line drug against metastatic melanoma. Photochemical & Photobiological Sciences2015;14: 2119-2127.
17. Anil L, & Kannan K. Microemulsion as drug delivery system for Peptides and Proteins. Journal of Pharmaceutical Sciences and Research. 2018;10(1):16-25.
18. Boonme P, Krauel K, Graf A, Rades T, & Junyaprasert V B. Characterization of microemulsion structures in the pseudoternary phase diagram of isopropyl palmitate/water/Brij 97: 1-butanol. Aaps Pharmscitech2006; 7: E99-E104.
19. Bayindir ZS and Yuksel N. Characterization of niosomes prepared with various nonionic surfactants for paclitaxel oral delivery. Pharmaceutical technology. 2010;99(4):2049-2060.
20. Basheer HS, Noordin MI, & Ghareeb MM . Characterization of microemulsions prepared using isopropyl palmitate with various surfactants and cosurfactants. Tropical Journal of Pharmaceutical Research. 2013;12(3), 305-310.
21. Nirmala MJ, Allanki SRI N IV A S, Mukherjee, A. M. I. T. A. V. A., & Chandrasekaran N. Enhancing the solubility of ramipril using a new essential oil based microemulsion system. Int J Pharm Pharm Sci. 2013;5(4):322-323.
22. Kalra R. Development and characterization of nanoemulsion formulations for transdermal Delivery of aceclofenac: A Research. Int. J. of drug formulation & Res. 2010; 1(1):359-86.
23. Thakkar PJ, Madan P, & Lin S. Transdermal delivery of diclofenac using water-in-oil microemulsion: formulation and mechanistic approach of drug skin permeation. Pharmaceutical development and technology. 2014;19(3):373-384.
24. Sadoon NA, and Ghareeb MM. Formulation and characterization of isradipine as oral nanoemulsion. Iraqi Journal of Pharmaceutical Sciences.2020; 29(1):143-153.
25. Dawood NM, Abdal-Hamid SN. Formulation and characterization of lafutidine nanosuspension for oral drug delivery system. Int J App Pharm 2018;10 Suppl 2:20-30.
26. Bansal S, Aggarwal G, Chandel P and Hirikumar SL.Design and development of cefdinir niosomes for oral delivery. Journal of pharmaceutical bioallied science. 2013;5(4):318-325.
27. Ali SK, Al-khedairy EBH. Solubility and Dissolution Enhancement of Atorvastatin Calcium using Solid Dispersion Adsorbate Technique. Iraqi J Pharm Sci. 2019;28(2):105–114.
28. Bergonzi MC, Hamdouch R, Mazzacuva F, Isacchi B, & Bilia AR. Optimization, characterization, and in vitro evaluation of curcumin microemulsions. LWT-Food Science and Technology. 2014;59(1):148-155.
29. Huang YB, Lin YH, Lu TM, Wang RJ, Tsai YH, Wu PC. Transdermal delivery of capsaicin derivative-sodium nonivamide acetate using microemulsions as vehicles. Int J Pharm 2008; 349:206–211.
30. Hammodi ID & Abd Alhammid SN. Preparation and Characterization of Topical Letrozole Nanoemulsion for Breast Cancer. Iraqi Journal of Pharmaceutical Sciences. 2020; 29(1):195-206.
31. Hamed SB, & Abd Alhammid SN. Formulation and Characterization of Felodipine as an Oral Nanoemulsions. Iraqi Journal of Pharmaceutical Sciences. 2021;30(1) :209-217.
32. Krstić M, Medarević Đ, Đuriš J, & Ibrić. Self-nanoemulsifying drug delivery systems (SNEDDS) and self-microemulsifying drug delivery systems (SMEDDS) as lipid nanocarriers for improving dissolution rate and bioavailability of poorly soluble drugs. In Lipid nanocarriers for drug targeting 2018:473-508.
33. Manev ED & Pugh RJ. Diffuse layer electrostatic potential and stability of thin aqueous films containing a nonionic surfactant. Langmuir. 1991;7(10): 2253-2260.
34. Park ES, Cui Y, Yun BJ, Ko IJ, & Chi SC. Transdermal delivery of piroxicam using microemulsions. Archives of pharmacal research. 2005; 28: 243-248.
35. Baroli B, López-Quintela MA, Delgado-Charro MB, Fadda, AM, & Blanco-Méndez J. Microemulsions for topical delivery of 8-methoxsalen. Journal of Controlled Release. 2000;69(1):209-218.
36. Sun J, Wang F, Sui Y, She Z, Zhai W, Wang C, & Deng Y. Effect of particle size on solubility, dissolution rate, and oral bioavailability: evaluation using coenzyme Q10 as naked nanocrystals. International journal of nanomedicine. 2012;5733-5744.
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Neamah MJ, Entidhar J. Al-Akkam. Preparation and characterization of vemurafenib microemulsion. Iraqi Journal of Pharmaceutical Sciences [Internet]. 2023 Nov. 4 [cited 2024 Nov. 5];32(Suppl.):316-25. Available from: https://bijps.uobaghdad.edu.iq/index.php/bijps/article/view/2607
