Design, Formulation and Characterization of Liposomal Preparation of Voriconazole (VRC

Ahmed M. Hamdan

Design, Formulation and Characterization of Liposomal Preparation of Voriconazole (VRC

Ahmed M. Hamdan

Abstract

Liposomes are drug delivery systems that may increase the penetration of lipophilic compounds through the skin, enhancing their topical effect. Voriconazole (VRC) is a broad-spectrum trizole antifungal medication that is active against invasive aspergillosis, candidiasis and certain emerging fungal infections. In this study, we formulated different compositions of liposomal preparations for VRC and we evaluated the physical characteristics of these preparations including vesicular shape, vesicular size, drug entrapment efficiency, drug loading capacity and drug release properties of VRC. Moreover, the antifungal properties of liposomal-loaded drug were evaluated against Aspergillus flavus, Fusarium oxysporum and Candida albicans. The formulation (lipo5) having 3% phospholipids and 40% ethanol showing the grater entrapment (92.3%) and optimal average vesicle size of formulation. The formulation (lipo9) having 3% phospholipids and 40% isopropyl alcohol showing the grater entrapment (96.4%). The size of the vesicles was increased with increasing lipid concentration. Moreover, it was observed that the size of the vesicles decreased with increasing ethanol concentration. Liposomal preparation of VRC has the advantage of having antifungal activity at lower concentration than the drug alone. Therefore, liposomal formulation was a promising candidate for drug delivery of VRC and can decrease the concentration of the used VRC improving the patient compliance.

Keywords

antifungal, voriconazole (VRC), liposomes, formulation

Full Text:

References

Malani AN, Kerr LE, Kauffman CA. Voriconazole: how to use this antifungal agent and what to expect. Semin Respir Crit Care Med. 2015;36(5):786–95.

Yamada T, Mino Y, Yagi T, Naito T, Kawakami J. Saturated metabolism of voriconazole N-oxidation resulting in nonlinearity of pharmacokinetics of voriconazole at clinical doses. Biol Pharm Bull. 2015;38(10):1496–503.

Sanchis M, Guarro J, Sutton DA, Fothergill AW, Wiederhold N, Capilla J. Voriconazole and posaconazole therapy for experimental Candida lusitaniae infection. Diagn Microbiol Infect Dis. 2016;84(1):48–51.

Touitou E. Compositions for applying active substances to or through the skin. United States Patent 5,540,934. Date of patent Jul. 30, 1996.

Touitou E. Compositions for applying active substances to or through the skin. United States patent 5,716,638. Date of patent Feb. 10, 1998.

Marc P, Andre B, Howard M. Handbook of Cosmetic Science and Technology. 1st ed. USA: Informa Healthcare; 2007. pp.181–5.

Bhalaria M, Naik S, Misra A. Ethosomes: A novel delivery system for antifungal drugs in the treatment of topical fungal disease. Indian J Exp Biol. 2009;47(5):368–75.

Mbah CC, Builders PF, Attama AA. Nanovesicular carriers as alternative drug delivery systems: ethosomes in focus. Expert Opin Drug Deliv. 2014;11(1):45–59.

Hironaka K, Inokuchi Y, Tozuka Y, Shimazawa M, Hara H, Takeuchi H. Design and evaluation of a liposomal delivery system targeting the posterior segment of the eye. J Control Release. 2009;136:247–53.

Bhatia A, Kumar R, Katare OP. Tamoxifen in topical liposomes: development, characterization and in-vitro evaluation. J Pharm Pharm Sci. 2004;7:252–9.

Szoka F Jr, Papahadjopoulos D. Procedure for preparation of liposomes with large internal aqueous space and high capture by reverse-phase evaporation. Proc Natl Acad Sci USA. 1978;75(9):

–8.

Hathout RM, Mansour S, Mortada ND, Guinedi AS. Liposomes as an ocular delivery system for acetazolamide: in vitro and in vivo studies. AAPS Pharm Sci Tech. 2007;8(1):1.

Palacín C, Sacristán A, Ortiz JA. In vivo activity of sertaconazole in experimental dermatophytosis in guinea pigs. Arzneimittelforschung. 1992;42(5A):714–8.

Soliman GM, Attia MA, Mohamed RA. Poly(ethylene glycol)-block-poly(?-caprolactone) nanomicelles for the solubilization and enhancement of antifungal activity of sertaconazole. Curr Drug Deliv. 2014;11(6):753–62.

Fathalla D, Soliman GM, Fouad EA. Development and in vitro/ in vivo evaluation of liposomal gels for the sustained. J Clin Exp Ophthalmol. 2015;6(1):1–9.

Verma P, Pathak K. Therapeutic and cosmeceutical potential of ethosomes: an overview. J Adv Pharm Technol Res. 2010;1(3): 274–782.

Touitou E, Dayan N, Bergelson L, Godin B, Eliaz M. Ethosomes - novel vesicular carriers for enhanced delivery: characterization and skin penetration properties. J Control Release. 2000;65(3):403–18.

Gu J, Mao X, Li C, Ao H, Yang X. A novel therapy for laryngotracheal stenosis: treatment with ethosomes containing 5-fluorouracil. Ann Otol Rhinol Laryngol. 2015;124(7):561–6.

Fathi-Azarbayjani A, Ng KX, Chan YW, Chan SY. Lipid vesicles for the skin delivery of diclofenac: cerosomes vs. other lipid suspensions. Adv Pharm Bull. 2015;5(1):25–33.

Garg BJ, Garg NK, Beg S, Singh B, Katare OP. Nanosized ethosomesbased hydrogel formulations of methoxsalen for enhanced topical delivery against vitiligo: formulation optimization, in vitro evaluation and preclinical assessment. J Drug Target. 2015;12:1–14.

Song CK, Balakrishnan P, Shim CK, Chung SJ, Chong S, Kim DD. A novel vesicular carrier, transethosome, for enhanced skin delivery of voriconazole: characterization and in vitro/in vivo evaluation. Colloids Surf B Biointerfaces. 2012;92:299–304. 22. Kirjavainen M, Mönkkönen J, Saukkosaari M, Valjakka-Koskela R, Kiesvaara J, Urtti A. Phospholipids affect stratum corneum lipid bilayer fluidity and drug partitioning into the bilayers. J Control Release. 1999;58(2):207–14.

Aggarwal D, Garg A, Kaur IP. Development of a topical niosomal preparation of acetazolamide: preparation and evaluation.J Pharm Pharmacol. 2004;56:1509–17.

Refbacks

There are currently no refbacks.

This work is licensed under a Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International License.

Journal of Pharmaceutical and Biomedical Sciences