TOPICAL BENZOPHENONE-3 MICROEMULSION-BASED GELS: PREPARATION, EVALUATION AND DETERMINATION OF MICROBIOLOGICAL UV BLOCKING ACTIVITY
Keywords:
Benzophenone-3, Microemulsion gel, In vitro SPF, Spreadability test, Permeation test, Sunscreen efficacy test, Microbiological UV blocking activityAbstract
Objective: Microemulsions (MEs) have been developed as active vehicles for sunscreens being physical sunscreens on their own.The aim of this study is to incorporate Benzophenone-3 (BZ-3), a chemical sunscreening agent into MEs resulting in a synergistic effect on its protective characteristics.
Methods: Screening of BZ-3 in different oils, surfactants and cosurfactants available for topical delivery was carried out. A full factorial study design (3.22) was adopted to study the effect of three independent variables namely;BZ-3, oil, and S/CoSmix(1:1) concentrations on the in-vitro SPF value of the prepared ME gel formulae.
Results: Formulae having SPF>30 were further evaluated regarding in-vitro permeation test. Finally, an in vitro microbiological assay was adopted to compare the survival percent of E.coli against UV exposure. Formula F11IPM ME gel consisting of 3% BZ-3 and 10% Isopropyl myristate as oil together with 60% w/w Tween80/Cremophore RH40 mix (1:1)as surfactant and cosurfactant respectively was chosen as the optimum formula having an in vitro SPF of 33.15±0.91,lowest permeation of 192±16.13µg/cm2 after eight hours and microbiological UV blocking activity of 88±5.84%which is not significantly different from the standard Spectra Ban plus (SPF=30) having a survival percent of 80±3.04%.
Conclusion: This study illustrated the potential use of microemulsified BZ-3 delivery system to improve the SPF of BZ-3.
Downloads
References
El-Badry M, Fetih G, Shakeel F. Comparative topical delivery of antifungal drug Croconazole using liposome and micro-emulsion based gel formulations. J Drug Deliv 2014;21(1):34-43.
Montenegro L, Carbone C, Puglisi G. Vehicle effects on in-vitro release and skin permeation of octylmethoxycinnamate from microemulsions. Int J Pharm 2011;405:162-8.
Paul BK, Moulik SP. Uses and applications of microemulsions. J Curr Sci 2001;80:990-1001.
Tenjarla S. Microemulsions:an overview and pharmaceutical applications. J Crit Rev Ther Drug Carrier Syst 1999;16:461-521.
Park KM, Kim CH. Preparation and evaluation of flurbiprofen-loaded microemulsion for parenteral delivery. Int J Pharm 1999;18:173-9.
Lawrence MJ, Rees GD. Microemulsion-based media as novel drug delivery systems. Adv Drug Del Rev 2000;45:89-121.
Tsai YH, Lee KF, Huang YB, Huang CT, Wu PC. In-vitro permeation and In-vivo whitening effect of topical hesperetinmicroemulsion delivery system. Int J Pharm 2010;388:257-62.
Soliman SMH, Abd El-Rehim AEA, El-Gazayerly ON, Abd El-Malak NS. Formulation of microemulsion gel systems for transdermal delivery of celecoxib:in vitro Permeation, anti-inflammatory activity and skin irritation tests. J Drug Discov Therap 2010;4(6):459-71.
Boonme P. Application of microemulsions in cosmetics. J Cosmet Dermatol 2007;6:223-8.
González S, Lorente MF, Calzada YG. The latest on skin photoprotection. J Clin Dermatol 2008;26:614-26.
Seite S, Fourtanier AM. The benefit of daily photoprotection. J Am Acad Dermatol 2008;58:160-66.
Wankhade RP, Pundir AR, Bhalerao SS. Microemulsion as Novel Cosmeceutical Drug Delivery System. J Pharm Cosmetol 2012;9(2):78-92.
Lautenschlager S, Wulf HC, Pittelkow MR.Photoprotection. J Lancet 2007;370:528-37.
Grampurohit N, Ravikumar P, Mallya R. Microemulsions for Topical Use-A Review. Ind J Pharm Edu Res 2011;45:100-7.
Patel M, Jain SK, Yadav AK, Gogna D, Agrawal GP. Preparation and Characterization of Oxybenzone-Loaded Gelatin Microspheres for Enhancement of Sunscreening Efficacy. Drug Deliv 2006;13:323-30.
Hernà ndez JRV, Goymann CCM. Artificial Sun Protection:Sunscreens and Their Carrier Systems. J Curr Drug Deliv 2006;3:405-15.
Treffel P, Gabard B. Topical bioavailability of sunscreen agents in stratum corneum:effect of vehicle and time. J Pharm Res 1996;13:770-4.
Hagedorn-Leweke U, Lippold BC. Absorption of Sunscreens and Other Compounds Through Human Skin in Vivo:Derivation of a Method to Predict Maximum Fluxes. J Pharm Res 1995;12:1354-60.
Hayden CG, Roberts MS, Benzon HAE. Systemic absorption of sunscreen after topical application. J Lancet 1997;350:863-4.
Yener G, Hadgraft J, Pugh WJ. Penetration of two sunscreens in various formulations through a synthethic membrane as compared to human skin in vitro. J Acta Pharm Turc 1998;40(1):27-32.
Gupta VK, Zatz JL, Rerek M. Percutaneous absorption of sunscreens through micro-Yucatan pig skin in vitro. J Pharm Res 1999;16:1602-7.
Badawi AA, Nour SA, Sakran WS, El Mancy SS. Preparation and evaluation of microemulsion systems containing salicylic acid. J AAPS Pharm Sci Tech 2009;10:1081-84.
Shakeel F, Baboota S, Ahuja A, Ali J, Aqil M, Shafiq S. Nanoemulsions as vehicles for transdermal delivery of aceclofenac. J AAPS Pharm Sci Tech 2007;8:E1-E9.
Such H, Jun HW. Physicochemical and release studies of Naproxen in poloxamer gels. Int J Pharm 1996;129:13-20.
El Maghraby GM. Transdermal delivery of hydrocortisone from eucalyptus oil microemulsion:Effects of cosurfactants. Int J Pharm 2008;355:285-92.
Djordjevic L, Primorac M, Stupar M. In-vitro release of diclofenacdiethylamine from caprylocaproylmacrogolglycerides based microemulsions. Int J Pharm 2005;296:73-9.
Azeem A, Rizwan M, Ahmad FJ, Iqbal Z, Khar RK, Aqil M et al. Nanoemulsion components screening and selection:a technical note. J AAPS Pharm Sci Tech 2009;10:69-76.
Nour SA, Shalaby SH, Afify NN, Abd El-Aal S, Mekhael MK. Formulation and evaluation of econazole nitrate emulgels. J Drug Res Egypt 2002;24:63-71.
Ambade KW, Jadhav KR, Gambhire MN, Kurmi SD, Kadam VJ, Jadhav KR. Formulation and evaluation of flurbiprofenmicroemulsion. J Curr Drug Deliv 2008;5:32-41.
Brime B, Moreno MA, Frutos G, Ballesteros MA, Frutos P. Amphotericin B in oil-water lecithin-based microemulsions: formulation and toxicity evaluation. J Pharm Sci 2002;91:1178-85.
Diffey BL, Robson J. The influence of pigmentation and illumination on the perception of erythema. J Photodermatol Photoimmunol Photomed 1992;9:45-7.
MarÃa CS, Revilla E, Miramontes E, Bautista J, MartÃnez AG, Romero E et al. Protection against free radicals (UVB irradiation) of a water-soluble enzymatic extract from rice bran. Study using human keratinocyte monolayer and reconstructed human epidermis. J Food Chem Toxicol 2010;48:83-88.
Vettor M, Perugini P, Scalia S, Conti B, Genta I, Modena Tet al. Polylactidenanoencapsulation to reduce photoinactivation of a sunscreen agent. Int J Cosmet Sci 2008;30:219-27.
Kaidbey KH, KligmanAM. Laboratory methods for appraising the efficacy of sunscreens. J Soc Cosmet Chem 1978;29:525-36.
Pathan IB, Setty CM. Stability evaluation of tamoxifen citrate nanoemulsion containing Cremophor RH 40 as surfactant. J Acta Pharm Sci 2011;53:127-34.
Yener G, Incegül T, Yener N. Importance of using solid lipid microspheres as carriers for UV filters on the example octylmethoxycinnamate. Int J Pharm 2003;258:203-7.
Yang J, Wiley CJ, Godwin DA, Felton LA. Influence of hydroxypropyl-b-cyclodextrin on transdermal penetration and photostability of avobenzone. Eur J Pharm Biopharm 2008;69:605-12.
American A, Washington DC. American Public Health Works Association and Water Pollution Control Federation;1989.p.
Munshi HA, Saeed MO, Green TN, Al-Hamza AA, Farooque MA, Ismail ARA. Impact of UV irradiation on controlling biofouling problems in NF-SWRO desalination process. International Desalination Association (IDA) World Congress: Conference Singapore; 2005.
Gomaa YAMM. Master Sc Thesis, Faculty of Pharmacy, Alexandria University;2006.p. 65, 74, 109, 128, 165, 188, 200, 205, 213.
Roszakt DB, Colwell RR. Metabolic activity of bacterial cells enumerated by direct viable count. J Appl Environ Microbiol 1987;53:2889-983.
Mazzola PG, Penna TCV, Martins AMS. Determination of decimal reduction time (D value) of chemical agents used in hospitals for disinfection purposes. J BMC Infect Dis;2003. http://www.biomedcentral.com/1471-2334/3/24.
White HR. The Heat Resistance of Streptococcus faecalis. J Gen Microbiol 1953;8:27-37.
Amin MM, Sheta NM, Abd El Gawad NA, Badawi AA. Preparation and characterization of Benzophenone-3 loaded polymeric nanoparticles of lactide-co É›-caprolactone as drug carriers. J pharm Res Opin 2012;2:28-41.
Abd El-Malak NS. PhD Thesis, Faculty of Pharmacy. Cairo University;2006.
Sanad RA, Abd El Malak NS, El Bayoomy TS, Badawi AA. Formulation of a Novel Oxybenzone-Loaded Nanostructured Lipid Carriers (NLCs). J AAPS Pharm Sci Tech 2010;11:1684-94.
Hathout RM. PhD Thesis, Faculty of Pharmacy, Ain Shams University;2010. p.45.
Schuch AP, Menck CFM. The genotoxic effects of DNA lesions induced by artificial UV-radiation and sunlight. J Photochem Photobiol B 2010;99:111-6.
Sambandan DR, Ratner D. Sunscreens:An overview and update. J Am Acad Dermatol 2011;64:748-58.
Chen H, Chang X, Weng T, Zhao X, Gao Z, Yang Y et al. A study of microemulsion systems for transdermal deliveryoftriptolide. J Control Rel 2004;98:427-36.
Gannu R, Palem CR, Yamsani VV, Yamsani SK, Yamsani MR. Enhanced bioavailability of lacidipine via microemulsion based transdermal gels:Formulation optimization, ex vivo and in-vivo characterization. Int J Pharm 2010;388:231-41.
Desai KGH. Enhanced skin permeation of rofecoxib using topical microemulsion gel. J Drug Dev Res 2004;63:33-40.
Shafiq S, Shakeel F, Talegaonkar S, Ali J, Baboota S, Ahuja A et al. Formulation Development and Optimization Using Nanoemulsion Technique:A Technical Note. J AAPS Pharm Sci Tech 2007;8:E1-E6.
Forestier S. Rationale for sunscreen development. J Am Acad Dermatol 2008;58:S133-S8.
Saukharev AR, Wojciechowska J. Microemulsion as potential ocular drug delivery systems: phase diagrams and physical properties depending on ingredients. J Acta Pol Pharm 2005;62:465-71.
Milosevic D, Solaja MM, Lj NTT, Stijepic MJ, Glusac JR. The survival of Escherichia coli upon exposure to irradiation with non-coherent polychromatic polarized light. J Vet Med 2011;56:520-527.