THE ENHANCEMENT EFFECT OF CASTOR OIL ON THE PERMEABILITY OF FLURBIPROFEN AS TRANSDERMAL GEL
Keywords:Gel, Transdermal, Flurbiprofen, Permeability, Enhancer, Castor oil
Objective: The object of this study was to improve flurbiprofen permeability transdermally using castor oil as penetration enhancer.
Methods: Castor oil with different concentrations (1%, 2%, 3%, 4%, and 5%) was used in this study as a natural enhancer to improve flurbiprofen permeation transdermally as a gel. The formulated gel of the drug was evaluated for several physicochemical characteristics. The in vitro release and permeability studies for the drug were performed using Franz cell diffusion apparatus across the synthetic membrane. Korsmeyer Pappas kinetic model was used to study the release mechanism of flurbiprofen from the gel.
Results: The results demonstrated that castor oil was safe with no skin irritation and the formulas were stable over time. Castor oil was significantly effective in increasing the percent of flurbiprofen permeability from 46%Â±2.9 for the gel without enhancer to 95%Â±2 for the gel with 5% castor oil and increasing its penetration is directly related to the oil concentration. Two mechanisms for the drug release from the gel were involved, which are non-Fickian (anomalous) and super case II transport.
Conclusion: Flurbiprofen gel was prepared and evaluated successfully for an in vitro parameters with a good permeation across a synthetic membrane. The results demonstrated that castor oil had an effective enhancement for permeation of flurbiprofen.
Finnin BC, Morgan TM. Transdermal penetration enhancers: applications, limitations and potential. J Pharm Sci 1999;88:955-8.
Hirva S, Jenisha P. Bicelle: a lipid nanostructure for transdermal delivery. J Crit Rev 2016;3:17-22.
Keleb E, Sharma RK, Mosa EB, Aljahwi AZ. Transdermal drug delivery system-designand evaluation. Int J Adv Pharm Sci 2010;1:201-11.
Bavaskar K, Jain A, Patil M, Kalamkar R. The impact of penetration enhancers on transdermal drug delivery system: physical and chemical approach. Int J Pharm Res Rev 2015;4:14â€“24.
Biswas GR, Majee SB, Roy A. Combination of synthetic and natural polymers in hydrogel: an impact on drug permeation. J Appl Pharm Sci 2016;6:158-64.
Li DX, Han MJ, Balakrishnan P, Yan YD, Oh DH. Enhanced oral bioavailability of flurbiprofen by combined use of micelle solution and inclusion compound. Arch Pharm Rev 2010;33:95-101.
Syed NHS, Mahboob R, Muhammad FA. Study of percutaneous absorption of diclofenac diethylamine in the presence of cetrimide through hairless rabbit skin. J Res Sci 2006;17:45-51.
Rambharose S, Kalhapure RS, Jadhav M, Govender T. Exploring unsaturated fatty acid cholesteryl esters as transdermal permeation enhancers. Drug Delivery Transl Res 2017;7:333â€“45.
Hussain A, Khan GM, Shah SU, Rahim N. Development of a novel ketoprofen transdermal patch: effect of almond oil as penetration enhancer on in vivo and ex-vivo penetration of ketoprofen through rabbit skin. Pak J Pharm Sci 2012;25:227-32.
Hussain A, Khan GM, Jan SU, Shah S, Shah K, Akhlaq M, et al. Effect of olive oil on the transdermal penetration of flurbiprofen from topical gel as an enhancer. Pak J Pharm Sci 2012;25:365-9.
Dash S, Murthy PN, Nath L, Chowdhury P. Kinetic modelling on drug release from controlled drug delivery systems. Acta Pol Pharm 2010;67:217-23.
Shah KP, Srivastava RS. Evaluation of anti-oxidant and anti-acne activities (in vitro) of the formulated herbal gel. Int J Curr Pharm Res 2015;7:47-50.
AL Haydar M. Enhancement effect of almond oil on the transdermal penetration of flurbiprofen topical gel. J Kerbala University 2015;13:156-63.
Verma A, Singh S, Kaur R, Jain UK. Formulation and evaluation of clobetasol propionate gel. Asian J Pharm Clin Res 2013;6:15-8.
The United State Pharmacopeia (USP), 30, NF28, USA: The United State Pharmacopia Convention Inc; 2010.
Lambers H, Piessens S, Bloem A, Pronk H, Finkel P. Natural skin surface pH is on average below 5, which is beneficial for its resident flora. Int J Cosmet Sci 2006;28:359â€“70.
Fox LT, Gerber M, Plessis JD, Hamman JH. Transdermal drug delivery enhancement by compounds of natural origin. Molecules 2011;16:10507-40.
Helal DA, El-Rhman DA, Abdel-Halim SA, El-Nabarawi MA. Formulation and evaluation of fluconazole topical gel. Int J Pharm Pharm Sci 2012;4:176-83.
Ariyana A, Sinurat D, Ervina I, Bangun H. Formulation and in vitro evaluation of alginate based metronidazole periodontal gel. Asian J Pharm Clin Res 2014;7:223-7.
Shukr M, Metwally GF. Evaluation of topical gel bases formulated with various essential oils for antibacterial activity against methicillin-resistant Staphylococcus aureus. Trop J Pharm Res 2013;12:877-84.
Jafari M, Kaffashi B. Mathematical kinetic modeling on isoniazid release from dex-HEMA-PNIPA Am Nanogels. Nanomed Res J 2016;1:90-6.
Marwah H, Garg T, Goyal AK, Rath G. Permeation enhancer strategies in transdermal drug delivery. Drug Delivery 2016;23:564â€“78.
Ramakrishna S, Mihira V, Tabitha K. Design and evaluation of drug release kinetics of diltiazem hydrochloride sustained release tablets. Int J Med Pharm Sci 2011;1:1-13.
Lakshmi Radhika G, Mahanthesha MK, Chinna Devi G. Formulation and in vitro evaluation of sustained release matrix tablets of flurbiprofen using hydroxypropyl methylcellulose. Int J Adv Res 2013;1:624-30.
Sohail MF, Akhtar Shah P, Tariq I, Saeedul-Hassan A, Amin U, Raza S, et al. Development and in vitro evaluation of flurbiprofen microcapsules prepared by a modified solvent evaporation technique. Trop J Pharm Res 2014;13:1031-8.
Najmuddin M, Patel V, Ahmed A, Shelar S, Khan T. Preparation and evaluation of flurbiprofen microcapsule for colonic drug delivery system. Int J Pharm Pharm Sci 2010; 2:83-7.