Preparation of Aminophylline Anticellulite Gel and Evaluation the Effect of D-limonen and Ethanol on the Permeation Enhancement of Drug through Shed Snake Skin

Document Type : Original Article

Authors

1 Nanotechnology Research Center, Department of Pharmaceutics, Faculty of Pharmacy, Ahvaz Jundishapur University of Medical Sciences, Ahvaz, Iran

2 Nanotechnology Research Center, Department of Pharmaceutics, Faculty of Pharmacy, Ahvaz Jundishapur University of Medical Sciences, Ahvaz, Iran.

Abstract

Background and Objective: This investigation aimed to prepare aminophylline gel and study the effect of ethanol and di-limonen on the permeation enhancement of drug through shed snake skin.
Subjects and Methods: Aminophylline gels were prepared using theophylline and ethylene diamine as raw materials of aminophyllineand hydroxypropylmethyl cellulose (HPMC) F4M and propylene glycol as gelling agent and cosolvent, respectively. Ethanol or di-limonen 5% was added as an enhancer.Drug permeability across polymeric membrane and shed snake skin was evaluated using Franz diffusion cells. Drug permeation parameters including flux (J), permeability coefficient (Kp) and enhancement factors (EFs) of each enhancer were calculated.
Results: Both accelerants significantly enhanced the absorption of aminophylline through skin model in comparison with control group (P <0.05). But they significantly reduced the drug permeability across polymeric membrane. Ethanol 60% showed a significant higher permeation effect (EF=6.61±1.05) in comparison with d-limonen 5% (EF=2.91±0.02). Both increased aminophyllin skin permeability after a lag time.
Conclusion: D-limonen and ethanol are able to increase absorption of aminophylline through shed snake skin. Reduction in drug permeability across non-biological membrane suggests that enhancement effect on the transdermal permeation of the drug can be attributed to time-dependent reconstruction of stratum corneum.

Keywords


1-Avram MM. Cellulite: a review of its physiology and treatment. J Cosmet Laser Ther 2004;6(4):181-5.
2-Draelos ZD, Marenus KD. Cellulite. Etiology and purported treatment. Dermatol Surg 1997;23(12):1177-81.
3-Rosenbaum M, Prieto V, Hellmer J, Boschmann M, Krueger J, Leibel RL, et al. An exploratory investigation of the morphology and biochemistry of cellulite. Plast Reconstr Surg 1998;101(7):1934-9 .
4-Lotti T, Ghersetich I, Grappone C, Dini G. Proteoglycans in so-called cellulite. Int J Dermatol 1990;29(4):272-4.
5-Alster TS, Tanzi EL. Cellulite treatment using a novel combination radiofrequency, infrared light, and mechanical tissue manipulation device. J Cosmet Laser Ther 2005;7(2):81-5.
6-Rosssi AB, Vergnanini AL. Cellulite: a review. J Eur Acad Dermatol Venereol 2000;14(4):251-62.
7-Kouchak M, Dabbagh MA, Moghbel AH, Ameri AG, Rahimi Z. Preparation and evaluation of some topical formulation of aminophylline for treatment of cellulite [dissertation]. Ahvaz: Ahvaz Jundishapur University of Medical Sciences; 2005. p. 30-3.
8-Deus P. The science of topical fat loss. Available From: URL: Http://www.bodybuilding.com/fun/par6.htm, april 2006. (10/20/2007).
9-Ansel HC, Allen LV, Popvich NG. Pharmaceutical dosage forms & drug delivery systems. 7th ed. Philadelphia: Lippincott Williams & Wilkins; 1999. p. 263-78.
10-Benson HAE. Transdermal Drug Delivery: Penetration Enhancement Techniques. Current Drug Delivery. 2005 //;2(1):23-33.
11-Jaydatt KJ, Sreenivas SA. Review on chemical permeation enhancer used in transdermal drug delivery system. Int J Sci Innov Discov. 2012; 2 (6): 204-217.
12-Gennaro AR, Marderosian AHD, Hanson GR, Medwick T, Popovich NG, Schnaare RL, et al. Remington: The science and practice of pharmacy. 20th ed. Pennsylvania: Mack Publishing Co; 2000. p. 307-10.
13-Sinko PJ. Martin's physical pharmacy and pharmaceutical sciences. 5th ed. Philadelphia: Lippincott William& Wilkins; 2006. P. 308-9.
14-Akomeah FK, Martin GP, Brown MB. Short-term iontophoretic and post-iontophoretic transport of model penetrants across excised human epidermis. Int J Pharm 2009;367(1-2):162–8.
15-Moghimipour E, Sajadi Tabassi SA, Kouchak M, Varghaei H. Combination strategies for enhancing transdermal absorption of theophylline through shed snake skin. Asian J Pharm Clin Res 2012;5(2):30-4.
16-Moghimipour E, Sajadi Tabassi SA, Ramezani Mohammad, Lobenberg R. [Enhanced permeability of gentamicin sulfate through shed snake-skin and liposomal membrane by different enhancers]. Iran J Basic Med Sci 2003;6(1):9-19. [In Persian]
17-Williams AC, Barry BW. Terpenes and the lipid-protein-partitioning theory of skin penetration enhancement. Pharm Res 1991;8(1):17–24
18-Sapra B, Jain S, Tiwary AK. Percutaneous permeation enhancement by terpenes: mechanistic view. AAPS J 2008;10(1):120-32.
19-Goates CY, Knutson K. Enhanced permeation and stratum corneum structural alterations in the present of dithiothrietol. Biochem Biophys Acta 1993;1153(2):281-98.
20-Bouwstra JA, Gooris GS, Van der Spek JA, Bras W. Structural investigations of human stratum corneum by small-angle X-ray scattering. J Invest Dermatol 1991;97:1005-12.