|| Bioinfo Publications || 153
EFFECT OF PENETRATION ENHANCERS ON IN VITRO PERMEATION OF NYSTATIN FROM
TOPICAL FORMULATIONS
International Journal of Drug Discovery
ISSN: 0975-4423 & E-ISSN: 0975-914X, Volume 4, Issue 2, 2012, pp.-153-159.
Available online at http://www.bioinfo.in/contents.php?id=24
MARZOUK M.A.*, AMMAR A.A., DARWISH M.K. AND EL-SAYED H.A.
Pharmaceutics Department, Faculty of Pharmacy (Girls), Al-Azhar University, Cairo, Egypt.
*Corresponding Author: Email- maboushady2000@yahoo.com
Received: July 10, 2012; Accepted: July 26, 2012
Abstract- Nystatin is a polyene antifungal drug that is of particular interest because it exhibits remarkable action against a wide range of
pathogenic and non-pathogenic yeast and fungi. Transdermal and topical delivery of drugs provide advantages over conventional oral
administration. The benefit of transdermal systems includes convenience, improved patient compliance and elimination of hepatic first
pass effect. The aim of this work is to formulate and evaluate topical gel containing nystatin and to improve the antifungal activity of nysta-
tin through using different penetration enhancers namely propylene glycol (PG) 10%, polyethyleneglycol (PEG) 400, ethanol, oleic acid,
eucalyptus oil, tween 80 each in concentration of 5% and dimethylformamide (DMF) 3%with objectives of prolonging its action. The formu-
lae showing the best drug release were selected to study the effect of storage on drug content and pH measurements over a period of 3
months and finally for microbiological evaluation. Among different penetration enhancers used, propylene glycol showed the highest effect
on the amount drug permeated followed by dimethylformamide.
Keywords- Nystatin, Enhancers, Gel- dimethylformamide, propylene glycol, polyethyleneglycol
Introduction
In vitro percutaneous absorption experiments are usually conduct-
ed in a model system using a diffusion cell, in which an artificial
membrane representative of the epidermal barrier is fixed. Animal
or human skin may also be used instead of the artificial membrane,
such a system does not simulate the in vivo condition in which an
efficient and variable blood supply removes the penetrating drug at
various rates.
Although in vitro methods are of limited values, yet they are im-
portant means of assessing the ability of a vehicle to release the
drug, to determine the general routes of penetration and to com-
pare the efficacy of various solvents, or other adjuvants on percuta-
neous absorption from a new dosage form.
Penetration enhancers are taken as additives incorporated into a
formulations in order to promote the absorption of drugs from oint-
ments or gels. In an attempt to enhance the drug release from the
prepared gels, a representative model from previous study contain-
ing carpobol 934 (Cp934 1%), sodium carboxymethyl cellulose
(NaCMC 5%), methyl cellulose (MC3%), hydroxypropylmethylcellu-
lose (HPMC3%) and Poloxamer 407 (Polox407 20%) were chosen
to modulate nystatin release by the use of various penetration en-
hancers namely propylene glycol, dimethylformamide, polyethylene
glycol 400, ethanol, eucaluptus oil, oleic acid and tween 80. These
enhancers are commonly used as effective penetration enhancers
for many drugs [1,4,6,14,15].
In this study, permeation rates of nystatin from different bases
through cellulose membrane and rabbit skin were studied. In addi-
tion, the effect of penetration enhancers on permeation rates of
nystatin from selected formula was investigated.
Materials
Nystatin pure sample and Carbopol 934 and triethanolamine were
kindly supplied by Delta pharma (Egypt). Disodium hydrogen phos-
phate, potassium dihydrogen phosphate, methyl cellulose and
Carboxymethylcellulose sodium powders from El- Nasr Pharma-
ceutical Co. (Egypt). Hydroxypropylmethylcellulose powder low
viscosity (6000) from Sigma Chemical Co. (USP). Poloxamer 407
was kindly supplied by the Egyptian International Pharmaceutical
Industries Co (EPICO), Egypt. Dimethylformamide (DMF) and pro-
pylene glycol (PG) (Misr Chemical co., Cairo, Egypt). Pure pharma-
ceutical grades of: Polyethylene glycol 400 (PEG), ethanol, euca-
lyptus oil, oleic acid and tween 80. Cellulose membrane, molecular
weight cut-off 10,000 (Arthur H. Thomas Co., Philadeliphia, Pa,
USA). Sabouraud's agar, consisting of 2% glucose, 1% neopep-
tone and 2% agar, Oxoid Co., (England). Strain of fungi such as
Candida albicans ATCC (American typing culture collection).
Citation: Marzouk M.A., et al (2012) Effect of Penetration Enhancers on In Vitro Permeation of Nystatin From Topical Formulations. Interna-
tional Journal of Drug Discovery, ISSN: 0975-4423 & E-ISSN: 0975-914X, Volume 4, Issue 2, pp.-153-159.
Copyright: Copyright©2012 Marzouk M.A., et al This is an open-access article distributed under the terms of the Creative Commons Attribu-
tion License, which permits unrestricted use, distribution and reproduction in any medium, provided the original author and source are credit-
ed.
International Journal of Drug Discovery
ISSN: 0975-4423 & E-ISSN: 0975-914X, Volume 4, Issue 2, 2012