Research Article
Newly Developed Topical Cefotaxime Sodium Hydrogels:
Antibacterial Activity and In Vivo Evaluation
Azza S. Zakaria,
1,2
Samar A. Afifi,
1,3
and Kadria A. Elkhodairy
4
1
Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 22452, Riyadh 11495, Saudi Arabia
2
Department of Microbiology, Faculty of Pharmacy, Alexandria University, P.O. Box 21500, Alexandria 21527, Egypt
3
Department of Pharmaceutics, National Organization for Drug Control and Research, P.O. Box 35521, Giza 12561, Egypt
4
Department of Industrial Pharmacy, Faculty of Pharmacy, Alexandria University, P.O. Box 21500, Alexandria 21527, Egypt
Correspondence should be addressed to Kadria A. Elkhodairy; elkhodairy53@yahoo.com
Received 18 January 2016; Revised 6 April 2016; Accepted 13 April 2016
Academic Editor: Kamla Pathak
Copyright © 2016 Azza S. Zakaria et al. Tis is an open access article distributed under the Creative Commons Attribution License,
which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
In an attempt to reach better treatment of skin infections, gel formulations containing Cefotaxime (CTX) were prepared. Te gel
was formulated using Carbopol 934 (C934), Hydroxypropyl Methylcellulose 4000 (HPMC 4000), Carboxymethylcellulose Sodium
(Na CMC), Pectin (PEC), Xanthan Gum (XG), or Guar Gum (GG). Tirteen diferent formulas were prepared and characterized
physically in terms of color, syneresis, spreadability, pH, drug content, and rheological properties. Drug-excipients compatibility
studies were confrmed by FTIR and then in vitro drug release study was conducted. In vitro and in vivo antibacterial activities of
CTX were studied against wound pathogens such as, Staphylococcus aureus (S. aureus), Escherichia coli (E. coli), and Pseudomonas
aeruginosa (P. aeruginosa), using either pure drug or Fucidin5 cream as control. F13 provides better spreadability compared to
F1 (XG) or F11 (HPMC). Moreover, the release of the drug from hydrogel F13 containing C934 was slower and sustained for 8h.
Stability study revealed that, upon storage, there were no signifcant changes in pH, drug content, and viscosity of the gels. Also, F13
showed the larger inhibition zone and highest antibacterial activity among other formulations. Histological analysis demonstrated
that afer single treatment with F13 gel formulation, a noticeable reduction in microbial bioburden occurred in case of both Gram
positive and Gram negative bacterial isolates.
1. Introduction
Several antimicrobial agents are available in the market in
diferent pharmaceutical dosage forms for the treatment of
skin and sof tissue infections (SSTIs). Tese preparations
are designed to be administered either orally or parenterally
or topically. Topical preparations have several benefts com-
pared with systemic therapy [1, 2]. Initially, the required con-
centration for antibiotic activity at the skin target site may be
more easily achieved afer topical dosing. Moreover, topical
administration results in much lower undetectable systemic
levels [3]. Additionally, it can avoid an unnecessary exposure
of gut fora that may exert selection for resistance. Terefore,
topical application of antimicrobial agents is considered an
important alternative using the stratum cornea as the target
organ of various antibiotic drug treatments [1].
Controlled release of antibiotics at site of infection is a
new strategy being employed to treat chronic infections [4, 5].
Localized delivery systems, based on biodegradable poly-
mers, are capable of slowing and controlling drug release for
a certain period of time, with initial burst efect to circumvent
the infection.
Hydrogels, swollen three-dimensional networks of
hydrophilic polymers held together by association bonds or
cohesive forces, are of special interest in controlled release
applications, because of their sof tissue biocompatibility,
the ease with which drugs are dispersed in matrix, and the
high degree of control achieved by selecting the physical
and chemical properties of polymer network. Hydrogels
have been investigated extensively for application as carriers
in difusion-controlled release devices [6]. Hydrogels are a
common form of topical application. Tey achieve sustained
Hindawi Publishing Corporation
BioMed Research International
Volume 2016, Article ID 6525163, 15 pages
http://dx.doi.org/10.1155/2016/6525163