Abstract
Topical administration of gentamicin, a hydrophilic aminoglycoside antibiotic, is limited by membrane impermeability and toxicity concerns. The purpose of this study was to develop and evaluate the antimicrobial activities of an alternative non-invasive, convenient and cost-effective transdermal drug delivery system (TDDS) containing gentamicin in biodegradable polyester-based matrices. The patches were formulated by solvent evaporation technique using PURASORB® polymers and evaluated for thermal properties, drug content, physicochemical performance, stability, skin irritation on rat skin and antimicrobial activities against five micro-organisms: Staphylococcus aureus, Escherichia coli, Salmonella typhi,Pseudomonas aeruginosa, and Klebsiella pneumoniae. The differential scanning calorimetry(DSC) results indicated compatibilty between the drug and the polymers. In addition, theformulations showed good drug encapsulation, stability, physicochemical properties, tolerability on rabbit skin and higher zones of inhibition compared with a commercially available gentamicin sulphate cream against S. aureus, E. coli, S. typhi and P. aeruginosa, while K. pneumoniae was mildly susceptible. Compared with the rest of the formulations, patches of PURASORB® PL 32 exhibited the best stability, tolerability on rat skin and bioactivity. This study has shown that transdermal patches of PURASORB® PL 32 represent an alternative delivery system for gentamicin for treatment of infections caused by gentamicin-susceptible micro-organisms. Key words: Antimicrobial activities, bioadhesive strength, gentamicin, PURASORB®polymers, transdermal patches.
Highlights
Transdermal drug delivery system is being extensively investigated as a viable alternative to drug delivery with improved bioavailability
The results revealed the compatibility of gentamicin and the polymers as well as the stability of the drug in the polymeric matrices
The results indicate that gentamicin loaded into transdermal patches produced very significant zones of inhibition against the Gram positive organism (S. aureus) and Gram negative organisms (S. typhi, E. coli, S. typhi, and P. aeruginosa) used in the study
Summary
Transdermal drug delivery system is being extensively investigated as a viable alternative to drug delivery with improved bioavailability. Transdermal drug administration generally refers to topical application of agents to healthy. Intact skin either for localized treatment of tissues underlying the skin or for systemic therapy (Valenta and Auner, 2004). It offers many advantages over conventional administration such as enhanced efficacy, increased safety, and greater convenience and improved patient compliance (Valenta and Auner, 2004; Dnyanesh and Vavia, 2003; Chandak and Verma, 2008). Transdermal route permits the use of a relatively potent drug with minimal risk of system toxicity and avoids gastrointestinal degradation and hepatic first-pass metabolism (Mundargi et al, 2007; Mutalik and Udupa, 2004). The transdermal patch can be removed by the patient (Chang et al, 2006)
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