Characterization and controlled release of gentamicin from novel hydrogels based on Poloxamer 407 and polyacrylic acids

Abstract

Parenteral administration of gentamicin, a hydrophilic aminoglycoside antibiotic commonly used in the control of Gram positive and Gram negative infections, is limited by adverse effects such as nephrotoxicity, ototoxicity and neurotoxicity. In this study, topical hydrogels of gentamicin were produced using three polymeric hydrogels of Poloxamer 407 and polyacrlic acids (Carbopols ® 971P and 974P), and evaluated in terms of drug content, pH, swellability in different media, viscosity, spreadability, skin irritation on rats and time-resolved stability. The in vitro permeation of gentamicin from the hydrogel formulations was carried out in phosphate buffered saline using a modified Franz diffusion apparatus. Results obtained indicate that gentamicin-loaded hydrogels showed good encapsulation, stability, pH-dependent swelling, tolerability on rats, greater percentage drug release than the commercially available gentamicin ointment and pure sample of gentamicin. Overall, Poloxamer 407 hydrogels of gentamicin gave the most desirable properties in terms of drug permeation, spreadability, pH, swellability and viscosity, superior to polyacrylic acids hydrogels of gentamicin. This study has shown that Poloxamer 407 hydrogels of gentamicin could offer a promising approach for topical delivery of gentamicin for the treatment of skin infections caused by gentamicinsusceptible bacteria.

<p>Film-Forming Sprays for Topical Drug Delivery</p>

“…The moisture loss and moisture uptake can be calculated by using the following equations. 115,125,126 Moisture loss % ð Þ ¼…”

“…The same volume of fluid is replaced after samples are collected. 34,80,81,126 Ex vivo Skin Permeation Study…”

Oral Gentamicin Preparation Using Solidified Lipid Particulate Delivery System

“…Microemulsion loaded with gentamicin was prepared according to the formula in table (1). The lipid microparticles were prepared using 1:1 (w/w) lipid matrices by a hot-emulsion technique using mixer followed by cooling at room temperature [24].…”

“…Gentamicin sulphate is an aminoglycoside antibiotic commonly used topically in the control of severe Gram positive and Gram negative microbial infections especially in burns and wounds as well as for treating bone and soft tissue infections [1]. It is a polarized watersoluble compound having very poor intestinal membrane permeability resulting in low oral bioavailability [2].…”

“…These include; use of labrasol [1], liposomes [15], solidified reverse micellar drug delivery systems [16][17][18], and hydrogels [19,20]. Gentamicin transdermal microgels had also been prepared by Nnamani et al in 2013 [21].…”