Preparation and characterization of polymeric cross-linked hydrogel patch for topical delivery of gentamicin (original) (raw)
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Polymers
Wound healing faces significant challenges in clinical settings. It often contains a series of dynamic and complex physiological healing processes. Instead of creams, ointments and solutions, alternative treatment approaches are needed. The main objective of the study was to formulate bacitracin zinc-loaded topical patches as a new therapeutic agent for potential wound healing. A free radical polymerization technique was optimized for synthesis. Polyethylene glycol-8000 (PEG-8000) was chemically cross-linked with acrylic acid in aqueous medium, using Carbopol 934 as a permeation enhancer and tween 80 as surfactant. Ammonium persulfate and N,N’-Methylenebisacrylamide (MBA) were utilized as initiator and cross-linker. FTIR, DSC, TGA, and SEM were performed, and patches were evaluated for swelling dynamics, sol-gel analysis, in vitro drug release in various media. A Franz diffusion cell was used for the permeation study. Irritation and wound healing with the drug-loaded patches were al...
2019
Background: This study aims to develop a hydrogel containing gentamicin and ethanol extract of Tetracarpidium conophorum (EETC) impregnated gauze to be used as potential wound dressing to promote wound healing via inhibition of growth of microorganisms by gentamicin, and removal of products of inflammation via high radical-scavenging capacity to facilitate wound healing. Method: A modification of free radical initial polymerisation of the alkyl acrylate polymer was utilised to formulate the gentamicin hydrogel with triethanolamine as the cross linker. The hydrogel membranes were evaluated via Fourier transform infrared and the formulations were assessed for swelling index, skin irritancy and in-vitro release of the gentamicin where kinetics were applied to study drug-release kinetics. Results: In-vivo wound healing tests and histopathology were performed with Carbopol® Ultrez 21 exhibiting higher swelling index (97.6–99.6%) due to the availability of more alkyl acrylate polymer chai...
Design and Evaluation of a Bioadhesive Patch for Topical Delivery of Gentamicin Sulphate
Current Drug Delivery, 2009
The use of aminoglycoside antibiotics for the topical treatment of gram positive and gram negative infections especially burns and wounds has increased markedly in recent years. Patch formulation for topical delivery can be advantageously used as an alternative to conventional topical dosage forms. The present study aims to prepare and evaluate gentamicin sulphate patches for topical application and to study the effect of different bioadhesive polymers on diverse characteristics of prepared patches. Drug patches were evaluated for weight and thickness uniformity, moisture absorption capacity, tensile strength and percentage elongation. In vitro release patterns of these patches were studied and analyzed. Skin irritation and susceptibility testing of gentamicin sulphate formulae were also evaluated and compared to commercially available gentamicin sulphate cream. The thickness of the films was found to be uniform. Tensile strength of the patches prepared using HPMC as bioadhesive polymer was the lowest compared to the other patches. The in vitro release of the patches followed a pattern close to diffusion model. Patches formulated using HPMC gave the most superior results as compared to other compositions.
Tropical Journal of Pharmaceutical Research, 2014
Purpose: To formulate hydrogels based on poloxamer 407 and polyacrylic acids (Carbopols® 971P and 974P), and evaluate its suitability for enhanced topical delivery of gentamicin, a potent but highly toxic aminoglycoside antibiotic. Methods: Topical hydrogels of gentamicin were produced using poloxamer 407 and polyacrlic acids (Carbopols® 971P and 974P), and evaluated in terms of drug content, pH, physical assessment, viscosity and stability. In vitro antimicrobial drug release was conducted using four microorganisms-Escherichia coli, Salmonella typhi, Staphylococcus aureus and Pseudomonas aeruginosa. Results: Stable gentamicin-loaded hydrogels with good encapsulation efficiency (maximum EE% of 85.76 to 90.66 %) as well as greater zones of inhibition against all organisms (maximum range: 22.34 ± 2.35 to 29.40 ± 3.07 mm) than commercially available gentamicin ointment and pure sample of gentamicin (p < 0.05), were produced. Overall, poloxamer 407 hydrogels of gentamicin gave the most desirable properties in terms of pH, viscosity and rapid concentration and time-dependent antibacterial activity on all tested microorganisms , superior to polyacrylic acids hydrogels of gentamicin. Conclusion: This study demonstrates that poloxamer 407 hydrogels of gentamicin may offer a promising approach for topical delivery of gentamicin for the treatment of skin infections caused by gentamicin-susceptible bacteria.
The Turkish Journal of Pharmaceutical Sciences
Amaç: İstatistiksel olarak tasarlanmış deneyler ile birleştirilmiş cevap yüzey metodolojisinin, çok değişkenli proseslerin optimize edilmesinde çok yararlı olduğu bulunmuştur. Bu çalışmanın amacı, iki bağımsız değişkenin, permeasyon arttırıcı/antioksidanların (transkutol ve tetrakarpidium conophorum EETC'nin etanolik ekstresi) ve karıştırma hızının, gentamisin hidrojelinin akışı ve permeasyonu üzerindeki etkisini değerlendirmektir. Gereç ve Yöntemler: Gentamisin hidrojelini formüle etmek için serbest radikal başlangıç polimerizasyonunun modifikasyonu kullanıldı. Daha sonra, permeasyon arttırıcı transkutol: EETC (X1), karıştırma hızı (X2) bağımsız değişkenlerinin etkisini araştırmak için, bağımlı değişkenler, akış (Y1) ve 12 saat ex vivo permeasyondan sonra elde edilen ilaç miktarı (Y2), için değerlendirilen, 14 formülasyon grubuyla, 32 faktöriyel merkez CCD kullanılmıştır. Objectives: Response surface methodology coupled with statistically designed experiments has been found to be very useful in optimising multivariable processes. The aim of this study was to evaluate the influence of two independent variables, a ratio of permeation enhancers/ antioxidants (transcutol and ethanolic extract of tetracarpidium conophorum EETC) and stirring rate, on the flux and permeation of gentamicin hydrogel. Materials and Methods: A modification of free radical initial polymerization was used to formulate the gentamicin hydrogel. A 32 factorial CCD was then used to investigate the effect of independent variables of the permeation enhancer transcutol: EETC (X1), stirring speed (X2) via 14 formulation batches, which were evaluated for dependent variables flux (Y1) and amount of drug permeated after 12 hours (Y2) ex vivo. Results: The results of ANOVA performed to determine the fit of the models revealed that the models were statistically significant (p<0.05) and did not show lack of fit (R2>0.80). The regression equation generated for flux was Y1=19.35-25.82X1-0.044X2 + 0.0097X1X2 + 11.86X21 and for cumulative permeation of gentamicin in 12 hours Y2=315.50-189.67X1 + 0.28X2-1.29X1X2 + 123.55X21. The validity of the statistical models used for predicting flux and drug permeation was confirmed by conducting three confirmation experimental runs at the identified optimum conditions. The results showed that there was no significant difference between the experimental results and those predicted by the statistical models. Conclusion: The excellent correlation between the predicted and measured values shows the validity of statistical models (R2=0.95). An antioxidant and permeation enhancer has been used for the first time to investigate the influence on dependent variables. Optimization of gentamicin hydrogel using central composite statistical design is valid for the prediction of drug permeation and flux using variables in formulation.
Formulation and evaluation of Hydrogel for wound healing
The hydrogels are 3-D networks which consists of physically or chemically cross-linked bonds of hydrophilic polymers. The insoluble hydrophilic structures designate a potential to absorb wound exudates and allows oxygen diffusion to fasten healing process. The aim of the present study is to formulate and evaluate a hydrogel of Neomycin sulfate for wound healing. Neomycin sulphate is an antibiotic used to treat bacterial skin infections. It is good effective in treatment of infected cuts, wounds, ruptured tissue and fatigue as well as minor burns. The neomycin sulfate hydrogel for wound healing topical application was formulated using guar gum and Carbopol-940 and evaluation were performed. Proper selection of polymers and their proportions is a prerequisite for designing and developing a transdermal drug delivery system. The formulated hydrogel showed good homogeneity, good stability and better drug release rates when compared to marketed formulation.
Biomaterials, 2004
Interpenetrating network hydrogels (IPNs) based on poly(acrylic acid) and gelatin (Ge) were evaluated for in vitro and in vivo biodegradation and in vivo release of gentamicin sulphate. In vitro and in vivo degradation studies demonstrated that with the increase of acrylic acid content in the polymer, the rate of degradation decreases, and a reverse phenomenon was observed with increasing Ge content in the hydrogel. The rate of in vivo degradation was much lower than in vitro degradation. Incorporation of gentamicin sulphate in hydrogel further reduces their degradation. In vitro and in vivo drug release profile showed a burst effect, followed by controlled release. Drug concentration was measured in the local skin tissue, blood serum, kidney, liver and spleen. The local skin tissue concentration of 50% and 100% gentamicin sulphate, loaded full IPNs (i.e., Ax-1 and Ax-2), was found to be higher (2072mg/g) than the minimum bactericidal concentration for Staphylococcus aureus (1.2 mg/g) and Pseudomonas aeruginosa (10mg/g), respectively, for a study time of 60 days.
DEVELOPMENT AND CHARACTERIZATION OF TOPICAL HYDROGEL CONTAINING ANTIFUNGAL DRUG
WORD JOURNAL OF PHARMACY AND PHARMACEUTICAL SCIENCES, 2023
An antifungal medication called griseofulvin is used to treat fungus infections. Griseofulvin undergoes hepatic first-pass metabolism and has a long list of possible adverse effects, hence oral usage is not advised. The purpose of this study was to develop and test a topical hydrogel formulation of griseofulvin for the treatment of cutaneous fungal infections. Several hydrophilic polymers, including carbopol 940 and guar gum, were used to develop topical hydrogel formulations of griseofulvin. Viscosity, spreadability, pH, assay, and in vitro drug release all underwent evaluation testing. An in vitro diffusion test in a Franz diffusion cell employed a cellophane membrane. The physicochemical properties of the formulations did not significantly change after exposure to accelerated temperature conditions (40 2oC). A gel formulation containing 1% w/v Guar gum and 1% w/v Carbopol 940 in a 1:1 ratio was shown to be suitable for topical administration based on an in vitro test. These results demonstrate the Griseofulvin topical gel formulation's viability.
African Journal of Pharmacy and Pharmacology, 2013
Parenteral administration of gentamicin, a hydrophilic aminoglycoside antibiotic commonlyused 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 hy...
Gentamicin nanogel films based on Carrageenan-Prosopis africana for improved wound healing
Precision Nanomedicine
Dermal injuries (e. g., trauma, surgical incisions, and burns) are burdensome health care issues in the world. The delayed healing process can be caused by aerobic and anaerobic bacteria infections, including Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus and Enterococcus species, Pseudomonas aeruginosa, Peptostreptococcus, and Coliforms. Therefore, reduction of bacterial burden to an acceptable level promotes healing. The rationale for this innovative wound dressing relies on good hydration as the single most important external factor responsible for optimal wound healing. Objective: To study the wound healing potential of GEN nanogel films based on natural polymers using carrageenan (CAR) and Prosopis africana (PRO), a local African plant. Method: Nanogel dispersions and films were characterized by their physical and technological properties, microenvironment, Zeta sizer, Differential Scanning Calorimetry, FTIR spectroscopy, in vitro drug release, and efficacy of...