Enhanced Local Anesthetic Efficacy of Bioadhesive Ropivacaine Gels

Cho, Cheong-Weon; Shin, Sang‐Chul

doi:10.4062/biomolther.2011.19.3.357

Cited by 5 publications

(2 citation statements)

References 24 publications

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“…In previous studies[15–17] on the effects of a penetration enhancer, thermal analysis and histological examinations suggested that the incorporation of a penetration enhancer decreases the lipid order and has a fluidizing effect on the lipids of the stratum corneum. The role of the penetration enhancer might be explained as an interfacial saturation phenomenon.…”

Section: Resultsmentioning

confidence: 99%

Enhanced controlled transdermal delivery of ambroxol from the EVA matrix

et al. 2012

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To avoid the systemic adverse effects that might occur after oral administration, transdermal delivery of ambroxol was studied as a method for maintaining proper blood levels for an extended period. Release of ambroxol according to concentration and temperature was determined, and permeation of drug through rat skin was studied using two chamber-diffusion cells. The solubility according to PEG 400 volume fraction was highest at 40% PEG 400. The rate of drug release from the EVA matrix increased with increased temperature and drug loading doses. A linear relationship existed between the release rate and the square root of loading rate. The activation energy (Ea) was measured from the slope of the plot of log P versus 1000/T and was found to be 10.71, 10.39, 10.33 and 9.87 kcal/mol for 2, 3, 4 and 5% loading dose from the EVA matrix, respectively. To increase the permeation rate of ambroxol across rat skin from the EVA matrix, various penetration enhancers such as fatty acids (saturated, unsaturated), propylene glycols, glycerides, pyrrolidones, and non-ionic surfactants were used. The enhancing effects of the incorporated enhancers on the skin permeation of ambroxol were evaluated using Franz diffusion cells fitted with intact excised rat skin at 37° using 40% PEG 400 solution as a receptor medium. Among the enhancers used, polyoxyethylene-2-oleyl ether increased the permeation rate by 4.25-fold. In conclusion, EVA matrix containing plasticizer and permeation enhancer could be developed for enhanced transdermal delivery of ambroxol.

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Section: Resultsmentioning

confidence: 99%

Enhanced controlled transdermal delivery of ambroxol from the EVA matrix

et al. 2012

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“…Oleic acid is used as a surfactant and permeation enhancer. Oleic acid-based surfactants showed an ability to self-aggregate into micelles and were readily biodegradable as compared to conventional surfactants [22][23][24]. Eucalyptus oil was used as flavorant as well as penetration enhancer.…”

Section: Introductionmentioning

confidence: 99%

Antiacne Gel Containing Aloe vera and Clindamycin Phosphate: Design, Characterization, and Optimization Using Response Surface Methodology

Rana,

Zaman,

Khan

et al. 2024

International Journal of Polymer Science

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Clindamycin phosphate is a topical antibiotic agent used to treat acne vulgaris, while Aloe vera has both antimicrobial and anti-inflammatory properties. The current study is aimed at formulating an antiacne gel with antioxidant and antimicrobial effects. The antiacne gels were prepared by using polymer HPMC K15M by cold dispersion method. Unveiling the intricacies of gel design, our research harnessed the power of Design Expert 11 to optimize critical parameters—viscosity, spreadability, and permeability. In vitro characterization tests, including pH, spreadability, viscosity, permeability, antimicrobial activity, antioxidant activity, and stability of the gels, were performed. The results of in vitro characterization tests showed that the gels had a mint-like odor, a pH of 6.8, and a spreadability of 21.5 g cm/sec. The gels had a viscosity of 34.2 Pa s and drug content ranging within 90%-110%, as per USP standards. Notably, in vitro permeation assays reveal an exceptional 86% drug release, showcasing the efficacy of our formulation. The uniqueness of our study lies not only in the robust optimization process but also in the multifaceted characterization. Our gel emerges as a promising candidate, exhibiting not only desired antimicrobial and antioxidant properties against acne vulgaris but also demonstrating stability under varied conditions. As we advance toward in vivo studies, our research paves the way for a nuanced understanding of the safety and efficacy of this distinctive antiacne gel.

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Development of prilocaine gels for enhanced local anesthetic action

Kang

Shin

2012

Arch. Pharm. Res.

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Prilocaine, one of local anesthetics, has been used for regional pain relief. When applied as an ointments or creams, it is hard to expect their effects to last for long time, because they are easily removed by wetting, movement and contacting. For more comfortable and better application, we developed a prilocaine gel system using a bioadhesive polymer, carboxymethyl cellulose (CMC). For suitable bioadhesion, the bioadhesive force of various polymers was tested using an auto-peeling tester. The bioadhesive force of various types of CMC such as 100MC, 150MC and 300MC, was 0.0264, 0.0461 and 0.0824 N, at 1.5% concentration, respectively. The CMC-300MC gels showed the most suitable bioadhesive forces. The effect of drug concentration on drug release was studied from the prepared 1.5% CMC gels using a synthetic cellulose membrane at 37 ± 0.5°C. As the concentration of drug increased, the drug release increased. The effects of temperature on drug release from the 1.0% prilocaine gels were evaluated at 27, 32, 37 and 42°C. As the temperature of the drug gels increased, drug release increased. The enhancing effects of penetration enhancers such as pyrrolidones, non-ionic surfactants, fatty acids and propylene glycol derivatives were studied. Among the enhancers used, polyoxyethylene 2-oleyl ether was superior. The anesthetic effects were studied by a tail flick analgesic meter. In the rat tailflick test, 1.0% prilocaine gels containing polyoxyethylene 2-oleyl ether showed the most prolonged local analgesic effects. The results support the view that prilocaine gels with enhanced local anesthetic action could be developed using CMC bioadhesive polymer.

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Enhanced Local Anesthetic Efficacy of Bioadhesive Ropivacaine Gels

Cited by 5 publications

References 24 publications

Enhanced controlled transdermal delivery of ambroxol from the EVA matrix

Enhanced controlled transdermal delivery of ambroxol from the EVA matrix

Antiacne Gel Containing Aloe vera and Clindamycin Phosphate: Design, Characterization, and Optimization Using Response Surface Methodology

Development of prilocaine gels for enhanced local anesthetic action

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