Antimicrobial Activity of Lidocaine, Bupivacaine, Mepivacaine and Ropivacaine on Staphylococcus epidermidis, Staphylococcus aureus and Bacillus subtilis

Neuwersch, S.; Köstenberger, M.; Sorschag, Sieglinde; Ilias, Wilfried; Likar, Rudolf

doi:10.2174/1876386301710010001

Cited by 3 publications

(2 citation statements)

References 5 publications

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“…Ocular procedures require the administration of a topical anesthetic such as bupivacaine hydrochloride being used before and after cataract surgery, which has an anesthetic role but also a prolonged analgesic effect [21]. In addition, bupivacaine hydrochloride has antimicrobial properties, which is a benefit for its use in ocular interventions [22,23]. Eye drops require repeated administration, but the gel has a longer residence time and thus decreases the number of administrations [19].…”

Section: Introductionmentioning

confidence: 99%

Development and Optimization of Chitosan-Hydroxypropyl Methylcellulose In Situ Gelling Systems for Ophthalmic Delivery of Bupivacaine Hydrochloride

et al. 2021

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The aim of this study was the development and optimization of chitosan and hydroxypropyl methylcellulose (HPMC) in situ gelling systems, loaded with bupivacaine hydrochloride for topical ocular administration. This study is based on the properties of two polymers: chitosan, which has mucoadhesive action and is a pH-sensitive polymer, but also the cellulose derivative hydroxypropyl methylcellulose, a thermosensitive polymer which has mucoadhesive properties and increases the viscosity of systems. The analysis and optimization of in situ gelling systems were performed based on an experimental design and response surface methodology. The following formulation parameters were considered: X1 = chitosan concentration (0.5%, 1%), X2 = HPMC E 5 LV concentration (2%, 5%) and X3 = Chitosan/HPMC E 5 LV ratio (1/1, 2/1). In addition, the parameters to be optimized were represented by the contact angle (CA (°)), viscosity and cumulative percentage of bupivacaine hydrochloride released in vitro. The results indicate that the designed in situ gelling systems are suitable for bupivacaine prolonged ophthalmic release and overcome the principal disadvantages of the liquid’s ocular formulations. An immediate therapeutic effect corresponding to ocular anesthetic installation was assured in the first stage: burst bupivacaine release. In the second phase, the gradual drug release was assured for over 6 h. This drug release profile, together with the corresponding rheological profile and a collection of superficial properties for good ocular adhesion balanced with an adequate hydrophilic character, assured the desired quality of the attributes for the proposed systems. The system, based on chitosan 1%, HPMC E 5 LV 5% and a 1/1 polymer ratio, could be a solution for the proposed formulation of in situ gelling colloidal systems, since the viscosity of the system was within the range of the optimal viscosity of the eye, and the amount of bupivacaine hydrochloride released after 6 h was the highest at 69.55%.

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Section: Introductionmentioning

confidence: 99%

Development and Optimization of Chitosan-Hydroxypropyl Methylcellulose In Situ Gelling Systems for Ophthalmic Delivery of Bupivacaine Hydrochloride

et al. 2021

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“…Interventions in the iris can irritate the ciliary nerves with discomfort, so association with intracameral anaesthesia is required [22]. In addition to analgesic action, bupivacaine possesses antimicrobial activity on Gram positive and Gram negative bacteria [1,24].…”

Section: Introductionmentioning

confidence: 99%

Contributions on Formulation and Preliminary Evaluation of Ocular Colloidal Systems of Chitosan and Poloxamer 407 With Bupivacaine Hydrochloride

Irimia¹

2019

FARMACIA

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The aim of this paper was the formulation and preliminary evaluation of colloidal systems with improved mechanical and mucoadhesive properties in order to increase ocular retention time and drug bioavailability. Polymeric mixtures of chitosan (0.3%), a pH-sensitive polymer, and poloxamer 407 (12%, 15%, 18%), thermoresponsive polymer, with bupivacaine hydrochloride (0.25%) were prepared. Gelling temperature, wettability, rheological behaviour and in vitro drug release were evaluated. The formulation containing 15% poloxamer 407 is converted to a colloidal dispersion at 35°C, the temperature of the ocular surface. Contact angle values of colloidal systems at physiological temperature (35°C) were lower than those corresponding to formulations at non-physiological temperature (25°C), indicating a higher spreadability over the ocular surface. Rheological studies have shown pseudoplastic behaviour and the poloxamer concentration increased the viscosity of the formulations. In vitro bupivacaine hydrochloride delivery from colloidal systems revealed that drug release mechanism followed Higuchi model. The colloidal dispersions with chitosan and poloxamer 407 could be viable alternatives to increase the bioavailability of bupivacaine hydrochloride in topical ocular anaesthesia. Rezumat Obiectivele acestei lucrări sunt formularea şi evaluarea preliminară a unor sisteme coloidale cu proprietăţi mecanice şi mucoadezive sporite care să asigure un timp de remanenţă crescut la nivel ocular şi o biodisponibilitate a substanţei medicamentoase îmbunătăţite. S-au preparat amestecuri polimerice de chitosan (0,3%), un polimer sensibil la variaţia de pH, şi poloxamer 407 (12%, 15%, 18%), polimer cu proprietăţi termoreversibile, în care a fost încorporată bupivacaină clorhidrat (0,25%). Pentru acestea s-au evaluat: temperatura de gelifiere, udabilitatea, comportamentul reologic şi cedarea in vitro a substanţei active. Formularea conţinând 15% poloxamer 407 s-a transformat într-o dispersie coloidală la 35°C, temperatura de la suprafaţa oculară. Valorile unghiurilor de contact pentru sistemele coloidale la temperatura fiziologică (35°C) au fost mai mici decât cele corespunzătoare formulărilor la temperatura nefiziologică (25°C), fapt ce indică o etalare corespunzătoare pe suprafaţa oculară. Studiile reologice au arătat un comportament pseudoplastic, iar la creşterea concentraţiei de poloxamer s-a înregistrat creşterea vâscozităţii preparatelor. Cedarea in vitro a bupivacainei clorhidrat din sistemele coloidale s-a realizat în conformitate cu modelul Higuchi. Dispersiile coloidale de chitosan şi poloxamer 407 pot reprezenta alternative viabile de creştere a biodisponibilităţii bupivacainei clorhidrat în anestezia topică oculară.

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Synthesis, sciatic nerve block activity evaluation and molecular docking of fluoro-substituted lidocaine analogs as local anesthetic agents

Yan

Chang

et al. 2019

Med Chem Res

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Antimicrobial Activity of Lidocaine, Bupivacaine, Mepivacaine and Ropivacaine on Staphylococcus epidermidis, Staphylococcus aureus and Bacillus subtilis

Abstract: Abstract:Introduction:

Cited by 3 publications

References 5 publications

Development and Optimization of Chitosan-Hydroxypropyl Methylcellulose In Situ Gelling Systems for Ophthalmic Delivery of Bupivacaine Hydrochloride

Development and Optimization of Chitosan-Hydroxypropyl Methylcellulose In Situ Gelling Systems for Ophthalmic Delivery of Bupivacaine Hydrochloride

Contributions on Formulation and Preliminary Evaluation of Ocular Colloidal Systems of Chitosan and Poloxamer 407 With Bupivacaine Hydrochloride

Synthesis, sciatic nerve block activity evaluation and molecular docking of fluoro-substituted lidocaine analogs as local anesthetic agents

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