Drug Delivery Systems for Local Anesthetics

Paula, Eneida de; Cereda, Cíntia Maria Saia; Tófoli, Giovana Radomille; Franz-Montan, Michelle; Fraceto, Leonardo Fernandes; Araújo, Daniele Ribeiro de

doi:10.2174/187221110789957228

Cited by 61 publications

(54 citation statements)

References 78 publications

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“…In fact, an initial uncontrolled large dose of drug release could be lethal for the organism and therefore must be avoided. 14,72 Moreover, LA nanoencapsulation increases the drug's efficacy, specificity, tolerability, and therapeutic index. 69 The LA release kinetics and the drug loading efficiency are influenced by the size of the system.…”

Section: From Micro To Nanomentioning

confidence: 99%

From micro- to nanostructured implantable device for local anesthetic delivery

Zorzetto

Brambilla

Marcello

et al. 2016

IJN

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Local anesthetics block the transmission of painful stimuli to the brain by acting on ion channels of nociceptor fibers, and find application in the management of acute and chronic pain. Despite the key role they play in modern medicine, their cardio and neurotoxicity (together with their short half-life) stress the need for developing implantable devices for tailored local drug release, with the aim of counterbalancing their side effects and prolonging their pharmacological activity. This review discusses the evolution of the physical forms of local anesthetic delivery systems during the past decades. Depending on the use of different biocompatible materials (degradable polyesters, thermosensitive hydrogels, and liposomes and hydrogels from natural polymers) and manufacturing processes, these systems can be classified as films or micro- or nanostructured devices. We analyze and summarize the production techniques according to this classification, focusing on their relative advantages and disadvantages. The most relevant trend reported in this work highlights the effort of moving from microstructured to nanostructured systems, with the aim of reaching a scale comparable to the biological environment. Improved intracellular penetration compared to microstructured systems, indeed, provides specific drug absorption into the targeted tissue and can lead to an enhancement of its bioavailability and retention time. Nanostructured systems are realized by the modification of existing manufacturing processes (interfacial deposition and nanoprecipitation for degradable polyester particles and high- or low-temperature homogenization for liposomes) or development of novel strategies (electrospun matrices and nanogels). The high surface-to-volume ratio that characterizes nanostructured devices often leads to a burst drug release. This drawback needs to be addressed to fully exploit the advantage of the interaction between the target tissues and the drug: possible strategies could involve specific binding between the drug and the material chosen for the device, and a multiscale approach to reach a tailored, prolonged drug release

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Section: From Micro To Nanomentioning

confidence: 99%

From micro- to nanostructured implantable device for local anesthetic delivery

Zorzetto

Brambilla

Marcello

et al. 2016

IJN

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“…Benzocaine (BZC) is an ester-type local anesthetic frequently used in topical formulations. Its parenteral administration is limited by the fact that it has low solubility in aqueous media (14,15). The anesthetic action of BZC is characterized by rapid onset, but short duration relative to the duration of pain.…”

Section: Introductionmentioning

confidence: 99%

Poly(Lactide-co-Glycolide) Nanocapsules Containing Benzocaine: Influence of the Composition of the Oily Nucleus on Physico-Chemical Properties and Anesthetic Activity

et al. 2011

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“…Local anesthetics carried in drug delivery systems such as cyclodextrins have been used as potential new formulations for pain treatment. 5,6 In previous studies by other workers 7,8 and by our own research group, [9][10][11] the inclusion of BVC or RVC in hydroxypropyl-β-cyclodextrin (HP-β-CD) increased the anesthetic effect after injection in the subarachnoid space or after sciatic nerve blockade, compared to plain solutions at the same concentration. However, for the development of new pharmaceutical formulations, such as the BVC-hydroxypropyl-β-cyclodextrin inclusion complex (BVC HP-β-CD ) or the RVC-hydroxypropyl-β-cyclodextrin inclusion complex (RVC HP-β-CD ), an assessment of toxicity is essential to provide the fundamental information required to ensure their safe application.…”

mentioning

confidence: 96%