Synthesis of lidocaine-loaded PLGA microparticles by flow focusing

Holgado, M.A.; Arias, José L.; Cózar, María José; Álvarez-Fuentes, Josefa; Gañán‐Calvo, Alfonso M.; Fernández‐Arévalo, M.

doi:10.1016/j.ijpharm.2008.02.012

Cited by 73 publications

(47 citation statements)

References 29 publications

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“…55 Drug can be released from the delivery system in a sustained manner to prolong exposure time and increase the drug-therapy efficacy. 56,57 Physically entrapped drugs were released mainly through the diffusion effect, so the driving force was reducing with the concentration of drugs in the core decreasing gradually. Therefore, both the release speed and release amount per day exhibited a trend of declining at later experimental points.…”

Section: In Vitro Releasementioning

confidence: 99%

Synthesis of three-arm block copolymer poly(lactic-<em>co</em>-glycolic acid)–poly(ethylene glycol) with oxalyl chloride and its application in hydrophobic drug delivery

Zhu¹,

Liu²,

Duan³

et al. 2016

IJN

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Section: In Vitro Releasementioning

confidence: 99%

Synthesis of three-arm block copolymer poly(lactic-<em>co</em>-glycolic acid)–poly(ethylene glycol) with oxalyl chloride and its application in hydrophobic drug delivery

Zhu¹,

Liu²,

Duan³

et al. 2016

IJN

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“…48 Another technique to produce monodisperse polymeric microspheres is flow-focusing. [49][50][51] This technique employs a microfluidic device consisting of coaxial capillaries. At the inlet of the capillary with the larger diameter, the drug (lidocaine 49,51 or bupivacaine 50 ) and polymer organic solution follows in a certain direction, surrounded by polyvinyl alcohol (PVA) aqueous solution flowing in the same 49,50 or opposite direction.…”

Section: Figurementioning

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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“…[17][18][19] Drug release systems are, in fact, able to compartmentalize the active substance and drive it to specific active sites, as well as control the rate of release without altering the chemical structure of the transported molecule. 20 The delivery of local anesthetics, which has been studied extensively by many research groups and also by our laboratory, can be achieved by the formation of inclusion complexes with cyclodextrins, 20-30 encapsulation in liposomes, [31][32][33][34][35][36][37][38][39] association to polymer microparticles [40][41][42][43] and association to polymeric nanostructured systems. [44][45][46][47][48] The use of colloidal systems of polymeric nanoparticles is often limited due to problems of stability over long periods of time.…”

Section: Introductionmentioning

confidence: 99%

“…The delivery of local anesthetics, which has been studied extensively by many research groups and also by our laboratory, can be achieved by the formation of inclusion complexes with cyclodextrins, 20-30 encapsulation in liposomes, 31-39 association to polymer microparticles [40][41][42][43] and association to polymeric nanostructured systems.…”

mentioning

confidence: 99%

Physicochemical stability of poly(lactide-co-glycolide) nanocapsules containing the local anesthetic Bupivacaine

Moraes

Paula

Rosa

et al. 2010

J. Braz. Chem. Soc.

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Neste trabalho foi realizada a preparação de nanocápsulas de poli (DL-lactídeo-co-glicolídeo) (PLGA) como um sistema carreador para o anestésico local bupivacaína. A preparação foi caracterizada e sua estabilidade físico-química avaliada. Os resultados da caracterização mostram uma distribuição de tamanho com um índice de polidispersão de 0,12, um diâmetro médio de 148 nm, um potencial zeta de -43,5 mV e uma eficiência de associação da BVC nas nanocápsulas de 75,8%. As propriedades físico-químicas das suspensões (diâmetro hidrodinâmico, índice de polidispersão, potencial zeta e eficiência de associação do fármaco) contendo nanocápsulas poliméricas foram avaliadas em função do tempo a fim de determinar sua estabilidade. Nenhuma grande alteração foi observada em função tempo para as suspensões de nanocápsulas avaliadas, sendo consideradas estáveis por um período de armazenagem de 120 dias a temperatura ambiente. Os resultados aqui apresentados, os quais se referem ao estudo desta nova formulação para anestésico local bupivacaína mostram-se promissores para futuros estudos in vivo.This paper describes the preparation of poly(DL-lactide-co-glicolide) (PLGA) nanocapsules as a drug carrier system for the local anesthetic bupivacaine. The system was characterized and its stability investigated. The results showed a size distribution with a polydispersity index of 0.12, an average diameter of 148 nm, a zeta potential of -43.5 mV and an entrapment efficiency of 75.8%. The physicochemical properties of polymeric nanocapsule suspensions (average diameter, polydispersity, zeta potential and drug association efficiency) were evaluated as a function of time to determine the formulation stability. The formulation did not display major changes in these properties over the time, and it was considered stable up to 120 days of storage at room temperature. The results reported here which refer to the initial characterization of these new formulations for the local anesthetic bupivacaine show a promising potential for future in vivo studies.Keywords: bupivacaine, local anesthetic, polymeric nanocapsules, PLGA, physical-chemical stability IntroductionNumerous studies today are focusing on the development of new pharmaceutical formulations based on nanocarriers, which have demonstrated several advantages over conventional formulations, making this research line a promising and innovative area of the pharmaceutical sector. 1,2Polymer nanoparticles (PN) are carriers of drugs or other active molecules whose sizes range from 10 to 1000 nm. Nanospheres (NS) or nanocapsules (NC) can be obtained, depending on the method of preparation and the materials employed. NC consists of a polymer casing and a nucleus (usually oily). The drug inside the NC may be dissolved in the oily nucleus or adsorbed on the polymeric wall. NS, on the other hand, consists of a polymer matrix and their composition does not include oil. In this system, the drug may be adsorbed or dispersed in the polymeric matrix. [2][3][4][5][6] Several polymers are used in the prepa...

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Synthesis of lidocaine-loaded PLGA microparticles by flow focusing

Cited by 73 publications

References 29 publications

Synthesis of three-arm block copolymer poly(lactic-<em>co</em>-glycolic acid)–poly(ethylene glycol) with oxalyl chloride and its application in hydrophobic drug delivery

Synthesis of three-arm block copolymer poly(lactic-<em>co</em>-glycolic acid)–poly(ethylene glycol) with oxalyl chloride and its application in hydrophobic drug delivery

From micro- to nanostructured implantable device for local anesthetic delivery

Physicochemical stability of poly(lactide-co-glycolide) nanocapsules containing the local anesthetic Bupivacaine

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Synthesis of lidocaine-loaded PLGA microparticles by flow focusing

Cited by 73 publications

References 29 publications

Synthesis of three-arm block copolymer poly(lactic-<em>co</em>-glycolic acid)&ndash;poly(ethylene glycol) with oxalyl chloride and its application in hydrophobic drug delivery

Synthesis of three-arm block copolymer poly(lactic-<em>co</em>-glycolic acid)&ndash;poly(ethylene glycol) with oxalyl chloride and its application in hydrophobic drug delivery

From micro- to nanostructured implantable device for local anesthetic delivery

Physicochemical stability of poly(lactide-co-glycolide) nanocapsules containing the local anesthetic Bupivacaine

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Product

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Synthesis of three-arm block copolymer poly(lactic-<em>co</em>-glycolic acid)–poly(ethylene glycol) with oxalyl chloride and its application in hydrophobic drug delivery

Synthesis of three-arm block copolymer poly(lactic-<em>co</em>-glycolic acid)–poly(ethylene glycol) with oxalyl chloride and its application in hydrophobic drug delivery